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Dictionary of drugs:D
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Dictionary of pharmaceutical drugs/medications sorted alphabetically
- A page 1 | A page 2 | A page 3
- C | C1 | C2
- M | M page 2
- S | page 2
- 0 - 9
Dictionary of drugs D
- D1/3-MAGE-3-His fusion protein
A recombinant fusion protein derived from the melanoma antigen MAGE-3 with potential immunostimulating and antineoplastic activities. Recognized by specific cytotoxic T lymphocytes, D1/3-MAGE-3-His fusion protein may boost antitumoral immune responses when used in a vaccine formulation. This recombinant chimeric protein is produced by fusing MAGE-3 with a lipidated protein D derived from H. influenzae at its N-terminus and a sequence of several histidine residues at its C-terminus.
- DAB389 epidermal growth factor
A recombinant fusion protein composed of the diphtheria toxin with the receptor-binding domain replaced by human epidermal growth factor (EGF). When administered, EGF binds to the endothelial cell growth factor receptor, EGFR, which is upregulated in many solid tumors. After binding to the EGF receptor, the agent is internalized by the cell, where the diphtheria toxin moiety exerts its cytotoxic effect, inhibiting protein synthesis through ADP-ribosylation of elongation factor 2.
- dabigatran etexilate mesylate
An orally available mesylate salt form of the etexilate prodrug of dabigatran, a benzimidazole and direct thrombin inhibitor with anticoagulant activity. Upon administration, dabigatran etexilate is hydrolyzed by esterases and is converted into dabigatran. Dabigatran reversibly binds to and inhibits the activity of thrombin, a serine protease that converts fibrinogen into fibrin. This disrupts the coagulation cascade and inhibits the formation of blood clots.
An orally bioavailable inhibitor of B-raf (BRAF) protein with potential antineoplastic activity. Dabrafenib selectively binds to and inhibits the activity of B-raf, which may inhibit the proliferation of tumor cells which contain a mutated BRAF gene. B-raf belongs to the the raf/mil family of serine/threonine protein kinases and plays a role in regulating the MAP kinase/ERKs signaling pathway, which may be constitutively activated due to BRAF gene mutations.
A triazene derivative with antineoplastic activity. Dacarbazine alkylates and cross-links DNA during all phases of the cell cycle, resulting in disruption of DNA function, cell cycle arrest, and apoptosis.
A humanized monoclonal antibody directed against the CD40 receptor with potential antineoplastic activity. Dacetuzumab specifically binds to and inhibits the CD40 receptor, thereby inducing apoptosis and inhibiting cellular proliferation via antibody-dependent cellular cytotoxicity (ADCC) in cells that overexpress this receptor. The CD40 receptor, a member of the tumor necrosis factor (TNF) receptor super-family, is highly expressed on most B-lineage hematologic malignancies including multiple myeloma, non-Hodgkin lymphoma, chronic lymphocytic leukemia, Hodgkin disease and acute lymphoblastic leukemia.
- DACH polymer platinate AP5346
A low molecular weight polymer-conjugated platinum complex with potential antineoplastic activity. This polymer drug delivery system consists of cytotoxic diaminocyclohexane (DACH)-platinum (Pt) coupled to a water-soluble biocompatible hydroxypropylmethacrylamide (HPMA) copolymer via a pH sensitive linker. Due to decreased pH in tumor sites, the linker is cleaved and the chelated active moiety DACH-Pt is released in tumor cells. DACH-Pt alkylates macromolecules and causes both inter- and intra-strand platinum-DNA crosslinks, which impede DNA replication and transcription, resulting in cell-cycle independent cytotoxicity. The HPMA-based drug delivery system increases the concentration and prolongs the half-life of DACH-Pt in tumor sites, while minimizing adverse effects on normal tissues.
- DACH-platin micelle NC-4016
Polymeric micellar nanoparticles containing diaminocyclohexane platinum (DACH-platin or DACH-Pt) with potential antineoplastic activity. DACH-platin micelle NC-4016 is prepared through the formation of a polymer-metal complex between DACH-platin and the polyethylene glycol-poly (glutamic acid) block copolymer, PEG-P(Glu). DACH-platin, an active metabolite of the platinum-based antineoplastic agent oxaliplatin, is highly hydrophobic and toxic when administered systemically. The use of polymeric micelles incorporating DACH-platin may both increase cell permeability and enhance the retention of the agent. This allows an extended half-life in the blood circulation and a selective and high accumulation of DACH-platin at tumor sites. This results in increased anticancer efficacy while reducing side effects due to DACH-platin toxicity. Upon intravenous administration and internalization by tumor cells, DACH-platin binds to and causes both inter- and intra-strand cross-links in DNA, forming platinum adducts and triggering tumor cell apoptosis.
An orally available inhibitor of the hepatitis C virus (HCV) non-structural protein 5A (NS5A) replication complex, with potential activity against HCV. Although the exact mechanism of action of daclatasvir has yet to be fully determined, this agent, upon oral administration and after intracellular uptake, appears to bind to domain I of the NS5A protein. This inhibits the activity of the NS5A protein and results in the disruption of the viral RNA replication complex, blockage of viral HCV RNA production, and inhibition of viral replication. NS5A, a zinc-binding and proline-rich hydrophilic phosphoprotein, plays a crucial role in HCV RNA replication. HCV is a small, enveloped, single-stranded RNA virus belonging to the Flaviviridae family.
A recombinant monoclonal antibody interleukin-2 receptor antagonist. Daclizumab binds specifically to the alpha subunit of the human interleukin-2 (IL-2) receptor expressed on the surface of activated lymphocytes in vivo, thereby inhibiting IL-2 binding and IL-2-mediated lymphocyte activation, a critical cellular immune response pathway.
Brand name for decitabine
An orally bioavailable, highly selective, second-generation small-molecule inhibitor of the pan-epidermal growth factor receptor (EGFR) family of tyrosine kinases (ErbB family) with potential antineoplastic activity. Dacomitinib specifically and irreversibly binds to and inhibits human EGFR subtypes, resulting in inhibition of proliferation and induction of apoptosis in EGFR-expressing tumor cells. EGFRs play major roles in tumor cell proliferation and tumor vascularization, and are often overexpressed or mutated in various tumor cell types.
A chromopeptide antineoplastic antibiotic isolated from the bacterium Streptomyces parvulus. Dactinomycin intercalates between adjacent guanine-cytosine base pairs, blocking the transcription of DNA by RNA polymerase; it also causes single-strand DNA breaks, possibly via a free-radical intermediate or an interaction with topoisomerase II.
- Dakin's solution
A highly diluted solution of sodium hypochlorite (0.5% w/v) with topical anti-infective activity. Dakin's solution is used as an antiseptic to clean infected topical wounds.
A soluble fusion protein containing the extracellular domain of activin receptor-like kinase-1 (ALK1) fused to a human Fc domain (ALK1-Fc fusion protein), with potential antiangiogenic and antineoplastic activities. Upon administration, dalantercept binds to various ALK1 ligands, preventing activation of tumor cell ALK1 receptors and so inhibiting the ALK1 signaling pathway; growth factor-induced angiogenesis is thus inhibited, which may result in the inhibition of tumor cell proliferation and tumor cell death. ALK1 is a type I cell surface receptor with serine/threonine kinase activity that mediates signaling by members of the transforming growth factor-beta (TGFbeta) superfamily and plays a key role in angiogenesis; ligands for this receptor include TGFbeta1 and TGFbeta2. The Fc moiety of this fusion protein mediates clearance of ligand-fusion protein complexes by the reticuloendothelial system (RES).
A second-generation, semi-synthetic lipoglycopeptide antibiotic, with bactericidal activity against a variety of gram-positive bacteria. Upon administration, dalbavancin binds, at a site different from that of penicillins and cephalosporins, tightly to the D-alanyl-D-alanine portion of peptidoglycan chains, thereby preventing peptidoglycan elongation and interfering with bacterial cell wall synthesis. This leads to activation of bacterial autolysins and induces cell wall lysis.
Brand name for roflumilast
A recombinant monoclonal antibody directed against the insulin-like growth factor 1 receptor (IGF1R) with potential antineoplastic activity. Dalotuzumab binds to membrane-bound IGF1R, preventing binding of the ligand IGF1 and the subsequent triggering of the PI3K/Akt signaling pathway; inhibition of this survival signaling pathway may result in the inhibition of tumor cell proliferation and the induction of tumor cell apoptosis. The activation of IGF1R, a tyrosine kinase and a member of the insulin receptor family, stimulates cell proliferation, enables oncogenic transformation, and suppresses apoptosis; IGF1R signaling has been highly implicated in tumorigenesis and metastasis.
- dalteparin sodium
The sodium salt of a low molecular weight, synthetic heparin. As an anticoagulant/antithrombotic agent, dalteparin binds to antithrombin and enhances the inhibition of Factor Xa. Compared to unfractionated heparins, the use of dalteparin is associated with lower incidences of osteoporosis and heparin-induced thrombocytopenia.
A synthetic androgen derived from ethinyl testosterone. Danazol indirectly reduces estrogen production by decreasing pituitary secretion of follicle-stimulating hormone and luteinizing hormone, and binds to sex hormone receptors in target tissues, thereby exhibiting antiestrogenic, anabolic and weakly androgenic effects.
A water-insoluble heterocyclic amide with potential antineoplastic activity. Daniquidone inhibits topoisomerases I and II, thereby inhibiting DNA replication and repair, and RNA and protein synthesis. The acetylated form of daniquidone is highly toxic and is capable of inducing unscheduled DNA synthesis; rapid acetylators are more likely to experience toxicity with this agent.
Brand name for danazol
A small-molecule 3-aminopyrazole derivative with potential antineoplastic activity. Dalotuzumab binds to and inhibits the Aurora kinases, which may result in cell growth arrest and apoptosis in tumor cells in which Aurora kinases are overexpressed. This agent may preferentially bind to and inhibit Aurora B kinase. Aurora kinases, a family of serine-threonine kinases, are important regulators of cellular proliferation and division.
An antisense oligonucleotide targeting signal transducer and activator of transcription 3 (STAT3) with potential antitumor activity. Danvatirsen binds to STAT3 mRNA, thereby inhibiting translation of the transcript. Suppression of STAT3 expression induces tumor cell apoptosis and decreases tumor cell growth. STAT3, a protein overexpressed in a variety of human cancers, plays a critical role in tumor cell growth and survival.
A small molecule with potential antineoplastic and antiangiogenic activities. Daporinad binds to and inhibits nicotinamide phosphoribosyltransferase (NMPRTase), inhibiting the biosynthesis of nicotinamide adenine dinucleotide (NAD+) from niacinamide (vitamin B3), which may deplete energy reserves in metabolically active tumor cells and induce tumor cell apoptosis. In addition, this agent may inhibit tumor cell prioduction of vascular endothelial growth factor (VEGF), resulting in the inhibition of tumor angiogenesis. The coenzyme NAD+ plays an essential role in cellular redox reactions, including the redox reaction linking the citric acid cycle and oxidative phosphorylation.
A synthetic derivative of diamino-sulfone with anti-inflammatory and anti-bacterial properties. As a structural analog of p-aminobenzoic acid (PABA), dapsone inhibits dihydropteroate synthase (DHPS), an enzyme important in folate synthesis, resulting in a depletion of the folate pool and a reduction in the amount of thymidylate available for DNA synthesis. Although the exact mechanism through which dapsone exerts its anti-inflammatory activity has yet to be fully elucidated, this agent interferes with the activation and oxidative damage of myeloperoxidase in neutrophils and inhibits the integrin-mediated adherence and chemotaxis of neutrophils. Dapsone's anti-inflammatory activities may contribute to the effects seen upon topical administration.
- dapsone gel, 5%
A gel containing 5% (w/w) dapsone, a synthetic derivative of diamino-sulfone with anti-infective properties. A structural analog of p-aminobenzoic acid (PABA), dapsone inhibits dihydropteroate synthase (DHPS), an enzyme important in folate synthesis, resulting in a depletion of the folate pool and a reduction in the amount of thymidylate available for DNA synthesis.
Brand name for diphtheria toxoid/tetanus toxoid/acellular pertussis vaccine adsorbed
A semi-synthetic cyclic lipopeptide antibiotic isolated form the bacterium Streptomyces roseosporus with broad-spectrum anitbiotic activity against Gram-positive bacteria. Daptomycin has a distinct mechanism of action, in which it binds to bacterial membrane and causes rapid depolarization of the cell membrane due to calcium-dependant potassium efflux; the loss of membrane potential leads to inhibition of DNA, RNA and protein synthesis, resulting in bacterial cell death. This agent does not penetrate the outer membrane of gram-negative bacteria.
Brand name for pyrimethamine
A fully human monoclonal antibody directed against the cell surface glycoprotein CD-38 with potential antineoplastic activity. The binding of daratumumab to natural killer (NK) cells mimics the normal CD38-CD31 interaction on the NK cell surface. CD38 is also present on multiple myeloma (MM) cells and plasma leukemia cells; this agent may preferentially bind these cells, triggering antitumoral antibody-dependent cellular cytotoxicity (ADCC) and complement-dependent cytotoxicity (CDC). CD38, a cell surface glycoprotein, is present on various immune cells and has been shown to regulate the cytotoxic response of activated NK cells.
A co-formulation composed of daratumumab, a human immunoglobulin (Ig) G1 kappa monoclonal antibody directed against the cell surface glycoprotein cluster of differentiation 38 (CD-38; CD38), and a recombinant form of human hyaluronidase (rHuPH20), with potential antineoplastic activity. Upon subcutaneous administration of daratumumab/rHuPH20, daratumumab targets and binds to CD38 on certain CD38-expressing tumors, such as multiple myeloma (MM) and plasma cell leukemia. This binding induces direct apoptosis through Fc-mediated cross-linking and triggers immune-mediated tumor cell lysis through antibody-dependent cellular cytotoxicity (ADCC), complement-dependent cytotoxicity (CDC), and antibody-dependent cellular phagocytosis (ADCP) immune responses. CD38, a transmembrane glycoprotein, is expressed in both hematopoietic and non-hematopoietic lineage cells. rHuPH20 hydrolyzes and degrades the glycosaminoglycan hyaluronic acid (HA), thereby decreasing interstitial viscosity and enhancing penetration of daratumumab through the interstitial space. This facilitates the delivery of daratumumab to CD38-expressing tumor cells.
- darbepoetin alfa
A recombinant analog of the endogenous cytokine erythropoietin, an erythropoiesis-stimulating protein. Due to the addition of two carbohydrate chains, darbepoetin alfa exhibits a three-fold greater half-life than does erythropoietin. Similar to erythropoietin, darbopoietin alfa binds to and activates epoetin receptors, thereby inducing the differentiation and maturation of erythrocyte progenitors, stimulating endothelial cell proliferation, and stimulating B-cell proliferation and immunoglobulin production.
A small-molecule organic arsenical with potential antineoplastic activity. Although the exact mechanism of action is unclear, darinaparsin, a highly toxic metabolic intermediate of inorganic arsenicals (iAs) that occurs in vivo, appears to generate volatile cytotoxic arsenic compounds when glutathione (GSH) concentrations are low. The arsenic compounds generated from darinaparsin disrupt mitochondrial bioenergetics, producing reactive oxygen species (ROS) and inducing ROS-mediated tumor cell apoptosis; in addition, this agent or its byproducts may initiate cell death by interrupting the G2/M phase of the cell cycle and may exhibit antiangiogenic effects. Compared to inorganic arsenic compounds such as arsenic trioxide (As2O3), darinaparsin appears to exhibit a wide therapeutic window.
A formulation containing an androgen receptor (AR) antagonist with potential antineoplastic activity. Darolutamide binds to ARs in target tissues; subsequently, inhibiting androgen-induced receptor activation and facilitating the formation of inactive complexes that cannot translocate to the nucleus. This prevents binding to and transcription of AR-responsive genes that regulate prostate cancer cell proliferation. This ultimately leads to an inhibition of growth in AR-expressing prostate cancer cells. Check for active clinical trialsusing this agent.
A combination of darleukin (L19-IL2), an immunocytokine consisting of the recombinant form of interleukin-2 (IL-2), fused to a human single-chain variable fragment (scFv) directed against the extra-domain B (ED-B) of fibronectin (L19), and fibromun (L19-TNFalpha), an immunocytokine consisting of human tumor necrosis factor alpha (TNFalpha) fused to a human scFv antibody fragment directed against the ED-B of L19, with potential antineoplastic and immunostimulating activities. Upon administration, the L-19 moieties of each immunocytokine bind to the ED-B domain of fibronectin on tumor cells in the tumor neovasculature. In turn, the IL-2 and TNF-alpha moieties of darleukin and fibromun, respectively, may locally induce an immune response against ED-B fibronectin-expressing tumor cells. ED-B is predominantly expressed during angiogenesis and tumor growth.
Brand name for daratumumab
A non-nucleoside inhibitor of the hepatitis C virus (HCV) non-structural protein 5B (NS5B), an RNA-dependent RNA polymerase, with potential activity against HCV. Upon administration and after intracellular uptake, dasabuvir binds HCV NS5B and blocks viral RNA synthesis and replication. The HCV NS5B protein is essential for the replication of the HCV RNA genome. HCV is a small, enveloped, single-stranded RNA virus belonging to the Flaviviridae family; HCV infection is associated with the development of hepatocellular carcinoma (HCC).
An orally bioavailable synthetic small molecule-inhibitor of SRC-family protein-tyrosine kinases. Dasatinib binds to and inhibits the growth-promoting activities of these kinases. Apparently because of its less stringent binding affinity for the BCR-ABL kinase, dasatinib has been shown to overcome the resistance to imatinib of chronic myeloid leukemia (CML) cells harboring BCR-ABL kinase domain point mutations. SRC-family protein-tyrosine kinases interact with a variety of cell-surface receptors and participate in intracellular signal transduction pathways; tumorigenic forms can occur through altered regulation or expression of the endogenous protein and by way of virally-encoded kinase genes.
- daunorubicin hydrochloride
The hydrochloride salt of an anthracycline antineoplastic antibiotic with therapeutic effects similar to those of doxorubicin. Daunorubicin exhibits cytotoxic activity through topoisomerase-mediated interaction with DNA, thereby inhibiting DNA replication and repair and RNA and protein synthesis. Check for active clinical trialsusing this agent.
- daunorubicin hydrochloride and cytarabine liposome
A liposomal formulation containing a fixed combination of the antineoplastic agents cytarabine and daunorubicin in a 5:1 molar ratio. Daunorubicin hydrochloride and cytarabine liposome has been designed to provide optimal delivery of a specific ratio of cytarabine to daunorubicin, one that has been shown to be synergistic in vitro. The antimetabolite cytarabine competes with cytidine for incorporation into DNA, inhibiting DNA synthesis. This agent also inhibits DNA polymerase, resulting in a decrease in DNA replication and repair. Daunorubicin, an intercalator and a topoisomerase II inhibitor, prevents DNA replication and inhibits protein synthesis. This agent also generates oxygen free radicals, resulting in the cytotoxic lipid peroxidation of cell membrane lipids.
Brand name for liposomal daunorubicin citrate
Brand name for glasdegib maleate
Brand name for galactomannan derivative
- DC-cholesterol liposome
A cationic cholesterol derivative mixed with dimethylaminoethane-carbamoyl and sonicated to form small unilamellar vesicles that can complex with DNA, DNA/protein complexes and other drug complexes and mediates the delivery into the cytosol from the endosome compartment.
- DC-OVA vaccine
An autologous, multivalent dendritic cell vaccine targeting ovarian cancer with potential immunostimulating and antineoplastic activities. DC-OVA vaccine is produced in vitro by pulsing autologous dendritic cells with killed autologous primary ovarian tumors as a source of tumor-associated antigens (TAAs); the pulsed DCs are then matured using various cytokines. Upon administration, DC-OVA vaccine may stimulate a cytotoxic T lymphocyte (CTL) response against ovarian cancer TAA-expressing ovarian cancer cells.
- DCR ligand-bearing liposome-encapsulated melanoma antigens vaccine
A cancer cell-based vaccine containing liposome encapsulated melanoma antigens and an immunomodulatory factor, attached, via a metal chelator, to a dendritic cell receptor (DCR) ligand-containing a metal-affinity tag, with potential immunomodulating and antineoplastic activity. Upon intravenous administration of DCR ligand-bearing liposome-encapsulated melanoma antigens vaccine, the DCR ligand moiety of this vaccine targets receptors on dendritic cells (DCs), thereby presenting the antigens to DCs which may, in turn, stimulate the DCs and may activate the immune system to mount a cytotoxic T lymphocyte (CTL) response against melanoma cancer cell associated antigens.
An analogue of the amino acid D-alanine with broad-spectrum antibiotic and glycinergic activities. D-cycloserine interferes with bacterial cell wall synthesis by competitively inhibiting two enzymes, L-alanine racemase and D-alanine:D-alanine ligase, thereby impairing peptidoglycan formation necessary for bacterial cell wall synthesis. This agent may be bactericidal or bacteriostatic, depending on its concentration at the infection site and the susceptibility of the organism. In addition, D-cycloserine is an excitatory amino acid and partial agonist at the glycine binding site of the NMDA receptor in the central nervous system (CNS); binding to the central NMDA receptor may result in amelioration of neuropathic pain.
Brand name for desmopressin acetate
- DEC-205/NY-ESO-1 fusion protein CDX-1401
A fusion protein consisting of a fully human monoclonal antibody directed against the endocytic dendritic cell (DC) receptor, DEC-205, linked to the tumor-associated antigen (TAA) NY-ESO-1 with potential immunostimulating and antineoplastic activities. The monoclonal antibody moiety of DEC-205/NY-ESO-1 fusion protein CDX-1401 binds to the endocytic DC receptor, which may result in DC endocytic internalization of this agent, specifically delivering the NY-ESO-1 moiety. DC processing of NY-ESO-1 may boost the immune system to mount a cytotoxic T-lymphocyte response (CTL) against cancer cells expressing NY-ESO-1. NY-ESO-1, a cell surface protein expressed in normal fetal and adult testes, is upregulated in a variety of tumor cell types.
Brand name for diphtheria toxoid/tetanus toxoid vaccine adsorbed
A cytidine antimetabolite analogue with potential antineoplastic activity. Decitabine incorporates into DNA and inhibits DNA methyltransferase, resulting in hypomethylation of DNA and intra-S-phase arrest of DNA replication.
Brand name for demeclocycline hydrochloride
An orally bioavailable, small-molecule focal adhesion kinase (FAK) inhibitor with potential antiangiogenic and antineoplastic activities. Defactinib inhibits FAK, which may prevent the integrin-mediated activation of several downstream signal transduction pathways, including those involving RAS/MEK/ERK and PI3K/Akt, thus inhibiting tumor cell migration, proliferation, survival, and tumor angiogenesis. The tyrosine kinase FAK, a signal transducer for integrins, is normally activated by binding to integrins in the extracellular matrix (ECM) but may be upregulated and constitutively activated in various tumor cell types. Check for active clinical trialsusing this agent.
A synthetic, orally bioavailable, achiral, tridentate triazole derived from salicylic acid with iron-chelating activity. Deferasirox chelates iron at a 2:1 (ligand:iron) ratio. Because of its oral availablity,and long plasma half-life, this agent may be superior to desferrioxamine (desferal, DFO), which is orally inactive and has a short plasma half-life.
An orally bioavailable bidentate ligand with iron chelating activity. Deferiprone binds to iron in a 3:1 (ligand:iron) molar ratio. By binding to iron, deferiprone is able to remove excess iron from the body.
- deferoxamine mesylate
The mesylate salt of an iron-chelating agent that binds free iron in a stable complex, preventing it from engaging in chemical reactions. Deferoxamine chelates iron from intra-lysosomal ferritin and ferrioxamine, a water-soluble complex excreted by the kidneys and in the feces via the bile. This agent does not readily chelate iron bound to transferrin, hemoglobin, myoglobin or cytochrome.
- defibrotide sodium
A polydeoxyribonucleotide with antithrombotic, thrombolytic, and fibrinolytic properties. Defibrotide sodium induces the release of prostaglandin 12 and reduces the expression of adhesion molecules on endothelial cells, thereby interfering with platelet and leukocyte adhesion to the endothelium. Check for active clinical trialsusing this agent.
Brand name for perflutren
Brand name for perflutren lipid microspheres
Brand name for defibrotide sodium
A long-acting, synthetic peptide with gonadotrophin-releasing hormone (GnRH) antagonistic properties. Degarelix targets and blocks GnRH receptors located on the surfaces of gonadotroph cells in the anterior pituitary, thereby reducing secretion of luteinizing hormone (LH) by pituitary gonadotroph cells and so decreasing testosterone production by interstitial (Leydig) cells in the testes. Check for active clinical trialsusing this agent.
- deglycosylated ricin A chain-conjugated anti-CD19/anti-CD22 immunotoxins
A combination preparation of 1:1 mixture of the immunotoxins HD37-dgA and RFB4-dgA with potential antineoplastic activity. Anti-CD19 IgG monoclonal antibody HD37 and anti-CD22 IgG monoclonal antibody RFB4 are attached individually to a deglycosylated ricin A chain (dgA) via N-succinimidyl-oxycarbonyl-alpha-methyl-alpha-(2-pyridyldithio) toluene (SMPT) linker. Deglycosylated ricin A chain-conjugated anti-CD19/anti-CD22 immunotoxins bind to CD19- and CD22-expressing tumor cells, specifically delivering cytotoxic ricin A chain to leukemia cells expressing these antigens. Ricin A chain is toxic to ribosomal activity and protein synthesis, and inhibits cell growth. CD19 and CD22 molecules are cell surface antigens present on the majority of B acute lymphoblastic leukemia (ALL) cells.
- dehydrated human amnion/chorion membrane
Tissue derived from portions of the placenta donated by the patient during a C-section, with potential regenerative activity. Upon placement of the tissue around or on the affected area, dehydrated human amnion/chorion membrane (dHCAM), which contains regenerative cytokines, promotes wound angiogenesis and may help heal the wound, restore tissue function and reduce risk of inflammation.
Brand name for diethylstilbestrol
An orally bioavailable synthetic P2 threonine boronic acid inhibitor of the chymotrypsin-like activity of the proteasome, with potential antineoplastic activity. Delanzomib represses the proteasomal degradation of a variety of proteins, including inhibitory kappaBalpha (IkappaBalpha), resulting in the cytoplasmic sequestration of the transcription factor NF-kappaB; inhibition of NF-kappaB nuclear translocation and transcriptional up-regulation of a variety of cell growth-promoting factors; and apoptotic cell death in susceptible tumor cell populations. In vitro studies indicate that this agent exhibits a favorable cytotoxicity profile toward normal human epithelial cells, bone marrow progenitors, and bone marrow-derived stromal cells relative to the proteasome inhibitor bortezomib. The intracellular protein IkappaBalpha functions as a primary inhibitor of the proinflammatory transcription factor NF-kappaB.
Brand name for testosterone enanthate
An analogue of tetrahydrocannabinol (THC) with antiemetic, anxiolytic, appetite-stimulating, analgesic, and neuroprotective properties. Delta-8-tetrahydrocannabinol (delta-8-THC) binds to the cannabinoid G-protein coupled receptor CB1, located in the central nervous system; CB1 receptor activation inhibits adenyl cyclase, increases mitogen-activated protein kinase activities, modulates several potassium channel conductances and inhibits N- and P/Q-type Ca2+ channels. This agent exhibits a lower psychotropic potency than delta-9-tetrahydrocannabinol (delta-9-THC), the primary form of THC found in cannabis. Check for active clinical trialsusing this agent.
Brand name for prednisolone
The orally bioavailable delta form of the naturally-occurring fat-soluble vitamin E, mostly found in soybean and corn oils, with potential antioxidant activity. Although the exact mechanism of action of this tocopherol has yet to be fully identified, delta-tocopherol appears to have the ability to scavenge free radicals, thereby protecting cells against oxidative damage.
A humanized monoclonal antibody directed against the N-terminal epitope of Notch ligand DLL4 (delta-like 4) with potential antineoplastic activity. Demcizumab binds to the membrane-binding portion of DLL4 and prevents its interaction with Notch-1 and Notch-4 receptors, thereby inhibiting Notch-mediated signaling and gene transcription, which may impede tumor angiogenesis. Activation of Notch receptors by DLL4 stimulates proteolytic cleavage of the Notch intracellular domain (NICD); after cleavage, NICD is translocated into the nucleus and mediates the transcriptional regulation of a variety of genes involved in vascular development. The expression of DLL4 is highly restricted to the vascular endothelium.
- demeclocycline hydrochloride
The hydrochloride salt of demeclocycline, a broad-spectrum, tetracycline derivative exhibiting antimicrobial, aquaretic and chelating activities. In bacteria, demeclocycline binds reversibly to the 30S ribosomal subunit and blocks the binding of aminoacyl-tRNA to the A-site of the mRNA-ribosome complex, resulting in the inhibition of protein synthesis and bacterial cell death. In mammals, this agent interferes with the action of antidiuretic hormone (ADH) at the level of the renal collecting tubule, resulting in aquaresis. In addition, demeclocycline, which like other tetracyclines chelates calcium in bone and exhibits a yellow fluorescence under ultraviolet (UV) light, may be used as a fluorescent bone-labeling agent in bone histomorphometry.
Brand name for meperidine hydrochloride
- demineralized bone matrix
Demineralized allograft bone with osteoinductive activity. Demineralized bone matrices are prepared by acid extraction of allograft bone, resulting in loss of most of the mineralized component but retention of collagen and noncollagenous proteins, including growth factors. The efficacy of a demineralized bone matrix (DBM) as a bone-graft substitute or extender may be related to the total amount of bone morphogenetic protein (BMP) present, and the ratios of the different BMPs present. BMPs belong to the transforming growth factor (TGF) superfamily of proteins.
Brand name for metyrosine
Brand name for idoxuridine
- dendritic cell-autologous lung tumor vaccine
A cancer vaccine consisting of lymphocytes harvested from a patient with lung cancer and induced to become antigen-presenting cells (APCs) known as dendritic cells. The dendritic cells are transduced with the gene encoding an antigen specific to the patient's cancer and then returned to the patient. In the host, the altered cells stimulate the immune system to mount a primary T cell response against lung tumor cells expressing the target antigen. Dendritic cell-autologous lung tumor vaccines have been investigated for use in cancer immunotherapy.
- dendritic cell-CEA peptide vaccine
A cancer vaccine consisting of dendritic cells harvested from a patient with cancer and pulsed or transduced with a peptide fragment of carcinoembryonic antigen (CEA), a tumor-associated antigen expressed by a wide range of cancers. When the altered dendritic cells are returned to the patient, they may stimulate the host immune system to mount a cytotoxic T-lymphocyte immune response against tumor cells expressing CEA.
- dendritic cell-gp100-MART-1 antigen vaccine
An autologous dendritic cell vaccine with antineoplastic property. Dendritic cells harvested from cancer patients are pulsed with human gp100 melanoma antigen and MART-1 antigen (a melanoma antigen recognized by T-cells); both antigens are up-regulated in melanomas. Vaccination with this vaccine may elicit the host immune response against MART-1 or gp100 expressing cells.
- dendritic cell-idiotype-keyhole limpet hemocyanin vaccine
A cell-based vaccine composed of allogeneic dendritic cells (DC), pulsed with patient-specific non-Hodgkin's lymphoma idiotype (Id) determinants conjugated to keyhole limpet hemocyanin (KLH), with potential antitumor activity. Upon administration, this vaccine may stimulate the host immune system to mount a specific cytotoxic T-lymphocyte (CTL) response against Id-expressing lymphoma cells, resulting in tumor cell lysis.
- dendritic cell-MART-1 peptide vaccine
A cancer vaccine consisting of dendritic cells harvested from a patient with cancer and pulsed or transduced with a peptide fragment of MART-1 (melanoma antigen recognized by T-cells), an antigen expressed by melanoma cells. When the altered dendritic cells are returned to the patient, they stimulate the host immune system to mount a cytotoxic T-lymphocyte immune response against tumor cells expressing MART-1.
- dendritic cell-precision multiple antigen T lymphocytes
A preparation of dendritic cell-precision multiple antigen T-cells (DC-PMAT) that have been induced to specifically target multiple undisclosed tumor-associated antigens (TAAs), with potential antitumor activity. Although the exact mechanism(s) of action through which DC-PMAT cells exert their effects has yet to be elucidated, upon infusion, these cells may stimulate the host immune system to mount a highly-specific cytotoxic T-lymphocyte (CTL) response against tumors expressing common TAAs, which leads to tumor cell lysis.
- dendritic cell-targeting lentiviral vector ID-LV305
An engineered lentiviral vector targeting dendritic cells (DCs) and containing nucleic acids encoding for the human tumor-associated cancer-testis antigen NY-ESO-1, with potential immunostimulatory and antineoplastic activities. Upon intradermal administration, the DC-targeting lentiviral vector ID-LV305 targets and binds to dermal DCs via the DC-specific intercellular adhesion molecule-3-grabbing non-integrin (DC-SIGN) receptor. Upon internalization of the vector, the NY-ESO-1 protein is expressed, stimulates DC maturation and activates the immune system to mount a cytotoxic T-lymphocyte (CTL) response against NY-ESO-1-expressing cells, which may result in tumor cell lysis. NY-ESO-1 is expressed in normal testes and on the surfaces of various tumor cells, and plays a key role in tumor cell proliferation and survival.
A recombinant peptide similar to or identical to endogenous human cytokine interleukin-21 (IL-21) with potential antineoplastic activity. Denenicokin binds to and activates IL-21 receptors, expressed on T-cells, B-cells, dendritic cells (DC), and natural killer (NK) cells, modulating the proliferation and/or differentiation of T and B cells, promoting T cell survival, and increasing the cytolytic activity of cytotoxic T lymphocytes (CTLs) and NK cells.
- denibulin hydrochloride
The hydrochloride salt of denibulin, a small molecular vascular disrupting agent, with potential antimitotic and antineoplastic activities. Denibulin selectively targets and reversibly binds to the colchicine-binding site on tubulin and inhibits microtubule assembly. This results in the disruption of the cytoskeleton of tumor endothelial cells, ultimately leading to cell cycle arrest, blockage of cell division and apoptosis. This causes inadequate blood flow to the tumor and eventually leads to a decrease in tumor cell proliferation., a small molecule vascular disrupting agent (VDA), with potential antimitotic and antineoplastic activity. Denibulin selectively targets and reversibly binds to the colchicine-binding site on tubulin and inhibits microtubule assembly. This results in the disruption of the cytoskeleton of tumor endothelial cells (EC), ultimately leading to cell cycle arrest, blockage of cell division and apoptosis. This causes inadequate blood flow to the tumor and eventually leads to a decrease in tumor cell proliferation.
- denileukin diftitox
A cytotoxic recombinant protein consisting of interleukin-2 (IL-2) protein sequences fused to diphtheria toxin. The IL-2 protein sequence moiety of denileukin difitox directs the cytocidal action of diphtheria toxin to cells that express IL-2 receptors. After the toxin moiety is internalized into target IL-2 receptor-expressing cells, its catalytic domain catalyzes the transfer of the ADP-ribose moiety of NAD to a posttranslationally modified histidine residue of elongation factor 2 (EF-2), called diphthamine. This covalent modification inactivates EF-2 and disrupts polypeptide chain elongation, resulting in cell death.
- denintuzumab mafodotin
An immunoconjugate consisting of an anti-CD19 monoclonal antibody conjugated to the auristatin derivative monomethyl auristatin F (MMAF), with potential antineoplastic activity. Upon administration of denintuzumab mafodotin, the antibody moiety targets the cell surface antigen CD19, found on a number of B-cell-derived cancers. Upon antibody/antigen binding and internalization, the immunoconjugate releases MMAF, which binds to tubulin and inhibits its polymerization. Inhibition of tubulin polymerization may result in G2/M phase arrest and tumor cell apoptosis. This causes inhibition of cell growth of CD19-expressing tumor cells. CD19, a B-cell antigen, is overexpressed by a variety of different cancer cell types.
A humanized monoclonal antibody directed against the receptor activator of nuclear factor kappa beta ligand (RANKL) with antiosteoclast activity. Denosumab specifically binds to RANKL and blocks the interaction of RANKL with RANK, a receptor located on osteoclast cell surfaces, resulting in inhibition of osteoclast activity, a decrease in bone resorption, and a potential increase in bone mineral density. RANKL, a protein expressed by osteoblastic cells, plays an important role in osteoclastic differentiation and activation.
- deoxycytidine analogue TAS-109
An analogue of the nucleoside deoxycytidine with potential antineoplastic activity. Nucleoside analogue TAS-109 is incorporated into DNA and directly inhibits the activity of DNA polymerase, which may result in inhibition of DNA replication and cell cycle arrest in the S and G2/M phases, DNA fragmentation, and tumor cell apoptosis.
Brand name for divalproex sodium
Brand name for valproic acid
Brand name for naltrexone hydrochloride
Brand name for valproic acid
Brand name for divalproex sodium
- Depakote ER
Brand name for divalproex sodium
Brand name for testosterone cypionate
- DEPDC1/MPHOSH1 peptide vaccine
A cancer vaccine containing HLA-A*2402-restricted epitopes derived from DEP domain containing 1 (DEPDC1) and M phase phosphoprotein 1 (MPHOSPH1) with potential immunostimulatory and antineoplastic activities. Upon administration, DEPDC1/MPHOSH1 peptide vaccine may elicit a specific cytotoxic T lymphocyte (CTL) response against tumor cells expressing DEPDC1 and MPHOSPH1, tumor antigens that are overexpressed in bladder cancer cells. HLA-A*2402 is an MHC class I molecule that presents antigenic peptides to CD8+ T cells; epitope design restricted to epitopes that bind most efficiently to HLA-A*2402 may improve antigenic peptide immunogenicity.
Brand name for penicillamine
Brand name for L-methylfolate
Brand name for cytarabine liposome
Brand name for dalteparin sodium
Brand name for methylprednisolone acetate
Brand name for medroxyprogesterone acetate
Brand name for testosterone cypionate
Brand name for testosterone cypionate
Brand name for therapeutic hydrocortisone
Brand name for acelullar cadaveric dermal matrix
- derma-membrane-structure topical cream
A topical cream formulation containing physiological lipids with potential anti-xerotic activity. Derma-membrane-structure topical cream contains ingredients that mirror the lipid component of the the skin, including hydrated phosphatidyl choline, but does not contain conventional emulsifiers that may disrupt the skin-lipid barrier. This cream can also be used as a vehicle or base for topically applied medications.
Brand name for deferoxamine mesylate
A fluorinated ether with general anesthetic and muscle relaxant activities. Although the exact mechanism of action has not been established, desflurane, administered by inhalation, appears to act on the lipid matirx of the neuronal membrane, resulting in disruption of neuronal transmission in the brain. This agent may also enhance the synaptic activity of the inhibitory neurotransmitter gamma-aminobutyric acid (GABA).
- desipramine hydrochloride
The hydrochloride salt form of desipramine, a secondary amine tricyclic antidepressant (TCA). In the central nervous system (CNS), desipramine hydrochloride blocks the re-uptake of neurotransmitters, including norepinephrine and serotonin. This leads to an increase in the amount of these neurotransmitters in the synaptic cleft and prolongs their activities postsynaptically.
- deslorelin acetate
A synthetic nonapeptide analogue of the natural gonadotrophin releasing hormone (GnRH) with potential antineoplastic activity. Deslorelin binds to and activates pituitary gonadotropin releasing hormone (GnRH) receptors. Continuous, prolonged administration of goserelin in males results in pituitary GnRH receptor desensitization and inhibition of pituitary secretion of follicle stimulating hormone (FSH) and luteinizing hormone (LH), leading to a significant decline in testosterone production; in females, prolonged administration results in a decrease in estradiol production.
- desmopressin acetate
An analogue of the hormone vasopressin with antidiuretic and antihemorrhagic properties. Desmopressin acetate has selective affinity for the V2 receptor and acts on the distal kidney tubule by increasing the cellular permeability thereby stimulating water reabsorption. This antidiuretic agent is used in the treatment of central diabetes insipidus. An unrelated action of desmopressin acetate is to increases circulating factor VIII and is used in patients with haemophilia and von Willebrand's disease.
A synthetic progestogen structurally related to levonorgestrel, with progesterone hormone receptor agonistic activity, used as a contraceptive and hormone replacement agent. Upon administration, desogestrel binds intracellular progesterone receptors in progesterone responsive tissue and the resultant complex interacts with DNA causing either gene transcription or gene repression. This eventually leads to an inhibition of gonadotropin releasing hormone (GnRH) secretion from the hypothalamus and a subsequent inhibition of luteinizing hormone (LH) and follicle-stimulating hormone (FSH) release. This prevents ovulation and alters the cervical mucus.
- desvenlafaxine succinate
The succinate salt form of desvenlafaxine, a synthetic phenethylamine bicyclic derivative with antidepressant activity. Desvenlafaxine is a selective reuptake inhibitor of serotonin and norepinephrine due to its high binding affinities to the pre-synaptic serotonin and norepinephrine transporters. By blocking both transporters, this agent prolongs neurotransmitter activities of both serotonin and norepinephrine, thereby alleviating depressive state.
A semi-synthetic derivative of the anthracycline antineoplastic antibiotic daunorubicin. Detorubicin intercalates into DNA and interacts with topoisomerase II, thereby inhibiting DNA replication and repair and RNA and protein synthesis. This agent also produces toxic free-radical intermediates and interacts with cell membrane lipids causing lipid peroxidation. Detorubicin is less toxic than daunorubicin. Check for active clinical trialsusing this agent.
- Detox-B adjuvant
A cancer vaccine adjuvant that consists of an oil droplet emulsion of monophosphoryl lipid A and mycobacterial cell wall skeleton. Detox-B adjuvant is a non-specific immunostimulant that may enhance the host immune response to certain cancer vaccines. Detox-B differs from Detox adjuvant in that Detox-B contains lecithin.
A detoxified, nonspecific immunostimulant consisting of a combination of the active monophosphoryl lipid A component of lipopolysaccharide (LPS) isolated from the bacterium Salmonella minnesota combined with a residue of the cell wall of the bacterium Mycobacterium phlei. Detox-PC differs from Detox adjuvant and Detox-B in that Detox-PC contains egg phosphatidylcholine and alpha-tocopherol. Check for active clinical trialsusing this agent.
- deuterated 3-methylhistidine
A derivative of the amino acid histidine labeled with heavy hydrogen (D) used in diagnostic procedures. Upon intake of deuterated 3-methylhistidine (3-MH), this agent is incorporated into muscle protein and then is subsequently excreted unchanged in the urine. By measuring the amount of 3-MH in the urine, via analysis of deuterium, the rate of protein muscle catabolism can be determined and the risk of skeletal muscle atrophy or cachexia can be assessed. 3-methylhistidine is a myofibrillar-specific amino acid and is mainly found in muscle myosin and actin; proteolysis of myofibrils releases 3-MH that is excreted unchanged in the urine.
- deuterated enzalutamide
A deuterated form of enzalutamide, an orally bioavailable, organic, non-steroidal small molecule targeting the androgen receptor (AR) with potential antineoplastic activity. Upon administration, deuterated enzalutamide competitively binds to and inhibits the activity of ARs expressed on prostate cancer cells, which impairs nuclear translocation and DNA binding, resulting in apoptosis of prostate cancer cells. This results in a reduction in prostate cancer cell growth. AR overexpression in prostate cancer represents a key mechanism associated with prostate cancer hormone resistance. Deuterium incorporation, by replacing the hydrogen atoms of the N-CH3 moiety with deuterium atoms, decreases enzalutamide's metabolism and allows for an increased pharmacokinetic profile, thereby enhancing its anti-tumor efficacy compared to non-deuterated enzalutamide. As the deuterated form can’t cross the blood-brain barrier (BBB), the deuterated form also reduces the unwanted brain-related side effects of enzalutamide and improves its safety profile.
- deuterated phenanthrene
A noncarcinogenic and structural analogue of polycyclic aromatic hydrocarbon (PAH), phenanthrene labeled with deuterium ([D10]Phe) with potential use in assessing an individual’s capacity for PAH metabolism by the diol epoxide pathway. Upon oral or inhalation administration, [D10]Phe is metabolized into the tetraol end product ([D10]PheT) via the diol epoxide pathway, and can be quantified in urine. [D10]PheT can be used as a biomarker to assess PAHs metabolic activation and may therefore determine an individual’s susceptibility to carcinogenicity upon PAH exposure.
- deuterium oxide
A stable, non-radioactive isotopic form of water, containing 2 atoms of deuterium (D) and one atom of oxygen (2D2O), with DNA-labeling activity. Upon ingestion of deuterium oxide, 2H is incorporated into the deoxyribose moiety of DNA of newly divided cells. Rapidly dividing cells, as in the case of B-cell chronic lymphocytic leukemia (B-CLL), can be labeled with deuterium oxide and measured using gas chromatography and/or mass spectrometry.
A synthetic adrenal corticosteroid with potent anti-inflammatory properties. In addition to binding to specific nuclear steroid receptors, dexamethasone also interferes with NF-kB activation and apoptotic pathways. This agent lacks the salt-retaining properties of other related adrenal hormones.
- dexamethasone intravitreal implant
An intravitreal implant containing the corticosteroid dexamethasone embedded in a biodegradable polymer matrix, with anti-inflammatory and macular edema-relieving activity. Upon insertion into the vitreous cavity, dexamethasone intravitreal implant is dissolved slowly and dexamethasone is released over an extended period of time. Dexamethasone inhibits inflammation thereby preventing leakage from the capillaries and a reduction of retinal edema. This may ultimately prevent vision impairment.
Brand name for dextroamphetamine sulfate
A synthetic, terpene-based cannabinoid derivative devoid of cannabinoid receptors 1 and 2 agonist activity and with potential neuroprotective, antiinflammatory and antineoplastic activities. Functioning as an N-Methyl-D-aspartate (NMDA) receptor antagonist, dexanabinol protects neuronal cells against NMDA and glutamate neurotoxicity. This agent also scavenges peroxy radicals and protects neurons from the damages of reactive oxygen species. Furthermore, dexanabinol inhibits the activity of nuclear factor kappa B (NF-kB), thereby preventing the expression of NF-kB target genes, such as tumor necrosis factor alpha, cytokines and inducible nitric oxide synthase. As a result, this agent may restore apoptotic processes in cancerous cells. NF-kB is activated in a variety of cancer cells and plays a key role in the regulation of apoptosis and cellular proliferation.
Brand name for dextroamphetamine sulfate
- dexmedetomidine hydrochloride
The hydrochloride salt form of dexmedetomidine, an imidazole derivate and active d-isomer of medetomidine with analgesic, anxiolytic and sedative activities. Dexmedetomidine selectively binds to and activates presynaptic alpha-2 adrenoceptors located in the brain, thereby inhibiting the release of norepinephrine from synaptic vesicles. This leads to an inhibition of postsynaptic activation of adrenoceptors, which inhibits sympathetic activity, thereby leading to analgesia, sedation and anxiolysis.
- dexpanthenol cream
An alcoholic analogue of D-pantothenic acid and cholinergic agent. Dexpanthenol acts as a precursor of coenzyme A necessary for acetylation reactions and is involved in the synthesis of acetylcholine. Although the exact mechanism of the actions of dexpanthenol is unclear, it may enhance the effect of acetylcholine. Dexpanthenol acts on the gastrointestinal tract and increases lower intestinal motility. It is also applied topically to the skin to relieve itching and to promote healing.
- dexpanthenol mouthwash
A mouthwash containing 5% dexpanthenol, the alcoholic analogue of the dextrorotatory isomer of pantothenic acid with potential antimucositis activity. Although the exact mechanism remains to be elucidated, upon rinsing with this solution dexpanthenol is converted to pantothenic acid (vitamin B5) which is required for coenzyme A synthesis as well as for the metabolism of proteins, carbohydrates, and fats. Coenzyme A is involved in fatty acids and sphingolipids synthesis crucial for cell membrane integrity. This mouthwash may have a protective and healing effect on the oral mucosa, may improve hydration and may potentially prevent or reduce radiation/chemotherapy-induced mucositis.
- dexrazoxane hydrochloride
The hydrochloride salt of a bisdioxopiperazine with iron-chelating, chemoprotective, cardioprotective, and antineoplastic activities. After hydrolysis to an active form that is similar to ethylenediaminetetraacetic acid (EDTA), dexrazoxane chelates iron, limiting the formation of free radical-generating anthracycline-iron complexes, which may minimize anthracycline-iron complex-mediated oxidative damage to cardiac and soft tissues. This agent also inhibits the catalytic activity of topoisomerase II, which may result in tumor cell growth inhibition.
Brand name for maltodextrin
- dextroamphetamine sulfate
The salt of the dextro-isomer of amphetamine and sympathomimetic amine with CNS stimulating properties. Dextroamphetamine sulphate acts by facilitating the release of catecholamines, particularly noradrenaline and dopamine, from nerve terminals in the brain and inhibits their uptake. This leads to an increase in motor activity, causes euphoria, mental alertness and excitement and suppresses appetite. This drug causes dependence and may cause an increase in heart rate and blood pressure. It is used in the treatment of narcolepsy and attention deficit hyperactivity disorder.
A combination of two synthetic agents with central nervous system stimulant activity. Both agents are non-catecholamine, sympathomimetic agents that elevate blood pressure and cause bronchodilation. These agents are commonly abused psychostimulant drugs that induce psychologic dependence manifested by elevated mood, increased wakefulness, concentration, physical performance and a feeling of well-being. Tolerance to various effects develops unequally, so that tachycardia and enhanced alertness diminish while psychotoxic effects (hallucinations and delusions) may occur.
- dextromethorphan hydrobromide
The hydrobromide salt form of dextromethorphan, a synthetic, methylated dextrorotary analogue of levorphanol, a substance related to codeine and a non-opioid derivate of morphine. Dextromethorphan exhibits antitussive activity and is devoid of analgesic or addictive property. This agent crosses the blood-brain-barrier and activates sigma opioid receptors on the cough center in the central nervous system, thereby suppressing the cough reflex.
- dextropropoxyphene hydrochloride
The hydrochloride salt of the d-isomer of the synthetic opiate propoxyphene with weak narcotic analgesic activity. Dextropropoxyphene mimics the effects of endogenous opiates by binding to mu receptors located throughout the central nervous system. The binding results in GTP to GDP exchanges on the mu-G-protein complex, by which the effector adenylate cyclase is inactivated, decreasing intracellular cAMP. This, in turn, inhibits the release of various nociceptive neurotransmitters, such as substance P, gamma-aminobutyric acid (GABA), dopamine, acetylcholine, noradrenaline, vasopressin, and somatostatin. In addition, dextropropoxyphene closes N-type voltage-gated calcium channels and opens calcium-dependent inwardly rectifying potassium channels, which results in neuronal hyperpolarization, a reduction in neuronal excitability, and a further decrease in the perception of pain.
Brand name for dextroamphetamine sulfate
The R-enantiomer of the calcium channel blocker verapamil. Dexverapamil competitively inhibits the multidrug resistance efflux pump P-glycoprotein (MDR-1), thereby potentially increasing the effectiveness of a wide range of antineoplastic drugs which are inactivated by MDR-1 mechanisms. This agent exhibits decreased calcium antagonistic activity and toxicity compared to racemic verapamil.
A fully humanized monoclonal IgG1 anti-serum amyloid P component (SAP) antibody, with potential anti-amyloid activity. Upon intravenous administration, dezamizumab binds to SAP in amyloid deposits, thereby activating compliment and triggering the rapid clearance of amyloid by macrophage-derived multinucleated giant cells. SAP is a universal component of amyloid deposits and contributes to the pathogenesis of amyloidosis.
- DHAP regimen
A chemotherapy regimen consisting of dexamethasone, high-dose cytarabine (ARA-C) and cisplatin (Platinol), used for the treatment of relapsed and refractory Hodgkin and non-Hodgkin lymphomas.
A prodrug comprised of the naturally occurring omega-3 fatty acid docosahexaenoic acid (DHA) covalently conjugated to the anti-microtubule agent paclitaxel. Because tumor cells take up DHA, DHA-paclitaxel is delivered directly to tumor tissue, where the paclitaxel moiety binds to tubulin and inhibits the disassembly of microtubules, thereby resulting in the inhibition of cell division. Paclitaxel also induces apoptosis by binding to and blocking the function of the apoptosis inhibitor protein Bcl-2 (B-cell Leukemia 2). DHA-paclitaxel exhibits improved pharmacokinetic and toxicity profiles when compared to conventional paclitaxel and has demonstrated antineoplastic activity in animal models of cancer.
- DHEA mustard
A steroidal alkylating agent with potential antineoplastic activity. Alkylating agents exert cytotoxic and, in some cases, chemotherapeutic effects by transferring alkyl groups to DNA, thereby damaging DNA and interfering with DNA replication and cell division.
- dHER2+AS15 vaccine
A cancer vaccine consisting of a truncated recombinant HER2/neu peptide (dHER2) combined with the immunoadjuvant AS15 with potential immunostimulatory and antineoplastic activities. Upon administration, dHER2+AS15 vaccine may stimulate the host immune response to mount a cytotoxic T-lymphocyte (CTL) response against tumor cells that overexpress the HER2/neu protein, resulting in tumor cell lysis. The tumor-associated antigen (TAA) HER2/neu is often overexpressed by a variety of tumor cell types; dHER2 includes amino acids 1-645 or 1-653 of the extracellular domain (ECD) and an immunogenic carboxyl terminal autophosphorylation portion of the intracellular domain (ICD). AS15 is an adjuvant formulation that contains the adjuvant systems AS01B and AS07A; AS01 B is composed of liposomes containing 3D-MPL and QS21 and AS07A is composed of the synthetic oligodeoxynucleotide (ODN) Toll-like receptor-9 (TLR9) agonist CpG 7909.
Brand name for glyburide
Brand name for chlorpropamide
- diacetylmorphine hydrochloride
The hydrochloride salt of a diacetyl derivative of the opiate morphine, a naturally occurring alkaloid extracted from the seedpod of the Asian poppy (Papaver sp.). Once administered, diamorphine (or diacetylmorphine) is rapidly hydrolyzed to 6-monoacetylmorphine (6-MAM) and then to the end-product morphine which binds to opiate receptors located throughout the mammalian nervous and gastrointestinal systems. Inducing a potent analgesia, the use of diamoprhine is often escalated due to a tolerance effect, resulting in abuse that is associated with fatal overdose, abortion, venous sclerosis, and opportunistic infections, among other adverse effects.
- diammonium glycyrrhizinate
The diammonium salt of glycyrrhizin and the active constituent in the traditional Chinese medicinal herb Glycyrrhiza uralensis (Chinese liquorice or Gan-Cao) with anti-inflammatory, antioxidant and hepatoprotective properties. Diammonium glycyrrhizinate (DG) is slowly metabolized within the cells into glycyrrhetic acid, which inhibits enzymes that control cortisol metabolism and contributes to this agent's anti-inflammatory effect. Although the exact mechanism of action remains to be fully elucidated, DG may prevent or reduce hepatotoxicity via the scavenging of free radicals. This agent also upregulates the expression of transcription coactivator PGC-1alpha and modulates hepatic enzymes such as alanine aminotransferase (ALT), aspartate aminotransferase (AST), superoxide dismutase and glutathion peroxidase.
Brand name for acetazolamide sodium
A bifunctional hexitol derivative with potential antineoplastic activity. Dianhydrogalactitol alkylates and cross-links DNA via an epoxide group during all phases of the cell cycle, resulting in disruption of DNA function and cell cycle arrest.
Brand name for diethylstilbestrol
A small-molecule inhibitor of the RAS/RAF/MAPK signaling pathway with potential antineoplastic activity. Diazepinomicin binds to and inhibits Ras kinase, thereby preventing the phosphorylation and activation of proteins downstream of the Ras signal transduction pathway, including serine/threonine kinase RAF (BRAF) and extracellular signal-regulated kinases 1 and 2 (ERK1 and ERK-2). This agent also selectively binds to the peripheral benzodiazepine receptor (PBR), a receptor highly expressed in certain tumor cell types cells, inducing cell cycle arrest and apoptosis in PBR-expressing cells. Diazepinomicin can cross the blood-brain barrier (BBB).
A synthetic bifunctional quinone derivative with potential antineoplastic activity. Diaziquone alkylates and cross-links DNA during all phases of the cell cycle, resulting in disruption of DNA function, cell cycle arrest, and apoptosis. This agent can also form free radicals, thereby initiating DNA damage via DNA strand breaks. Due to its lipophilicity, diaziquone readily crosses the blood brain barrier.
An L-glutamine diazo analogue amino acid antibiotic isolated from a species of the bacterial genus Streptomyces with potential antineoplastic activity. Diazooxonorleucine inhibits several glutamine-dependent biosynthetic pathways involved in the the syntheses of D-glucosamine phosphate, purines and pyrimidines. This agent inhibits phosphate-activated glutaminase, a key enzyme for the synthesis of releasable glutamine, depleting cells of this essential amino acid and reducing their capacity to proliferate.
A benzothiadiazine derivate with antihypertensive and hyperglycemic activities. Diazoxide increases membrane permeability to potassium ions in vascular smooth muscle, thereby stabilizing the membrane action potential and preventing vascular smooth muscle contraction; this results in peripheral vasodilatation and decreases in peripheral vascular resistance. This agent also inhibits insulin release by interacting with ATP-sensitive potassium channels of pancreatic islet beta-cells.
Brand name for phenoxybenzamine hydrochloride
A chlorinated methotrexate derivative. Dichloromethotrexate inhibits the enzyme dihydrofolate reductase, thereby preventing the synthesis of purine nucleotides and thymidylates and inhibiting DNA and RNA synthesis. This agent is metabolized and excreted by the liver.
- diclofenac epolamine patch
A topical patch containing the epolamine salt form of the nonsteroid anti-inflammatory drug (NSAID) diclofenac, with anti-inflammatory, anti-pyretic and analgesic activities. Upon topical application of the diclofenac epolamine patch to a specific area, the patch releases diclofenac epolamine into the skin. Diclofenac locally binds to cyclooxygenase isoforms 1 and 2 (COX-1 and -2). The inhibition of COX-2 by diclofenac prevents the COX-2-mediated synthesis of proprostaglandins (PGs) and thereby locally relieves PG-mediated pain, fever and inflammation.
- diclofenac sodium
The sodium salt form of diclofenac, a benzene acetic acid derivate and nonsteroidal anti-inflammatory drug (NSAID) with analgesic, antipyretic and anti-inflammatory activity. Diclofenac sodium is a non-selective reversible and competitive inhibitor of cyclooxygenase (COX), subsequently blocking the conversion of arachidonic acid into prostaglandin precursors. This leads to an inhibition of the formation of prostaglandins that are involved in pain, inflammation and fever.
- diclofenac sodium gel
A gel formulation of the sodium salt of diclofenac, a nonsteroidal benzeneacetic acid derivative with analgesic, antipyretic and anti-inflammatory activities. Diclofenac binds to and chelates both isoforms of cyclooxygenase (COX-1 and-2), thereby blocking the conversion of arachidonic acid (AA) to pro-inflammatory prostaglandins. This agent may also inhibit lipoxygenases, resulting in the inhibition of pro-inflammatory leukotriene synthesis from AA.
A synthetic nucleoside analogue of deoxyadenosine in which the 3' hydroxyl on the ribose moiety is replaced by a hydrogen atom. In vivo, didanosine is converted to the active triphosphate form, which is incorporated into DNA. The absence of the 3' hydroxyl inhibits DNA elongation because phosphodiester bonds cannot be made with the substituted hydrogen.
- didemnin B
A cyclic depsipeptide extracted from the Caribbean tunicate Trididemnum cyanophorum. Didemnin B activates caspase, thereby inducing apoptosis, and prevents eukaryotic elongation factor 2 (eEF-2)-dependent translocation, thereby inhibiting protein synthesis. This agent also has immunosuppressive and antiviral properties.
A synthetic nucleoside analogue of deoxyadenosine and a prodrug of didanosine in which the 3' hydroxyl group on the ribose moiety is replaced by a hydrogen atom. Dideoxyadenosine competitively inhibits adenylyl cyclase, thereby reducing levels of cyclic adenosine monophosphate (cAMP). By inhibiting cAMP-mediated gene activation in tumor cells, this agent may retard tumor cell proliferation. Check for active clinical trialsusing this agent.
An orally-active, semisynthetic, fourth generation, nonethinylated progestogen with potential antiproliferative, antiandrogenic, anti-inflammatory and antiangiogenic activities that is used in hormone therapy and as a female contraceptive. Upon oral administration, dienogest binds intracellular progesterone receptors which then translocate to the nucleus where the drug-receptor complex interacts with progesterone response elements, thus altering the expression of target genes. Dienogest reduces the production of estradiol, prevents ovulation and alters the cervical mucus and endometrium. In addition, dienogest appears to suppress the expression of cell cycle regulator cyclin D1. Altogether, this may prevent the growth of endometrial epithelial cells and may reduce symptoms associated with leiomyoma.
A sulfhydryl-containing carbamate that is the primary in vivo metabolite of disulfiram. Diethyldithiocarbamate chelates zinc, thereby inhibiting metalloproteinases, thereby preventing the degradation of the extracellular matrix and inhibiting an initial step in cancer metastasis and angiogenesis. A known inhibitor of superoxide dismutase, this agent can either potentiate or protect against cell oxidative damage caused by ionizing radiation, depending on the time of administration.
DES; the acronym for diethylstilbestrol, a synthetic, nonsteroidal form of estrogen. A well-known teratogen and carcinogen, DES inhibits the hypothalamic-pituitary-gonadal axis, thereby blocking the testicular synthesis of testosterone, lowering plasma testosterone, and inducing a chemical castration. Check for active clinical trialsusing this agent.
Brand name for benzydamine hydrochloride
Brand name for dimethicone-containing botanicals-based lotion
Brand name for fluconazole
A difluorophenyl derivate of salicylic acid and a nonsteroidal anti-inflammatory drug (NSAID) with antipyretic, analgesic and anti-inflammatory properties. Diflunisal competitively inhibits both cyclooxygenase (COX) -1 and -2, with higher affinity for COX-1, and subsequently blocks the conversion of arachidonic acid to prostaglandin precursors. This leads to an inhibition of the formation of prostaglandins that are involved in pain, inflammation and fever. Diflunisal differs from other salicylates, in that it is not metabolized to salicylic acid, hence it has a longer half-life.
A cardiac glycoside. Digoxin inhibits the sodium potassium adenosine triphosphatase (ATPase) pump, thereby increasing intracellular calcium and enhancing cardiac contractility. This agent also acts directly on the atrioventricular node to suppress conduction, thereby slowing conduction velocity. Apparently due to its effects on intracellular calcium concentrations, digoxin induces apoptosis of tumor cells via a pathway involving mitochondrial cytochrome c and caspases 8 and 3.
A synthetic nucleoside analogue of deoxycytidine. Dihydro-5-azacytidine inhibits DNA methyltransferase, thereby interfering with abnormal DNA methylation patterns that are associated with genetic instability in some tumor cells. Inhibition of this enzyme may restore expression of tumor-suppressor genes and result in antitumor activity.
A butyrophenone that has been investigated for antineoplastic activity.
- dihydroorotate dehydrogenase inhibitor AG-636
An orally available inhibitor of dihydroorotate dehydrogenase (DHODH), with potential antineoplastic activity. Upon administration, AG-636 specifically targets, binds to and prevents the activation of DHODH, thereby preventing the fourth enzymatic step in de novo pyrimidine synthesis. This prevents uridine monophosphate (UMP) formation, DNA synthesis, cell division and cellular proliferation, causes reactive oxygen species (ROS) formation, enables differentiation and induces apoptosis in susceptible tumor cells. DHODH, a mitochondrial enzyme, catalyzes the conversion of dihydroorotate (DHO) to orotate in the endogenous synthesis of UMP.
- dihydroorotate dehydrogenase inhibitor ASLAN003
An orally available inhibitor of dihydroorotate dehydrogenase (DHODH), with potential antineoplastic activity. Upon administration, ASLAN003 specifically targets, binds to and prevents the activation of DHODH, thereby preventing the fourth enzymatic step in de novo pyrimidine synthesis. This prevents uridine monophosphate (UMP) formation, DNA synthesis, cell division and cellular proliferation, causes reactive oxygen species (ROS) formation, enables differentiation and induces apoptosis in susceptible tumor cells. DHODH, a mitochondrial enzyme, catalyzes the conversion of dihydroorotate (DHO) to orotate in the endogenous synthesis of UMP.
- dihydroorotate dehydrogenase inhibitor BAY2402234
An orally available inhibitor of dihydroorotate dehydrogenase (DHODH), with potential antineoplastic activity. Upon administration, BAY2402234 specifically targets, binds to and prevents the activation of DHODH, thereby preventing the fourth enzymatic step in de novo pyrimidine synthesis. This prevents uridine monophosphate (UMP) formation, DNA synthesis, cell division and cellular proliferation, causes reactive oxygen species (ROS) production, enables differentiation and induces apoptosis in susceptible tumor cells. DHODH, a mitochondrial enzyme, catalyzes the conversion of dihydroorotate (DHO) to orotate in the endogenous synthesis of UMP.
The most potent androgen, required for sex development. Dihydrotestosterone is synthesized from testosterone in the prostate gland, testes, hair follicles and adrenal glands by 5-alpha reductase. Dihydrotestosterone exerts its action similar to testosterone, which binds to and activates specific nuclear androgen receptors. After translocation into the nucleus, the activated hormone-receptor complex binds to the androgen response elements on the DNA and activates gene expressions that are required for sex development. Dihydrotestosterone is responsible for the formation of male primary sex characteristics and most male secondary sex characteristics during puberty, such as muscular growth, facial and body hair growth, and deepening of the voice.
A phytonutrient and plant indole found in cruciferous vegetables including broccoli, brussels sprouts, cabbage, cauliflower and kale, with potential antiandrogenic and antineoplastic activities. As a dimer of indole-3-carbinol, diindolylmethane (DIM) promotes beneficial estrogen metabolism in both sexes by reducing the levels of 16-hydroxy estrogen metabolites and increasing the formation of 2-hydroxy estrogen metabolites, resulting in increased antioxidant activity. Although this agent induces apoptosis in tumor cells in vitro, the exact mechanism by which DIM exhibits its antineoplastic activity in vivo is unknown.
Brand name for hydromorphone hydrochloride
- Dilaudid HP
Brand name for hydromorphone hydrochloride
- DI-Leu16-IL2 immunocytokine
A recombinant fusion protein consisting of de-immunized and humanized anti-CD20 monoclonal antibody Leu16 fused to human cytokine interleukin-2 (IL2) with potential antineoplastic activity. The antibody moiety of DI-Leu16-IL2 immunocytokine binds to tumor cells expressing the CD20 antigen, which may result in an antibody-dependent cell-mediated cytotoxicity (ADCC) towards CD20-expressing tumor cells; the localized IL2 moiety of this fusion protein may stimulate natural killer (NK) and T-lymphocyte mediated immune responses, enhancing the ADCC response. De-immunization involves the modification of potential helper T cell epitopes that bind to MHC class II molecules; humanization involves combining recombinant murine variable (V) regions with human immunoglobulin light and heavy chain constant regions. CD20 antigen, a hydrophobic transmembrane protein located on normal pre-B and mature B lymphocytes, is overexpressed by various cancer cell types.
- diltiazem hydrochloride
A benzothiazepine calcium channel blocking agent. Diltiazem hydrochloride inhibits the transmembrane influx of extracellular calcium ions into select myocardial and vascular smooth muscle cells, causing dilatation of coronary and systemic arteries and decreasing myocardial contractility. Because of its vasodilatory activity, this agent has been shown to improve the microcirculation in some tumors, thereby potentially improving the delivery of antineoplastic agents to tumor cells.
Brand name for liposomal T4N5 lotion
A synthetic derivative of dithio-ethane sulfonate with uroprotective properties. In the kidney, dimesna undergoes reduction to the free thiol compound, mesna, which reacts chemically with the urotoxic ifosfamide metabolites acrolein and 4-hydroxy-ifosfamide, resulting in their detoxification. This agent also inhibits cyclophosphamide-induced hemorrhagic cystitis.
- dimethicone-containing botanicals-based lotion
A skin lotion containing various proprietary botanical ingredients and the skin protectant dimethicone, a silicon-based polymer, with potential to prevent radiation dermatitis (RD). Upon topical application to the affected area before and after radiation therapy, the phytochemicals in the dimethicone-containing botanicals-based lotion may act as free radical scavengers and exert an antioxidant effect. The dimethicone component of the skin lotion protects against damage, and moisturizes and soothes the skin. Check for active clinical trialsusing this agent.
- dimethyl fumarate
An orally bioavailable methyl ester of fumaric acid and activator of nuclear factor erythroid 2 [NF-E2]-related factor 2 (Nrf2, Nfe2l2), with potential neuroprotective, immunomodulating and radiosensitizing activities. Although the exact mechanism of action through which dimethyl fumarate exerts its neuroprotective and immunomodulatory effects have yet to be fully understood, upon oral administration, dimethyl fumarate is converted into its active metabolite monomethyl fumarate (MMF) and MMF binds to Nrf2. Subsequently, Nrf2 translocates to the nucleus and binds to the antioxidant response element (ARE). This induces the expression of a number of cytoprotective genes, including NAD(P)H quinone oxidoreductase 1 (NQO1), sulfiredoxin 1 (Srxn1), heme oxygenase-1 (HO1, HMOX1), superoxide dismutase 1 (SOD1), gamma-glutamylcysteine synthetase (gamma-GCS), thioredoxin reductase-1 (TXNRD1), glutathione S-transferase (GST), glutamate-cysteine ligase catalytic subunit (Gclc) and glutamate-cysteine ligase regulatory subunit (Gclm); this also increases the synthesis of the antioxidant glutathione (GSH). The intraneuronal synthesis of GSH may protect neuronal cells from damage due to oxidative stress. Dimethyl fumarate also appears to inhibit the nuclear factor-kappa B (NF-kB)-mediated pathway, modulates the production of certain cytokines and induces apoptosis in certain T-cell subsets. Its radiosensitizing activity is due to this agent's ability to bind to and sequester intracellular GSH, thereby depleting intracellular GSH and preventing its anti-oxidative effects. This enhances the cytotoxicity of ionizing radiation in hypoxic cancer cells. Nrf2, a leucine zipper transcription factor, plays a key role in redox homeostasis and cytoprotection against oxidative stress.
- dimethyl sulfoxide
A polar organic solvent. DMSO is a free radical scavenger that has been used to treat extravasation damage caused by anthracycline-based chemotherapy.
An aliphatic analogue of busulfan with potential antineoplastic activity. As an alkylating agent, dimethylbusulfan induces neutropenia and has been shown to exhibit antitumor effects in some animal models. Alkylating agents exert cytotoxic and chemotherapeutic effects by transferring alkyl groups to DNA, thereby damaging DNA and interfering with DNA synthesis and cell division. Check for active clinical trialsusing this agent.
Brand name for hydromorphone hydrochloride
A pyrazolo[1,5-a]pyrimidine with potential antineoplastic activity. Dinaciclib selectively inhibits cyclin dependent kinases CDK1, CDK2, CDK5, and CDK9; inhibition of CDK1 and CDK2 may result in cell cycle repression and tumor cell apoptosis.
A small molecule containing 2 phenol rings, characterized as a hapten for use in vaccine preparation. Dinitrophenyl by itself will not elicit any immune response nor bind to antigen. Dinitrophenyl compound is commonly used to couple with peptides in vaccine preparation to enhance the immunogenicity of otherwise weak immunogenic antigens.
- dinoprost tromethamine
A synthetic analogue of the naturally occurring prostaglandin F2 alpha. Prostaglandin F2 alpha stimulates myometrial activity, relaxes the cervix, inhibits corpus luteal steroidogenesis, and induces luteolysis by direct action on the corpus luteum.
A chimeric mouse/human monoclonal antibody with potential antineoplastic activity. Dinutuximab binds to the ganglioside GD2 and induces antibody-dependent cell-mediated cytotoxicity and complement-dependent cytotoxicity against GD2-expressing tumor cells. GD2 is overexpressed in malignant melanoma, neuroblastoma, osteosarcoma, and small cell carcinoma of the lung.
- Dioscorea nipponica Makino extract DNE3
An extract of the plant Dioscorea nipponica Makino and inhibitor of both the serine/threonine protein kinase Akt (protein kinase B) and members of the phosphatidylinositol 3-kinase (PI3K) family of lipid kinases, with potential antineoplastic and anti-metastatic activities. Dioscorea nipponica Makino extracted with ethyl acetate (DNE3) binds to and inhibits PI3K and Akt. This inhibits PI3K/Akt-mediated signaling and prevents both growth and survival of PI3K/Akt-overexpressing tumor cells. In addition, DNE3 increases the expression of tissue inhibitor of metalloproteinase-2 (TIMP-2), inhibits the secretion of matrix metalloproteinases (MMPs), primarily MMP-2 and MMP-9, and inhibits the serine protease urokinase (urokinase-type plasminogen activator; u-PA). This inhibits tumor cell invasion, migration, motility, and adhesion. This agent also inhibits the activation of both cAMP response element-binding (CREB) and activating protein-1 (AP-1), and increases the expression of IkappaB (IkB), which inhibits the activation of nuclear factor-kappa B (NF-kB). These processes further contribute to this agent's anti-tumor potential in susceptible tumor cells.
Brand name for valsartan
A synthetic, potent allergic contact sensitizer with potential immunostimulatory activity. After sensitization process by repeated topical application of diphencyprone to a specific area, further application of this agent to the affected area may stimulate an immune response and may potentially be useful to clear the affected area from infection or cancer.
- diphenhydramine hydrochloride
The hydrochloride salt form of diphenhydramine, an ethanolamine and first-generation histamine antagonist with anti-allergic activity. Diphenhydramine hydrochloride competitively blocks H1receptors, thereby preventing the actions of histamine on bronchial smooth muscle, capillaries, and gastrointestinal (GI) smooth muscle. This prevents histamine-induced bronchoconstriction, vasodilation, increased capillary permeability, and GI smooth muscle spasms.
- diphenhydramine hydrochloride/dexamethasone/nystatin magic mouthwash
An oral suspension containing diphenydramine hydrochloride, dexamethasone and nystatin, with anithistaminic, antiinflammatory, and antifungal activities. Diphenhydramine hydrochloride/dexamethasone/nystatin magic mouthwash inhibits the cytokine-mediated inflammation and yeast colonization of the oral mucosa associated with chemotherapy and radiation therapy.
- diphtheria toxin fragment-interleukin-2 fusion protein E7777
A cytotoxic recombinant fusion protein consisting of the human cytokine interleukin-2 (IL-2) fused to diphtheria toxin fragments A and B, containing both the catalytic and translocation domains, with potential antineoplastic activity. Upon administration, the IL-2 moiety of diphtheria toxin fragment-IL-2 fusion protein E7777 binds to IL-2 receptors. After internalization by IL-2 receptor-expressing cells via endocytosis, the agent is proteolytically cleaved. This releases the catalytic domain of the toxin moiety, which catalyzes the transfer of the ADP-ribose moiety of NAD to a diphthamide residue of elongation factor 2 (EF-2). This covalent modification inactivates EF-2 and disrupts polypeptide chain elongation, resulting in an inhibition of translation and cell death. E7777 has the same amino acid sequence as denileukin diftitox (DD), but has an increased purity profile and an increased percentage of monomeric, active protein, which improves its efficacy.
- diphtheria toxoid/tetanus toxoid vaccine adsorbed
A vaccine containing detoxified tetanus toxoid and detoxified diphtheria toxoid adsorbed on aluminum phosphate with active immunizing activity against diphtheria and tetanus. Intramuscular injection with this vaccine activates the immune system to develop antibodies against tetanus toxin and diphtheria toxin.
- diphtheria toxoid/tetanus toxoid/acellular pertussis adsorbed, recombinant hepatitis B/inactivated poliovirus vaccine combined
A vaccine consisting of detoxified tetanus toxoid, detoxified diphtheria toxoid, acellular pertussis antigens, inactivated poliovirus (IPV) types 1,2 and 3 and hepatitis B (HBV) surface antigen, with active immunizing activities against diphtheria, tetanus, pertussis, hepatitis B, and poliomyelitis. The acellular pertussis components in this vaccine, produced by Bordetella pertussis, are detoxified pertussis toxin (PT), filamentous hemagglutinin (FHA) and pertactin (PRN). Upon intramuscular injection, this vaccine activates the immune system to develop antibodies against tetanus toxin, diphtheria toxin, B. pertussis antigens, polioviruses and HBV. The diphtheria and tetanus toxoids and pertussis antigens (inactivated PT, FHA, and pertactin) are adsorbed onto aluminum hydroxide; the hepatitis B antigen is adsorbed onto aluminum phosphate.
- diphtheria toxoid/tetanus toxoid/acellular pertussis vaccine adsorbed
A vaccine containing detoxified tetanus toxoid, detoxified diphtheria toxoid and acellular pertussis antigens, adsorbed on aluminum phosphate, with active immunizing activity against diphtheria, tetanus and pertussis. The acellular pertussis vaccine components, produced by Bordetella pertussis, are detoxified pertussis toxin (PT), filamentous hemagglutinin (FHA), pertactin (PRN) and fimbriae types 2 and 3 (FIM). Intramuscular injection with this vaccine activates the immune system to develop antibodies against tetanus toxin, diphtheria toxin and B. pertussis antigens.
- diphtheria-tetanus-acellular pertussis-inactivated poliomyelitis-Haemophilus influenzae type b vaccine
A vaccine consisting of detoxified diphtheria toxoid (D), detoxified tetanus toxoid (T), acellular pertussis (aP) antigens, inactivated poliovirus (IPV) types 1, 2 and 3, and Haemophilus influenzae type b (Hib) capsular polysaccharide (polyribosylribitol phosphate; PRP) covalently bound to tetanus protein, suspended in water for injection and with active immunizing activity against diphtheria, tetanus, pertussis, poliomyelitis and H. influenzae type b. The five purified pertussis antigens in this vaccine are pertussis toxin (PT), filamentous hemagglutinin (FHA), pertactin (PRN) and fimbriae types 2 and 3 (FIM). Upon intramuscular injection of the diphtheria-tetanus-acellular pertussis-inactivated poliomyelitis-Haemophilus influenzae type b vaccine (DTaP-IPV-Hib), this vaccine activates the immune system to develop antibodies against diphtheria toxin, tetanus toxin, B. pertussis antigens, polioviruses and Hib, thereby providing active immunization against these diseases. The diphtheria and tetanus toxoids and pertussis antigens (inactivated PT, FHA, PRN and FIM) are adsorbed separately onto aluminum phosphate and then combined with IPV and PRP.
Brand name for propofol
A synthetic agent derivative of pyrimido-pyrimidine, with antiplatelet properties. Dipyridamole inhibits adenosine uptake by platelets and endothelial cells, triggering an accumulation of cyclic adenosine monophosphate (cAMP), and inhibiting the stimulation of platelet aggregation by agents such as platelet activating factor and collagen.
- disaccharide tripeptide glycerol dipalmitoyl
A lipophilic disaccharide tripeptide derivative of muramyl dipeptide (MDP) with immunomodulatory activity. Disaccharide tripeptide glycerol dipalmitoyl (DTP-GDP)stimulates macrophage activity and increases serum levels of tumor necrosis factor alpha (TNF alpha), neopterin, interleukin (IL)-1 alpha, IL-1 beta, IL-6, IL-8, and IL-12, which may activate host immune system antitumor functions. DTP-GDP may be packaged in liposomes for improved delivery. The immunomodulatory effects of this agent may be superior to those of MDP.
- distilled water
An ultra-pure form of water with potential antineoplastic activity. Derived by boiling impure water and condensing the resultant steam in a sterile container, distilled water has been shown to kill bladder cancer cells in vitro through osmotic lysis (cytolysis).
An orally bioavailable carbamoyl derivative and a proteasome inhibitor that is used in the treatment of alcoholism, with potential antineoplastic and chemosensitizing activities. Disulfiram (DSF) may help to treat alcoholism by irreversibly binding to and inhibiting acetaldehyde dehydrogenase, an enzyme that oxidizes the ethanol metabolite acetaldehyde into acetic acid. Inhibition of acetaldehyde dehydrogenase leads to an accumulation of acetaldehyde and produces a variety of very unpleasant symptoms, which together are referred to as the disulfiram-ethanol reaction (DER). In addition, DSF has a strong ability to chelate metals and its antineoplastic activity is highly dependent upon binding to copper (Cu), a metal that selectively accumulates in cancer cells. DSF/Cu generates reactive oxygen species (ROS) and inhibits proteasome activity, leading to an accumulation of ubiquitinated proteins; both of these processes result in induction of apoptosis. Also, DSF/Cu inhibits various cancer-specific pathways, which leads to inhibition of tumor cell growth.
Brand name for dapsone
Brand name for oxybutynin chloride
- divalproex sodium
A stable coordination compound comprised of sodium valproate and valproic acid with anticonvulsant and antiepileptic activities. Divalproex dissociates to the valproate ion in the gastrointestinal tract. This agent binds to and inhibits gamma-aminobutyric acid (GABA) transaminase and its anticonvulsant activity may be exerted by increasing brain concentration of GABA and by inhibiting enzymes that catabolize GABA or block the reuptake of GABA into glia and nerve endings. Divalproex may also work by suppressing repetitive neuronal firing through inhibition of voltage-sensitive sodium channels.
- Divine 9 with Carragel
Brand name for carrageenan-containing gel
A semi-synthetic, orally bioavailable taxane derivative with potential antineoplastic properties. Oral taxane derivative DJ-927 binds to tubulin, promoting microtubule assembly and stabilization and preventing microtubule depolymerization, thereby inhibiting cell proliferation. As it represents poor substrate for P-glycoprotein-related drug resistance mechanisms, this agent may be useful for treating multi-drug resistant tumors. As the first oral taxane derivative, oral taxane derivative DJ-927 is more potent than paclitaxel and docetaxel.
- DKK1-neutralizing monoclonal antibody DKN-01
A humanized monoclonal antibody directed against Wnt antagonist Dickkopf-1 (DKK1) with potential anti-osteolytic activity. DKK1-neutralizing monoclonal antibody DKN-01 binds to and inhibits DKK1, which restores Wnt pathway signaling. Reactivation of the Wnt signaling pathway may result in the differentiation and activation of osteoblasts within the bone matrix and the reversal of tumor-induced osteolytic disease. Elevated levels of circulating DKK1, a potent Wnt signaling pathway antagonist, is associated with a number of neoplastic diseases.
- DLK1/ EPHA2/HBB/NRP1/RGS5/TEM1 peptide-pulsed alpha-type-1 polarized dendritic cell vaccine
A cell-based cancer vaccine composed of mature polarized dendritic cells (alphaDC1) pulsed with six human leukocyte antigen (HLA)-A2-presented tumor blood vessel antigen (TBVA)-derived peptides, with potential immunostimulatory and antineoplastic activities. Dendritic cells (DCs) were treated with a “type-1 polarizing cytokine cocktail”, including interleukin-1beta, tumor necrosis factor alpha (TNF-a), interferon-alpha (IFN-a), IFN-gamma and polyinosinic:polycytidylic acid (pI:C) to produce mature alpha type-1 polarized DCs (alphaDC1) that are capable of producing high levels of interleukin-12p70 (IL-12p70). The alphaDC1 are subsequently pulsed with TBVA-derived peptides, including delta-like homologue 1 (DLK1) 310-318, EPH receptor A2 (EPHA2) 883-891, beta-globin (HBB) 31-39, neuropilin-1 (NRP1) 433-441, regulator of G-protein signaling 5 (RGS5) 5-13 and tumor endothelial marker 1 (TEM1) 691-700. Upon administration, these DCs are able to induce a potent cytotoxic T-lymphocyte (CTL) response against the TBVAs expressed on tumor-associated stromal cells, which results in stromal cell lysis and inhibition of angiogenesis. Disrupting the surrounding tumor vasculature inhibits tumor cell growth and survival. alphaDC1 are able to induce a potent tumor antigen-specific CTL response due to their high co-stimulatory activity and the secretion of anti-cancer cytokines, such as IL-12p70.
- DM4-conjugated anti-Cripto monoclonal antibody BIIB015
A humanized IgG1 monoclonal antibody directed against the cell surface-associated protein Cripto and conjugated to the maytansinoid DM4 with potential antineoplastic activity. The monoclonal antibody moiety of DM4-conjugated anti-Cripto monoclonal antibody BIIB015 binds to the tumor associated antigen (TAA) Cripto; upon internalization, the DM4 moiety binds to tubulin and disrupts microtubule assembly/disassembly dynamics, resulting in inhibition of cell division and cell growth of Cripto-expressing tumor cells. Constitutively expressed during embryogenesis, Cripto belongs to the EGF-CFC family of growth factor-like molecules and plays a key role in signaling pathways of certain transforming growth factor-beta superfamily members; as a TAA, Cripto is overexpressed in carcinomas such as those of the breast, ovary, stomach, lung, and pancreas while its expression is absent in normal tissues.
A cholesterol carbonate derivative of 4-demethylpenclomedine (DM-PEN) with potential antineoplastic alkylating activity. Upon intravenous administration of 4-demethylcholesteryloxycarbonylpenclomedine, the carbonium moiety binds to and alkylates DNA at the N7 guanine position, thereby causing DNA crosslinks. This prevents DNA replication, inhibits cellular proliferation and triggers apoptosis. In addition, due to its lipophilic cholesteryl moiety this agent is able to cross the blood brain barrier (BBB) and therefore can be given intravenously compared to other alkylating agents that need to be given intra-cranially.
- D-methionine formulation MRX-1024
A proprietary oral formulation of D-methionine with antioxidant and antimucositis activities. D-methionine formulation MRX-1024 may selectively protect the oral mucosa from the toxic effects of chemotherapy and radiation therapy without compromising antitumor activity. D-methionine may be converted into the L- isomer in vivo, particlualry in instances of L-methionine deprivation; both isomers have antioxidant activity which may be due, in part, to their sulfur moieties and chelating properties. L-methionine, an essential amino acid, also may help to maintain the ratio of reduced glutathione to oxidized glutathione in cells undergoing oxidative stress and may provide a source of L-cysteine for glutathione synthesis.
- DNA interference oligonucleotide PNT2258
A liposomal formulation of the 24-mer oligonucleotide PNT100, with potential antineoplastic activity. PNT2258 targets and complements to untranscribed DNA sequence upstream of BCL2 promoters, thereby interfering with DNA replication and transcription of the BCL2 gene. This may promote and restore the apoptotic pathway in BCL2-overexpressing tumor cells. BCL2, an anti-apoptotic protein, is overexpressed in a wide variety of tumors.
- DNA minor groove binding agent PM060184
A marine-derived, synthetically produced compound with potential antineoplastic activity. DNA minor groove-binding agent PM060184 covalently binds to residues lying in the minor groove of DNA, which may result in delayed progression through S phase, cell cycle arrest in the G2/M phase and cell death.
- DNA minor groove binding agent SG2000
A sequence-selective pyrrolobenzodiazepine (PBD) dimer with potential antineoplastic activity. Following intravenous administration, DNA minor groove binding agent SG2000 preferentially and covalently binds to purine-GATC-pyrimidine sequences, with the imine/carbinolamine moieties of SG2000 binding to the N2 positions of guanines on opposite strands of DNA. This induces interstrand cross-links and inhibits both DNA replication and gene transcription, which leads to the inhibition of cell growth. With a preference for binding to purine-GATC-pyrimidine sequences, SG2000 adducts do not appear to be susceptible to p53-mediated DNA excision repair.
- DNA plasmid encoding interleukin-12 INO-9012
A plasmid DNA vaccine encoding the human pro-inflammatory cytokine interleukin-12 (IL-12) with potential immunoactivating activity. Upon intramuscular delivery by electroporation of DNA plasmid encoding interleukin-12 INO-9012, IL-12 is translated in cells and activates the immune system by promoting the activation of natural killer cells (NK cells), inducing secretion of interferon-gamma and promoting cytotoxic T-cell responses against tumor cells. This may result in both immune-mediated tumor cell death and the inhibition of tumor cell proliferation.
- DNA plasmid vector pPRA-PSM vaccine
A cancer vaccine consisting of a DNA plasmid encoding epitopes of the human preferential antigen of melanoma (PRAME) and the prostate specific membrane antigen (PSMA) with potential immunostimulating activity. Upon direct administration of this vaccine into lymph nodes, peptides expressed by DNA plasmid vector pPRA-PSM may activate the immune system, resulting in a cytotoxic T-lymphocyte (CTL) response against PRAME- and PSMA-expressing cells. PRAME and PSMA are tumor associated antigens upregulated in a number of cancer cell types. As part of the MKC1106-PP regimen exploiting the 'prime-boost strategy', this plasmid is responsible for priming the immune response and is used in conjunction with a peptide vaccine consisting of PRAME and PSMA that boosts the immune system against PRAME- and PSMA-expressing tumor cells.
- DNA plasmid-encoding interleukin-12/HPV DNA plasmids therapeutic vaccine MEDI0457
A DNA-based combination immunotherapeutic, MEDI0457, composed of VGX-3100, a preparation of DNA plasmids encoding the E6 and E7 genes of human papillomavirus (HPV) subtypes 16 and 18, combined with INO-9012, a DNA plasmid encoding the immune activator and pro-inflammatory cytokine human interleukin-12 (IL-12) with potential immunoactivating and antineoplastic activities. Upon intramuscular delivery by electroporation of VGX-3100, the HPV E6 and E7 proteins are translated in cells and elicit a cytotoxic T-lymphocyte (CTL) response against cancer cells expressing the E6 and E7 antigens, resulting in tumor cell lysis. HPV type 16 and HPV type 18 are associated with the development of certain types of cancer. Upon intramuscular delivery by electroporation of MEDI0457, IL-12 is expressed and activates the immune system by promoting the activation of natural killer cells (NK cells), inducing secretion of interferon-gamma (IFN-g) and promoting CTL responses against tumor cells. This boosts the immune response and results in increased CTL-mediated tumor cell death as compared with the administration of VGX-3100 alone.
- DNA vaccine VB10.16
A therapeutic DNA vaccine composed of three parts, one encodes the E6/E7 fusion protein of human papillomavirus (HPV) type 16 (HPV16), the second is a dimerization entity and the third part encodes a protein that specifically binds to antigen presenting cells (APCs), with potential immunostimulating and antineoplastic activities. Upon intramuscular administration, the DNA vaccine VB10.16 expresses HPV16 E6/7 and a protein that targets receptors on APCs. Upon binding to APCs and subsequent internalization, the APCs mature and the HPV16 E6/7 antigenic protein is presented by the APCs. This attracts and stimulates B-lymphocytes, CD4-positive T-lymphocytes and elicits a cytotoxic T-lymphocyte (CTL) response against cancer cells expressing HPV16-associated E6 and E7 oncoproteins, which result in tumor cell lysis. HPV16 E6/7, a viral antigen, plays a key role in the development of certain types of cancer.
- DNA-dependent protein kinase inhibitor VX-984
An ATP-competitive inhibitor of the catalytic subunit of DNA-dependent protein kinase (DNA-PK), with potential sensitizing and enhancing activities for both chemo- and radiotherapies. Upon administration, DNA-PK inhibitor VX-984 binds to and inhibits the catalytic subunit of DNA-PK, thereby interfering with the non-homologous end joining (NHEJ) process and preventing repair of DNA double strand breaks (DSBs) caused by ionizing radiation or chemotherapeutic treatment. This increases chemo- and radiotherapy cytotoxicity and leads to enhanced tumor cell death. The enhanced ability of tumor cells to repair DSBs plays a major role in the resistance of tumor cells to chemo- and radiotherapy; DNA-PK plays a key role in the NHEJ pathway and DSB repair.
- DNA-dependent protein kinase-targeting siDNA DT01
A proprietary preparation of small interfering DNA (siDNA) molecules with potential chemo/radiosensitizing activity. By mimicking DNA double strand breaks (DSBs), DNA-dependent protein kinase-targeting siDNA DT01 inhibits the non-homologous end joining (NHEJ) process, one of the main DNA repair mechanisms, via binding to and activating DNA-dependent protein kinase (DNA-PK), a core component of the NHEJ complex. DNA-PK activation causes hyper-phosphorylation of histone variant H2AX on DNA and results in a different phosphorylated pattern of H2AX upon ionizing radiation treatment. This ultimately interferes with the repair of DNA DSBs during chemo- or radiotherapy, thereby increasing tumor cell death. The enhanced ability of tumor cells to repair DSBs plays a major role in the resistance of tumor cells to chemo- and radiotherapy.
- DNAi® drug PNT2258
Brand name for DNA interference oligonucleotide PNT2258
- DNA-PK/TOR kinase inhibitor CC-115
A dual inhibitor of DNA-dependent protein kinase (DNA-PK) and mammalian target of rapamycin (mTOR), with potential antineoplastic activity. CC-115 binds to and inhibits the activity of DNA-PK and both raptor-mTOR (TOR complex 1 or TORC1) and rictor-mTOR (TOR complex 2 or TORC2), which may lead to a reduction in cellular proliferation of cancer cells expressing DNA-PK and TOR. DNA-PK, a serine/threonine kinase and a member of the PI3K-related kinase subfamily of protein kinases, is activated upon DNA damage and plays a key role in repairing double-stranded DNA breaks via the DNA nonhomologous end joining (NHEJ) pathway; mTOR, a serine/threonine kinase that is upregulated in a variety of tumors, plays an important role downstream in the PI3K/Akt/mTOR signaling pathway.
- DNP-modified autologous renal cell carcinoma tumor cell vaccine
A cancer vaccine consisting of autologous renal cell carcinoma (RCC) tumor cells modified with the hapten 2,4-dinitrophenol (DNP) with potential immunostimulating and antineoplastic activities. Administration of DNP-modified autologous renal cell carcinoma tumor cell vaccine may induce a cytotoxic T-lymphocyte (CTL) response against renal cell carcinoma tumor cells. DNP conjugation may enhance the immunogenicity of weakly immunogenic antigens.
- DNR-expressing nasopharyngeal carcinoma-specific cytotoxic T lymphocytes
A preparation of autologous, dominant-negative receptor (DNR)-expressing nasopharyngeal carcinoma (NPC)-specific cytotoxic T-lymphocytes (CTLs), with potential antineoplastic activity. The DNR-expressing NPC-specific CTLs specifically target Epstein-Barr virus (EBV) nuclear antigen 1 (EBNA1), latent membrane proteins (LMP) and BamHIA rightward frame 1 (BARF1), and are transduced with a retroviral vector expressing DNR, a dominant-negative form of the transforming growth factor beta (TGFb) receptor, which blocks TGF-beta-mediated signaling. Upon administration, the CTLs recognize and target NPC cells, which may result in both CTL-mediated cell lysis and the inhibition of tumor cell proliferation. Tumor-expressed TGF-beta inhibits T-lymphocyte activation and expansion; resistance to TGF-beta allows for optimal CTL activity. EBV infection plays a key role in NPC tumorigenesis.
A synthetic catecholamine with sympathomimetic activity. Dobutamine is a direct-acting inotropic agent and an adrenergic agonist that stimulates primarily the beta-1 adrenoceptor, with lesser effect on beta-2 or alpha receptors. Via beta-1 adrenoceptor of the heart, this agent induces positive inotropic effect with minimal changes in chronotropic activities or systemic vascular resistance. Dobutamine also causes vasodilation by stimulating beta-2 adrenergic receptors in blood vessels, augmented by reflex vasoconstriction resulting in increased cardiac output.
A semi-synthetic, second-generation taxane derived from a compound found in the European yew tree Taxus baccata. Docetaxel displays potent and broad antineoplastic properties; it binds to and stabilizes tubulin, thereby inhibiting microtubule disassembly which results in cell- cycle arrest at the G2/M phase and cell death. This agent also inhibits pro-angiogenic factors such as vascular endothelial growth factor (VEGF) and displays immunomodulatory and pro-inflammatory properties by inducing various mediators of the inflammatory response. Docetaxel has been studied for use as a radiation-sensitizing agent. Check for active clinical trialsusing this agent.
- docetaxel emulsion ANX-514
An injectable emulsion formulation containing the taxane docetaxel, a semisynthetic analogue of paclitaxel, with antineoplastic activity. Docetaxel binds specifically to the beta-tubulin subunit of the microtubule, stabilizing tubulin and inhibiting microtubule disassembly, which results in cell-cycle arrest at the G2/M phase and cell death. This agent also inhibits pro-angiogenic factors such as vascular endothelial growth factor (VEGF) and induces various mediators of the inflammatory response. Docetaxel emulsion ANX-514 is formulated without polysorbate 80 or other detergents in order to reduce the incidence and severity of hypersensitivity reactions. In addition, the exclusion of polysorbate 80 in this formulation precludes foaming during the preparation process, thus facilitating preparation and administration. Check for active clinical trialsusing this agent.
- docetaxel formulation CKD-810
An injectable formulation containing the taxane docetaxel, a semisynthetic analogue of paclitaxel, with antineoplastic activity. Docetaxel binds specifically to the beta-tubulin subunit of the microtubule, stabilizing tubulin and inhibiting microtubule disassembly, which results in cell-cycle arrest at the G2/M phase and cell death. This agent also inhibits pro-angiogenic factors such as vascular endothelial growth factor (VEGF) and induces various mediators of the inflammatory response.
- docetaxel lipid microspheres
A lipid microsphere (LM)-based formulation containing the poorly water soluble taxane docetaxel, a semi-synthetic analogue of paclitaxel, with antineoplastic activity. Docetaxel binds specifically to the beta-tubulin subunit of the microtubule, stabilizing tubulin and inhibiting microtubule disassembly, which causes cell cycle arrest at the G2/M phase and leads to cell death. This agent also inhibits pro-angiogenic factors such as vascular endothelial growth factor (VEGF) and induces various mediators of the inflammatory response. Compared to docetaxel alone, the LM formulation may enhance stability, improve efficacy and may reduce toxicity; this formulation does not contain toxic detergents needed to solubilize docetaxel which further improves its side effect profile.
- docetaxel nanoparticle CPC634
A polymeric nanoparticle (PNP) formulation containing the poorly water-soluble taxane docetaxel, a semi-synthetic analogue of paclitaxel, with antineoplastic activity. Upon intravenous administration of the docetaxel nanoparticle CPC634, the nanoparticles are able to accumulate at the tumor site due to the unique characteristics of the tumor’s vasculature, while avoiding normal, healthy tissue. In turn, docetaxel is released locally at the target tumor site, binds specifically to the beta-tubulin subunit of the microtubule, stabilizing tubulin and inhibiting microtubule disassembly, which results in cell-cycle arrest at the G2/M phase, thereby preventing cell proliferation. This agent also inhibits pro-angiogenic factors such as vascular endothelial growth factor (VEGF) and induces various mediators of the inflammatory response. Compared to docetaxel alone, this formulation may enhance stability and improve delivery, thereby increasing docetaxel’s efficacy while avoiding systemic exposure, which minimizes its toxicity.
- docetaxel-loaded nanopharmaceutical CRLX301
A nanoparticle-based formulation containing the poorly water-soluble, second-generation taxane analog docetaxel, with antineoplastic activity. Upon intravenous administration of the docetaxel-loaded nanopharmaceutical CRLX301, the nanoparticles are able to accumulate at the tumor site due to the unique characteristics of the tumor’s vasculature, while avoiding normal, healthy tissue. In turn, CRLX301 is taken up by the tumor cell via macropinocytosis. Subsequently, docetaxel is slowly released into the cytoplasm where it binds to and stabilizes the beta-subunit of tubulin, thereby stabilizing microtubules and inhibiting microtubule disassembly. This prevents mitosis and results in cell death. Compared to the administration of docetaxel alone, this formulation is able to increase docetaxel’s efficacy while avoiding systemic exposure, which minimizes its toxicity.
A polymeric nanoparticle (PNP) formulation containing the taxane docetaxel, a semi-synthetic analogue of paclitaxel, with antineoplastic activity. Docetaxel binds specifically to the beta-tubulin subunit of the microtubule, stabilizing tubulin and inhibiting microtubule disassembly, which results in cell-cycle arrest at the G2/M phase, preventing cell proliferation. This agent also inhibits pro-angiogenic factors such as vascular endothelial growth factor (VEGF) and induces various mediators of the inflammatory response. Compared to docetaxel alone, the PNP formulation may enhance stability and improve delivery. Check for active clinical trialsusing this agent.
A polyunsaturated very long-chain fatty acid with a 22-carbon backbone and 6 double bonds, originating from the 3rd, 6th, 9th, 12th, 15th and 18th positions from the methyl end.
- docosahexaenoic acid
A polyunsaturated very long-chain fatty acid with a 22-carbon backbone and 6 double bonds. Four separate isomers can be called by this name.
- dolasetron mesylate
An indole derivative with antiemetic activity. As a selective serotonin receptor antagonist, dolasetron mesylate competitively blocks the action of serotonin at 5HT3 receptors, resulting in suppression of chemotherapy- and radiotherapy-induced nausea and vomiting.
- dolastatin 10
A pentapeptide originally isolated from the marine mollusk Dolabella auricularia with potential antineoplastic activity. Binding to tubulin, dolastatin 10 inhibits microtubule assembly, resulting in the formation of tubulin aggregates and inhibition of mitosis. This agent also induces tumor cell apoptosis through a mechanism involving bcl-2, an oncoprotein that is overexpressed in some cancers.
An orally administered analog of the human endogenous natriuretic hormone uroguanylin and guanylate cyclase C (GC-C) agonist, with potential laxative, anti-nociceptive and anti-inflammatory activities. Upon administration, dolcanatide, by mimicking uroguanylin, binds to and activates GC-C locally on endothelial cells in the gastrointestinal (GI) tract, without entering the systemic circulation. Activation of GC-C results in an increase in cyclic guanosine monophosphate (cGMP). Increased concentrations of cGMP lead to the activation of the anion channel cystic fibrosis transmembrane conductance regulator (CFTR). CFTR activation increases the secretion of negatively charged ions, particularly chloride and bicarbonate, into the GI tract lumen, which further drives sodium ions and then water into the lumen. This leads to increased fluid secretion in the GI tract, accelerated transit and changes in stool consistency. In addition, ion channel modulation may decrease muscle contractions and the activity of pain-sensing nerves, thereby decreasing intestinal pain. Also, GC-C may inhibit the secretion of pro-inflammatory cytokines, which may ameliorate GI inflammation. Uroguanylin, a naturally occurring human GI peptide, is a ligand for GC-C and plays a key role in anti-inflammatory processes in the GI tract.
Brand name for diflunisal
Brand name for methadone hydrochloride
An orally bioavailable integrase strand transfer inhibitor (INSTI), with activity against human immunodeficiency virus type 1 (HIV-1) infection. Upon oral administration, dolutegravir binds to the active site of integrase, an HIV enzyme that catalyzes the transfer of viral genetic material into human chromosomes. This prevents integrase from binding to retroviral deoxyribonucleic acid (DNA), and blocks the strand transfer step, which is essential for the HIV replication cycle. This prevents HIV-1 replication.
An orally bioavailable benzamide and inhibitor of human class I histone deacetylases (HDACs) isoenzymes 1, 2 and 3, with potential antineoplastic activity. Domatinostat selectively binds to and inhibits class I HDACs leading to an accumulation of highly acetylated histones. This may result in an induction of chromatin remodeling, the selective transcription of tumor suppressor genes, and the tumor suppressor protein-mediated inhibition of tumor cell division and eventually the induction of tumor cell apoptosis. This may inhibit tumor cell proliferation in susceptible tumor cells. HDACs, upregulated in many tumor types, are a class of enzymes that deacetylate chromatin histone proteins.
Brand name for diethylstilbestrol
Brand name for therapeutic hydrocortisone
- donepezil hydrochloride
The hydrochloride salt of a piperidine derivative with neurocognitive-enhancing activity. Donepezil reversibly inhibits acetylcholinesterase, thereby blocking the hydrolysis of the neurotransmitter acetylcholine and, consequently, increasing its activity. This agent may improve neurocognitive function in Alzheimer's disease, reduce sedation associated with opioid treatment of cancer pain, and improve neurocognitive function in patients who have received radiation therapy for primary brain tumors or brain metastases.
- donor lymphocytes
A population of lymphocytes from the blood of a donor and administered to a patient who has already received a stem cell transplant from the same donor (allogeneic hematopoietic stem cell transplantation). The donor lymphocytes may be able to boost the patient's immune system and kill remaining cancer cells.
- donor regulatory T lymphocytes
Donor-derived regulatory T-cells (Tregs), with potential immunomodulating activity. Tregs are a subset of CD4+ T cells that express high levels of CD25 (interleukin 2 receptor) and the transcription factor Foxp3. The donor CD4+CD25+ Tregs modulate immune responses and may induce tolerance to allogeneic organ transplants, such as hematopoietic stem cell transplants (HSCTs), thereby preventing graft-versus-host disease (GVHD).
- donor-derived CD34+ hematopoietic stem and progenitor cells plus CD3+ T cells MDR-101
A preparation of allogeneic, organ donor-derived CD34-positive hematopoietic stem and progenitor cells (HPCs) and CD3-positive T cells that can be used after organ transplantation to potentially prevent organ rejection. Upon infusion of the organ donor-derived CD34+ HPCs plus CD3+ T cells MDR-101 after organ transplantation, these cells mix and co-exist with the recipient's blood and immune cells, thereby inducing hematologic mixed chimerism and enabling the recipient's immune system to become immune tolerant to the donor cells. This increases acceptance of the transplanted organ, decreases the risk of organ transplant rejection, increases organ survival and may decrease the need for additional immunosuppressive agents. The cells in MDR-101 are ex vivo processed in a specific and unique way which has yet to be fully elucidated. Cell doses are dependent on the degree of human leukocyte antigen (HLA)-match/HLA-mismatch between the recipient and donor.
- donor-derived cytokine-induced memory-like natural killer cell
A population of donor-derived cytokine-induced, memory-like, cytotoxic natural killer (NK) cells (CIML NKs), with potential antitumor activity. Allogeneic NK cells are pre-activated ex vivo with various cytokines, which induces the differentiation of the NK cells into CIML NK cells. The pretreated NK cells exhibit enhanced activation and interferon-gamma (IFN-g) responses, and may exert enhanced cytotoxicity against tumor cells. Upon administration, the CIML NKs may induce an anti-tumor immune response and kill tumor cells.
- donor-derived WT1/PRAME/NY-ESO-1/survivin-specific T-lymphocytes
Allogeneic T-lymphocytes specifically reactive to the tumor-associated antigens (TAAs) human Wilms tumor protein-1 (WT1), Preferentially Expressed Antigen in Melanoma (PRAME), the cancer-testis antigen NY-ESO-1, and survivin, with potential antineoplastic activity. Donor derived T-cells are mixed, ex vivo, with protein fragments derived from the TAAs WT1, PRAME, NY-ESO-1, and survivin. Upon intravenous administration, the donor-derived WT1/PRAME/NY-ESO-1/Survivin-specific T-lymphocytes recognize and kill cancer cells expressing these TAAs. WT1, NY-ESO-1, PRAME, and survivin, are expressed on certain tumor cell types and play key role in tumor cell proliferation and survival.
- dopamine–somatostatin chimeric molecule BIM-23A760
A chimeric molecule directed against dopamine and somatostatin receptors with potential antineoplastic activity. Combining two pharmacological moieties, a somatostatin analogue and a dopamine agonist, dopamine–somatostatin chimeric molecule BIM-23A760 binds with high affinity to dopamine D2 receptor (D2R) and somatostatin receptor subtype 2 (SSTR2), and to a lesser extent to somatostatin receptor subtype 5 (SSTR5). This agent appears to exert its effect mainly by binding to D2R to activate the ERK1/2 and p38 MAPK pathways, thus inducing apoptosis and inhibiting cellular proliferation in non-functioning pituitary adenoma (NFPA) and neuroendocrine tumors. By binding to SSTR2, this agent may inhibit the secretion of growth hormone (GH) by the pituitary gland.
Brand name for levodopa
Brand name for avatrombopag maleate
- dornase alfa
A recombinant human deoxyribonuclease I (rhDNAse) with selective DNA cleaving activity. Upon intrapleural administration, dornase alfa catalyzes the degradation of extracellular DNA in airway secretions, which can reduce their viscosity. Thus, dornase alfa may both promote the clearing of airway mucus and improve pulmonary function.
- dornase alfa inhalation solution
A highly purified solution of recombinant human deoxyribonuclease I (rhDNAse) with selective DNA cleaving activity. Administrated through inhalation of the nebulized solution, dornase alpha catalyzes DNA degradation in viscous airway secretions, which may render airway secretions less viscous, thus promoting the clearing of airway mucous plugging and improvement in pulmonary function.
Brand name for cabergoline
- DOTAP:chol-Fus1 liposome complex
A formulation composed of DOTAP:cholesterol liposomal nanoparticles complexed with a plasmid expression cassette encoding human FUS1 protein, with potential antineoplastic activity. Upon administration, DOTAP:chol-Fus1 liposome complex accumulates mainly in the lungs and particularly in cancer cells. Upon transfer of the Fus1 gene into tumor cells, the expression of Fus1 may induce tumor cell apoptosis and suppress tumor cell proliferation. Fus1, a potent tumor-suppressor protein, is present in normal, healthy cells but often absent in certain cancer cells. DOTAP:cholesterol liposome is composed of cationic lipid dioleoyl-trimethylammonium propane (DOTAP) and cholesterol at a molar ratio of 1:1. Check for active clinical trialsusing this agent.
Brand name for gadoterate meglumine
- dovitinib lactate
The orally bioavailable lactate salt of a benzimidazole-quinolinone compound with potential antineoplastic activity. Dovitinib strongly binds to fibroblast growth factor receptor 3 (FGFR3) and inhibits its phosphorylation, which may result in the inhibition of tumor cell proliferation and the induction of tumor cell death. In addition, this agent may inhibit other members of the RTK superfamily, including the vascular endothelial growth factor receptor; fibroblast growth factor receptor 1; platelet-derived growth factor receptor type 3; FMS-like tyrosine kinase 3; stem cell factor receptor (c-KIT); and colony-stimulating factor receptor 1; this may result in an additional reduction in cellular proliferation and angiogenesis, and the induction of tumor cell apoptosis. The activation of FGFR3 is associated with cell proliferation and survival in certain cancer cell types.
Brand name for calcipotriene
- doxazosin mesylate
The mesylate salt form of doxazosin, a quinazoline compound with smooth muscle relaxing activity. Doxazosin mesylate selectively antagonizes alpha-1-adrenergic receptors in smooth muscle of the bladder neck and prostate, thereby relaxing the smooth muscle and decreasing the obstruction and urethral resistance seen with benign prostate hyperplasia (BPH). This may improve BPH symptoms. This agent also blocks alpha-1-adrenergic receptors in peripheral vascular smooth muscle, which leads to vasodilatation and a subsequent decrease in peripheral vascular resistance.
- doxepin hydrochloride
A dibenzoxepin derivative and tricyclic antidepressant with antipruritic and sedative activities. Doxepin blocks the reuptake of norepinephrine and serotonin into presynaptic terminals thereby prolonging the availability of the monoaminergic neurotransmitters within the synaptic cleft and enhancing their action leading to sedative effects. Doxepin also has antagonistic effects on histamine (H1 and H2), 5-HT2, alpha-1 adrenergic, and muscarinic receptors. The antipruritic effect of this agent is the result mediated through inhibition of histamine receptors.
A synthetic analog of vitamin D with potential antineoplastic activity. In the liver, doxercalciferol is converted to its biologically active vitamin D metabolites, which control the intestinal absorption of dietary calcium, the tubular reabsorption of calcium by the kidney and, in conjunction with parathyroid hormone (PTH), the mobilization of calcium from the skeleton. Through interaction with specific receptor proteins in target tissues, these vitamin D metabolites act directly on osteoblasts to stimulate skeletal growth, and on the parathyroid glands to suppress PTH synthesis and secretion. This agent has also been shown to inhibit the growth of retinoblastomas, and may exhibit some antiproliferative activity against prostate cancer cells.
A fluoropyrimidine derivative and oral prodrug of the antineoplastic agent 5-fluorouracil (5-FU) with antitumor activity. Doxifluridine, designed to circumvent the rapid degradation of 5-FU by dihydropyrimidine dehydrogenase in the gut wall, is converted into 5-FU in the presence of pyrimidine nucleoside phosphorylase. 5-FU interferes with DNA synthesis and subsequent cell division by reducing normal thymidine production and interferes with RNA transcription by competing with uridine triphosphate for incorporation into the RNA strand.
Brand name for doxorubicin hydrochloride liposome
- doxorubicin hydrochloride
The hydrochloride salt of doxorubicin, an anthracycline antibiotic with antineoplastic activity. Doxorubicin, isolated from the bacterium Streptomyces peucetius var. caesius, is the hydroxylated congener of daunorubicin. Doxorubicin intercalates between base pairs in the DNA helix, thereby preventing DNA replication and ultimately inhibiting protein synthesis. Additionally, doxorubicin inhibits topoisomerase II which results in an increased and stabilized cleavable enzyme-DNA linked complex during DNA replication and subsequently prevents the ligation of the nucleotide strand after double-strand breakage. Doxorubicin also forms oxygen free radicals resulting in cytotoxicity secondary to lipid peroxidation of cell membrane lipids; the formation of oxygen free radicals also contributes to the toxicity of the anthracycline antibiotics, namely the cardiac and cutaneous vascular effects.
- doxorubicin hydrochloride liposome
A liposome-encapsulated form of the hydrochloride salt of the anthracycline antineoplastic antibiotic doxorubicin. Doxorubicin intercalates between base pairs in the DNA helix, thereby preventing DNA replication and ultimately inhibiting protein synthesis. Additionally, doxorubicin inhibits topoisomerase II which results in an increased and stabilized cleavable enzyme-DNA linked complex during DNA replication and subsequently prevents the ligation of the nucleotide strand after double-strand breakage. Doxorubicin also forms oxygen free radicals resulting in cytotoxicity secondary to lipid peroxidation of cell membrane lipids. Liposomal delivery of doxorubicin HCL improves drug penetration into tumors and decreases drug clearance, thereby increasing the duration of therapeutic drug effects; a liposomal formulation of doxorubicin also modulates toxicity, specifically the cardiac effects commonly seen with anthracycline antitumor drugs.
- doxorubicin-eluting beads
A drug-device combination product consisting of small polymeric beads impregnated with the anthracycline antibiotic doxorubicin with potential antineoplastic activity. The beads consist of polyvinyl alcohol (PVA) microspheres modified with sulfonic acid groups and loaded with doxorubicin. During transarterial chemoembolization (TACE), doxorubicin-eluting beads embolize to the tumor vasculature and release cytotoxic doxorubicin, which may result in both ischemic necrosis of tumor tissue due to mechanical blockage of the tumor vasculature and doxorubicin-mediated inhibition of tumor cell proliferation.
- doxorubicin-HPMA conjugate
A copolymer conjugate of the antineoplastic anthracycline doxorubicin and the water-soluble polymer N-(2-hydroxypropyl) methacrylamide (HPMA). Doxorubicin, an intercalator and a topoisomerase II inhibitor, prevents DNA replication and ultimately inhibits protein synthesis. This agent also generates oxygen free radicals, resulting in cytotoxic lipid peroxidation of cell membrane lipid. HPMA conjugation enhances the permeability and retention of this agent within the tumor vasculature. Poorly cleared by the lymphatic system, this formulation undergoes increased cleavage by tumor cell lysosomal proteinases, resulting in increased, sustained intracellular concentrations of free doxorubicin. Compared to other doxorubicin-containing formulations, this formulation may exhibit an improved toxicity profile due to the lower concentrations of free doxorubicin to which non-malignant tissues are exposed.
- doxorubicin-loaded EGFR-targeting nanocells
A nanocell formulation targeting the epidermal growth factor receptor (EGFR) using bispecific antibodies (bsAb) against EGFR and containing the antineoplastic anthracycline antibiotic doxorubicin, with potential antineoplastic activity. Upon administration of doxorubicin-loaded EGFR-targeting nanocells, the nanocells are stable in the bloodstream and the anti-EGFR bsAb moiety targets and binds to EGFR-expressing tumor cells. Upon binding, the nanocell allows for specific delivery of doxorubicin to tumor cells overexpressing EGFR. Upon endocytosis by the tumor cells, the nanocell is broken down and releases doxorubicin, which intercalates into DNA and interferes with topoisomerase II activity, thereby inhibiting DNA replication and RNA synthesis. Compared to doxorubicin alone or liposomal doxorubicin, targeted delivery of doxorubicin improves efficacy while lowering the toxicity profile. EGFR, a tyrosine kinase receptor, is overexpressed in many cancer cell types. The nanocell is a bacterially derived nanosphere; the bacterial components are unlikely to induce an immune response in the immunosuppressed tumor microenvironment.
- doxorubicin-magnetic targeted carrier complex
A formulation of the anthracycline antibiotic doxorubicin in which doxorubicin is bound to microscopic beads of activated carbon and iron as a magnetic-targeted carrier (MTC). Doxorubicin, an intercalator and a topoisomerase II inhibitor, prevents DNA replication and ultimately inhibits protein synthesis. This agent also generates oxygen free radicals, resulting in cytotoxic lipid peroxidation of cell membrane lipids. Guided by the placement of a magnet on the body surface overlying a tumor site, the doxorubicin-MTC complex delivers doxorubicin directly to the tumor site, thereby targeting and prolonging the duration of doxorubicin-mediated cytotoxicity to the tumor bed while minimizing systemic toxicity.
- doxycycline calcium
The calcium salt form of doxycycline exhibiting antimicrobial activity. Doxycycline blocks binding of aminoacyl-tRNA to the mRNA-ribosome complex, thereby inhibiting protein synthesis. In addition, this agent has exhibited inhibition of collagenase activity.
- doxycycline hyclate injection
The hyclate salt form of doxycycline, a synthetic, broad-spectrum tetracycline antibiotic exhibiting antimicrobial activity. Doxycycline hyclate binds reversibly to the 30S ribosomal subunit, possibly to the 50S ribosomal subunit as well, thereby blocking the binding of aminoacyl-tRNA to the mRNA-ribosome complex. This leads to an inhibition of protein synthesis. In addition, this agent has exhibited inhibition of collagenase activity.
- DPT/BCG/measles/Serratia/pneumococcus vaccine
A proprietary lipid emulsion containing five vaccines: diphtheria, pertussis, tetanus (DPT), Bacille Calmette-Guerin (BCG), measles, Serratia marcescens and pneumococcal, with potential immunostimulating activity. Subcutaneous administration of the DPT/BCG/measles/Serratia/pneumococcus vaccine activates the immune system and may both abrogate tumor-induced immune tolerance and induce an antitumor immune response, which may eradicate the tumor.
- DPT/typhoid/Staphylococcus aureus/paratyphoid A/paratyphoid B vaccine
A proprietary lipid emulsion containing five vaccines: diphtheria, pertussis, tetanus (DPT), typhoid, Staphylococcus aureus, paratyphoid A and paratyphoid B, with potential immunostimulating activity. Subcutaneous administration of the DPT/typhoid/Staphylococcus aureus/paratyphoid A/paratyphoid B vaccine activates the immune system and may both abrogate tumor-induced immune tolerance and induce an antitumor immune response, which may eradicate the tumor.
- DR5 HexaBody agonist GEN1029
An agonistic hexamer formation-enhanced mixture of two antibodies (HexaBody) that target two separate epitopes on death receptor type 5 (DR5; TNFRSF10B; tumor necrosis factor-related apoptosis-inducing ligand receptor 2; TRAILR2), with potential antineoplastic activity. Upon administration, DR5 HexaBody agonist GEN1029 specifically binds to and activates DR5. This results in the activation of caspase cascades and the induction of apoptosis in DR5-expressing tumor cells. DR5, a cell surface receptor and member of the tumor necrosis factor receptor superfamily (TNFRSF), is involved in the promotion of caspase-dependent apoptosis. Compared to other DR5 antibody-based agonists, the antibodies in GEN1029 (DR5-01 and DR5-05) elicit increased receptor activation because they exhibit enhanced formation of antibody hexamers and receptor clusters at the cell surface due to E430G mutations in the Fc domains of both antibodies.
An isomer of tetrahydrocannabinol (THC) that is the main and most active isomer found in the cannabis sativa L. plant, with potential anti-emetic, analgesic and appetite stimulating activities. Upon administration, dronabinol, also called delta-9-THC, targets and binds to cannabinoid receptors (CBRs) located in the central nervous system (CNS). Dronabinol acts directly on the appetite and vomiting control centers in the brain to stimulate appetite and prevent emesis. In addition, this agent induces analgesia. Urine levels may be used as a marker to determine the exposure to certain preparations containing parts of the cannabis plant, such as marijuana.
A butyrophenone with anti-emetic, sedative and anti-anxiety properties. Although the exact mechanism through which droperidol exerts its effects is unknown, droperidol may block dopamine receptors in the chemoreceptor trigger zone (CTZ), which may lead to its anti-emetic effect. This agent may also bind to postsynaptic gamma-aminobutyric acid (GABA) receptors in the central nervous system (CNS), which increases the inhibitory effect of GABA and leads to sedative and anti-anxiety activities. Check for active clinical trialsusing this agent.
Brand name for hydroxyurea
- DTA-H19 plasmid
A plasmid DNA encoding the A chain of the diphtheria toxin (DT-A) driven by the transcriptional regulatory sequences of human H19, with potential antineoplastic activity. Because the expression of DT-A is under the control of H19 promotor elements, DT-A is selectively expressed in tumor cells capable of turning on H-19. DT-A catalyzes ADP-ribosylation of translation elongation factor 2 (EF-2), resulting in the inhibition of protein synthesis and apoptosis. In addition, DT-A protein released from lysed cells cannot enter and kill neighboring cells because of the absence of the DT-B chain, further enhancing the selective cytotoxicity of this agent. Human H19 is a paternally-imprinted, oncofetal gene encoding an RNA product; it acts as a "riboregulator" in gene expression and is found at substantial levels in different human tumor cell types while its expression in normal adult tissue is limited.
- dual PI3 kinase/mTOR inhibitor GDC-0980
An orally available agent targeting phosphatidylinositol 3 kinase (PI3K) and mammalian target of rapamycin (mTOR) kinase in the PI3K/mTOR signaling pathway, with potential antineoplastic activity. PI3K/mTOR kinase inhibitor GDC-0980 inhibits both PI3K kinase and mTOR kinase, which may result in tumor cell apoptosis and growth inhibition of cancer cells overexpressing PI3K/mTOR. Activation of the PI3K/mTOR pathway promotes cell growth, survival, and resistance to chemotherapy and radiotherapy; mTOR, a serine/threonine kinase downstream of PI3K, may also be activated in a PI3K-independent fashion.
- dual variable domain immunoglobulin ABT-165
A dual-specific, tetravalent immunoglobulin (Ig)G-like molecule targeting two as of yet not publicly known targets, with potential antineoplastic activity. The target-binding variable domains of two monoclonal antibodies, which are not publicly known, are combined, via linkers, to create the tetravalent, dual-targeting single agent ABT-165. Upon administration of dual variable domain immunoglobulin (DVD-Ig) ABT-165, the target-binding variable domains specifically recognize and simultaneously bind to their two antigens expressed on tumor cells. This may both prevent antigen-mediated signaling and lead to an inhibition of cellular proliferation in susceptible tumor cells. The antigen targets are overexpressed on certain tumor cell types. The DVD-Ig may have enhanced physicochemical and pharmacokinetic properties as compared to their antibody counterparts.
- dual-affinity B7-H3/CD3-targeted protein MGD009
An Fc-bearing humanized bispecific dual-affinity re-targeting (DART) protein composed of Fv regions derived from monoclonal antibodies against the immunoregulatory protein B7-homologue 3 (B7-H3, CD276) and the T-cell surface antigen CD3, with potential immunostimulating and antineoplastic activities. Upon administration of the MGD009 DART protein, the anti-B7-H3 component targets and binds to the cell surface antigen B7-H3; at the same time, the anti-CD3 component binds to human CD3. This cross-links the T cells to B7-H3-expressing tumor cells, activates and redirects endogenous T cells to kill B7-H3-expressing tumor cells, and inhibits proliferation of B7-H3-expressing tumor cells. B7-H3, a type I transmembrane protein and a member of the B7 co-stimulatory protein superfamily, is overexpressed on certain tumor cell types and on various immune cells but is minimally expressed by normal human tissues. B7-H3 is a negative regulator of T-cell activation and its overexpression plays a key role in immuno-evasion, tumor cell invasion and metastasis, and its expression is correlated with poor prognosis.
Brand name for conjugated estrogens/bazedoxifene
An anthracycline antineoplastic antibiotic with therapeutic effects similar to those of doxorubicin. Duborimycin exhibits cytotoxic activity through topoisomerase-mediated interaction with DNA, thereby inhibiting DNA replication and repair and RNA and protein synthesis.
A recombinant human soluble protein corresponding to amino acids 114-281 of the Apo2 ligand/tumor necrosis factor-related apoptosis-inducing ligand (RhApo2L/TRAIL) with potential antineoplastic activity. Dulanermin binds to and activates TRAIL receptors 1 and 2 (TRAIL-R1/R2), which may activate caspases and induce p53-independent apoptosis in TRAIL-R1/R2-expressing tumor cells. The pro-apoptotic cell surface receptors TRAIL-R1 and -R2, also known as DR4 (death receptor 4) and DR5 (death receptor 5), are members of the TNF receptor family and are overexpressed by a variety of cancer cell types. Check for active clinical trialsusing this agent.
- duloxetine hydrochloride
The hydrochloride salt of duloxetine, a fluoxetine derivative belonging to the class of selective serotonin (5-HT) and norepinephrine (NE) reuptake inhibitors (SSNRIs) and exhibiting antidepressant activity. Duloxetine selectively prevents the reuptake of 5-HT and NE via transporter complexes on the pre-synaptic membrane, thereby increasing the level of these neurotransmitters within the synaptic cleft. As a result, this agent potentiates serotonergic and noradrenergic activities in the central nervous system, and alleviates depression and neuropathy sensations, such as pain and tingling. Furthermore, duloxetine does not show significant affinity for dopaminergic, adrenergic, cholinergic, histaminergic, opioid, glutamate, and gamma-aminobutyric acid (GABA) receptors.
Brand name for dydrogesterone
A Fc optimized monoclonal antibody directed against programmed cell death-1 ligand 1 (PD-L1; B7 homolog 1; B7H1), with potential immune checkpoint inhibitory and antineoplastic activities. Upon intravenous administration, durvalumab binds to PD-L1, thereby blocking its binding to and activation of its receptor programmed death 1 (PD-1) expressed on activated T cells. This may reverse T-cell inactivation and activate the immune system to exert a cytotoxic T-lymphocyte (CTL) response against PD-L1-expressing tumor cells. PD-L1, a member of the B7 protein superfamily, is overexpressed on certain tumor cell types and on various tumor-infiltrating immune cells. PD-L1 binding to PD-1 on T cells suppresses the immune system and results in increased immune evasion. The Fc region of durvalumab is modified in such a way that it does not induce either antibody-dependent cytotoxicity (ADCC) or complement-dependent cytotoxicity (CDC).
A synthetic 4-azasteroid compound with antiandrogenic activity. Dutasteride competitively and specifically binds to isoenzymes 1 and 2 of 5-alpha-reductase, forming stable enzyme complexes and inhibiting the conversion of testosterone to 5α-dihydrotestosterone (DHT); the reduction in DHT activity may mitigate or prevent enlargement of the prostate gland. The type 2 5-alpha-reductase isoenzyme is primarily active in the reproductive tissues while the type 1 isoenzyme is also active in skin and the liver. Check for active clinical trialsusing this agent.
- dUTPase inhibitor TAS-114
An orally bioavailable inhibitor of both deoxyuridine triphosphatase (dUTPase) and dihydropyrimidine dehydrogenase (DPD), with potential antineoplastic adjuvant activity. Upon oral administration in combination with a prodrug of the pyrimidine antagonist 5-fluorouracil (5-FU), TAS-114 inhibits (DPD), the liver enzyme responsible for rapid catabolism of 5-FU into inactive metabolites. This prevents first-pass metabolism of 5-FU, allowing oral administration of the 5-FU prodrug and increasing the efficacy of 5-FU. In addition, as a dUTPase inhibitor, TAS-114 enhances the antitumor activity of 5-FU by preventing the hydrolysis and breakdown of 5-fluoro-deoxyuridine triphosphate (FdUTP) and deoxyuridine triphosphate (dUTP), which are active metabolites of 5-FU. This promotes DNA polymerase-dependent incorporation of these antimetabolites into DNA and leads to DNA damage and tumor cell death. Co-administration with TAS-114 allows lower dosing of 5-FU prodrugs, which decreases 5-FU-related toxicity, while maintaining therapeutic levels of 5-FU at the tumor site.
An orally bioavailable, highly selective and potent small molecule inhibitor of the delta and gamma isoforms of phosphoinositide-3 kinase (PI3K) with potential immunomodulating and antineoplastic activities. Upon administration, duvelisib prevents the activation of the PI3K delta/gamma-mediated signaling pathways which may lead to a reduction in cellular proliferation in PI3K delta/gamma-expressing tumor cells. Unlike other isoforms of PI3K, the delta and gamma isoforms are overexpressed primarily in hematologic malignancies and inflammatory and autoimmune diseases. By selectively targeting these PI3K isoforms, PI3K signaling in normal, non-neoplastic cells is minimally or not affected which would result in a more favorable side effect profile.
An orally available agent that may prevent the formation of gallstones.
Brand name for dyclonine hydrochloride
- dyclonine hydrochloride
The hydrochloride salt of Dyclonine, an unclassified compound with local anesthetic effect. Dyclonine reversibly binds to activated sodium channels on the neuronal membrane, thereby decreasing the neuronal membrane's permeability to sodium ions, leading to an increased threshold for excitation. This reversibly stabilizes the membrane and inhibits depolarization, leading to the failure of a propagated action potential and subsequent conduction blockade. This results in a transient and reversible loss of sensation in a localized area of the body.
A synthetic, orally active progestin that may be useful in the treatment of disorders attributed to progesterone deficiency. Upon administration, dydrogesterone binds to progesterone receptors with high affinity and helps regulate the healthy growth and normal shedding of the uterine lining. Dydrogesterone appears to have no affinity for androgenic, estrogenic, glucocorticoid or mineralocorticoid receptors. Check for active clinical trialsusing this agent.
Brand name for acetohexamide
Brand name for minocycline hydrochloride
Brand name for botulinum toxin type A