N-Desmethyl Apalutamide

Modify Date: 2024-01-02 18:18:10

N-Desmethyl Apalutamide Structure
N-Desmethyl Apalutamide structure
Common Name N-Desmethyl Apalutamide
CAS Number 1332391-11-3 Molecular Weight 463.41
Density N/A Boiling Point N/A
Molecular Formula C20H13F4N5O2S Melting Point N/A
MSDS N/A Flash Point N/A

 Use of N-Desmethyl Apalutamide


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].

 Names

Name N-Desmethyl Apalutamide

 N-Desmethyl Apalutamide Biological Activity

Description 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].
Related Catalog
Target

CYP3A4 and CYP2B6[1];Androgen receptor[2]

References

[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.

 Chemical & Physical Properties

Molecular Formula C20H13F4N5O2S
Molecular Weight 463.41
Storage condition 2-8°C