Temsirolimus

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Information about Temsirolimus

Temsirolimus is an inhibitor of cell proliferation and anticancer agent that is used as treatment of advanced renal cell cancer. 

Liver safety of Temsirolimus

Temsirolimus therapy is frequently associated with mild serum enzyme elevations, but has yet to be linked to instances of clinically apparent liver injury with jaundice. 

Mechanism of action of Temsirolimus

Temsirolimus (tem" sir oh' li mus) is an ester of sirolimus, both of which bind to the same intracellular receptor as tacrolimus and cyclosporine, but which block the "mammalian target of rapamycin" (mTOR) rather than calcineurin.  mTOR is a serine/threonine kinase which plays an important role in signaling pathways of several cytokines and growth factors, which are involved in carcinogenesis and cancer progression.  Inhibition of mTOR causes a decrease in protein synthesis and cell cycle arrest.  Temsirolimus therapy has been shown to inhibit progression and prolong survival in patients with advanced and metastatic renal cell cancer. 

FDA approval information for Temsirolimus

Temsirolimus was approved for use in the United States in 2007 and current indications are limited to therapy of advanced renal cell cancer. 

Dosage and administration for Temsirolimus

Temsirolimus is being actively investigated as therapy of other solid tumors.  Temsirolimus is available as liquid solution for injection in vials of 25 mg/mL under the brand name of Torisel.  The recommended dose is 25 mg intravenously once weekly until disease progression or unacceptable toxicity. 

Side effects of Temsirolimus

Temsirolimus has many, largely dose dependent, side effects including hypersensitivity reactions, oral ulcers, diarrhea, nausea, poor appetite, fatigue, peripheral edema, rash, anemia and interstitial pneumonitis.   

Antineoplastic Agents

Alkylating Agents - Altretamine, Bendamustine, Busulfan, Carmustine, Chlorambucil, Cyclophosphamide, Dacarbazine, Ifosfamide, Lomustine, Mechlorethamine, Melphalan, Procarbazine, Streptozocin, Temozolomide, Thiotepa, Trabectedin

Platinum Coordination Complexes - Carboplatin, Cisplatin, Oxaliplatin

Antibiotics Cytotoxic - Bleomycin, Dactinomycin, Daunorubicin, Doxorubicin, Epirubicin, Idarubicin, Mitomycin, Mitoxantrone, Plicamycin, Mithramycin, Valrubicin

Antimetabolites Antifolates - Methotrexate, Pemetrexed, Pralatrexate, Trimetrexate

Purine Analogues - Azathioprine, Cladribine, Clofarabine, Fludarabine, Mercaptopurine, Nelarabine, Pentostatin, Thioguanine

Pyrimidine Analogues - Azacitidine, Capecitabine, Cytarabine, Decitabine, Floxuridine, Fluorouracil, Gemcitabine, Trifluridine/Tipracil

Biologic Response Modifiers - Aldesleukin (IL-2), Denileukin Diftitox, Interferon gamma

Histone Deacetylase Inhibitors - Belinostat, Panobinostat, Romidepsin, Vorinostat

Hormonal Agents Antiandrogens - Abiraterone, Bicalutamide, Cyproterone, Enzalutamide, Flutamide, Nilutamide

Antiestrogens (including Aromatase Inhibitors) - Anastrozole, Exemestane, Fulvestrant, Letrozole

Selective Estrogen Receptor Modulators - Raloxifene, Tamoxifen, Toremifene

Gonadotropin Releasing Hormone Analogues - Degarelix, Goserelin, Histrelin, Leuprolide, Triptorelin

Peptide Hormones - Lanreotide, Octreotide, Pasireotide

Monoclonal Antibodies - Alemtuzumab, Atezolizumab, Avelumab, Bevacizumab, Blinatumomab, Brentuximab, Cetuximab, Daratumumab, Dinutuximab, Durvalumab, Elotuzumab, Gemtuzumab, Inotuzumab Ozogamicin, Ipilimumab, Necitumumab, Nivolumab, Ofatumumab, Olaratumab, Panitumumab, Pembrolizumab, Pertuzumab, Ramucirumab, Rituximab, Tositumomab, Trastuzumab

Protein Kinase Inhibitors - Abemaciclib, Acalabrutinib, Afatinib, Alectinib, Axitinib, Bortezomib, Bosutinib, Brigatinib, Cabozantinib, Carfilzomib, Ceritinib, Cobimetinib, Copanlisib, Crizotinib, Dabrafenib, Dasatinib, Enasidenib, Erlotinib, Gefitinib, Ibrutinib, Idelalisib, Imatinib, Ivosidenib, Ixazomib, Lapatinib, Lenvatinib, Neratinib, Nilotinib, Niraparib, Olaparib, Osimertinib, Palbociclib, Pazopanib, Ponatinib, Regorafenib, Ribociclib, Rucaparib, Ruxolitinib, Sonidegib, Sorafenib, Sunitinib, Trametinib, Vandetanib, Vemurafenib, Vismodegib

Taxanes - Cabazitaxel, Docetaxel, Paclitaxel

Topoisomerase Inhibitors - Etoposide, Irinotecan, Teniposide, Topotecan

Tyrosine Kinase Receptor Inhibitors See Protein Kinase Inhibitors

Vinca Alkaloids - Vinblastine, Vincristine, Vinorelbine

Miscellaneous - Asparaginase (Pegaspargase), Bexarotene, Eribulin, Everolimus, Hydroxyurea, Ixabepilone, Lenalidomide, Mitotane, Omacetaxine, Pomalidomide, Temsirolimus, Thalidomide, Venetoclax

 

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