Microbial Metabolism. Part 11. Metabolites of Flutamide
نویسندگان
چکیده
منابع مشابه
Bioactivation of flutamide metabolites by human liver microsomes.
Flutamide, a widely used nonsteroidal antiandrogen drug for the treatment of prostate cancer, has been associated with rare incidences of hepatotoxicity in patients. It is believed that bioactivation of flutamide and subsequent covalent binding to cellular proteins is responsible for its toxicity. A novel N-S glutathione adduct has been identified in a previous bioactivation study of flutamide ...
متن کاملFlutamide metabolism in four different species in vitro and identification of flutamide metabolites in human patient urine by high performance liquid chromatography/tandem mass spectrometry.
A new metabolic scheme of flutamide is proposed in this article. Some patients treated with flutamide, a nonsteroidal antiandrogen, have developed severe hepatic dysfunction. Toxic metabolites have been proposed to be responsible for these negative effects. In this study, the qualitative aspects of the in vitro metabolism of flutamide in liver microsomes from human, dog, pig, and rat were evalu...
متن کاملMicrobial metabolites of harman alkaloids.
Several microorganisms showed the ability to transform the harman alkaloids, harmaline (1), harmalol (2) and harman (5). Harmaline (1) and harmalol (2) were converted by Rhodotorula rubra ATCC 20129 into the tryptamines, 2-acetyl-3-(2-acetamidoethyl)-7-methoxyindole (3) and 2-acetyl-3-(2-acetamidoethyl)-7-hydroxyindole (4), respectively. Harman (5) was biotransformed by Cunninghamella echinulat...
متن کاملMetabolism of the antiandrogenic drug (Flutamide) by human CYP1A2.
The antiandrogenic drug, flutamide, is widely used in the treatment of carcinoma of the prostate. The present study examines the metabolism of flutamide by human liver microsomes and purified recombinant human cytochrome P450s (CYP), expressed as fusion proteins. These studies show the principal role of CYP1A2 in the metabolism of flutamide to 2-hydroxyflutamide. A minor metabolite is formed du...
متن کاملFocus Issue on Metabolism: Metabolites, Metabolites Everywhere.
Metabolic studies have arguably been conducted since the 13th centurywith Ibn al-Nafis stating that “the body and its parts are in a continuous state of dissolution and nourishment, so they are inevitably undergoing permanent change” (Mahdi, 1974). However, it was studies in yeast in the last decades of the 19th century and the first decades of the 20th century (Kühne, 1877; Buchner, 1897; Sumn...
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ژورنال
عنوان ژورنال: Chemical and Pharmaceutical Bulletin
سال: 2010
ISSN: 0009-2363,1347-5223
DOI: 10.1248/cpb.58.562