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]

N-Desmethylapalutamide
Clinical data
Other namesDesmethylapalutamide; Norapalutamide
Drug classNonsteroidal antiandrogen
Pharmacokinetic data
Protein binding95%[1]
Identifiers
PubChem CID
Chemical and physical data
FormulaC20H13F4N5O2S
Molar mass463.41 g·mol−1
3D model (JSmol)

References



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