N-Desmethyl-Apalutamide |
| Catalog No.GC61117 |
N-Desmethyl Apalutamide는 Apalutamide의 활성 대사 산물입니다. N-데스메틸 아팔루타미드는 안드로겐 수용체의 덜 강력한 길항제이며 아팔루타미드 활성의 1/3을 담당합니다. N-Desmethyl Apalutamide의 형성은 주로 CYP2C8 및 CYP3A4에 의해 매개됩니다. N-Desmethyl Apalutamide는 중간에서 강한 CYP3A4 및 CYP2B6 유도제이며 우수한 혈장-단백질 결합 농도를 가지고 있습니다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1332391-11-3
Sample solution is provided at 25 µL, 10mM.
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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.
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