Biological Activity
Flutamide-d7 is intended for use as an internal standard for the quantification of flutamide by GC- or LC-MS. Flutamide is an androgen receptor antagonist (Kis = 1.3 and 7.5 μM for the cytosolic rat ventral prostate and anterior pituitary receptors, respectively) and prodrug form of 2-hydroxy flutamide .1 Flutamide is converted to 2-hydroxy flutamide by the cytochrome P450 (CYP) isoform CYP1A2 in human liver microsomes.1 It is cytotoxic to PC3 and LNCaP prostate cancer cells with IC50 values of 98.8 and 81.8 μM, respectively.2 Flutamide (50 mg/kg per day) reduces tumor growth in a PC-82 mouse xenograft model.3 Formulations containing flutamide have been used in the treatment of prostate cancer.
References
1.Shet, M.S., McPhaul, M., Fisher, C.W., et al.Metabolism of the antiandrogenic drug (flutamide) by human CYP1A2Drug Metab. Dispos.25(11)1298-1303(1997)
2.Shi, Q., Wada, K., Ohkoshi, E., et al.Antitumor agents 290. Design, synthesis, and biological evaluation of new LNCaP and PC-3 cytotoxic curcumin analogs conjugated with anti-androgensBioorg. Med. Chem.20(13)4020-4031(2012)
3.Nnane, I.P., Long, B.J., Ling, Y.Z., et al.Anti-tumour effects and pharmacokinetic profile of 17-(5'-isoxazolyl)androsta-4,16-dien-3-one (L-39) in mice: An inhibitor of androgen synthesisBr. J. Cancer83(1)74-82(2000)
