| Description: |
Ifosfamide is a nitrogen mustard alkylating agent used in the treatment of cancer.Ifosfamide (IF) is a prodrug requiring metabolic activation to produce 4-hydroxyifosfamide (4-OHIF), which breaks down to form isophosphoramide mustard. Ifosfamide (also marketed as Ifex) is a nitrogen mustard alkylating agent used in the treatment of cancer.
in vitro: Ifosfamide mustard significantly decreased the growth of both cancer cell lines in a dose-dependent manner (p < 0.001). The different combined treatments of NAC alone, sodium 2-mercaptoethanesulfonate alone, or NAC plus sodium 2-mercaptoethanesulfonate did not significantly interfere with the tumor cytotoxic effect of ifosfamide mustard. CP and IF inhibited testosterone 6 beta-hydroxylation mediated by P450s 3A but not P450 1A2-dependent 7-ethylresorufin O-deethylation, P450 2C-dependent tolbutamide methyl hydroxylation or P450 2E1-mediated N-nitrosodimethylamine N-demethylation. Kinetic analysis indicated that the drugs were reversible (competitive)inhibitors of testosterone 6 beta-hydroxylation (Km, 94 +/- 8 microM) in human liver microsomes (KiS, 510 +/- 20 microM and 490 +/- 40 microM for CP and IF, respectively).
in vivo: Elevations in DNA damage could be determined in all patients after IFO administration. The degree of damage increased to a peak at 72 h, but had returned to pretreatment values prior to the next dose of chemotherapy. |
