Ifosfamide

Chemical formula: C₇H₁₅Cl₂N₂O₂P  Molecular mass: 261.086 g/mol  PubChem compound: 3690

Pharmacodynamic properties

Ifosfamide is an antineoplastic, a cytotoxic alkylating agent. It is a prodrug and shows no in vitro cytotoxic activity until activated by microsomal enzymes. The cytotoxic activity of Ifosfamide (alkylation of the nucleophilic centres in the cells) is associated with the activated oxazaphosphorine ring hydroxylated at the C4 atom which interacts with DNA-DNA cross linking. This activity manifests itself by blocking the late S and early G2 phases of the cell cycle.

Pharmacokinetic properties

Ifosfamide is rapidly absorbed from the site of administration, activation of Ifosfamide is primarily in the liver by microsomal mixed function oxidases. Elimination of metabolised Ifosfamide is primarily via the kidneys. The serum half-life ranges between 4-8 hours depending on the dose and dosage regimen. Over 80% of a single dose of ifosfamide was excreted in the urine within 24 hours. Approximately 80% of the dose was excreted as parent compound. Significant quantities of unchanged ifosfamide were found in the cerebrospinal fluid consistent with the high lipid solubility of the drug.

Preclinical safety data

Not relevant.

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