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Anti-Cancer Drug

QuestionAnswer
Cell cycle-nonspecific (CCNS) drugs Cyclphosphamide, chlorambucil, carmustine, dacarbazine, busulfan, L-asparginase, cisplatin, procarbazine and actinomycin D
cell cycle-specific G1 – vincristine S –Mtx, cytarabine, 6-thioguanine, 6-MP, 5-FU, daunorubicin, doxorubicin G2 – Daunorubicin, bleomycin M –Vincristine, vinblastine, paclitaxel
What cause the Resistance to Cytotoxic Drugs Increased expression of MDR-1 gene for a cell surface glycoprotein, P-glycoprotein
What is the MOA for MDR-1? MDR-1 gene is involved with drug efflux
What drugs can be used to reverse multidrug resistance from increase expression MDR? Verapamil Quinidine Cyclosporine.
What are subclasses of the Alkylating Agents? Nitrogen Mustards Ethylenimines Alkyl Sulfonates Nitrosourea
Nitrogen Mustard Cyclophosphamide Chlorambucil Mechlorethamine Melphalan Ifosfamide
Ethylenimines Thio-TEPA Hexamethylmelamine
Alkyl Sulfonate Busulfan
Nitrosourea Carmustine Streptozocin Lomustine
Triazine Procarbazine Dacarbazine Temozolomide
What are the ADR of cyclophosphamide? Gastrointestinal distress, myelosuppression/Bone suppression, alopecia, and Hemorrhagic cystitis.
What is use to Tx hemorrhagic cystitis? MESNA--> mercaptoethanesulfonate
Why is Nitrosourea best for brain cancers? Highly lipid soluble, crosses BBB
What regimen is used to Tx Hodgkin lymphoma? M--> Mechlorethamine O-->Oncovin/Vincristine P--> Procarbazine P--> Prednisone
Thio-TEPA use to Tx Ovarian Cancer
Busulfan use to Tx chronic myeloid leukemia
Nitrosoureas use to Tx brain tumors
Streptozocin use to Tx insulin-secreting islet cell carcinoma of the pancreas
What are subclasses of the Antimetabolites? Folic Acid Analogs Purine Antagonist Pyrimidine Antagonist
Pyrimidine analogs 5-Fluorouracil Cytarabine (cytosine arabinoside) Capecitabine Gemcitabine
Purine analogs 6-Mercaptopurine 6-Thioguanine Azathioprine Fludarabine
Folic acid analog Methotrexate, Pemetrexed
MOA for Folic acid analog MTX prevents the formation of THF, causing an intracellular deficiency of folate coenzymes and accumulation of the toxic inhibitory substrate, DHFpolyglutamate
Mechanism of Resistance for Methotrexate 1. Decreased drug transport 2. Altered DHFR 3. Decreased polyglutamate formation (folylpolyglutamate synthetase reduced) 4. Increased levels of DHFR
What is use to Tx Bone marrow suppression toxicity (Methotrexate) Calcium Leucovorin/Folinic Acid
What is use to Tx nephrotoxicity (Methotrexate) Sodium bicarbonate to alkalinize the urine
What are the purine antagonist? Mercaptopurine Thioguanine Fludarabine Cladribine
Mercaptopurine MOA Inhibit the conversion of Inosine monophosphate to adenine and guanine nucleotides – building blocks for DNA and RNA
What does Genetic def. of Thiopurine S-methyltransferase (TPMT) causes? More susceptible to 6-MP induced myelosuppression, mucositis and gut damage
What are the pyrimidines antagonist? Fluorouracil Capecitabine Cytarabine Gemcitabine
Fluorouracil MOA 5-FU inhibits thymidylate synthase therefore causing depletion of Thymidylate. 5-FU inhibits RNA processing
What are the topoisomerase-2 inhibitor? (late S and early G2 phase) Etoposide Teniposide
What are the topoisomerase-1 inhibitor? Topotecan Irinotecan
What are the CCS Drugs? Vinca Alkaloids Podophyllotoxin Camptothecin Taxanes Bleomycin (Accumulation of cells in G2 phase)
Which Vinca Alkaloid is Bone marrow sparing but neurotoxic? Vincristine
Which drug is a taxane but has a MOA of binding to the Beta Tubulin and inhibits its polymerization into microtubules? Paclitaxel
What is bleomycin main ADR? Pulmonary Fibrosis
Created by: Jameel D. Wilson
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