Flutamide-d7 (Synonyms: SCH 13521-d7)

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 (K_is = 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.

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)