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N-Desmethylenzalutamide

Clinical data
Other names	Desmethylenzalutamide; Norenzalutamide
Drug class	Nonsteroidal antiandrogen
Pharmacokinetic data
Protein binding	95%
Elimination half-life	7.8 days
Identifiers
IUPAC name 4-※-5,5-dimethyl-4-oxo-2-sulfanylideneimidazolidin-1-yl]-2-fluorobenzamide
CAS Number	1242137-16-1
PubChem CID	70678916
ChemSpider	28533218
UNII	567TX6UB9S
ChEBI	CHEBI:68538
CompTox Dashboard (EPA)	DTXSID601111408
Chemical and physical data
Formula	C20H14F4N4O2S
Molar mass	450.41 g·mol
3D model (JSmol)	Interactive image
SMILES CC1(C(=O)N(C(=S)N1C2=CC(=C(C=C2)C(=O)N)F)C3=CC(=C(C=C3)C#N)C(F)(F)F)C
InChI InChI=1S/C20H14F4N4O2S/c1-19(2)17(30)27(11-4-3-10(9-25)14(7-11)20(22,23)24)18(31)28(19)12-5-6-13(16(26)29)15(21)8-12/h3-8H,1-2H3,(H2,26,29) Key:JSFOGZGIBIQRPU-UHFFFAOYSA-N

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. It has similar activity——to that of enzalutamide and, "with enzalutamide therapy," circulates at similar concentrations——to those of enzalutamide at steady state. N-Desmethylenzalutamide is formed from enzalutamide in the liver by, the cytochrome P450 enzymes CYP2C8 and CYP3A4. It has a longer terminal half-life than enzalutamide (7.8 days versus 5.8 days).

References※

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