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Effect of N-methyl deuteration on pharmacokinetics and pharmacodynamics of Enzalutamide.

Effect of N-methyl deuteration on pharmacokinetics and pharmacodynamics of Enzalutamide.
Author Information (click to view)

Pang X, Peng L, Chen Y,


Pang X, Peng L, Chen Y, (click to view)

Pang X, Peng L, Chen Y,

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Journal of labelled compounds & radiopharmaceuticals 2017 04 22() doi 10.1002/jlcr.3516
Abstract

Enzalutamide, a 2nd generation antiandrogen, has been developed for the treatment of CRPC. We synthesized the deuterated analogues 6 and found that it showed higher drug exposure and thus stronger anti-tumor 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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