N-DesmethylApalutamide是Apalutamide的活性代谢产物，是一种低活性的雄激素受体拮抗剂，其作用力是Apalutamide活性的三分之一。N-DesmethylApalutamide的形成主要由CYP2C8和CYP3A4介导。N-DesmethylApalutamide是中等至强的CYP3A4和CYP2B6诱导剂，并具有优异的血浆蛋白结合浓度。
货号:ajcx31166
CAS:1332391-11-3
分子式:C20H13F4N5O2S
分子量：463.41
溶解度:N/A
纯度：98%
存储：Store at -20°C
库存：现货

Background:

N-Desmethyl Apalutamide is an active metabolite of Apalutamide. N-Desmethyl Apalutamide is a less potent antagonist of the androgen receptor and is responsible for one-third of the activity of Apalutamide. The formation of N-Desmethyl Apalutamide mediated predominantly by CYP2C8 and CYP3A4. N-Desmethyl Apalutamide is moderate to strong CYP3A4 and CYP2B6 inducer and has an excellent plasma-proteins bound concentration[1][2][3].

[1]. PÉrez-Ruixo C, et al. Population Pharmacokinetics of Apalutamide and its Active Metabolite N-Desmethyl-Apalutamide in Healthy and Castration-Resistant Prostate Cancer Subjects. Clin Pharmacokinet. 2019 Aug 20. [2]. Smith MR, et al. Phase 2 Study of the Safety and Antitumor Activity of Apalutamide (ARN-509), a Potent Androgen Receptor Antagonist, in the High-risk Nonmetastatic Castration-resistant Prostate Cancer Cohort. Eur Urol. 2016 May 6. pii: S0302-2838(16)30133 [3]. May MB, et al. Apalutamide: A new agent in the management of prostate cancer. J Oncol Pharm Pract. 2019 Dec;25(8):1968-1978.