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Antineoplastic Drugs

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yekexoko's version from 2017-09-28 06:13

BMS is bone marrow suppression

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Mecholorethamine (IV)Alkylating agent that targets the nitrogens and oxygens in purines and pyrimidines (mainly guanine). Causes leukopenia, thrombocytopenia, teratogenic, and tissue damage at injection site. Treats Hodgkin's and NHL
Cholarmbucil (oral)Least toxic and slowest acting alkylating agent that targets the nitrogens and oxygens in purines and pyrimidines (mainly guanine). Causes leukopenia, thrombocytopenia, risk of AML, and tissue damage at injection site. Treats CLL
Melphan (oral, IV)Alkylating agent that targets the nitrogens and oxygens in purines and pyrimidines (mainly guanine). Causes leukopenia, thrombocytopenia, risk of AML, and tissue damage at injection site. Treats myeloma, ovarian and breast cancer
Cyclophosphamide (oral, IV, IM)Prodrug alkylating agent that targets the nitrogens and oxygens in purines and pyrimidines (mainly guanine). Causes leukopenia, thrombocytopenia, hemorrhagic cystitis, alopecia, amenorrhea, sterility, nausea and vomiting, but NOT tissue damage at injection site. Treats lymphomas, leukemias, mycosis fungoides, multiple myeloma, and a variety of other cancers.
MENSAdrug that can prevent cyclophosphamide-induced hemorrhagic cystitis if co-administered with the drug.
Carmustine (IV) & lomustine (oral)Alkylating and carbamoylating agents (nitrosureas) that pass the blood-brain barrier well. May cause pulmonary fibrosis, BMS, and nausea/vomiting. Used from brain tumors, lymphomas, colon cancer, and multiple myeloma
Dacarbazine (IV)Metabolite that acts like an alkylating agent. Moderately myelosuppressive. Treats Hodgkin disease, malignant melanoma, and soft tissue sarcomas.
Temozolomide (Oral)Metabilite that acts as an alkylating agent and crosses the blood-brain barrier. Can cause BMS, nausea, and vomiting Treats malignant gliomas, melanoma, and uterine leiomyosarcoma.
Bendamustine (IV)Alkylating agent that inhibits mitotic checkpoints and induces mitotis catastrophe. Causes BMS, hypersensitivity. Treats CLL and NHL.
Cisplatin (IV)Cross-links guanine with platinum. Causes major nausea/vomiting, renal toxicity, ototoxicity and irreversible peripheral neural toxicity, but only minor BMS. Used for testicular, head/neck, ovarian, small-cell lung, and colon cancers
Oxaliplatin (IV)Cross-links guanine with platinum. Causes some nausea/vomiting, major reversible peripheral neuropathy, mild BMS, but no renal or ototoxicity. Used in testicular, ovarian, and small cell lung cancer. No cross-reaction with other platinum coordinate complexes
Carboplatin (IV)Cross-links guanine with platinum. Causes minor nausea/vomiting, renal, ototoxicity, peripheral neuropathy, and major BMS. Used in colorectal cancer.
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Methotrexate (oral, IM, IV, IT)Folic acid analogue that inhibits dihydrofolate reductase preventing N5,N10-methylene TH4 formation and indirectly preventing the de novo conversion of UMP into TMP. Causes BMS, mucositis, liver toxicity (especially with alcohol), radiation recall, & neural/renal toxicity. Used to treat acute leukemias, astma, arthritis, psoriasis, oropharyngeal tumors, and choriocarcinoma
LeucovorinDrug used to "rescue" the patient from the toxicity of methotrexase by converting into an essential cofactor for TMP synthesis. It enters normal cells better than cancer cells
pemetrexed (IV)Targets thymidylate synthetase (main) and dihydrofolate reducatse (de novo TMP synth), GARFT, and AICARFT (de novo purine synth). Causes BMS, rash, mucositis, diarrhea. Used in mesothelioma and non-small cell lung cancer
Folic acid and vitamin B12Used to reduce toxicities of pemetrexed without affecting anti-cancers
5-FU (IV, topical)Prodrug that inhibits thymidylate synthetase. causes nausea/vomiting, mucositis, BMS, cerebellar ataxia, alopecia, and teratogenicity. Used for solid tumors, breast cancer, carcinomas of the GI tract, and topically for skin keratosis or psoriasis
CapecitabineProdrug of 5-FU. Causes nausea vomiting, but less BMS. Used for metastatic breast cancer.
Cytarabine (IV, IT)Cytosine analogue that inhibits DNA pol. Causes BMS, nausea/vomiting, mucositis, and stomatitis. Used for AML, ALL, and CML.
GemcitabineCytosine analogue that inhibits DNA pol and ribonucleotide reductase. Causes mild BMS, mild vomiting/nausea. Used for solid tumors, non-small cell lung cancer, and pancreatic cancer
6-mercaptopurine (oral)Hypoxanthine analog that competes the molecule for HGPRT. The product of the interaction with HGPRT competes with IMP for the formation of purines. Causes bone marrow depression, nausea, vomiting, stomatitis, liver toxicity, and gout. Used for ALL.
6-thioguanineGuanine analog that damages DNA after incorporation and inhibits the synthesis of purines. Causes bone marrow depression, nausea, and vomiting. Used for AML
Fludarabine (IV)Adenosine analog that is converted into 2-fluoro-ara-ATP and inhibits DNA pol and ribonucleotide reductase. Causes bone marrow depression, nausea/vomiting, and rare neurological effects. Used for CLL
CladribineDeoxyadenosine analog with additional chlorine that is activated by phosphorylation and incorporated into DNA, where it inhibits DNA synthesis and repair while inducing DNA strand breaks. Causes BMS, nephrotoxicity, and neurotoxicity. Used to treat Hairy cell leukemia.
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Hydroxyurea (oral)Inhibits ribonucleotide reductase, the rate-limiting step of DNA synthesis (rNDP to dNDP). Causes bone marrow depression, stomatitis, GI ulceration, hyperpigmented skin, sensitivity to radiation, and radiation recall
VinblastineAggregate the free tubulin dimers so they cannot form a polymer of microtubules. Causes tissue damage at injection sites, neurotoxicity, BMS (Major), and alopecia. Used for Hodgkin, NHL, choriocarcinoma, and testicular cancer
VincristineAggregate the free tubulin dimers so they cannot form a polymer of microtubules. Causes tissue damage at injection sites, neurotoxicity (major), BMS, and alopecia. Used for ALL, Hodgkin, and other anti-tumor indications
VinorelbineAggregate the free tubulin dimers so they cannot form a polymer of microtubules. Causes tissue damage at injection sites, neurotoxicity (intermediate), BMS (intermediate), and alopecia. Used for non-small cell lung cancer, breast cancer
PaclitaxelPrevents the shortening of microtubules to inhibit mitosis. Causes BMS, neurotoxicity, hypersensitivity (use corticosteroids first), radiation recall, and cardiotoxic bradycardia. Used for breast cancer and ovarian cancer.
EtoposideInhibits topoisomerase II DNA repair enzymes. Causes bone marrow depression, GI problems, tissue damage at injection site, GI problems, radiation recall, and secondary leukemias.
Camptothecins (hycamtin and camptosar)Binds to DNA-topo I preventing the release of torsional strain during DNA replication. Causes BMS and (severe) diarrhea
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Anthracenes/anthracycliens (doxorubicin, daunorubicin, idarubicin, epirubicin)Intercalates into the DNA distorting DNA struction so RNA pol cannot use DNA template. Causes tissue damage at injection site, red urine, and CARDIOTOXICITIY (irreversible), BMS, GI problems, radiation recall. See notes for indications.
Bleomycine (IV, IM)Glycoprotein that binds to DNA forming a bleomycin-iron-oxygen complex which breaks DNA. Causes PULMONARY FIBROSIS/TOXICITY (poss. fatal), hypersensitivity, fever, blistering, and GI problems. Causes very little BMS. Used for testicular cancer
L-asparaginaseInhibits aspartic acid synthesis, limiting protein synthesis. Causes hypersensitive, neurotoxicity, fever, renal an liver toxicity, pancreatitis, excessive NH3, and coagulation deficiencies. However, it lacks BMS, GI problems, and alopecia. Used for ALL
Arsenic trioxideInduces differentiation of promyelocytic leukemia cells and induces apoptosis by stimulating SUMOylation, ubiquitination, and degradation. Causes QT prolongation leading to ventricular arrhytmia, GI problems, rash, and tachycardia. Used for APL in patients refractory for tentinoin or anthracyclines
TrentinonInduces differentiation of APL cells to normal myelocytic cells by binding to a nuclear receptor and affecting transcription. Causes vitamin A toxicity, fever, skin dryness and rash, CNS toxicities, and teratogenicity.
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PrednisoneBinds to glucocorticoid receptors. The complex then binds to DNA sequences, glucocorticoid response elements, which ultimately repressor activate transcription for specific genes, causing apoptosis to lymphocytes. Causes truncal obesity, moon facies, osteoporosis, thin fragile skin, susceptibility to infections. Used for leukemia, Hodgkin, NHL, breast cancer, pain reduction, reduction of cerebral edema, and suppression of chemo-induced nausea/vomiting. Must withdraw slowly or patient will get adrenal insufficiency
CetuximabChimeric antibody that binds to the EGFR receptor on the surface, inhibits the tyrosine kinase pathway, and causes apoptosis. Causes severe rash, infusion reactions, and interstitial lung disease. Used for EGFR-positive colorectal cancer, head/neck cancer
PanitumumabHuman antibody that binds to the EGFR receptor on the surface, inhibits the tyrosine kinase pathway, and causes apoptosis. Causes severe rash and interstitial lung disease. Used for EGFR-positive colorectal cancer, head/neck cancer
Gefitinib and erlotinibAntibody that is a selective cytosolic inhibitor of EGFR-tyrosine kinase (prevents autophosphorylation). Causes mild rash and diarrhea, interstitial lung disease (esp. in patients with prior chemo/radiation, GI perforation, and teratogenicity. Used for non-small cell lung cancer with specific mutations
ImatinibCompetitive inhibitor of ATP binding site on c-abl, c-KIT, and PDGFR tyrosine kinase. Causes GI problems, liver toxicity, rashes, fatigue, fluid retention, neutropenia, and thrombocytopenia. Used for CML.
NilotinibBinds to inactive BCR-ABL with higher affinity than imatinib. Causes less severe side effects than imantinib. Used against imatinib-resistant clones without T3151 mutation.
DasatinibBinds to various protein kinases as well as inactive and active BCR-ABL with higher affinity than imatinib. Causes high BMS, GI problems, liver toxicity, rashes, fatigue, and fluid retention. Used against all imatinib-resistant clones without T3151 mutation
SorafenibSmall molecule that inhibits Raf and various cell surface kinases, preventing angiogenesis, growth, and metastasis. Causes GI rash, fatigue, hand-and-foot syndrome, and hypertension. Used for renal cell carcinoma.
SunitinibTyrosine kinase inhibitors that prevent cell growth, angiogenesis, and tumor metastasis. Causes hypertension, cardiac dysfunction. Used for renal cell carcinoma, and GI stromal tumors.
VemurafenibLMW inhibitor of BRAF-V600E, a mutated BRAF serine threonine kinase. Causes hypersensitivity, QT prolongation. Used for metastatic melanoma with BRAF-V600E mutation.
TemsirolimusInhibitor of mTOR, leading to protein kinase and cell growth inhibition, G1 arrest and apoptosis. Casuses hypersensitivity, immunosuppression, high sugar, lipid, and triglycerides. Used for advanced renal cell carcinoma.
BortezomibSmall molecule that inhibits 26S protoeasomes, leading to apoptosis of cancer cells and increased sensitivity to radiation and anti-cancer drugs. Causes BMS, constipation, peripheral neuropathy, and GI effects. Used for multiple myeloma and mantle cell lymphoma.
BevacizumabSuppresses formation of new blood vessels, depriving solid tumors of expanding blood supply by binding to VEGF. May cause thromboembolism, hypertensive crisis, kidney damage, GI perforation, pulmonary hemorrhage, and disrupted wound healing. But NO BMS or resistance. Used in metastatic colon, breast (HER-2-neg)., nonsquamous non-small cell lung cancers.
ThalidomideSuppresses angiogensis by inhibiting FGF and TNF-alpha, but costimulates T-cells. Causes neuropathy, constipation, teratogenicity. Used for multiple myeloma
LenalidomideSuppresses angiogenesis by inhibiting FGF and TNF-alpha, but costimulates T-cells. Causes teratogenicity, BMS, and thrombocytopenia. Used for multiple melanoma
RituximabMonoclonal antibody against CD20 on B-cells. B-cells are killed by apoptosis and immune attack. Causes cardiac events, hypersensitivity, HBV reactivation, and lymphopenia. Used for B-cell NHL, CL, and arthritis.
Ibritumomab tiuxetanMonoclonal antibody against CD20 that has a chelator attached that provieds high affinity binding site for radioactive isotopes. B-cells are killed by radiation. Causes hypersensitivity, cardiac event, lymphopenia, and severe BMS. Used in NHL
Tositumomab/131-I-tositumomabMonoclonal antibody against CD20 on B-cells linked with radioactive iodine. B-cells are killed by immune attack and radiation. Causes severe BMS, hypersensitivity, infusion reactions, GI toxicity, hypothyroidism, and teratogenicity. Used for rituximab refractory NHL
AlemtuzumabMonoclonal antibody against the CD52 antigen on B-cells, T-cells, macrophages, and platelets. Induces apoptosis after binding. Causes infusion reactions, BMS. Used for B-cell CLL after alkylating agens/fludarabine failed.
ImpilimumabBlocks the CTLA-4, activating the T-cell mediated antitumor immune response. Causes enterocolitis, hepatitis, neuropathy, and rash. Used for metastatic melanoma with dacarbazine.
Brentuximab vedotinCD30 directed drug conjugate linked with a microtubule disrupting agent (MMAE) and protease linker. The antibody binds CD30 and is internalized. MMAE binds to tubuline and causes apoptosis. Used for Hodkin's after failure of autologous stem cell transplant.
VorinostateHDAC inhibitor that increases acetylation of histones and regulatory proteins in the cell nucleus. Acetylation increases cell-cycle arrest and apoptosis. Causes GI, anemia, thrombocytopenia, and pulmonary embolism. Used for cutaneous T-cell lymphoma.
Interferon alfa-2a or 2bBind to cell surface receptors causing gene expressions that result in enhancement of host immune response and direct antiproliferative effects on cancer cells. Causes flu-like symptoms, depression, and cardiac problems. Used for CML with chemo, Hairy cell, Kaposi, NHL, and hepatitis B and C.
AldesleukinLarge glycoprotein, human IL-2 that stimulates the immune function, enhancing production and cytotoxicity of lymphocytes. Causes significant toxicity, capillary leak syndrome, sinus tachycardia, renal and liver problems, pulmonary congestion. Used for metastatic renal cell cancer and melanoma.
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