Identification of the Additional Mitochondrial Liabilities of 2-Hydroxyflutamide When Compared With its Parent Compound, Flutamide in HepG2 Cells

This study has identified for the first time, the additional mitochondrial liabilities of the major metabolite, 2-hydroxyflutamide compared with its parent drug, flutamide. Given the rapid production of this metabolite upon administration of flutamide, but not bicalutamide, we propose that the additional mitochondrial toxicity of 2-hydroxyflutamide may fundamentally contribute to the idiosyncratic DILI seen in flutamide-treated, but not bicalutamide-treated patients.

Source: Toxicological Sciences - September 25, 2016 Category: Toxicology Authors: Ball, A. L., Kamalian, L., Alfirevic, A., Lyon, J. J., Chadwick, A. E. Tags: Metabolite of Flutamide Causes Mitochondrial Dysfunction Source Type: research