Carmustine — Drug Monograph

Brand names: BiCNU, Gliadel

Drug class: Alkylating Agent

Mechanism of Action

Carmustine is a nitrosourea derivative that acts as a cell-cycle non-specific alkylating agent. It undergoes spontaneous hydrolysis to form reactive electrophilic carbonium ions that cause DNA cross-linking (both interstrand and intrastrand) and carbamoylation of proteins, particularly lysine residues. These actions inhibit DNA, RNA, and protein synthesis, eventually leading to apoptosis. Its high lipophilicity allows it to readily cross the blood-brain barrier, making it effective for central nervous system malignancies.

FDA Indications

Common Side Effects

Clinical Pearl

The hallmark of carmustine toxicity is its delayed and cumulative myelosuppression, with nadirs often not reached for 4 to 6 weeks, requiring extended intervals between cycles. Clinicians must be vigilant about lifetime cumulative doses to minimize the risk of irreversible pulmonary fibrosis. For IV administration, the use of alcohol as a diluent can cause a "drunk" sensation or flushing, so patients should be monitored for infusion-related hypotension. The Gliadel wafer form requires careful…

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