Anti Cancer Drugs

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Cyclophosphamide

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Akylating Agent: mustard agent, broad spectrum

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Ifosfamide

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Alkylating Agent: mustard agent, broad spectrum

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Cyclophosphamide mech

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P450 to hydroxylated form then broken down to active form, phosphamide mustard and acrolein, and reacts with DNA

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Ifosfamide mech

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P450 to hydroxylated form then broken down to active form, phosphamide mustard and acrolein, and reacts with DNA

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Cyclophosphamide route

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Oral, minimal amounts of parent compound in feces or in urine

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Ifosfamise route

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Oral, minimal amounts of parent compound in feces or in urine

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Cyclosphosphamide AE

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Bone marrow depression, hemorrhagic cystitis (fibrosis of bladder, due to acrolein in the urine). High dose may cause congestive heart failure

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Ifosfamide AE

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Bone marrow depression, hemorrhagic cystitis, due to toxic metabolites

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Hemorrhagic cystitis tx

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Adequate hydration and intravenous Mesna, which neutralizes acrolein

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Mechlorethamine

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The prototype nitrogen mustard, historically used in the treatment of Hodgkin's disease, it forms cross-linkages between guanine residues in the DNA chains

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Melphalan

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A nitrogen mustard for the treatment of multiple myeloma

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Chlorambucil

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A nitrogen mustard used for the treatment of CLL

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Dacarbazine

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An alkylating agent, used in the treatment of Hodgkin's disease, a prodrug via P450 to MITC

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Temozolomide

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An alkylating agent, used in the treatment of brain cancers in combination with radiation, a prodrug, biotransformed at physiological pH to active MTIC

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Procarbazine

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An alkylating agent, treatment on Hodgkin's disease and brain tumors, a weak MAOi, and causes disulfuram-like reaction (avoid alcohol)

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Busulfan

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An alkylating agent, used in the treatment of CML, toxicity of skin pigmentation, pulmonary fibrosis, veno-occlusive disease of the liver

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Thiotepa

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An alkyating agent, an organophosphorus compound used in the treatment of ovarian cancer, an alternative for superficial bladder cancer

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Altremtamine

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An alkylating agent, used in the pallatative treatment or recurrent ovarian cancer

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Carmustine

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An Alkyalting agent, nitrosurease

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Lomustine

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An alkylating agent, nitrosurea

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Streptozocin

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An alkylating agent, a nitrosurea used in the treatment of insulinomas because of its specific toxicity to Beta cells of the islets of Lnagehans

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Platinum coordination complex action

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Remains neutral in blood, then lose chloride ions in the low-chloride environment of the cell bind N7 of Guanine in DNA, formation of intrastrand and interstrand cross-links, thereby inhibiting DNA synthesis and function

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Platinum coordination complex therapeutic uses

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Broad spectrum cytotoxic agents used in the treatment of solid tumors

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Cisplastin

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Platinum agent, synergistic cytotoxicity with radiation and other chemotherapeutic agents

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Carboplatin

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Platinum agent, used in patietns who cannot tolerate vigorous hydration, have kidney dysfunction, or who are prone to neuro-or ototoxicity

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Oxaliplatin

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Platinum, has shown excellent activity against advance colorectal cancer

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Cisplatin dose limiting

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nephrotoxicity, highly emetogenic, manage with vigorous hydration and diuresis with furosemide or mannitol

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Cisplatin toxicities

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Nephrotoxicity, hypocalcemia and hypomagnesmia, ototoxicity, mild bone marrow suppression, some neurotoxicity

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Carboplatin dose limiting

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myelosuppression, but less renal and GI toxicity than cisplatin

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Oxliplatin dose limiting

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neurotoxicity, characterized by a peripheral sensory neuropathy

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Methotrexate

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Antimetabolite, folate antagonist, enteres via active transport and inhibits folate synthesis, inhibits conversion of dihydrofolate to THFR, to depletion of thymidine, and decrease in DNA/RNA and protein. Also becomes polyglutamated and accumulates in cells and increases inhibitory effects on enzymes involved in folate metabolism and increase in duration of action

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Pemetrxed

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Antimetabolite, Folate antagonist, prodrug and polyglutamates inhibit at least four enzymes involved in folate metabolism

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Methotrexate resistance

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decrease in drug transport, formation of cytotoxic polyglutamates, synthesis on increased levels of DHFR, or altered DHFR affinity.

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Methotrexate therapeutic

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ALL, Burkett's lymphoma in children, breast cancer, head and neck cancer, intrathecally for cancers sequestered in CNS

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Premetrxed therapeutic

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Broad spectrum of antitumor activity

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Folate antagonist toxicity

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Myelosuppression and GI. bone marrow depression with leukopenia and thrombocytopenia, diarrhea, mucositis, stomatitis, alopecia

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Leucovorin

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Management of folate antagonist toxicity, rescue normal cells from undue toxicity, also in accidental drug overdose

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6-Mercaptopurine

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Purine antagonist, prodrug, metabolized by HGPRT, to 6-thioinosinic acid (active metabolite), which inhibits several enzymes of de novo purine nucleotide synthesis

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6-MP therapeutic

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used primarily in the treatment of childhood acute leukemia

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6-Thioguanine

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Purine antaonist, related to 6-MP

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Resistance to purine antagonists

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decreased HGPRT expression, or degradation of the drug by induces cancer cell enzymes

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6-MP metabolism

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via xanthine oxidase to inactive 6-thiouric acid and excreted renally

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6-TG metabolism

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via deamination to xanthine oxidase to inactive 6-thiouric acid and renally excreted

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Toxicity of purine antagonists

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myelosuppression, immunosuppression and hepatotoxicity

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Allopurinol

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Affect 6-MP, but not 6-TG, so decrease levels of 6-MP

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Fludaradine

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A Purine nucleotide analog, used chiefly in the treatment of low-grade NHL and CLL

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Cladribidine

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A Purine nucleotide analog, treatment of hairy cell leukemia, activity in CLL, and low-grade NHL.

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5-Fluorouracil

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Antimetabolite, Pyrimidine antagonist, enters the cell via carrier-mediated transport. Prodrug to 5-fluorodeoxyuridine monophosphate which competes with deoxyuridine monophosphate for thymidylate synthase, acts on S phase. Thymineless death. also interferese with RNA synthesis. Leucovorin increases effectiveness

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5-Fluorouracil resistance

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Cancer cells do not convert 5-FU to 5-FdUMP, altered or increases thymidylate synthase levels

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5-Fluorouracil Therapeutic

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slowly growing solid tumors, such as colorectal, breat, ovarian, pancreatic, gastric carcinomas

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5-Fluorouracil toxicities

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myelosuppression and GI toxicity typical of antineoplastic agents

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Capecitabine

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Antimetabolite, pyrimidine antagonist, Oral hydrolyzed to 5-FU, inhibits thymidylate synthase, used in the treatment of colorectal cancer, and metastatic breast cancer resistant to first-line drugs

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Floxuridine

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Antimetabolite, pyrimidine antagonist, an analog of 5-FU, it is biotransformed in the liver. IV administration. palliative care of GI adenocarcinoma that has metastasized to the liver

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Cytarabine

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Antimetabolite, pyrimidine antagonist, activated in cell by phosphorylation to cytotoxic Ara-CTP, then incorporated into nuclear DNA, then interfes with chain elongation, and is also incorporated into RNA. used in treatment of AML, and NHL.

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Gemcitabine

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Antimetabolite, Pyrimidine antagonist, phosphorylation in the cell to triphosphate forms of the drug, incorporated into growing DNA in the place of cytosine, and causes DNA termination

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Vincristine

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Natural, Mictotubule inhibitor,remission induction in ALL, Hodgkin's and NHL and Multiple myeloma, rhabsomyosarcoma, neuroblastmona, Ewing's sarcoma, and Wilm's tumor

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Vinblastine

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Natural, Mictotubule inhibitor, Hodgkin's disease, NHL, breast cancer, and germ cell cancer

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Vinca Alkaloids

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Binds to tubulin, inhibition of tubulin polymerization and causes disruption of microtubule assembly and block mitosis in the M phase. IV, P450, bile and fecal excretion,

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Vinorelbine

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Natural, Microtubule inhibitor, non small cell lung cancer and breast cancer

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Vinca Alkaloid therapeutic

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Different spectra of activity, although they all produce cytotoxicity by the same mechanism

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Vinca Alkaloid toxicity

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Myelosuppression, GI toxicities and alopecia typical of antineoplastic agents. Potent vesicants: phlebitis, cellulites, extravasation during injection, intrathecal administration is contraindicated

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Vincristine toxicity

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peripheral neuropathy characterized by paresthesias, loss of reflexes, foot drop, ataxia, constipation, syndrome of inappropriate antidiuretic hormone

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Vinblastine toxicity

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more potent myelosuppression

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Vinorelbine toxicity

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myelosuppression, with neutropenia (dose limiting toxicity)

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Taxanes

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High affinity reversible binding to Beta-tubulin subunit of microtubules, promotes tubulin polymerization and stabilizes the polymer, accumulation, chromosome degradation dose not occur, cell death in G2/M phase

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Taxane resistance

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P-glycoprotein-mediated drug efflux, alterations in microtubulin protein

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Vinca Alkaloids resistance

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P-glycoprotein mediated drug efflux, and alteration in microtubulin protein

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Taxane Pk

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IV, large volume of distribution (not enter CNS), P450, biliary secretion and fecal excretion

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Taxane therapeutic

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Broad range of solid tumors

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Paclitaxel

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Natural, Taxane, used in ovarian, advanced breast cancer, non-small cell and small cell lung, head and neck, esophageal, prostate, and bladder cancers and AIDS-related Kaposi's sarcoma

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Docetaxel

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Natural, Taxane, used in advanced breast cancer, non-small cell lung cancer, head and neck cancer, small cell lung cancer, gastric cancer, advanced platinum-refractory ovarian cancer, and bladder cancer

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Taxane toxicity

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neutropenia is dose-limiting, peripheral neuropathy can develop with either drug

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Paclitaxel toxicity

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Serious hypersensitivity reactions, including dyspnea, urticaria, and hypotension. Premedication for all pateints with dexamethasone, diphenhydramine and ranitidine or other H2 blocking agent

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Docetaxel toxicity

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Fluid retention

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Antracyclines

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Intercalation in the DNA, inhibition of topoisomerase II, binding to cellular membranes, Generation of oxygen free radicals

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Antracyclines generation of oxygen free radicals

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Tumors and cardiac tissue are low in superoxide dismutase

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Antracyclines resistance

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multidrug resistance is common

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Antracycline Pk

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IV, plasma and tissue protein binding (wide distribution), not go thru BBB or testes, hepatic metabolism, fecal and urinary excretion

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Doxorubicin

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Antibiotic, antracycline, broad spectrum hematologic and wide range of solid tumors. one of the most widely used. turns urine red

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Daunorubicin

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Antibiotic, antracycline, AML, limited efficacy in solid tumors, and turns urine red

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Idarubicin

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Antibiotic, antracycline, AML (more effective tha daunorubicin in producing complete remission when combined with cytarabine

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Epirubicin

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Antibiotic, antracycline, Breast cancer and gastric cancer

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Valrubicin

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Antibiotic, antracycline, intravesical therapy for BCG-refractory bladder carcinoma in situ.

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Anthracycline toxicity

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Extravasation, cardiotoxicity (irreversible, dose dependent: irradiation of the thorax increases risk and addition of tratuzumab to protocol increases CHF)

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Anthracayline cardiotoxicity management

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Liposomal formulation of doxorubicin and dexrazosane and iron chelation (not to be used for initiation of doxorubicin therapy)

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Mitoxantrone

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Antibiotic, a related anthracenedoine, produces strand breakage and inhibits DNA/RNA synthesis, used in advanced hormone refractory prostate cancer and low-grade NHL, breast cancer, ped/adult AML and cuases a blue coloration of fingernails, sclera, and urine

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Dactinomycin

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Antibiotic, used in solid tumors in children and in choriocarcinoma. binds dsDNA via intercalcalation between G and C, and inhibits DNA/RNA synthesis. ribosomal RNA formation is the most sensitive

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Mitomycin

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Antibiotic, alkylating agen, cross link DNA, intravesicle for superficial bladder cancer. Myelosuppression that may be delayed and cumulative with recovery after 6-8 weeks, dangerous hemoyltic uremic syndrome, hemolysis, neurological abnormalities, interstitial pneumonia, glomerulonephritis, pulmnonary fibrosis and CHF

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Bleomycin

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Antibiotic, small peptide that contains a DNA binding region and an iron binding domain at opposite ends. causes scission of DNA by an oxidative process

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Camptothecins

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inhibit the activity of topoisomerase I by binding to the enzyme-DNA complex, prevent religation of the breaks of the single DNA strands

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Camptothecins Pk

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IV, metabolized by hydrolysis, urinary excretion

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Topotecan

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Camptothecin

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Irinotecan

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Camptothecin

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Epidophyllotoxins

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Inhibition of topoisomerase II, forms a ternary complex of the drug, DNA and enzyme, damages DNA via strand breakage

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Epidophyllotoxin Pk

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IV, highly bound to plasma proteins and widely distributes, conjugates and excreted in urine

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Eroposide

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Epidophyllotoxin, used in oat cell carcinoma of lung, testicular cancer with bleomycin and cisplatin, Hodgkin's and NHL and gastric cancer

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Teniposide

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Epidophyllotoxin, second line for ALL

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Epidophyllotoxin toxicity

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Typical of antineoplastic, dose-limiting myelosuppression, primarily leucopenia

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Hydroxyurea

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Used for CML, inhibits ribonucleoside phosphate reductase (essential for DNA synthesis, conversion of ribo to deoxy)

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Tretinoin

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A retinoid, induces a high rate of complete remission in M5, in combo with anthracyclines, binds to PML/RAT alpha fusion gene, and activates differentiation and degradation of the gene

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Arsenic Trioxide

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Used in replased M5, promotes differentiation and degradation of PML/RAT alpha protein and induces apoptosis

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Trastuzumab

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Monoclonal, anti-HER2 for breast cancer, toxicity of cardiomyopathy and pulmonary toxicity

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Rituximab

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monoclonal, anti-CD20 for NHL, and inflammatory diseases

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Bevacoximab

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monoclonal, inhibits angiogenesis and neovascularization for treatment of colorectal cancer, nonsquamous, nonsmall cell lung cancer, breast cancer (HER2 negative), toxicity of hypertension, pulmonary hemorrhage, GI preforation, CHF, thromboembolism, and wound healing complications

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Imatinib

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Small molecule tyrosine kinase inhibitor, Ph chromosome CML, GI stromal tumor. toxicity of fluid retention and myalgias

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Erlotinib

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Small molecule tyrosine kinase inhibitors, locally advanced or metastatic HSCLC

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Bortezomib

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Proteasome inhibitor, (which regulate protein hemostasis within the cell,) inducing cell cycle arrest and apoptosis. Used for multiple myeloma, replased of refractory mantle cell lymphoma, and NHL

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Prednisone

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Steroid hormone, Potent synthetic, anti-inflammatory corticosteroid with ledd mineralcorticoid activicy than cortisol. Used primarily to induce remission in patients with ALL and in treatment of Hodgkin's and NHL. Reduced by 11-beta-hydroxysteroid dehydrogenase to prednisolone

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Tamoxifen

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Selective estrogen receptor modulator, Competitlvely binds to ligand-binding pocket ofr both ERalpha a beta and block estradiol binding. used in treatment of metastatic breast cancer, treatment and prophylaxis estrogen receptor positive breast cancer, adjuvant therapy following mastectomy or radiation

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Raloxifen

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Selective estrogen receptor modulator, Competitlvely binds to ligand-binding pocket ofr both ERalpha a beta and block estradiol binding. Risk reduction for invasive breast cancer in postmenopausal women with osterporosis and in postmenopausal women with high risk for invasive breast cancer

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SERMs AEs

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Headache, nausea, vasomotor symptoms (hot flushes, sweating)

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SERMs SAEs

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increased risk of thomboembolism, increased risk of uterine cancer (not in raloxifene), QT prolongation in toremifene

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Toremifene

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Selective estrogen receptor modulator, Competitlvely binds to ligand-binding pocket ofr both ERalpha a beta and block estradiol binding. Used for metastatic breast cancer in postmenopausal women with estrogen receptor positive or unknown tumors