Chemistry:N-Desmethylenzalutamide
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Short description: Chemical compound
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| Other names | Desmethylenzalutamide; Norenzalutamide |
| Drug class | Nonsteroidal antiandrogen |
| Pharmacokinetic data | |
| Protein binding | 95%[1] |
| Elimination half-life | 7.8 days[2][1] |
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| Chemical and physical data | |
| Formula | C20H14F4N4O2S |
| Molar mass | 450.41 g·mol−1 |
| 3D model (JSmol) | |
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N-Desmethylenzalutamide is a nonsteroidal antiandrogen (NSAA) and the major metabolite of enzalutamide, an NSAA which is used as a hormonal antineoplastic agent in the treatment of metastatic prostate cancer.[3][4][2] It has similar activity to that of enzalutamide and, with enzalutamide therapy, circulates at similar concentrations to those of enzalutamide at steady state.[3][4][2] N-Desmethylenzalutamide is formed from enzalutamide in the liver by the cytochrome P450 enzymes CYP2C8 and CYP3A4.[4] It has a longer terminal half-life than enzalutamide (7.8 days versus 5.8 days).[2]
References
- ↑ 1.0 1.1 https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/203415s011lbl.pdf [bare URL PDF]
- ↑ 2.0 2.1 2.2 2.3 "Pharmacokinetic Aspects of the Two Novel Oral Drugs Used for Metastatic Castration-Resistant Prostate Cancer: Abiraterone Acetate and Enzalutamide". Clin Pharmacokinet 55 (11): 1369–1380. 2016. doi:10.1007/s40262-016-0403-6. PMID 27106175.
- ↑ 3.0 3.1 "Enzalutamide: a review of its use in chemotherapy-naïve metastatic castration-resistant prostate cancer". Drugs Aging 32 (3): 243–9. 2015. doi:10.1007/s40266-015-0248-y. PMID 25711765.
- ↑ 4.0 4.1 4.2 "Metastatic castration-resistant prostate cancer: critical review of enzalutamide". Clin Med Insights Oncol 7: 235–45. 2013. doi:10.4137/CMO.S11670. PMID 24179414.
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