Ifosfamide

What it is and how it works

Mechanism of Action Ifosfamide is a prodrug that requires metabolic activation by hepatic cytochrome P450 isoenzymes to exert its cytotoxic activity. Activation occurs by hydroxylation at the ring carbon atom forming the unstable intermediate 4-hydroxyifosfamide and its ring-opened aldo tautomer, which decomposes to yield the cytotoxic and urotoxic compound acrolein and an alkylating isophosphoramide mustard as well as multiple other nontoxic products. The exact mechanism of action of ifosfamide has not been determined, but its cytotoxic action is primarily through DNA crosslinks caused by alkylation by the isophosphoramide mustard at guanine N-7 positions.

Mechanism class: Alkylating Activity

Indications

Ifosfamide for Injection is indicated for use in combination with certain other approved antineoplastic agents for third-line chemotherapy of germ cell testicular cancer. It should be used in combination with mesna for prophylaxis of hemorrhagic cystitis. Ifosfamide for Injection is an alkylating drug indicated for use in combination with certain other approved antineoplastic agents for third-line chemotherapy of germ cell testicular cancer. It should be used in combination with mesna for prophylaxis of hemorrhagic cystitis.

Dosage and administration (summary)

Ifosfamide for Injection should be administered intravenously at a dose of 1.2 grams per m 2 per day for 5 consecutive days. Treatment is repeated every 3 weeks or after recovery from hematologic toxicity. In order to prevent bladder toxicity, Ifosfamide for Injection should be given with extensive hydration consisting of at least 2 liters of oral or intravenous fluid per day. Mesna should be used to reduce the incidence of hemorrhagic cystitis. Ifosfamide for Injection should be administered as a slow intravenous infusion lasting a minimum of 30 minutes. Studies of Ifosfamide for Injection in patients with hepatic or renal impairment have not been conducted .

Contraindications

Ifosfamide for Injection is contraindicated in patients with: • Known hypersensitivity to administration of ifosfamide. • Urinary outflow obstruction. • Known hypersensitivity to administration of ifosfamide. • Urinary outflow obstruction.

Warnings and precautions

• Myelosuppression: Can be severe and lead to fatal infections. Monitor blood counts prior to and at intervals after treatment. • Neurotoxicity: Severe and fatal neurotoxicity can occur. Carefully monitor the patient for CNS toxicity and other neurotoxic effects. Discontinue therapy should encephalopathy develop. • Urotoxicity: Severe nephrotoxicity with renal failure and death can occur. Monitor for nephrotoxicity with serum and urine chemistries. Mesna should be used to reduce hemorrhagic cystitis.

Pregnancy

Pregnancy Pregnancy Category D . Ifosfamide for Injection can cause fetal harm when administered to a pregnant woman. Fetal growth retardation and neonatal anemia have been reported following exposure to ifosfamide-containing chemotherapy regimens during pregnancy.

Storage and supply

Ifosfamide for Injection, USP, is available in single-dose vials as follows: Product No. NDC No. 104210 63323-142-10 1 gram single dose vial, packaged individually. 104300 63323-143-00 3 grams single dose vial, packaged individually. The container closure is not made with natural rubber latex.

Source: Ifosfamide (Ifosfamide) — US FDA prescribing information, 2026-04-09, DailyMed. Summarised and shortened; the full label governs. Iranian registration, indications and labelling may differ.