Enzalutamidecarboxylicacid(MDV3100carboxylicacid)是Enzalutamide(MDV3100)的非活性代谢产物。Enzalutamide是雄激素受体(AR)拮抗剂。
Enzalutamide carboxylic acid (MDV3100 carboxylic acid) is an inactive metabolite of Enzalutamide (MDV3100). Enzalutamide is an androgen receptor (AR) antagonist[1].
Enzalutamide is converted into its major metabolites, N-desmethyl enzalutamide and carboxylic acid enzalutamide, by cytochrome P450 (CYP) 3A4/5 and CYP2C8, respectively. N-desmethyl enzalutamide has clinically relevant anti-androgen capacities similar to enzalutamide, whereas carboxylic acid enzalutamide is inactive[1].
[1]. van Nuland M, et al. Exposure-Response Assessment of Enzalutamide and Its Major Metabolites in a Real-World Cohort of Patients with Metastatic Castration-Resistant Prostate Cancer. Pharmacotherapy. 2019 Dec;39(12):1137-1145.
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