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Paper II — 2022 May (Supplementary) (2010 Scheme) — Q5

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Paper II
2022 May (Supplementary) (2010 Scheme)

Question

Alkylating agents

Q53 marksShort Notes

Answer

Alkylating agents are cell-cycle-nonspecific cytotoxic drugs (act on both dividing and resting cells).

Examples: Cyclophosphamide, Ifosfamide, Busulfan, and the mechanistically alkylator-like platinum compounds (Cisplatin, Carboplatin).

MOA: alkylating agent → forms covalent bonds with DNA (classically cross-linking guanine bases, particularly interstrand cross-links) → prevents strand separation during replication → lethal DNA damage. Cyclophosphamide is a prodrug, requiring hepatic CYP450 activation.

Uses: lymphomas, leukemias, solid tumors, and (cyclophosphamide specifically) as an immunosuppressant in autoimmune disease.

Adverse effects: bone marrow suppression, hemorrhagic cystitis (from acrolein, cyclophosphamide/ifosfamide’s toxic activation byproduct — prevented by co-administered mesna), nausea/vomiting, alopecia, gonadal toxicity/infertility, secondary malignancy risk with long-term use.

  1. 1Cancer Chemotherapy

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