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Cyclophosphamide


Mechanism of action:

Cyclophosphamide is an alkylating agent and a derivative of the nitrogen mustards. Cyclophosphamide itself is a prodrug and must be metabolized in the liver by cytochrome P450 enzymes, especially CYP2B6 and CYP3A4, into the active metabolites phosphoramide mustard and acrolein. Phosphoramide mustard is the main active molecule of the drug. It forms covalent bonds with DNA, primarily at the N7 position of guanine, causing DNA cross-linking. This interferes with DNA replication and transcription and ultimately leads to apoptosis.

Reference(s):

1. Khan O et al. (2007). The therapeutic potential of O6-alkylguanine DNA alkyltransferase inhibitors. Expert Opin Investig Drugs. 


2. Schmidt E et al. (2007). Sun-induced life-threatening lupus nephritis. Ann N Y Acad Sci.

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