Chemistry:N-Desmethylapalutamide
From HandWiki
Short description: Chemical compound
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| Clinical data | |
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| Other names | Desmethylapalutamide; Norapalutamide |
| Drug class | Nonsteroidal antiandrogen |
| Pharmacokinetic data | |
| Protein binding | 95%[1] |
| Identifiers | |
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| PubChem CID | |
| Chemical and physical data | |
| Formula | C20H13F4N5O2S |
| Molar mass | 463.41 g·mol−1 |
| 3D model (JSmol) | |
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N-Desmethylapalutamide is a nonsteroidal antiandrogen (NSAA) and the major active metabolite of apalutamide, an NSAA which is used as a hormonal antineoplastic agent in the treatment of metastatic prostate cancer.[2][1] It has similar activity to that of apalutamide and, with apalutamide therapy, circulates at similar concentrations to those of apalutamide at steady state.[1][failed verification] N-Desmethylapalutamide is formed from apalutamide in the liver by the cytochrome P450 enzymes CYP2C8 and CYP3A4.[1]
References
- ↑ 1.0 1.1 1.2 1.3 "ERLEADATM (apalutamide) tablets, for oral use". Janssen Biotech, Inc. U.S. Food and Drug Administration. https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210951s000lbl.pdf.
- ↑ "Population Pharmacokinetics of Apalutamide and its Active Metabolite N-Desmethyl-Apalutamide in Healthy and Castration-Resistant Prostate Cancer Subjects". Clinical Pharmacokinetics 59 (2): 229–244. February 2020. doi:10.1007/s40262-019-00808-7. PMID 31432469.
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