Effect of  N ‐methyl deuteration on pharmacokinetics and pharmacodynamics of enzalutamide | Zendy

Pang Xuehai | Zendy; Peng Lingling | Zendy; Chen Yuanwei | Zendy

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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.

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