Cyclophosphamide: Mechanism of Action, Toxicokinetics, and Toxicity Profile

Cyclophosphamide is a widely used alkylating agent in the treatment of various malignancies and autoimmune disorders. It acts as a prodrug that is metabolized in the liver by the cytochrome P450 system to form active metabolites, including phosphoramide mustard, which interferes with DNA replication and induces cell death. Due to its broad antineoplastic activity, cyclophosphamide is commonly used in lymphoma, leukemia, and solid tumors. However, its clinical use is associated with several adverse effects, such as hepatotoxicity, nephrotoxicity, lung damage, neurotoxicity, cardiac toxicity reproductive toxicity and hemorrhagic cystitis. Understanding its mechanism of action and toxicity profile is essential for optimizing its therapeutic application.