N-Desmethylapalutamide
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.[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] N-Desmethylapalutamide is formed from apalutamide in the liver by the cytochrome P450 enzymes CYP2C8 and CYP3A4.[1]
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Other names | Desmethylapalutamide; Norapalutamide |
Drug class | Nonsteroidal antiandrogen |
Pharmacokinetic data | |
Protein binding | 95%[1] |
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Chemical and physical data | |
Formula | C20H13F4N5O2S |
Molar mass | 463.41 g·mol−1 |
3D model (JSmol) | |
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