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Antineoplastic agents h

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  • H1299 tumor cell lysate vaccine - A cell lysate derived from a lung cancer cell line, H1299, with potential immunostimulatory and antineoplastic activities. Upon intramuscular administration, the H1299 tumor cell lysate exposes the immune system to an undefined amount of tumor associated antigens (TAA), particularly cancer testis antigens (CTAs), which may result in the induction of both anti-tumoral cytotoxic T-lymphocytes (CTL) and antibody-dependent responses against TAA-expressing cells, leading to tumor cell lysis. CTAs, such as MAGE, are selectively expressed in a variety of cancers but are not expressed in normal, healthy cells outside the testis.
  • H3.3k27m-specific peptide vaccine - A vaccine composed of a peptide derived from histone H3.3 containing the amino acid substitution mutation lysine (Lys) 27-to-methionine (H3.3K27M), with potential immunoactivating and antineoplastic activities. Upon administration of the H3.3K27M-specific peptide vaccine, the immune system may exert a cytotoxic T-lymphocyte (CTL)-mediated immune response against H3.3K27M-expressing tumor cells. The H3.3K27M mutation alters the methylation and acetylation profile of the histone H3 variant H3.3 at Lys 27. Modification of H3.3 at Lys 27 regulates gene expression, and the H3.3K27M mutation occurs in a variety of cancer cell types.
  • Haah lambda phage vaccine sns-301 - A nanoparticle-based cancer vaccine composed of a neutralized bacteriophage Lambda construct that is genetically engineered to contain peptide fragments of human aspartyl/asparaginyl beta-hydroxylase (HAAH; ASPH) on its surface and are fused to the C-terminus of the head protein of phage lambda gpD, with potential immunostimulating and antineoplastic activities. HAAH lambda phage vaccine SNS-301 also contains DNA fragments representing the phage CpG motif that activate the MHC class II pathway. Upon intradermal administration of the HAAH lambda phage vaccine SNS-301, the bacteriophage exposes the immune system to HAAH, producing a HAAH-specific antibody response, and may activate the immune system to induce a cytotoxic T-lymphocyte (CTL)-mediated immune response against HAAH-expressing tumor cells. HAAH is a transmembrane protein and highly conserved enzyme that catalyzes the hydroxylation of aspartyl and asparaginyl residues in epidermal growth factor-like domains of substrate proteins. HAAH is normally expressed in fetal development and is upregulated in a variety of cancer cell types, while its expression is nearly absent in healthy, normal cells. HAAH plays a key role in cancer cell growth, cell motility and invasiveness. Its expression is associated with a poor prognosis.
  • Hafnium oxide-containing nanoparticles nbtxr3 - A suspension of nanoparticles containing inert inorganic hafnium oxide (HfO2) crystals with potential antineoplastic activity. Upon injection of NBTXR3 in the tumor, the hafnium oxide-containing nanoparticles accumulate into the tumor cells. Subsequent application of radiation beams to the tumor tissue causes HfO2 particles to emit huge amounts of electrons. This results in the formation of free radicals within the tumor cells, which in turn causes targeted destruction of the cancer cells. Compared to standard radiotherapy, because of the inert nature of NBTXR3, this agent emits electrons only during its exposure to radiation which improves radiotherapy efficiency.
  • Halichondrin analogue e7130 - A halichondrin analogue derived from a marine sponge with potential antineoplastic activity. Upon intravenous infusion, halichondrin analogue E7130 may bind to the vinca domain of tubulin and inhibit the polymerization of tubulin and the assembly of microtubules, thereby inhibiting mitotic spindle assembly and inducing cell cycle arrest at the G2/M phase.
  • Halofuginone - An orally-active quinazolinone alkaloid with potential antineoplastic activity. Halofuginone interferes with the signaling pathway of transforming growth factor beta (TGF beta) and inhibits expression of matrix metalloproteinase 2, thereby inhibiting collagen type I synthesis and inducing extracellular matrix degradation, resulting in inhibition of angiogenesis, tumor growth, or metastasis.
  • Halofuginone hydrobromide - The hydrobromide salt of halofuginone, a semisynthetic quinazolinone alkaloid anticoccidial derived from the plant Dichroa febrifuga, with antifibrotic and potential antineoplastic activities. Halofuginone specifically inhibits collagen type I gene expression and matrix metalloproteinase 2 (MMP-2) gene expression, which may result in the suppression of angiogenesis, tumor stromal cell development, and tumor cell growth. These effects appear to be due to halofuginone-mediated inhibition of the collagen type I and MMP-2 promoters. Collagen type I and MMP-2 play important roles in fibro-proliferative diseases.
  • Haploidentical natural killer cells k-nk002 - A population of ex-vivo expanded and activated haploidentical donor-derived natural killer (NK) cells, with potential immunomodulating and antineoplastic activities. Upon administration prior to and following haploidentical hematopoietic cell transplantation, the haploidentical NK cells K-NK002 may induce an anti-tumor immune response and may exert cytotoxicity against tumor cells.
  • Hcv dna vaccine ino-8000 - A multi-antigen DNA vaccine consisting of plasmids encoding the hepatitis C virus (HCV) nonstructural proteins 3 (NS3), 4A (NS4A), 4B (NS4B) and 5A (NS5A), with potential immunomodulating and cancer preventive activities. Administered via intramuscular injection followed by electroporation, cells transfected with the HCV DNA vaccine INO-8000 express the encoded HCV proteins, which may elicit a cytotoxic T-lymphocyte (CTL) response against HCV-infected liver cells expressing the NS3, NS4A, NS4B or NS5A proteins. This results in the eradication of HCV-infected cells. HCV, a small, enveloped, single-stranded RNA virus belonging to the Flaviviridae family, is associated with the development of hepatocellular carcinoma (HCC).
  • Hdac class i/iib inhibitor hg146 - An orally available inhibitor of histone deacetylase (HDAC) classes I and IIb with potential antineoplastic activities. Upon oral administration, HDAC I/IIb inhibitor HG146 selectively inhibits the catalytic activity of class I and IIb HDACs, which results in an accumulation of highly acetylated chromatin histones, the induction of chromatin remodeling and an altered pattern of gene expression. This leads to the inhibition of tumor oncogene transcription, and the selective transcription of tumor suppressor genes, which inhibits tumor cell division and induces tumor cell apoptosis. HDAC, an enzyme upregulated in many tumor types, deacetylates chromatin histone proteins. Class I HDACs are located in the nucleus and include HDACs 1, 2, 3, and 8; class IIb HDACs include HDAC 6 and 10 and are located in both the nucleus and the cytoplasm.
  • Hdac inhibitor ar-42 - An orally available phenylbutyrate-derived histone deacetylase (HDAC) inhibitor, with potential antineoplastic activity. Upon oral administration, AR-42 inhibits the catalytic activity of HDAC, which results in an accumulation of highly acetylated chromatin histones, the induction of chromatin remodeling and an altered pattern of gene expression. This leads to the inhibition of tumor oncogene transcription, and the selective transcription of tumor suppressor genes, which inhibits tumor cell division and induces tumor cell apoptosis. HDAC, an enzyme upregulated in many tumor types, deacetylates chromatin histone proteins.
  • Hdac inhibitor ckd-581 - A highly water-soluble, pan histone deacetylase (HDAC) inhibitor, with potential antineoplastic activity. Upon administration, HDAC inhibitor CKD-581 targets and inhibits HDAC, resulting in an accumulation of highly acetylated histones, the induction of chromatin remodeling, and an altered pattern of gene expression. This leads to the inhibition of tumor oncogene transcription, and the selective transcription of tumor suppressor genes, which results in the inhibition of tumor cell division and the induction of tumor cell apoptosis. HDACs, upregulated in many tumor cell types, are a family of metalloenzymes responsible for the deacetylation of chromatin histone proteins.
  • Hdac inhibitor cxd101 - A novel histone deacetylase (HDAC) inhibitor with potential antineoplastic activity. Although the exact therapeutic mechanism of action for CXD101 is not known, oral administration of this agent should inhibit the catalytic activity of HDAC, which results in an accumulation of highly acetylated histones, followed by the induction of chromatin remodeling and an altered pattern of gene expression. HDAC, a family of enzymes upregulated in many tumor types, deacetylates chromatin-associated histone proteins.
  • Hdac inhibitor mpt0e028 - An orally bioavailable N-hydroxyacrylamide-derived inhibitor of both human pan-histone deacetylase (HDAC) enzymes and the serine/threonine protein kinase Akt (protein kinase B), with potential antineoplastic activity. Upon administration, HDAC inhibitor MPT0E028 selectively binds to and inhibits HDACs, which inhibits deacetylation of histone proteins and leads to the accumulation of highly acetylated histones. This may result in both an induction of chromatin remodeling, and the selective transcription of tumor suppressor genes. This prevents cell division and induces both cell cycle arrest and apoptosis, which may inhibit the proliferation of susceptible tumor cells. In addition, MPT0E028 inhibits the phosphorylation and activation of Akt, which prevents the activation of downstream signaling pathways, independent of its HDAC inhibitory activity. HDACs, upregulated in many tumor cell types, are a family of enzymes that deacetylate histone proteins. Akt, overexpressed in many tumor cell types, plays a key role in tumor cell proliferation and survival.
  • Hdac inhibitor obp-801 - An inhibitor of histone deacetylase (HDAC) enzymes, with potential antineoplastic activity. Upon administration, OBP-801 inhibits the activity of HDACs; this results in an accumulation of highly acetylated chromatin histones, the induction of chromatin remodeling and an altered pattern of gene expression. This leads to selective transcription of tumor suppressor genes, tumor suppressor protein-mediated inhibition of tumor cell division and induction of tumor cell apoptosis. This may inhibit proliferation of susceptible tumor cells. HDAC, which is upregulated in many tumor cell types, deacetylates chromatin histone proteins.
  • Hdac/egfr/her2 inhibitor cudc-101 - A multi-targeted, small-molecule inhibitor of histone deacetylase (HDAC), epidermal growth factor receptor tyrosine kinase (EGFR/ErbB1), and human epidermal growth factor receptor 2 tyrosine kinase (HER2/neu or ErbB2) with potential antineoplastic activity. HDAC/EGFR/HER2 inhibitor CUDC-101 inhibits the activity of these three enzymes but the exact mechanism of action is presently unknown. This agent may help overcome resistance to inhibition of EGFR and Her2 through a simultaneous, synergistic inhibition of EGFR, Her2, and HDAC.
  • Hdac6 inhibitor ka2507 - An orally bioavailable inhibitor of histone deacetylase (HDAC) type 6 (HDAC6; HDAC-6), with potential antineoplastic activity. Upon administration, KA2507 targets, binds to and inhibits the activity of HDAC6. This results in an accumulation of highly acetylated chromatin histones, the induction of chromatin remodeling and an altered pattern of gene expression. Specifically, inhibition of HDAC6 prevents STAT3 activity, which leads to a reduction in programmed death-1 (PD-1) expression. Eventually, this results in a selective transcription of tumor suppressor genes, tumor suppressor protein-mediated inhibition of tumor cell division and an induction of apoptosis in tumor cells that overexpress HDAC6. HDAC6, which is upregulated in many tumor cell types, deacetylates chromatin histone proteins.
  • Hdac8 inhibitor nbm-bmx - An orally bioavailable inhibitor of histone deacetylase (HDAC) type 8 (HDAC8; HDAC-8), with potential antineoplastic activity. Upon administration, NBM-BMX targets and inhibits the activity of HDAC8. This results in an accumulation of highly acetylated chromatin histones, chromatin remodeling, and selective transcription of tumor suppressor genes, ultimately promoting cell-cycle arrest and induction of tumor cell apoptosis. HDAC8, a class 1 histone deacetylase, plays a key role in transcriptional regulation and cell cycle progression. Aberrant expression of HDAC8 or deregulated interactions with transcription factors may contribute to tumorigenesis. Isotype-selective HDAC inhibitors may be associated with fewer adverse effects compared to pan-HDAC inhibitors.
  • Hdm2 inhibitor mk-8242 - An orally bioavailable inhibitor of human homolog of double minute 2 (HDM2), with potential antineoplastic activity. Upon oral administration, HDM2 inhibitor MK-8242 inhibits the binding of the HDM2 protein to the transcriptional activation domain of the tumor suppressor protein p53. By preventing this HDM2-p53 interaction, the degradation of p53 is inhibited, which may result in the restoration of p53 signaling. This induces p53-mediated tumor cell apoptosis. HDM2 is a member of the RING finger-type family of E3 ubiquitin protein ligases and targets p53 for degradation; it is often overexpressed in cancer cells and has been implicated in cancer cell proliferation and survival.
  • Heat-treated bacterium mycobacterium obuense imm-101 - A suspension of heat-killed Mycobacterium (M.) obuense, a non-pathogenic and naturally-occurring bacterium, with potential immunomodulating and antineoplastic activities. Upon intradermal administration of heat-killed M. obuense IMM-101, the bacteria are able to activate the innate and adaptive immune system. Specifically, IMM-101 activates immature dendritic cells (DCs), which leads to the induction of a type-1 immune response (cDC1). This may induce a cytotoxic T-lymphocyte (CTL)-mediated immune response against cancer cells. It also activates macrophages and natural killer cells (NKs), gamma delta T (gdT) cells, and induces a type 1 T helper (Th1) cell immune response against cancer cells.
  • Hedgehog inhibitor ipi-609 - A novel proprietary small molecule, and a selective inhibitor of sonic hedgehog signaling pathway, with potential anti-tumor activity. The hedgehog signaling pathway is normally active during neuronal development in embryos and quiescent in adult cells. However, aberrant activation of the hedgehog pathway in adults has been implicated in many cancers, including cancers of the pancreas, prostate, lung (small cell), and brain (glioma). IPI-609 exerts its effect through inhibiting the hedgehog signaling pathway and thereby alters gene expressions of the cancer cells.
  • Hematoporphyrin derivative - A complex mixture of monomeric and aggregated porphyrins with photosensitizing activity. Upon systemic administration, hematoporphyrin derivatives accumulate in tumor cells and, once activated by red laser light (630 nm), in the presence of oxygen, produce singlet oxygen and other reactive oxygen radicals, resulting in local radical-mediated tumor cell death.
  • Hemiasterlin analog e7974 - An analog of the sponge-derived anti-microtubule tripeptide hemiasterlin with antimitotic and potential antineoplastic activities. Hemiasterlin analog E7974 binds to the Vinca domain on tubulin, resulting in inhibition of tubulin polymerization and microtubule assembly; depolymerization of existing microtubules; inhibition of mitosis; and inhibition of cellular proliferation. This agent may have more affinity for the beta-3 tubulin isotype.
  • Henatinib maleate - The maleate salt form of henatinib, an orally bioavalable, multitargeted tyrosine kinase inhibitor with potential antitumor and antiangiogenic activities. Henatinib inhibits vascular endothelial growth factor receptor type 2 (VEGFR2), a tyrosine kinase receptor upregulated in many tumor cells that plays a key role in angiogenesis. This may result in an inhibition of angiogenesis and eventually tumor cell proliferation. Henatinib, structurally similar to sunitinib, also inhibits, though to a lesser extent, mast/stem cell growth factor receptor (c-Kit) and, platelet-derived growth factor receptor (PDGFR) alpha and beta.
  • Heparan sulfate glycosaminoglycan mimetic m402 - A low molecular weight heparin derivative and heparan sulfate proteoglycan (HSPG) mimetic with no or minimal anticoagulant activity and potential antineoplastic activities. Upon administration, M402 mimics HSPGs by binding to and inhibiting various heparin-binding growth factors, chemokines, and cytokines such as VEGF, HGF, FGF2, SDF-1a, heparanase and P-selectin all of which are essential for tumor angiogenesis and metastasis to occur. This inhibits heparin binding growth factor-mediated signaling and disrupts tumor-stromal interactions eventually leading to an inhibition of angiogenesis and tumor cell progression. In addition, M402 may enhance the cytotoxic effect of other chemotherapeutic agents.
  • Her2 ecd+tm virus-like replicon particles vaccine avx901 - A cancer vaccine based on virus-like replicon particles (VRP) packaged with an alphaviral vector encoding the extracellular domain (ECD) and transmembrane (TM) regions of the human epidermal growth factor receptor 2 (EGFR2, NEU or HER2), with potential antineoplastic activity. After immunization with HER2 ECD+TM virus-like replicon particles vaccine AVX901, the VRPs infect cells and express HER2 ECD+TM protein that may activate the immune system to elicit a cytotoxic T-lymphocyte (CTL) response against HER2-expressing tumor cells. The alphaviral replicon of this vaccine is an attenuated strain of the Venezuelan equine encephalitis virus (VEEV) in which 3 of the 7 viral genes were substituted with a truncated HER2 gene to create a self-amplifying replicon RNA. HER2, a tyrosine kinase involved in several cell growth signaling pathways, is dysregulated or overexpressed in a wide variety of cancer cell types.
  • Her2 inhibitor cp-724,714 - An orally bioavailable quinazoline with potential antineoplastic activity. CP-724,714 selectively binds to the intracellular domain of HER2, reversibly inhibiting its tyrosine kinase activity and resulting in suppression of tumor cell growth. HER2, a member of the epidermal growth factor receptor (EGFR) family, is overexpressed in many adenocarcinomas, particularly breast cancers.
  • Her2 inhibitor dzd1516 - An orally bioavailable, blood brain barrier (BBB) penetrable inhibitor of the receptor tyrosine kinase human epidermal growth factor receptor 2 (HER2; ErbB2; HER-2), with potential antineoplastic activity. Upon oral administration, HER2 inhibitor DZD1516 selectively binds to and inhibits the activity of HER2. This prevents HER2-mediated signaling and leads to cell death in HER2-expressing tumor cells. HER2, a receptor tyrosine kinase overexpressed on a variety of tumor cell types, plays an important role in tumor cell proliferation and tumor vascularization.
  • Her2 inhibitor tas0728 - An orally available covalent inhibitor of human epidermal growth factor receptor 2 (HER2; ERBB2), with potential antineoplastic activity. Upon oral administration, HER2 inhibitor TAS0728 specifically and irreversibly binds to and inhibits the activity of HER2. This prevents HER2-mediated signaling and leads to cell death in HER2- and HER3 (ErbB3)-expressing tumor cells. HER2, a receptor tyrosine kinase mutated or overexpressed in many tumor cell types, play key roles in tumor cell proliferation and tumor vascularization. HER3 has no active kinase domain but is activated through heterodimerization with other members of the EGFR receptor family, such as HER2.
  • Her2 tri-specific natural killer cell engager df1001 - An engineered molecule based on tri-specific natural killer (NK) cell engager therapies (TriNKET) that is directed against human epidermal growth factor receptor 2 (EGFR2; HER2; ErbB2), with potential immunostimulating and antineoplastic activities. Upon administration, HER2 tri-specific NK cell engager DF1001 targets and binds to HER2 on tumor cells and simultaneously binds to NK cells, thereby bringing HER2-expressing tumor cells and NK cells together, which stimulates the NK cells and results in the selective NK cell-mediated tumor cell lysis of HER2-expressing tumor cells. The binding of HER2-expressing tumor cells and NK cells may also lead to the activation of T-cells and B-cells, potentiating the immune response against HER2-expressing tumor cells. HER2, a receptor tyrosine kinase (RTK) mutated or overexpressed in many tumor cell types, plays a key role in tumor cell proliferation and tumor vascularization.
  • Her-2/neu intracellular domain protein - The cytoplasmic domain or intracellular domain (ICD) of the HER2/neu protein that exhibits tyrosine kinase activity. Based on sensitization theory, co-administration of trastuzumab (anti-HER-2/neu monoclonal antibody) and HER-2/neu intracellular domain protein may result in the potentiation of a HER2/neu-specific cytotoxic T lymphocyte (CTL) response against tumor cells overexpressing the HER2/neu protein. HER-2/neu protein, a glycoprotein cell surface receptor that is composed of an extracellular domain (ECD), a transmembrane domain, and an ICD, is overexpressed by many adenocarcinomas including breast adenocarcinoma.
  • Her-2/neu peptide vaccine - A cancer vaccine comprised of peptides derived from the extracellular domain of the tumor-associated antigen Her-2/neu with potential antineoplastic activity. HER-2/neu peptide vaccine may induce antibodies with anti-tumor activity and may also elicit a specific CD8 T-cell response against specific tumor cell types.
  • Her2bi-armed activated t cells - Activated T cells (ATC) that have been coated with bispecific antibodies (BiAb), with potential antineoplastic and immunomodulating activities. In vitro, T cells are activated through exposure to the anti-CD3 murine monoclonal antibody OKT3 and interleukin 2 for 14 days and then armed with anti-CD3 x anti-Her2 bispecific antibody (Her2Bi). Upon administration, HER2Bi-armed activated T cells attach to CD3-expressing T cells and HER2/neu-expressing tumor cells, selectively cross-linking T cells and tumor cells; this may result in the recruitment and activation of cytotoxic T lymphocyte (CTLs), CTL perforin-mediated tumor cell cytolysis, and the secretion of antitumor cytokines and chemokines.
  • Her-2-positive b-cell peptide antigen p467-dt-crm197/montanide vaccine imu-131 - A cancer vaccine consisting of a fusion peptide, composed of three peptides derived from the extracellular domain (ECD) of the HER2 peptide antigen found on B-cells (P4, P6 and P7; P467), conjugated to the carrier protein DT-CRM197, a non-toxic, mutated form of diphtheria toxin (DT), and combined with the immunoadjuvant montanide ISA 51, with potential immunostimulatory and antineoplastic activities. Upon administration, IMU-131 vaccine induces the production of polyclonal antibodies against the HER2 protein. In turn, the antibodies bind to three separate binding sites on HER2 expressed on tumor cells and inhibit HER2 dimerization and activity, which leads to the inhibition of HER2-mediated signal transduction pathways. This induces apoptosis in and reduces cellular proliferation of HER2-overexpressing tumor cells. In addition, IMU-131 induces a cytotoxic T-lymphocyte (CTL) response against the HER2-expressing tumor cells. The tumor-associated antigen (TAA) HER2, also called Neu or ErbB2, is a tyrosine kinase receptor for epidermal growth factor (EGF) and is often overexpressed by a variety of tumor cell types. Montanide ISA 51, also known as incomplete Freund's adjuvant or IFA, is a stabilized water-in-oil (w/o) emulsion adjuvant containing mineral oil with mannide oleate added as a surfactant that non-specifically stimulates cell-mediated immune responses to antigens. DT-CRM197 is used to increase the immunogenicity of the HER2/neu peptide antigen. In P467, the three B-cell epitopes were combined in a specific order into a single 49 amino acid peptide antigen.
  • Her2-pulsed autologous type-1 polarized dendritic cell vaccine - A dendritic cell (DC)-based cancer vaccine composed of autologous, type-1 polarized dendritic cells (DCs) pulsed with human leukocyte antigen (HLA)-A2-restricted HER-2-derived peptides, with potential immunomodulatory and antineoplastic activities. Autologous DCs were treated with GM-CSF, interleukin-4, interferon-gamma and bacterial lipopolysaccharide (LPS), a toll-like receptor type 4 agonist, to produce highly polarized DCs (alphaDC1) that are capable of producing high levels of interleukin-12p70 (IL-12p70). Upon administration, HER2-pulsed autologous DC vaccine may stimulate a potent cytotoxic T-lymphocyte (CTL) response against HER-2-positive tumor cells, which may result in tumor cell death and decreased tumor growth. HER-2, a tyrosine kinase receptor for epidermal growth factor (EGF) (also known as neu and ErbB2), is overexpressed by a variety of cancers.
  • Her2-targeted darpin mp0274 - A proprietary, designed ankyrin repeat proteins (DARPin)-based agent targeting the tyrosine kinase receptor epidermal growth factor receptor 2 (HER2; ErbB2), with potential antineoplastic activity. Compared to antibodies, DARPins are small in size, have favorable pharmacokinetics and allow for both high affinity binding and efficacy. Upon administration, the HER2-targeted DARPin MP0274 binds to two distinct non-overlapping epitopes on HER2, thereby inhibiting the activity of HER2 and promoting HER2 internalization. This prevents HER2-mediated signaling, induces apoptosis and inhibits the growth of HER2-overexpressing tumor cells. DARPin also binds to human serum albumin, which extends the half-life of MP0274. HER2 is overexpressed in a variety of cancer cell types and is associated with increased tumor cell proliferation.
  • Her2-targeted liposomal doxorubicin hydrochloride mm-302 - An antibody-targeted lipidic nano-carrier containing the antineoplastic anthracycline antibiotic doxorubicin encapsulated within liposomes, and conjugated to a monoclonal antibody against the human epidermal growth factor receptor 2 (HER2), with potential antitumor activity. Upon administration of HER2-targeted liposomal doxorubicin hydrochloride MM-302, the immunoliposome allows for specific delivery of doxorubicin to tumors overexpressing the HER2 receptor. Once inside the HER2-expressing tumor cells, doxorubicin intercalates into DNA and interferes with topoisomerase II activity, thereby inhibiting DNA replication and RNA synthesis. Compared to doxorubicin alone or liposomal doxorubicin, targeted liposomal delivery of doxorubicin improves efficacy while lowering the toxicity profile. HER2, a tyrosine kinase receptor, is overexpressed in many cancer cell types.
  • Her2-targeting antibody fc fragment fs102 - A proprietary, antibody fragment composed of a constant (Fc) region that is engineered to bind to the tumor-associated antigen human epidermal growth factor receptor-2 (HER2), with potential antineoplastic activity. HER2-targeted antibody Fc fragment FS102 specifically binds to its HER2 epitope, and causes downregulation of HER2-mediated signaling. This leads to tumor cell apoptosis. HER2, a member of the receptor tyrosine kinase (RTK) epidermal growth factor receptor (EGFR) superfamily, is overexpressed on the cell surface of various solid tumors.
  • Herba scutellaria barbata - A Chinese herb isolated from the plant Scutellaria barbata D. Don (Lamiaceae) with potential antineoplastic activity. Containing the antioxidant flavone scutellarin, herba Scutellaria barbata has been shown to induce apoptosis of ovarian and breast tumor cells in vitro.
  • Herbimycin - A benzoquinone antineoplastic antibiotic isolated from the bacterium Streptomyces hygroscopicus. Herbimycin binds to and inhibits the cytosolic chaperone functions of heat shock protein 90 (HSP90). HSP90 maintains the stability and functional shape of many oncogenic signaling proteins; the inhibition of HSP90 promotes the proteasomal degradation of oncogenic signaling proteins that may be over-expressed or overactive in tumor cells.
  • Heterodimeric interleukin-15 - A fusion protein complex composed of heterodimeric IL-15 (hetIL-15), which consists of a synthetic form of the endogenous cytokine interleukin-15 chain (IL-15) complexed to the soluble IL-15 binding protein IL-15 receptor alpha chain (IL-15Ra) (IL15:sIL-15Ra), with potential immunomodulatory, anti-infective and antineoplastic activities. Upon administration, hetIL-15 binds to the IL-2/IL-15 receptor beta-common gamma chain (IL-2Rbeta-gamma) receptor on natural killer (NK) and T-lymphocytes, which activates and increases the levels of NK cells and CD8+ and CD4+ T-cells. The T-cells enhance the secretion of the cytokine interferon-gamma (IFN-g), which further potentiates the immune response against tumor cells. Altogether, this enhances tumor cell killing and decreases tumor cell proliferation. By coupling IL-15 to IL15Ra, this agent has an improved pharmacokinetic profile, shows an increased ability to bind IL-2Rbeta-gamma, and shows increased immunostimulatory activity as compared to IL-15 alone.
  • Hexamethylene bisacetamide - A hybrid polar-planar compound with potential antineoplastic activity that induces terminal differentiation, inhibits cell growth, and causes apoptosis in several tumor cell lines. Its precise mechanism of action is unknown.
  • Hexaminolevulinate - The hexyl ester of 5-aminolevulinic acid (ALA) with photodynamic properties. As a precursor of photoactive porphorins, hexyl 5-aminolevulinate induces the endogenous production of the photosensitizer protoporphyrin IX (PPIX) which accumulates selectively in tumor tissue. When exposed to specific wavelengths of light, PPIX is activated and, depending on the wavelength and/or intensity of light, either fluoresces, thereby allowing tumor imaging, or induces tumor cell apoptosis.
  • Hexylresorcinol - A substituted phenol with bactericidal, antihelminthic and potential antineoplastic activities. Hexylresorcinol is used as an antiseptic in mouthwashes and skin wound cleansers. Hexylresorcinol may also inhibit oxidative DNA damage by enhancing the activity of antioxidant enzymes, including glutathione peroxidase and glutathione reductase, which facilitate scavenging reactive oxygen molecules by glutathione (GSH).
  • Hif-1alpha inhibitor px-478 - An orally active small molecule with potential antineoplastic activity. Although its mechanism of action has yet to be fully elucidated, HIF1-alpha inhibitor PX-478 appears to inhibit hypoxia-inducible factor 1-alpha (HIF1A) expression, which may result in decreased expression of HIF1A downstream target genes important to tumor growth and survival, a reduction in tumor cell proliferation, and the induction of tumor cell apoptosis. The inhibitory effect of this agent is independent of the tumor suppressor genes VHL and p53 and may be related to derangements in glucose uptake and metabolism due to inhibition of glucose transporter-1 (Glut-1).
  • Hif2a rnai aro-hif2 - An RNA interference (RNAi) targeting hypoxia-inducible factor 2alpha (HIF-2a), with potential antineoplastic activity. Upon administration of HIF2a RNAi ARO-HIF2, the agent binds to and neutralizes mRNA HIF2a, thereby preventing the production of HIF2a. This may lead to an inhibition of tumor cell proliferation. HIF2a, overexpressed in certain cell types, plays a key role in proliferation, progression and metastasis of tumors.
  • Hif-2alpha inhibitor pt2385 - An orally active, small molecule inhibitor of hypoxia inducible factor (HIF)-2alpha, with potential antineoplastic activity. Upon oral administration, HIF-2alpha inhibitor PT2385 allosterically binds to HIF-2alpha, thereby preventing HIF-2alpha heterodimerization and its subsequent binding to DNA. This results in decreased transcription and expression of HIF-2alpha downstream target genes, many of which regulate tumor cell growth and survival. Blocking HIF-2alpha reduces the proliferation of HIF-2alpha-expressing tumor cells. HIF-2alpha, a heterodimeric transcription factor overexpressed in many cancers, promotes tumorigenesis.
  • High-selenium brassica juncea - A formulation of the mustard plant Brassica juncea grown in a medium that has been enriched with the trace element selenium with potential chemopreventive and chemopotentiating activities. Brassica juncea hyperaccumulates trace elements in soil. Selenium amino acid species found in selenized Brassica juncea include methylselenomethionine (MeSeMet) and methylselenocysteine (MeSeCys); both may be incorporated into selenoproteins in vivo. Selenium functions as a cofactor for antioxidant enzymes such as glutathione peroxidases and thioredoxin reductase, which protect cells from the free radical damage. In addition, in vitro MeSeCys has been shown to potentiate the antitumor effects of the irinotecan metabolite SN-38, by inducing phosphorylation of checkpoint kinase 2 (chk2) at threonine 68, which results in poly(ADP-ribose) polymerase cleavage, caspase 3 activation, and DNA fragmentation.
  • Histone-lysine n-methyltransferase ezh2 inhibitor gsk2816126 - A small molecule selective and S-adenosyl methionine (SAM) competitive inhibitor of histone-lysine N-methyltransferase EZH2, with potential antineoplastic activity. Upon administration, histone-lysine N-methyltransferase EZH2 inhibitor GSK2816126 inhibits the activity of EZH2 and specifically prevents the methylation of histone H3 lysine 27 (H3K27). This decrease in histone methylation alters gene expression patterns associated with cancer pathways and results in decreased tumor cell proliferation in cancer cells that overexpress this enzyme. EZH2, which belongs to the class of histone methyltransferases (HMTs), is overexpressed or mutated in a variety of cancers and plays a key role in tumor cell proliferation.
  • Histrelin acetate - The acetate salt form of histrelin, a long-acting, synthetic nonapeptide analog of gonadotropin-releasing hormone (GnRH) with potential anti-tumor activity. Upon administration, histrelin binds to and activates GnRH receptors; prolonged administration results in pituitary GnRH receptor desensitization and inhibition of follicle stimulating hormone (FSH) and luteinizing hormone (LH) secretion, leading to a significant decline in testosterone production in males and may inhibit androgen receptor-positive tumor progression; in females, prolonged administration results in decreased estradiol production.
  • Hla-a*0201 restricted tert(572y)/tert(572) peptides vaccine vx-001 - A peptide-based cancer vaccine consisting of two human leukocyte antigen (HLA)-A*0201 restricted 9-mer epitopes derived from the human telomerase reverse transcriptase (hTERT), TERT 572Y (YLFFYRKSV; TYR-Vx001) and TERT 572 (RLFFYRKSV; ARG-Vx001), with potential immunostimulating and antineoplastic activities. Subcutaneous injection of TERT(572Y) peptide followed by subcutaneous administration of the TERT(572) peptide may elicit a specific and possibly optimal cytotoxic T cell (CTL) response against hTERT-expressing tumor cells. hTERT, the catalytic subunit of human telomerase, is an human leukocyte antigen-A*0201-restricted cryptic epitope of telomerase. TERT is expressed in the majority of human cancer cells, is not expressed or is expressed at very low levels in normal cells and plays a key role in tumorigenesis. TERT572Y is the optimized variant of the native cryptic peptide TERT572 in which tyrosine has been substituted for an arginine at position 1; TERT572Y shows increased HLA-A*0201 binding affinity compared to TERT572.
  • Hla-a*0201-restricted trp2-gp100-epha2-her2 multipeptide vaccine - A cancer vaccine containing four HLA-A*0201-restricted peptide epitopes with potential immunostimulatory and antitumor activities. Vaccine peptide epitopes are derived from the tumor associated antigens (TAAs) tyrosinase-related protein 2 (TRP2), glycoprotein 100 (gp100), Ephrin receptor A2 (EphA2) and human epidermal growth factor receptor 2 (HER2). Upon administration, HLA-A*0201-restricted TRp2-gp100-EphA2-HER2 multipeptide vaccine may stimulate a cytotoxic T lymphocyte (CTL) response against TRP2-gp100-EphA2-HER2-expressing tumor cells, resulting in tumor cell lysis and decreased tumor cell proliferation. HLA-A*0201 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*0201 may improve antigenic peptide immunogenicity.
  • Hla-a*0201-restricted urlc10-vegfr1-vegfr2 multipeptide vaccine - A cancer vaccine containing three HLA-A*0201-restricted peptide epitopes with potential immunostimulatory, antiangiogenic, and antitumor activities. Vaccine peptide epitopes are derived from the tumor associated antigen (TAA) URLC (up-regulated in lung cancer 10) and vascular endothelial growth factor receptors (VEGFR) 1 and 2. Upon administration, HLA-A*0201-restricted URLC10-VEGFR1-VEGFR2 multipeptide vaccine may stimulate a cytotoxic T lymphocyte (CTL) response against URLC10-expressing tumor cells and the tumor microvasculature expressing VEGFR 1 and 2 peptides; this may result in tumor cell lysis, the inhibition of tumor angiogenesis, and decreased tumor growth. HLA-A*0201 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*0201 may improve antigenic peptide immunogenicity.
  • Hla-a*0201-restricted vegfr1 peptide vaccine - A cancer vaccine containing an HLA-A*0201-restricted vascular endothelial growth factor receptor 1 (VEGFR1) peptide (sequence: TLFWLLLTL) with potential immunostimulatory and antitumor activities. Upon administration, HLA-A*0201-restricted VEGFR1-derived peptide vaccine may stimulate a cytotoxic T lymphocyte (CTL) response against tumor cells expressing VEGFR1, resulting in tumor cell lysis and decreased tumor growth. HLA-A*0201 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*0201 may improve antigenic peptide immunogenicity.
  • Hla-a*0201-restricted vegfr1-vegfr2 multipeptide vaccine - A cancer vaccine containing two HLA-A*0201-restricted peptide epitopes with potential immunostimulatory and antitumor activities. Peptide epitopes in this vaccine are derived from: vascular endothelial growth factor receptors (VEGFR) 1 and 2. Upon administration, HLA-A*0201-restricted VEGFR1-VEGFR2 multipeptide vaccine may stimulate a cytotoxic T lymphocyte (CTL) response against tumor cells expressing VEGFR 1 and 2 peptides, resulting in tumor cell lysis and decreased tumor growth. HLA-A*0201 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*0201 may improve antigenic peptide immunogenicity.
  • Hla-a*2402-restricted cdca1-a24-56 peptide vaccine - A cancer vaccine containing the HLA-A*2402-restricted peptide epitope derived from cell division associated gene 1 (CDCA1), with potential immunostimulatory and antitumor activities. Upon administration, HLA-A*2402-restricted CDCA1-A24-56 peptide vaccine may stimulate a cytotoxic T lymphocyte (CTL) response against CDCA1-expressing tumor cells, resulting in tumor cell lysis and decreased tumor cell proliferation. 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.
  • Hla-a*2402-restricted cdca1-kif20a multipeptide vaccine - A cancer vaccine containing two HLA-A*2402-restricted peptide epitopes derived from cancer-testis antigens with potential immunostimulatory and antitumor activities. The peptide epitopes are derived from cell division associated 1 (CDCA1) and kinesin-like family member 20A (KIF20A). Upon administration, HLA-A*2402-restricted CDCA1-KIF20A multipeptide vaccine may stimulate a cytotoxic T lymphocyte (CTL) response against CDCA1- and KIF20A-expressing tumor cells, resulting in tumor cell lysis and decreased tumor cell proliferation. 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.
  • Hla-a*2402-restricted cdca1-urlc10-kif20a-depdc1-mphosph1 multipeptide vaccine - A cancer vaccine containing five HLA-A*2402-restricted peptide epitopes with potential immunostimulatory and antitumor activities. Peptide epitopes in this vaccine are derived from CDCA1 (cell division cycle-associated protein 1), URLC10 (up-regulated lung cancer 10), KIF20A (kinesin-like family member 20A), DEPDC1 (DEP domain containing 1), and MPHOSPH1 (M phase phosphoprotein 1). Upon administration, this peptide vaccine may stimulate a cytotoxic T lymphocyte (CTL) response against CDCA1-,URLC10-,KIF20A-,DEPDC1-, or MPHOSPH1-expressing tumor cells, resulting in tumor cell lysis and decreased tumor growth. 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.
  • Hla-a*2402-restricted koc1-ttk-co16-depdc1-mphosph1 multipeptide vaccine - A cancer vaccine containing five HLA-A*2402-restricted peptide epitopes with potential immunostimulatory and antitumor activities. Peptide epitopes in this vaccine are derived from IGF II mRNA binding protein 3 (KOC1); TTK protein kinase (TTK); URLC10 (up-regulated lung cancer 10); DEP domain containing 1 (DEPDC1); and M phase phosphoprotein 1 (MPHOSPH1). Upon administration, HLA-A*2404-restricted KOC1-TTK-CO16-DEPDC1-MPHOSPH1 multipeptide vaccine may stimulate a cytotoxic T lymphocyte (CTL) response against tumor cells expressing KOC1, TTK, CO16, DEPDC1 and MPHOSPH1 peptides, resulting in tumor cell lysis and decreased tumor growth. 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.
  • Hla-a*2402-restricted multipeptide vaccine s-488410 - A cancer vaccine composed of HLA-*2402-restricted epitopic peptides derived from three cancer/testis (CT) antigens, with potential antineoplastic activity. Upon subcutaneous administration, HLA-A*2402-restricted multipeptide vaccine S-488410 may elicit a cytotoxic T-lymphocyte (CTL) response against tumor cells expressing these CT antigens. CT antigens, normally expressed only in germ cells of the testis, are overexpressed in a wide variety of human cancers.
  • Hla-a*2402-restricted urlc10 peptides vaccine - A cancer vaccine containing HLA-A*2402-restricted epitope peptides URLC10 (up-regulated lung cancer 10) with potential immunostimulatory and antineoplastic activities. Upon administration, HLA-A*2402-restricted URLC10 peptides vaccine may stimulate a cytotoxic T lymphocyte (CTL) response against URLC10-expressing tumor cells. URLC10, a tumor associated antigen, is often overexpressed in lung, esophageal and gastric cancers. 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.
  • Hla-a*2402-restricted urlc10-cdca1-kif20a multipeptide vaccine - A cancer vaccine containing three HLA-A*2402-restricted peptide epitopes derived from cancer-testis antigens with potential immunostimulatory and antitumor activities. The peptide epitopes are derived from up-regulated lung cancer 10 (URLC10); cell division cycle associated 1 (CDCA1); and kinesin-like family member 20A (KIF20A). Upon administration, HLA-A*2402-restricted URLC10-CDCA1-KIF20A multipeptide vaccine may stimulate a cytotoxic T lymphocyte (CTL) response against URL10-, CDCA1-, and KIF20A-expressing tumor cells, resulting in tumor cell lysis and decreased tumor cell proliferation. 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.
  • Hla-a*2402-restricted urlc10-cdca1-vegfr1-vegfr2 multipeptide vaccine - A cancer vaccine containing four HLA-A*2402-restricted peptide epitopes with potential immunostimulatory and antitumor activities. The peptide epitopes are derived from URLC10 (up-regulated lung cancer 10); CDCA1 (cell division associated 1); and vascular endothelial growth factor receptors (VEGFRs) 1 and 2. Upon administration, HLA-A*2402-restricted URLC10-CDCA1-VEGFR1-VEGFR2 multipeptide vaccine may stimulate a cytotoxic T lymphocyte (CTL) response against URL10-, CDCA1-, VEGFR1- and VEGFR2-expressing tumor cells, resulting in tumor cell lysis and decreased tumor cell proliferation. 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.
  • Hla-a*2402-restricted urlc10-koc1-vegfr1-vegfr2 multipeptide vaccine - A cancer vaccine containing four HLA-A*2402-restricted peptide epitopes with potential immunostimulatory and antitumor activities. Peptide epitopes in this vaccine are derived from URLC10 (up-regulated lung cancer 10 or CO16); KOC1 (IGF II mRNA Binding Protein 3); and vascular endothelial growth factor receptors (VEGFRs) 1 and 2. Upon administration, this multipeptide vaccine may stimulate a cytotoxic T lymphocyte (CTL) response against URL10-, KOC1-, VEGFR1- and VEGFR2-expressing tumor cells, resulting in tumor cell lysis and decreased tumor growth. 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.
  • Hla-a*2402-restricted urlc10-ttk-koc1 multipeptide vaccine - A cancer vaccine containing three HLA-A*2402-restricted peptide epitopes with potential immunostimulatory and antitumor activities. Peptide epitopes in this vaccine are derived from URLC10 (up-regulated lung cancer 10); TTK (TTK protein kinase); and KOC1 (IGF II mRNA Binding Protein 3). Upon administration, URLC10-TTK-KOC1 multipeptide vaccine may stimulate a cytotoxic T lymphocyte (CTL) response against tumor cells expressing URLC10, TTK and KOC1 peptides, resulting in tumor cell lysis and decreased tumor growth. 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.
  • Hla-a*2402-restricted urlc10-ttk-vegfr1-vegfr2 multipeptide vaccine - A cancer vacine containing four HLA-A*2402-restricted peptide epitopes with potential immunostimulatory and antitumor activities. Peptide epitopes in this vaccine are derived from: URLC10 (up-regulated lung cancer 10), TTK (TTK protein kinase), and VEGFRs (vascular endothelial growth factor receptors) 1 and 2. Upon administration, URLC10-TTK-KOC1-VEGFR1-VEGFR2 multipeptide vaccine may stimulate a cytotoxic T lymphocyte (CTL) response against tumor cells expressing URLC10, TTK, VEGFR 1 and 2 peptides, resulting in cell lysis and decreased tumor growth. 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.
  • Hla-a*2402-restricted vegfr1 peptide vaccine - A cancer vaccine containing the HLA-A*2402-restricted vascular endothelial growth factor receptor 1 (VEGFR1) peptide epitope with potential immunostimulatory and antitumor activities. Upon administration, HLA-A*2402-restricted VEGFR1 peptide vaccine may stimulate a cytotoxic T lymphocyte (CTL) response against tumor cells expressing VEGFR 1 peptide, resulting in tumor cell lysis and decreased tumor growth. 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.
  • Hla-a*2402-restricted vegfr1/2 multipeptide vaccine - A cancer vaccine containing two HLA-A*2402-restricted peptide epitopes with potential immunostimulatory and antitumor activities. Peptide epitopes in this vaccine are derived from vascular endothelial growth factor receptors (VEGFRs) 1 and 2. Upon administration, this peptide vaccine may stimulate a cytotoxic T lymphocyte (CTL) response against VEGFR1- and VEGFR2-expressing tumor cells, resulting in tumor cell lysis and decreased tumor growth. 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.
  • Hla-a*2404-restricted rnf43-tomm34-vegfr1-vegfr2 multipeptide vaccine - A cancer vaccine containing four HLA-A*2402-restricted peptide epitopes with potential immunostimulatory and antitumor activities. Peptide epitopes in this vaccine are derived from ring finger protein 43 (RNF43); translocase of outer mitochondrial membrane 34 (TOMM34); and vascular endothelial growth factor receptors (VEGFR) 1 and 2. Upon administration, HLA-A*2404-restricted RNF43-TOMM34-VEGFR1-VEGFR2 multipeptide vaccine may stimulate a cytotoxic T lymphocyte (CTL) response against tumor cells expressing RNF43, TOMM34, and VEGFR 1 and 2 peptides, resulting in tumor cell lysis and decreased tumor growth. 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.
  • Hla-a1, a2, b35-restricted survivin peptides/montanide isa-51 vaccine - A peptide vaccine comprised of synthetic HLA-A1, -A2 and -B35 restricted survivin epitopes combined with the adjuvant Montanide ISA-51 with potential antineoplastic activity. Upon administration, HLA-A1, A2, B35-restricted survivin peptides/Montanide ISA-51 vaccine may stimulate a cytotoxic T cell response against tumor cells that overexpress survivin, resulting in tumor cell lysis. Montanide ISA-51, also known as incomplete Freund's adjuvant or IFA, is a stabilized water-in-oil emulsion adjuvant containing mineral oil with mannide oleate added as a surfactant that non-specifically stimulates cell-mediated immune responses to antigens.
  • Hla-a1-binding mage-1/mage-3 multipeptide-pulsed autologous dendritic cell vaccine - A cell-based cancer vaccine composed of autologous dendritic cells (DCs) pulsed with human leukocyte antigen (HLA)-A1-binding melanoma-associated antigen peptides MAGE-1 and MAGE-3 with potential immunomodulating and antineoplastic activity. Upon vaccination, HLA-A1-binding MAGE-1/MAGE-3 multipeptide-pulsed autologous dendritic cell vaccine may stimulate the host immune system to mount an anti-tumoral cytotoxic T lymphocyte (CTL) and antibody responses against MAGE1- and MAGE-3-expressing cancer cells, resulting in tumor cell lysis. HLA-A1 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-A1 may improve antigenic peptide immunogenicity.
  • Hla-a2, a3-restricted fgf-5 peptides/montanide isa-51 vaccine - A peptide vaccine comprised of synthetic HLA-A2- and HLA-A3-binding peptides, derived from amino acid sequences of fibroblast growth factor-5 (FGF-5), combined with the adjuvant Montanide ISA-51 with potential antineoplastic activity. HLA-A2, A3-restricted FGF-5 peptides contain motifs recognized by the MHC class I molecules HLA-A2 and HLA-A3 and may stimulate a cytotoxic T-cell response against tumor cells that overexpress FGF-5. Montanide ISA-51, a stabilized water-in-oil emulsion adjuvant containing mineral oil with mannide oleate added as a surfactant, non-specifically stimulates cell-mediated immune responses to antigens.
  • Hla-a2-binding tyr/mart-1/gp100 multipeptide-pulsed autologous dendritic cell vaccine - A cell-based cancer vaccine composed of autologous dendritic cells (DCs) pulsed with human leukocyte antigen (HLA)-A2-restricted melanoma-associated antigen peptides tyrosinase (TYR), MART-1(melanoma antigen recognized by T-cells) and melanoma antigen glycoprotein 100 (gp100), with potential immunomodulating and antineoplastic activity. Upon vaccination, HLA-A2-binding TYR/MART-1/gp100 multipeptide-pulsed autologous dendritic cell vaccine may stimulate the host immune system to mount an anti-tumoral cytotoxic T lymphocyte (CTL) and antibody responses against Tyr-, MART-1 and gp100-expressing cancer cells, resulting in tumor cell lysis. HLA-A2 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-A2 may improve antigenic peptide immunogenicity.
  • Hla-a2-restricted il-13ra2/epha2/survivin/tetanus toxoid t-helper epitopes-montanide 51 vaccine - A peptide vaccine comprised of synthetic human leukocyte antigen (HLA)-A2-restricted peptides derived from the tumor-associated antigens (TAAs) interleukin-13 receptor alpha-2 (IL-13Ra2), the tyrosine kinase receptor Ephrin receptor A2 (EphA2), and the apoptosis inhibitor protein survivin, combined with the adjuvant tetanus toxoid (TT)-derived helper T-cell peptide, and emulsified in the immunoadjuvant Montanide ISA-51, with potential immunostimulating and antineoplastic activities. Specifically, this vaccine contains the epitopes: IL-13Ralpha2 345-353:1A9V, which is an engineered peptide based on amino acids 345-353 of IL-13Ra2 where the amino acids at the first and ninth positions of the peptide have been replaced with alanine and valine, respectively, EphA2 883-891, and survivin 96-104. Upon administration, the HLA-A2-restricted IL-13Ra2/EphA2/survivin/TT T-helper epitopes-Montanide 51 vaccine may stimulate a HLA-A2-restricted cytotoxic T-lymphocyte (CTL) response against tumor cells that overexpress IL-13Ra2, EphA2, or survivin, and results in tumor cell lysis. TT T-helper peptide binds to class II major histocompatibility molecules (MHC) molecules as a nonspecific vaccine helper epitope, resulting in long-term immunopotentiation by increasing the helper T-cell response. Montanide ISA-51, a stabilized water-in-oil emulsion adjuvant containing mineral oil with mannide monooleate added as a surfactant, non-specifically stimulates cell-mediated immune responses to antigens. IL-13Ra2, EphA2 and survivin, TAAs that are overexpressed in certain tumor cell types, play key roles in tumor cell proliferation. HLA-A2 presents antigenic peptides to CD8+ T-cells; epitope design restricted to epitopes that bind most efficiently to HLA-A2 may improve peptide immunogenicity.
  • Hla-a2-restricted melanoma-specific peptides vaccine grn-1201 - A cancer peptide vaccine composed of four human leukocyte antigen (HLA)-A2 (HLA-A*02)-restricted peptides derived from four specific and separate tumor-associated antigens (TAAs) expressed by melanoma cells, with potential antineoplastic activity. Upon administration of the HLA-A2-restricted melanoma-specific peptides vaccine, the melanoma specific antigens in the vaccine activate the immune system to exert a cytotoxic T-lymphocyte (CTL) response against the HLA-A2-positive melanoma cells.
  • Hla-a2-restricted synthetic glioma antigen peptides vaccine - A synthetic peptide cancer vaccine consisting of HLA-A2-restricted peptides derived from glioma-associated antigens (GAA) with potential immunostimulating and antineoplastic activities. Upon administration, HLA-A2-restricted synthetic glioma antigen peptides vaccine may stimulate the host immune system to mount a cytotoxic T lymphocyte (CTL) response against tumor cells expressing the corresponding GAAs, resulting in glioma tumor cell lysis. HLA-A2 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-A2 may improve antigenic peptide immunogenicity.
  • Hla-b44-restricted mage-3 peptide - A peptide comprised of the synthetic human leukocyte antigen (HLA)-B44-binding peptides derived from amino acid sequences of MAGE-3 with potential antitumor activity. Vaccination with HLA-B44-restricted MAGE-3 peptide may elicit a cytotoxic T lymphocyte immune response against tumor cells expressing MAGE-3. MAGE-3 is an antigen found on many tumor cell types, including melanoma and lung, prostate, colon, thyroid, and breast cancers.
  • Hla-b44-restricted tyrosinase peptide - A synthetic peptide consisting of synthetic human leukocyte antigen (HLA)-B44-binding peptides derived from amino acid sequences of the melanoma-associated enzyme tyrosinase with potential antitumor activity. Vaccination with HLA-B44-restricted tyrosinase peptide may stimulate cytotoxic T lymphocyte response against tyrosinase-expressing tumor cells, resulting in decreased tumor growth and cell lysis.
  • Hla-dp0401/0402-restricted mage-a3-reactive t cell receptor-transduced autologous t cells - Human autologous T-lymphocytes transduced with a retroviral vector encoding a T-cell receptor (TCR) specific for the human leukocyte antigen (HLA)-DP0401/0402-restricted, melanoma antigen A3 (MAGE-A3), with potential antineoplastic activity. CD4-positive cells are isolated from a patient, transduced with an anti-MAGE-A3-DP0401/0402 restricted TCR, expanded ex vivo, and reintroduced into the HLA-DP0401/0402 positive patient. Then, the HLA-DP0401/0402-restricted, MAGE-A3-reactive TCR-transduced autologous T cells bind to tumor cells expressing the MAGE-A3 antigen, which may result in both an inhibition of growth and increased cell death for MAGE-A3-expressing cancer cells. The tumor-associated antigen MAGE-A3 is overexpressed by a variety of cancer cell types.
  • Hm2/mmae antibody-drug conjugate alt-p7 - An antibody-drug conjugate (ADC) composed of the trastuzumab biobetter HM2 conjugated, in a site-specific manner, to monomethyl auristatin E (MMAE), an auristatin derivative and potent microtubule disrupting agent, with potential antineoplastic activity. Upon administration of ALT-P7, the antibody moiety targets and binds to human epidermal growth factor receptor 2 (HER2) on tumor cells. Upon antibody/antigen binding and internalization, the MMAE moiety is released, binds to tubulin and inhibits its polymerization, which results in G2/M phase arrest and apoptosis. HER2 is a receptor tyrosine kinase (RTK) that is overexpressed by many cancer cell types.
  • Hodgkin's antigens-gm-csf-expressing cell vaccine - An allogeneic vaccine consisting of Hodgkin lymphoma cells transfected with the granulocyte macrophage-colony-stimulating factor (GM-CSF) gene with potential antineoplastic activity. Upon vaccination, Hodgkin antigens-GM-CSF-expressing cell vaccine may stimulate a cytotoxic T-lymphocyte (CTL) immune response against Hodgkin lymphoma-associated antigens, which may result in the lysis of tumor cells expressing these antigens. In addition, transfected Hodgkin lymphoma cells secrete GM-CSF, which may potentiate the CTL response against Hodgkin lymphoma-associated antigens.
  • Holmium ho 166 poly(l-lactic acid) microspheres - Holmium Ho166 containing poly l-lactic acid (PLA) microspheres with potential antineoplastic actvity. Upon intra-arterial hepatic administration of holmium 166 microspheres, this agent is able to emit both beta particles direct killing cells and gamma photons for nuclear imaging. In addition, since holmium 166 is paramagnetic, this agent can be used for magnetic resonance imaging (MRI).
  • Hpph - A lipophilic, second-generation, chlorin-based photosensitizer. Upon intravenous administration, HPPH selectively accumulates in the cytoplasm of cancer or pre-cancerous cells. When laser light is applied, a photodynamic reaction between HPPH and oxygen occurs, resulting in the production of cytotoxic free radicals and singlet oxygen and free radical-mediated cell death. Compared to the first-generation photosensitizer porfimer sodium, HPPH shows improved pharmacokinetic properties and causes only mild skin photosensitivity which declines rapidly within a few days after administration.
  • Hpv 16 e6/e7-encoding arenavirus vaccine hb-202 - A cancer vaccine consisting of replication-attenuated arenavirus encoding the inactivated fusion protein of the viral oncoproteins E6 and E7 derived from the human papillomavirus (HPV) serotype 16, with potential immunomodulating and antineoplastic activities. Upon administration, HPV 16 E6/E7-encoding arenavirus vaccine HB-202 induces expression of the E6/E7 proteins and stimulates the host immune system to mount a cytotoxic T-lymphocyte (CTL) response against tumor cells expressing HPV16 E6 and E7, resulting in tumor cell lysis. Oncoproteins E6 and E7 play a key role in the development of cervical intraepithelial neoplasia (CIN) and cervical carcinoma.
  • Hpv 16 e7 antigen-expressing lactobacillis casei vaccine bls-ilb-e710c - An orally available Lactobacillis casei (L. casei)-based vaccine expressing the human papillomavirus (HPV) type 16 isoform E7 protein linked to the poly-gamma-glutamate synthetase complex gene pgsA, with potential immunostimulating activity. Upon oral administration, the expressed HPV 16 E7 may stimulate the immune system to mount a mucosal cytotoxic T-lymphocyte (CTL) response against HPV 16 E7-expressing tumor cells. The poly-glutamic acid synthetase PgsA from Bacillus subtilis acts as an anchoring motif that facilitates the expression of the HPV antigen protein on the surface of the bacteria. HPV 16 E7, a cell surface glycoprotein and tumor associated antigen, is overexpressed in various viral-related cancers.
  • Hpv 16 e7:12-20 peptide vaccine - A peptide based vaccine consisting of amino acids 12 through 20 of the E7 gene of the Human Papilloma Virus type 16. HPV-16 E7 12-20 peptide vaccine may elicit a specific CD8 T-cell response to the E7 oncogene protein, thereby inhibiting the abrogation of p53 and pRb function and thus prevent tumorigenesis.
  • Hpv 16 e7:86-93 peptide vaccine - A synthetic peptide vaccine consisting of amino acids 86 through 93 (TLGIVCPI) of the viral oncoprotein human papillomavirus (HPV) 16 E7. Vaccination with HPV-16 E7:86-93 peptide, which binds to HLA-A* 0201 molecule, may stimulate the host immune system to mount a cytotoxic T-lymphocyte (CTL) response against tumor cells positive for HPV-16 E7.
  • Hpv e6/e7 dna vaccine gx-188e - A therapeutic DNA vaccine encoding the E6/E7 fusion protein of human papillomavirus (HPV) subtypes 16 and 18, plus the immune-enhancer, Fms-like tyrosine kinase-3 ligand (FLT3L), with potential immunostimulating and antineoplastic activities. DNA vaccine GX-188E is administered using a proprietary delivery system that electroporates the vaccine into cervical cells. Expression of the E6/E7 fusion product may elicit a cytotoxic T-lymphocyte (CTL) response against cervical cancer cells expressing E6 and E7 oncoproteins, resulting in tumor cell lysis. FLT3L is a ligand for the FLT3 tyrosine kinase receptor, which upon activation stimulates the proliferation of hematopoietic progenitor cells. HPV type 16 and 18 are the most common HPV types involved in cervical carcinogenesis.
  • Hpv e6/e7-encoding arenavirus vaccine hb-201 - A cancer vaccine consisting of a replication-attenuated arenavirus lymphocytic choriomeningitis virus (LCMV) encoding the inactivated fusion protein of the viral oncoproteins E6 and E7 derived from the human papillomavirus (HPV) serotype 16, with potential immunomodulating and antineoplastic activities. Upon administration, HPV E6/E7-encoding arenavirus vaccine HB-201 induces expression of the E6/E7 proteins and stimulates the host immune system to mount a cytotoxic T-lymphocyte (CTL) response against tumor cells expressing HPV16 E6 and E7, resulting in tumor cell lysis. Oncoproteins E6 and E7 play a key role in the development of cervical intraepithelial neoplasia (CIN) and cervical carcinoma.
  • Hpv types 16/18 e6/e7-adenoviral transduced autologous lymphocytes/alpha-galactosylceramide vaccine bvac-c - An immunotherapeutic vaccine composed of the immunoadjuvant alpha-galactosylceramide (a-GC) and autologous antigen presenting cells (APCs), specifically B-lymphocytes and monocytes transfected with an adenoviral vector that expresses the tumor-associated antigens (TAAs) E6 and E7 derived from human papillomavirus (HPV) types 16 and 18 (HPV-16/18 E6/E7), with potential immunostimulating and antineoplastic activities. Upon administration of BVAC-C, the APCs stimulate the immune system to mount a TAA-specific cytotoxic T-lymphocyte (CTL) response, as well as natural killer (NK) cell, NK T-cell (NKT), helper T-cell and antibody-mediated immune responses, against the tumor cells. This directly or indirectly kills the TAA-expressing tumor cells. HPV-16/18 E6/E7 are overexpressed on certain tumor cell types and play key roles in tumor cell proliferation. a-GC, an NKT cell ligand, is used to specifically stimulate NKT cells and to further stimulate an anti-tumor immune response.
  • Hpv-16 e6 peptides vaccine/candida albicans extract - A human papillomavirus (HPV) type 16 vaccine containing four E6 peptides in combination with an extract of Candida albicans, with potential immunomodulating and antineoplastic activities. Upon administration of HPV-16 E6 peptides vaccine/Candida albicans extract, the four HPV-16 E6 peptides and the Candida albicans may activate the immune system to mount a cytotoxic T-lymphocyte (CTL) response against cells expressing the E6 oncoprotein, resulting in tumor cell lysis. The HPV 16 transforming protein E6 is expressed in precancerous and malignant cervical lesions, and HPV may be a cause of some head and neck squamous cell carcinomas (HNSCCs). Candida albicans allergenic extract may be used as a recall antigen to stimulate the immune system against HPV.
  • Hpv-16 e7 tcr expressing t-cells - A preparation of allogeneic, genetically engineered T-lymphocytes transduced with a retroviral vector MSGV1 that encodes a T-cell receptor (TCR) targeting a specific epitope of the human papillomavirus (HPV) type 16 oncoprotein E7 (HPV-16 E7 TCR), with potential antineoplastic activity. The TCR especially recognizes and binds with high affinity to the HPV 16 E7 11-19 epitope. Upon administration, HPV-16 E7 expressing T-cells target and bind to tumor cells expressing the HPV-16 E7 antigen leading to selective cytotoxicity in HLA-A2-positive, HPV-16 E7-expressing tumor cells. HPV16 E7, a tumor-associated antigen (TAA), overexpressed in a variety of tumor cell types while not expressed in normal, healthy cells, plays a key role in tumor cell proliferation. E7 11-19 is a naturally processed epitope of HPV-16 E7 that binds specifically to human leukocyte antigen (HLA)-A*02:01 and that has been isolated from the surface of HPV-16 positive, HLA-A*02:01-positive tumor cells.
  • Hpv16 e7-specific hla-a*02:01-restricted igg1-fc fusion protein cue-101 - A fusion protein composed of a human leukocyte antigen (HLA) complex, HLA-A*0201, with a peptide epitope derived from the human papillomavirus type 16 (HPV16) E7 protein (amino acid residues 11-20), a reduced affinity human interleukin-2 (IL-2) variant, and an effector attenuated human immunoglobulin G1 (IgG1) Fc domain, with potential antineoplastic and immunostimulatory activities. Upon administration, CUE-101 targets and selectively binds to E7-specific CD8-positive T-cells present in patients with HPV16-driven malignancies. This may induce the secretion of inflammatory cytokines such as interferon gamma (IFN gamma) and promote the activation and expansion of tumor-specific CD8-positive cells, which may lead to T-cell-mediated elimination of tumor cells expressing the HPV16 E7 antigen. The HPV16 E7 oncoprotein is a cell surface glycoprotein and tumor-associated antigen (TAA) that is overexpressed in various HPV-associated cancers.
  • Hpv16 l2/e6/e7 fusion protein vaccine ta-cin - A recombinant human papillomavirus (HPV), genetically engineered fusion protein vaccine in which the three HPV16 viral proteins L2, E6 and E7 are fused together in a single tandem fusion protein (TA-CIN; HPV16 L2\E6\E7), with potential immunoprotective and antineoplastic properties. Upon administration, HPV16 L2\E6\E7 fusion protein vaccine TA-CIN may stimulate the immune system to generate HPV16 E6\E7-specific CD4+ and CD8+ T-cell responses as well as the induction of L2-specific antibodies. In addition, this vaccine may prevent infection and the development of other HPV16-associated diseases. L2, a minor viral capsid protein, is able to induce a strong antibody response against certain HPV types.
  • Hpv6/11-targeted dna plasmid vaccine ino-3107 - A DNA vaccine consisting of plasmids encoding E6 and E7 genes of human papilloma virus subtype 6 (HPV-6) and 11 (HPV-11), with potential immunostimulating and antineoplastic activities. Upon administration via intramuscular electroporation, the HPV-6/11-targeted DNA plasmid vaccine INO-3107 expresses the HPV-6/11 E6 and E7 proteins, which may elicit a cytotoxic T-lymphocyte (CTL) response against tumor cells that are expressing HPV6 and/or HPV11 E6 and E7 proteins, resulting in tumor cell lysis. HPV-6/11 infections are associated with aerodigestive malignancies.
  • Hpv-6-targeting immunotherapeutic vaccine ino-3106 - A DNA vaccine consisting of plasmids encoding the E6 and E7 genes of human papilloma virus subtype 6 (HPV-6), with potential immunostimulating and antineoplastic activities. Administered via intramuscular electroporation, HPV-6-targeting immunotherapeutic vaccine INO-3106 expresses the HPV-6 E6 and E7 proteins, which may elicit a cytotoxic T-lymphocyte (CTL) response against tumor cells that are expressing those proteins, resulting in tumor cell lysis. HPV-6 infections are associated with aerodigestive malignancies.
  • H-ras antisense oligodeoxynucleotide isis 2503 - A synthetic oligodeoxynucleotide. Functioning as an anti-sense agent, it hybridizes to the translation initiation region of the human mRNA for the oncogene H-Ras. ISIS 2503 selectively inhibits the expression of H-Ras, and may inhibit the growth of some Ras-dependent tumor cells.
  • Hsp70-peptide tkd/il-2-activated autologous natural killer cells - A preparation of autologous natural killer (NK) cells that are stimulated ex vivo by a 14-mer heat shock protein 70 (Hsp70) TKD peptide and interleukin-2 (IL-2), with potential tumor-selective cytolytic activity. Upon re-infusion into the patient, the treated NK cells recognize and bind to Hsp70-expressing tumor cells, which induces NK-mediated tumor cell lysis. Hsp70, a membrane-bound, stress-inducible protein, is overexpressed on almost all tumor cells; however, it is absent or minimally present on normal, healthy cells. TKD is the C-terminal substrate-binding domain of Hsp70 and is the structure recognized by the activated NK cells.
  • Hsp90 antagonist kw-2478 - An agent that targets the human heat-shock protein 90 (Hsp90) with potential antineoplastic activity. Although the mechanism of action remains to be fully elucidated, Hsp90 antagonist KW-2478 appears to inhibit Hsp90, resulting in impaired signal transduction, inhibition of cell proliferation, and the induction of apoptosis in tumor cells. HSP90 is a molecular chaperone that plays a key role in the conformational maturation of oncogenic signaling proteins, such as HER2/ERBB2, AKT, RAF1, BCR-ABL, and mutated p53, as well as many other molecules that are important in cell cycle regulation or immune responses.
  • Hsp90 inhibitor ab-010 - An orally bioavailable nanoparticle albumin-bound inhibitor of heat shock protein 90 (Hsp90) with potential antineoplastic activity. Hsp90 inhibitor AB-010 selectively binds to Hsp90, inhibiting its chaperone function and promoting the degradation of oncogenic signaling proteins involved in tumor cell proliferation and survival. This agent may inhibit the growth of a wide variety of cancer cell types; the incorporation of albumin into its formulation may facilitate its endothelial transcytosis through the gp60-regulated albumin transport pathway. Hsp90, a chaperone protein upregulated in a variety of tumor cells, regulates the folding and degradation of many oncogenic signaling proteins.
  • Hsp90 inhibitor biib021 - An orally active inhibitor of heat shock protein 90 (HSP90) with potential antineoplastic activity. HSP90, a chaperon protein upregulated in a variety of tumor cells, regulates the folding and degradation of many oncogenic signaling proteins. HSP90 inhibitor BIIB021 specifically blocks active HSP90, thereby inhibiting its chaperon function and promoting the degradation of oncogenic signaling proteins involved in tumor cell proliferation and survival. As a result, CNF2024 has the potential to inhibit the growth of a wide range of cancer cells in both solid tumors and blood-based cancers.
  • Hsp90 inhibitor biib028 - A small-molecule inhibitor of heat shock protein (Hsp) 90 with potential antineoplastic activity. Hsp90 inhibitor BIIB028 blocks the binding of oncogenic client proteins to Hsp90, which may result in the proteasomal degradation of these proteins and so the inhibition of tumor cell proliferation. Hsp90 is a molecular chaperone that plays a key role in the conformational maturation of oncogenic signaling proteins, such as Her2/Erbb2, Akt, Raf1, Bcr-Abl, and mutated p53, in addition to other molecules involved in cell cycle regulation and immune responses.
  • Hsp90 inhibitor debio 0932 - An orally active and small molecule inhibitor of heat shock protein 90 (Hsp90) with potential antineoplastic activity. Hsp90 inhibitor Debio 0932 specifically blocks Hsp90, thereby inhibiting its chaperone function and promoting the degradation of its client proteins, many of which are oncogenic signaling proteins involved in tumor cell proliferation and survival. This may lead to an inhibition of tumor cell proliferation. Hsp90, a chaperone protein upregulated in a variety of tumor cells, regulates the folding, stabilization and degradation of many oncogenic signaling proteins.
  • Hsp90 inhibitor ds-2248 - An orally active and small molecule inhibitor of heat shock protein 90 (Hsp90), with potential antineoplastic activity. Upon oral administration, Hsp90 inhibitor DS-2248 specifically blocks Hsp90, which inhibits its chaperone function and promotes the proteasomal degradation of oncogenic signaling proteins involved in tumor cell proliferation and survival. This may lead to an inhibition of tumor cell proliferation. Hsp90, a chaperone complex protein upregulated in a variety of tumor cell types, regulates the folding and degradation of many oncogenic signaling proteins.
  • Hsp90 inhibitor hsp990 - An orally bioavailable inhibitor of human heat-shock protein 90 (Hsp90) with potential antineoplastic activity. Hsp90 inhibitor Hsp990 binds to and inhibits the activity of Hsp90, which may result in the proteasomal degradation of oncogenic client proteins, including HER2/ERBB2, and the inhibition of tumor cell proliferation. Hsp90, upregulated in a variety of tumor cells, is a molecular chaperone that plays a key role in the conformational maturation, stability and function of oncogenic signaling proteins, such as HER2/ERBB2, AKT, RAF1, BCR-ABL, and mutated p53, as well as many other molecules that are important in cell cycle regulation and/or immune responses.
  • Hsp90 inhibitor mpc-3100 - An orally bioavailable, synthetic, second-generation small-molecule inhibitor of heat shock protein 90 (Hsp90) with potential antineoplastic activity. Hsp90 inhibitor MPC-3100 selectively binds to Hsp90, thereby inhibiting its chaperone function and promoting the degradation of oncogenic signaling proteins involved in tumor cell proliferation and survival; this agent may inhibit the growth and survival of a wide variety of cancer cell types. Hsp90, a chaperone protein upregulated in a variety of tumor cells, regulates the folding, stability, and degradation of many oncogenic signaling proteins.
  • Hsp90 inhibitor snx-5422 mesylate - The orally bioavailable mesylate salt of a synthetic prodrug targeting the human heat-shock protein 90 (Hsp90) with potential antineoplastic activity. Although the mechanism of action remains to be fully elucidated, Hsp90 inhibitor SNX-5422 is rapidly converted to SNX-2112, which accumulates more readily in tumors relative to normal tissues. SNX-2112 inhibits Hsp90, which may result in the proteasomal degradation of oncogenic client proteins, including HER2/ERBB2, and the inhibition of tumor cell proliferation. Hsp90 is a molecular chaperone that plays a key role in the conformational maturation of oncogenic signaling proteins, such as HER2/ERBB2, AKT, RAF1, BCR-ABL, and mutated p53, as well as many other molecules that are important in cell cycle regulation or immune responses.
  • Hsp90 inhibitor snx-5542 mesylate - The orally bioavailable mesylate salt of a synthetic prodrug targeting the human heat-shock protein 90 (Hsp90) with potential antineoplastic activity. Although the mechanism of action remains to be fully elucidated, Hsp90 inhibitor SNX-5542 is rapidly converted to SNX-2112, which accumulates in tumors relative to normal tissues. SNX-2112 inhibits Hsp90, which may result in the proteasomal degradation of oncogenic client proteins, including HER2/ERBB2, and the inhibition of tumor cell proliferation. Hsp90 is a molecular chaperone that plays a key role in the conformational maturation of oncogenic signaling proteins, such as HER2/ERBB2, AKT, RAF1, BCR-ABL, and mutated p53, as well as many other molecules that are important in cell cycle regulation or immune responses.
  • Hsp90 inhibitor tqb3474 - An inhibitor of heat shock protein 90 (Hsp90), with potential antineoplastic activity. Upon administration, Hsp90 inhibitor TQB3474 specifically blocks Hsp90, which inhibits its chaperone function and promotes the proteasomal degradation of oncogenic signaling proteins involved in tumor cell proliferation and survival. This may lead to an inhibition of tumor cell proliferation. Hsp90, a chaperone complex protein upregulated in a variety of tumor cell types, regulates the folding and degradation of many oncogenic signaling proteins.
  • Hsp90 inhibitor xl888 - An orally bioavailable, ATP-competitive, small-molecule inhibitor of heat shock protein 90 (Hsp90) with potential antineoplastic activity. Hsp90 inhibitor XL888 specifically binds to Hsp90, inhibiting its chaperone function and promoting the proteasomal degradation of oncogenic signaling proteins involved in tumor cell proliferation and survival; inhibition of tumor cell proliferation may result. Hsp90, a chaperone complex protein upregulated in a variety of tumor cell types, regulates the folding and degradation of many oncogenic signaling proteins, including Her-2 and Met.
  • Hsp90-targeted photosensitizer hs-201 - A conjugate consisting of a heat shock protein 90 (Hsp90) inhibitor connected via a linker to verteporfin, a photosensitizing agent, with potential imaging, photodynamic and antineoplastic activities. Upon administration, the Hsp90 inhibitor moiety of HS-201 selectively binds to the Hsp90 ATP binding domain in tumor cells and HS-201 accumulates in tumor cells. The verteporfin moiety of HS-201 allows for visualization and photodynamic therapy of the tumors. Hsp90, a chaperone protein upregulated in a variety of tumor cells, regulates the folding, stability and degradation of many oncogenic signaling proteins. Verteporfin is a synthetic photosensitizer with photodynamic activity.
  • Hsp90-targeted sn-38 conjugate pen-866 - A miniature drug conjugate composed of the irinotecan metabolite 7-ethyl-10-hydroxy-camptothecin (SN-38) conjugated, through a cleavable linker, to a ligand of chaperone protein heat shock protein 90 (Hsp90), with potential antineoplastic activity. Upon administration of HSP90-targeted SN-38 conjugate PEN-866, the HSP90 ligand moiety targets HSP90, which allows the conjugate to penetrate, accumulate and be retained in the tumor cell. Once the linker is cleaved, the SN-38 moiety is released in a sustained manner. SN-38 then binds to and inhibits topoisomerase I by stabilizing the cleavable complex between topoisomerase I and DNA, which results in DNA breaks, inhibition of DNA replication and apoptosis. Compared to SN-38 alone, PEN-866 preferentially targets, accumulates and is retained in the tumor cells due to its binding to Hsp90, which results in increased concentrations of SN-38 at the tumor site. This allows sustained release of SN-38 and leads to increased and prolonged efficacy while reducing toxicity to normal, healthy tissues. Hsp90, a chaperone protein upregulated and activated in a variety of tumor cells compared to normal healthy tissue, regulates the folding, stability and degradation of many oncogenic signaling proteins.
  • Hsv-tk-transduced donor lymphocytes - A preparation of donor lymphocytes transduced with the suicide gene herpes simplex virus thymidine kinase (HSV-TK) with potential immunomodulating activity. Administration of HSV-TK-transduced lymphocytes after T cell-depleted allogeneic stem cell transplantation allows an early controllable immune reconstitution, which takes advantage of the antitumor effect of donor lymphocytes and helps to mitigate the risk of post-transplant opportunistic infection. To control graft-versus-host disease (GvHD) due to donor lymphocyte infusion, HSV-TK-transduced donor lymphocytes are selectively eliminated by administration of the antiviral agent ganciclovir. Ganciclovir, a prodrug, is readily phosphorylated by the suicide gene HSV-TK within HSV-TK-transduced lymphocytes to its monophosphate form and, subsequently, converted into its active triphosphate form, which specifically kills HSV-TK- transduced donor lymphocytes.
  • Htert i540/r572y/d988y multipeptide vaccine - A peptide vaccine consisting of multiple epitopes derived from the human telomerase reverse transcriptase (hTERT), the catalytic subunit of human telomerase, with potential immunostimulating and antineoplastic activities. hTERT I540/R572Y/D988Y multipeptide vaccine contains strongly antigenic peptide epitopes I540 (9-mer), R572Y (9-mer) and D988Y (10-mer). Vaccination with this agent may elicit a cytotoxic T cell (CTL) response against telomerase-expressing tumor cells. Directly linked to tumorigenesis, telomerase is expressed in the majority of human cancer cells but is infrequently expressed in normal cells.
  • Htert mrna/survivin peptide-double-loaded autologous dendritic cell vaccine - A cancer vaccine containing autologous dendritic cells (DCs) that are pulsed with mRNA encoding human telomerase reverse transcriptase (hTERT) and survivin peptide, with potential immunostimulatory and antineoplastic activities. Upon administration, hTERT mRNA/survivin peptide-double-loaded autologous dendritic cell vaccine may elicit an immune response against cancer cells expressing hTERT and survivin by activating cytotoxic T-cells (CTLs), natural killer cells (NKs), and B-lymphocytes. The tumor associated antigens (TAAs) hTERT, the catalytic subunit of human telomerase, and survivin, a member of the inhibitor of apoptosis (IAP) family of proteins, may be upregulated in certain tumor cell types and play key roles in tumor cell growth and survival.
  • Htert multipeptide/montanide isa-51 vg/imiquimod vaccine gx 301 - A therapeutic cancer vaccine consisting of four epitopes derived from the human telomerase reverse transcriptase (hTERT), the catalytic subunit of human telomerase, including hTERT (540-548) acetate, hTERT (611-626) acetate, hTERT (672-686) acetate and hTERT (766-780) acetate, emulsified individually in the adjuvant montanide ISA-51 VG and administered with the immune response modifier (IRM) imiquimod, with potential immunostimulating and antineoplastic activities. Each hTERT peptide emulsion is administered individually by intradermal injection. Subsequently, imiquimod is applied topically to the injection site(s). Vaccination with GX 301 may elicit a cytotoxic T-cell (CTL) response against telomerase-expressing tumor cells. Telomerase is expressed in the majority of human cancer cells, infrequently expressed in normal cells, and is directly linked to tumorigenesis. Imiquimod stimulates cytokine production through the activation of toll-like receptor 7 (TLR-7), and also exhibits antiproliferative effects. Montanide ISA-51, also known as incomplete Freund's adjuvant (IFA), is a stabilized water-in-oil emulsion containing mineral oil with mannide oleate, which contains vegetable-grade (VG) oleic acid derived from olive oil. ISA-51 non-specifically stimulates cell-mediated immune responses to antigens.
  • Htert vaccine v934/v935 - A cancer vaccine directed against human telomerase reverse transcriptase (hTERT), the catalytic subunit of human telomerase, with potential immunostimulating and antineoplastic activities. Upon administration, hTERT vaccine V934/V935 may elicit a cytotoxic T cell (CTL) response against telomerase-expressing tumor cells, which may result in tumor cell death. Telomerase is involved in the restoration and maintenance of telomere length and so the functional lifespan of cells. Abnormally reactivated in tumorigenesis, telomerase is expressed in the majority of human cancer cells but is not expressed or is expressed at very low levels in normal cells.
  • Htert/survivin/cmv multipeptide vaccine - A vaccine containing multiple peptides derived from the human telomerase reverse transcriptase (hTERT), survivin and cytomegalovirus (CMV), with potential immunostimulating and antineoplastic activities. Upon administration, hTERT/survivin/CMV multipeptide vaccine may elicit a cytotoxic T cell (CTL) response against tumor cells espressing hTERT, survivin and CMV. hTERT, the catalytic subunit of telomerase, and the inhibitor of apoptosis (IAP) family member survivin, both often upregulated in tumor cells, play key roles in tumor cell growth and survival. Further, CMV expression is correlated with certain types of cancer.
  • Htert/survivin/melanoma tumor cell-derived mrna-transfected dendritic cell vaccine - A cancer vaccine containing dendritic cells (DCs) that are transfected with messenger RNA (mRNA) encoding human telomerase reverse transcriptase (hTERT) and survivin in addition to patient-specific melanoma-derived mRNA with potential immunostimulatory and antineoplastic activities. Upon administration, hTERT/survivin/melanoma tumor cell-derived mRNA-transfected dendritic cell vaccine may elicit a highly specific cytotoxic T-cell (CTL) response against melanoma cells expressing hTERT, survivin, and patient-specific melanoma-associated antigens. hTERT, the catalytic subunit of human telomerase, and survivin, a member of the inhibitor of apoptosis (IAP) family of proteins, may be upregulated in certain tumor cell types, playing key roles in tumor cell growth and survival.
  • Htert-encoding dna vaccine invac-1 - A DNA vaccine consisting of a plasmid encoding a modified, inactive form of the human telomerase reverse transcriptase (hTERT), the catalytic subunit of human telomerase which synthesizes telomeric DNA at the chromosome ends, fused to ubiquitin, with potential immunostimulating and antineoplastic activities. Upon intradermal vaccination of the hTERT encoding DNA vaccine INVAC-1 in combination with electroporation, hTERT protein is expressed and activates the immune system to mount a cytotoxic T-cell (CTL) response against telomerase-expressing tumor cells, which may result in tumor cell death. Telomerase prolongs the functional lifespan of cells via the restoration and maintenance of telomere length. Abnormally activated in tumorigenesis, telomerase is expressed in the majority of human cancer cells, but its expression is low or non-existent in normal cells. hTERT conjugation to ubiquitin, a 76 amino-acid peptide involved in the regulation of normal protein intracellular turnover in the cytoplasm, enhances proteasome-dependent degradation of the hTERT protein, increases hTERT presentation by major histocompatibility complex (MHC) class I molecules and results in an increased immune response against hTERT.
  • Hu14.18-il2 fusion protein emd 273063 - A recombinant protein consisting of the hu14.18 monoclonal antibody fused to the cytokine interleukin-2 (IL2) with potential antineoplastic activity. The monoclonal antibody portion of the hu14.18-IL2 EMD 273063 fusion protein binds to tumor cells expressing the GD2 antigen (melanoma, neuroblastoma and certain other tumors); the Fc component of the fusion protein antibody moiety and natural killer (NK) cells mediate antibody-dependent cell-mediated cytotoxicity (ADCC) and complement-dependent cellular cytotoxicity (CDCC) towards GD2-expressing tumor cells. The localized IL2 moiety of the fusion protein stimulates NK and T-cell antitumor cellular immune responses.
  • Huachansu - A traditional Chinese medicine (TCM) containing a water soluble Bufo toad skin extract that includes the cardiac glycosides bufalin, cinobufagin and resibufogenin with potential antineoplastic and antiangiogenic activities. Although the exact mechanism of action of this TCM has yet to be fully elucidated, huachansu, which may be administered in an injectable form, may induce cell cycle arrest and apoptosis by suppressing the expression of anti-apoptotic proteins, such as Bcl-2, while inducing the expression of pro-apoptotic proteins, such as BAX.
  • Huaier extract granule - An orally bioavailable traditional Chinese medicine (TCM) composed of a granule containing an aqueous extract of Trametes robiniophila murr (Huaier), a mushroom found on hardwood tree trunks, with potential antineoplastic and anti-angiogenic activities. Although the exact mechanism of action through which Huaier exerts its effects is largely unknown, upon administration, this agent induces cell cycle arrest and apoptosis, and inhibits proliferation and migration of susceptible cancer cells through the modulation of various signal transduction pathways involved in carcinogenesis and angiogenesis.
  • Huang lian - A Chinese herb of a desiccated root from the plant Coptis chinensis. Although the mechanism of action remains to be fully elucidated, Huang Lian has antibacterial, antifungal, and antiprotozoal activities. In addition, this herb exhibits antioxidant property that influences positively on lipid metabolism, cause dilation of blood vessels, and may slow the growth of tumor cells. This herb contains rich amount of phytogens, such as berberine, palmatine, jatrorrhizine, columbamine, geniposide, and anti-HIV compound baicalin, which might explain the broad effects of this herb. Huang Lian is commonly used to treat diarrhea or dysentery in Chinese medicine.
  • Hubc1-huil12 fusion protein as1409 - An immunoconjugate consisting of the anti-tumor cytokine interleukin-12 (IL-12) fused to the tumor-targeting antibody BC1 with potential immunostimulatory and antineoplastic activities. The antibody moiety of huBC1-huIL12 fusion protein AS1409 binds to the human fibronectin splice variant ED-B, delivering IL-12 directly to the tumor vasculature; tumor vasculature-targeted IL-12 initiates localized immune cascade responses and exhibits cytotoxic and anti-angiogenic activity while minimizing the systemic side effects of IL-12. The human fibronectin splice variant ED-B is over-expressed in the extracellular matrix and blood vessels of tumor tissues.
  • Hucc49deltach2-pa-dota - An immunoconjugate comprised of a humanized monoclonal antibody with antitumor activity. The monoclonal antibody CC49 is developed from the murine monoclonal antibody B72.3 and is humanized by grafting the hypervariable regions onto the variable light (VL) and variable heavy (VH) frameworks of the monoclonal antibodies LEN and 21/28' CL. In addition the CH2 domain in the constant region is deleted to increase plasma clearance. The resultant antibody binds to the pancarcinoma tumor-associated glycoprotein (TAG)-72 with high affinity. Furthermore, the antibody is conjugated to PA-DOTA, a bifunctional chelating agent and commonly radiolabeled, resulting in an effective agent for radioimmunotherapy.
  • Human anti-cd30 car-expressing autologous t-lymphocytes - A preparation of autologous T-lymphocytes that have been genetically modified to express a chimeric antigen receptor (CAR) consisting of a single chain variable fragment (scFv) derived from a human anti-CD30 monoclonal antibody, with potential immunostimulating and antineoplastic activities. Upon administration, the human anti-CD30 CAR-expressing autologous T-lymphocytes specifically recognize and bind to CD30-expressing tumor cells, resulting in tumor cell lysis. CD30, a cell surface receptor and a member of the tumor necrosis factor (TNF) receptor superfamily, is transiently expressed on activated lymphocytes and is constitutively expressed in hematologic malignancies. Compared to CAR-T cells that use murine scFv-based CARs, CAR-T cells containing CARs with human scFv regions reduces the immunogenicity of the CAR-T cells and may improve their longevity.
  • Human gp100 plasmid dna vaccine - A vaccine consisting of a plasmid DNA encoding the human melanoma-associated antigen gp100. Upon administration, expressed gp100 antigen may stimulate a cytotoxic T cell HLA-A2.1-restricted immune response against tumor cells that express this antigen, resulting in tumor cell lysis. (NCI05)
  • Human mhc non-restricted cytotoxic t-cell line tall-104 - An allogeneic human cytotoxic T-lymphocyte cell line (TALL-104) with potential antineoplastic activity. TALL-104 is an IL-2-dependent human leukemic T cell line, expressing CD8 and T-cell receptor CD3, but not CD16. Because these cells are endowed with MHC-non-restricted killer activity, TALL-104 has destructive potential against a broad range of tumors, while sparing normal cells. Upon administration, TALL-104 targets and interacts with tumor cells and activates apoptotic and necrotic pathways, eventually leading to lysis of tumor cells. In addition, TALL-104 may induce secretion of various cytokines, such as interferon-gamma, thereby potentially enhancing the cytotoxic activity.
  • Human moab lico 28a32 - A human monoclonal immunoglobulin M (IgM) antibody with potential antineoplastic activity. Human MOAB LICO 28a32 binds to the colon tumor-associated antigen 28A32 (CTAA 28A32) found on the cell surface and in the cytoplasm of colon carcinoma cells.
  • Human monoclonal antibody 216 - A naturally-occurring human IgM monoclonal antibody with potential antineoplastic activity. Human monoclonal antibody 216, derived from the gene VH4-34, binds to the glycosylated epitope CDIM on the surface of both malignant and normal B cells. Upon binding to B cells, this antibody may crosslink two or more CDIM molecules, resulting in the formation of cell membrane pores, the disruption of cell membrane integrity, and B cell lysis; this mechanism of antibody-mediated cell death is direct and does not involve mechanisms of complement-mediated cytotoxicity or antibody-dependent cell-mediated cytotoxicity (ADCC). CDIM is the glyco-moiety of a 75kD B-cell cell surface glycoprotein.
  • Human monoclonal antibody b11-hcg beta fusion protein cdx-1307 - A human monoclonal antibody (B11) directed against the mannose receptor and linked to the beta-subunit of human chorionic gonadotropin (hCG beta) with potential immunostimulating and antineoplastic activities. The monoclonal antibody moiety of human monoclonal antibody B11-hCG beta fusion protein CDX-1307 binds to mannose receptors on antigen presenting cells (APCs), including human dendritic cells (DCs) and macrophages. Upon internalization and processing, APCs present the processed hCG beta antigen on their cell surfaces, which may initiate an antibody-dependent cell-mediated cytotoxicity (ADCC) response against hCG beta-expressing tumor cells. The tumor-associated antigen (TAA) hCG beta is selectively overexpressed by a number of tumors including breast, colorectal, pancreatic, bladder and ovarian tumors; its expression may correlate with the stage of disease.
  • Human papillomavirus 16 e7 peptide - A peptide vaccine consisting of amino acids 12 through 20 of the viral oncoprotein human papillomavirus (HPV) 16 E7. Vaccination with HPV-16 E7 peptide may stimulate the host immune system to mount a cytotoxic T lymphocyte (CTL) response against tumor cells positive for HPV-16 E7, resulting in decreased tumor growth. HPV-16 infection is tumorigenic and highly associated with cervical cancer.
  • Human papillomavirus 16 e7 peptide/padre 965.10 - A synthetic agent derived from human papillomavirus (HPV) E7 nuclear protein which is used to produce vaccines against HPV infection and HPV-related neoplasms. HPV E7 oncogenic protein binds the retinoblastoma tumor suppressor protein, pRB, as well as a number of other cellular proteins, and serves as a transcriptional activator. This protein is important in the induction and maintenance of cellular transformation and is co-expressed in the majority of HPV-containing carcinomas. PADRE(R) is a proprietary family of molecules that enhances the immune systems response against an administered immunogen such as the HPV E7 nuclear protein.
  • Human papillomavirus tumor antigen vaccine - A vaccinia viral based vaccine, encoding epitopes of E6 and E7 proteins from human papillomavirus (HPV) types 16 and 18, with immunostimulatory and antineoplastic activities. HPV types 16 and 18 account for approximately 70% of cervical cancers. Vaccination with this HPV-TA (tumor antigen) vaccine may stimulate the host immune system to mount a cytotoxic T lymphocyte (CTL) response against tumor cells positive for E6 and E7 from either type 16 or 18 HPV, resulting in decreased tumor growth.
  • Human prostate-specific membrane antigen plasmid dna vaccine - A vaccine consisting of a plasmid DNA encoding the human prostate-specific membrane antigen (PSMA). Upon administration, expressed PSMA may stimulate a cytotoxic T cell response against tumor cells that express this antigen, resulting in tumor cell lysis. (NCI05)
  • Hvegf26-104/rfase peptide vaccine - A therapeutic cancer vaccine containing a truncated, synthetic peptide mimic of the human angiogenic activator vascular endothelial growth factor (VEGF), consisting of 79 amino acids (amino acids 26-104 of VEGF), and emulsified in the immunoadjuvant RFASE, with potential immunostimulatory and antitumor activities. Upon intramuscular vaccination, the hVEGF26-104 moiety of hVEGF26-104/RFASE acts as an antigen and induces an immune response against VEGF, which results in anti-VEGF antibody binding to and neutralization of endogenous VEGF. This prevents the binding of endogenous VEGF to the VEGF receptor (VEGFR) and blocks VEGFR-mediated endothelial cell signaling, resulting in an inhibition of both angiogenesis and tumor cell proliferation. VEGF plays a key role in angiogenesis, tumor cell proliferation and invasion. RFASE, which belongs to the group of sulpholipopolysaccharides (SLPs), is a synthetic polysaccharide covalently coupled to lipid groups and sulphate groups, and is able to induce a strong humoral immune response upon antigen administration.
  • Hycanthone - A thioxanthene derivative of lucanthone with anti-schistosomal activity and potential antineoplastic activity. Hycanthone interferes with parasite nerve function, resulting in parasite paralysis and death. This agent also intercalates into DNA and inhibits RNA synthesis in vitro.
  • Hydralazine hydrochloride - The hydrochloride salt of hydralazine, a phthalazine derivative with antihypertensive and potential antineoplastic activities. Hydralazine alters intracellular calcium release and interferes with smooth muscle cell calcium influx, resulting in arterial vasodilatation. This agent also inhibits the phosphorylation of myosin protein and chelation of trace metals required for smooth muscle contraction, resulting in an increase in heart rate, stroke volume and cardiac output. In addition to its cardiovascular effects, hydralazine inhibits DNA methyltransferase, which may result in inhibition of DNA methylation in tumor cells.
  • Hydroxychloroquine - A 4-aminoquinoline with immunosuppressive, antiautophagy, and antimalarial activities. Although the precise mechanism of action is unknown, hydroxychloroquine may suppress immune function by interfering with the processing and presentation of antigens and the production of cytokines. As a lysosomotropic agent, hydroxychloroquine raises intralysosomal pH, impairing autophagic protein degradation; hydroxychloroquine-mediated accumulation of ineffective autophagosomes may result in cell death in tumor cells reliant on autophagy for survival. In addition, this agent is highly active against the erythrocytic forms of P. vivax and malariae and most strains of P. falciparum but not the gametocytes of P. falciparum.
  • Hydroxyprogesterone caproate - A synthetic progestational agent similar to the endogenous progesterone used in hormone therapy or as a female contraceptive. Mimicking the action of progesterone, hydroxyprogesterone caporate binds to and activates nuclear progesterone receptors in the reproductive system and causes the ligand-receptor complex to be translocated to the nucleus where it binds to and promotes expression of target genes. Due to the negative feedback mechanism seen with progesterone, this agent also blocks luteinizing hormone (LH) release from the pituitary gland, thereby leading to an inhibition of ovulation and an alteration in the cervical mucus and endometrium. Furthermore, without stimulation of LH, estrogen release from the ovaries is stopped, hence impeding the growth of estrogen-sensitive tumor cells.
  • Hydroxytyrosol - A phenolic phytochemical naturally occurring in extra virgin olive oil, with potential antioxidant, anti-inflammatory and cancer preventive activities. Although the mechanisms of action through which hydroxytyrosol exerts its effects have yet to be fully determined, this agent affects the expression of various components of the inflammatory response, possibly through the modulation of the nuclear factor-kappa B (NF-kB) pathway. The effects include the modulation of pro-inflammatory cytokines, such as the inhibition of interleukin-1alpha (IL-1a), IL-1beta, IL-6, IL-12, and tumor necrosis factor-alpha (TNF-a); increased secretion of the anti-inflammatory cytokine IL-10; inhibition of the production of certain chemokines, such as C-X-C motif chemokine ligand 10 (CXCL10/IP-10), C-C motif chemokine ligand 2 (CCL2/MCP-1), and macrophage inflammatory protein-1beta (CCL4/MIP-1b); and inhibition of the expression of the enzymes inducible nitric oxide synthase (iNOS/NOS2) and prostaglandin E2 synthase (PGES), which prevent the production of nitric oxide (NO) and prostaglandin E (PGE2), respectively. In addition, hydroxytyrosol is able to regulate the expression of other genes involved in the regulation of tumor cell proliferation, such as extracellular signal-regulated and cyclin-dependent kinases. Also, hydroxytyrosol scavenges free radicals and prevents oxidative DNA damage. This induces apoptosis and inhibits proliferation in susceptible cancer cells.
  • Hydroxyurea - A monohydroxyl-substituted urea (hydroxycarbamate) antimetabolite. Hydroxyurea selectively inhibits ribonucleoside diphosphate reductase, an enzyme required to convert ribonucleoside diphosphates into deoxyribonucleoside diphosphates, thereby preventing cells from leaving the G1/S phase of the cell cycle. This agent also exhibits radiosensitizing activity by maintaining cells in the radiation-sensitive G1 phase and interfering with DNA repair.
  • Hypericin - An anthraquinone derivative that is naturally found in the yellow flower of Hypericum perforatum (St. John's wort) with antidepressant, potential antiviral, antineoplastic and immunostimulating activities. Hypericin appears to inhibit the neuronal uptake of serotonin, norepinephrine, dopamine, gamma-amino butyric acid (GABA) and L-glutamate, which may contribute to its antidepressant effect. Hypericin may also prevent the replication of encapsulated viruses probably due to inhibition of the assembly and shedding of virus particles in infected cells. This agent also exerts potent phototoxic effects by triggering apoptotic signaling that results in formation of reactive oxygen species.
  • Hypoxia-activated prodrug th-4000 - A proprietary, hypoxia-activated prodrug with potential antineoplastic activity. Upon administration, the hypoxia-activated prodrug TH-4000 is activated in the hypoxic cells within tumors into an irreversible pan-HER inhibitor via a mechanism of action not yet fully elucidated. As a result, this agent inhibits cellular proliferation and differentiation of tumor cells overexpressing HER kinases, which belong to the epidermal growth factor receptor (EGFR) family of receptor tyrosine kinases. Healthy, normal tissues may be spared due to the hypoxia-specific activity of this agent, potentially reducing systemic toxicity.

Alphabetic list of antineoplastic agents - 0-9 - A1 - A2 - A3 - A4 - A5 -A6 - B - C - D - E - F - G - H - I - JK - L - M - NO - PQ - R - S - T - UVW - XYZ

 

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