N-desmethyl Enzalutamide

• CAT Number: I000962
• CAS Number: 1242137-16-1
• Molecular Formula: C20H14F4N4O2S
• Molecular Weight: 450.41
• Purity: ≥95%
• Synonyms: 4-[3-[4-cyano-3-(trifluoromethyl)phenyl]-5,5-dimethyl-4-oxo-2-sulfanylideneimidazolidin-1-yl]-2-fluorobenzamide
• 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)
• InChIKey: JSFOGZGIBIQRPU-UHFFFAOYSA-N
• 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

N-desmethyl Enzalutamide is the active metabolite of Enzalutamide.N-desmethyl Enzalutamide is the active metabolite of Enzalutamide. N-desmethyl Enzalutamide demonstrates primary and secondary pharmacodynamics of similar potency to Enzalutamide and circulates at approximately the same plasma concentrations as enzalutamide[1].
N-desmethyl Enzalutamide is an active metabolite that is thought to contribute to the clinical effects of Enzalutamide because it demonstrates primary and secondary pharmacodynamics of similar potency to Enzalutamide and circulates at approximately the same plasma concentrations as Enzalutamide. The carboxylic acid metabolite is pharmacologically inactive and circulates at approximately 25 % lower plasma concentrations than Enzalutamide[1].

Reference

[1]. Gibbons JA, et al. Pharmacokinetic Drug Interaction Studies with Enzalutamide. Clin Pharmacokinet. 2015 Oct;54(10):1057-69.
 [Content Brief]