Cancer Chemotherapeutics

Question 1

Methotrexate

Answer 1

• Anti-metabolite (Cell-Cycle Specific)
• MOA: inhibitor of dihydrofolate reductase (decreasing the production of thymidylate, purine nucleotides and amino acids)
• Side Effects: Bone marrow suppression (BMS) [can be minimized using Leucovorin = Folinic acid]

Question 2

Vincristine

Answer 2

• Natural Products (Cell-Cycle Specific)
• MOA: block formation of mitotic spindles (prevents the assembly of tubulin dimers into microtubules)(M-phase)
• Side Effects: peripheral neuropathy

Question 3

Bleomycin

Answer 3

• antibiotic (Cell-Cycle Specific)
• MOA: an anthracycline antibiotic that generates free radicals (results in DNA breaks) (G2-Phase)
• Side Effects: pulmonary toxicity, peripheral neuropathy

Question 4

Cyclophosphamide

Answer 4

• Alkylating Agent (Cell-Cycle Non Specific)
• MOA: = form reactive molecular species that alkylate nucleophilic groups on DNA bases that leads to cross-linking of bases, abnormal base-pairing and DNA strand breakage (prodrug that requires action by CYP450 )
• Side Effects: hemorrhagic cystitis, BMS [Mesnacan be used to minimize hemorrhagic cystitis as an antioxidant]

Question 5

Imatinib and Dasatinib

Answer 5

• Kinase Inhibitors and Antibodies
• MOA: inhibitor of BCR-ABL tyrosine kinase receptor
• Side Effects: BMS, fluid retention, heart failure

Question 6

Veemurafenib and Dabrafenib

Answer 6

• BRAF Inhibitor
• MOA: inhibitor of the B-Raf/MEK/ERK pathway
• Side Effects: skin lesions

Question 7

Rituximab

Answer 7

• B Cell Inhibitor
• MOA: monoclonal antibody that binds to CD20 protein on B cells activating complement-mediated lysis, direct cytotoxicity and induce apoptosis
• Side Effects: rash