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Effect of N ‐methyl deuteration on pharmacokinetics and pharmacodynamics of enzalutamide
Author(s) -
Pang Xuehai,
Peng Lingling,
Chen Yuanwei
Publication year - 2017
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/jlcr.3516
Subject(s) - enzalutamide , chemistry , prostate cancer , pharmacokinetics , potency , pharmacodynamics , pharmacology , antiandrogen , medicine , cancer , androgen receptor , in vitro , biochemistry
Enzalutamide, a second‐generation antiandrogen, has been developed for the treatment of castration‐resistance prostate cancer. We synthesized the deuterated analogues 6 and found that it showed higher drug exposure and thus stronger antitumor potency in preclinical settings. Compound 6 is being developed clinically for the potential to be differentiated from enzalutamide through reduced dosages and a higher safety margin.