Cytotoxic agents

The tables below summarises the mechanism of action and major adverse effects of
commonly used cytotoxic agents.
Alkylating agents

Cytotoxic

Mechanism of action

Adverse effects

Cyclophosphamide

Alkylating agent - causes

cross-linking in DNA

Haemorrhagic cystitis, myelosuppression,

transitional cell carcinoma

Cytotoxic antibiotics

Cytotoxic

Mechanism of action

Adverse effects

Bleomycin

Degrades preformed DNA

Lung fibrosis

Doxorubici
n

Stabilizes DNA-topoisomerase II complex inhibits DNA &

RNA synthesis

Cardiomyopathy

Antimetabolites

Cytotoxic

Mechanism of action

Adverse effects

Methotrexate

Inhibits dihydrofolate reductase and

thymidylate synthesis

Myelosuppression, mucositis,
liver fibrosis, lung fibrosis

Fluorouracil (5FU)

Pyrimidine analogue inducing cell cycle arrest

and apoptosis by blocking thymidylate
synthase (works during S phase)

Myelosuppression, mucositis,
dermatitis

Cytotoxic

Mechanism of action

Adverse effects

6mercaptopurine

Purine analogue that is activated by

HGPRTase, decreasing purine synthesis

Myelosuppression

Cytarabine

Pyrimidine antagonist. Interferes with DNA

synthesis specifically at the S-phase of the cell
cycle and inhibits DNA polymerase

Myelosuppression, ataxia

Acts on microtubules

Cytotoxic

Mechanism of action

Adverse effects

Vincristine,
vinblastine

Inhibits formation of microtubules

Vincristine: Peripheral neuropathy

(reversible) , paralytic ileus
Vinblastine: myelosuppression

Docetaxel

Prevents microtubule depolymerisation &

disassembly, decreasing free tubulin

Neutropaenia

Other cytotoxic drugs

Cytotoxic

Mechanism of action

Adverse effects

Cisplatin

Causes cross-linking in DNA

Ototoxicity, peripheral
neuropathy, hypomagnesaemia

Hydroxyurea
(hydroxycarbamide)

Inhibits ribonucleotide reductase,

decreasing DNA synthesis

Myelosuppression

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