Literature DB >> 28432800

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

Xuehai Pang1,2, Lingling Peng3, Yuanwei Chen1,2,3,4.   

Abstract

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.
Copyright © 2017 John Wiley & Sons, Ltd.

Entities:  

Keywords:  CRPC; LNCaP/AR xenograft; PK/PD; deuterated drug; enzalutamide

Mesh:

Substances:

Year:  2017        PMID: 28432800     DOI: 10.1002/jlcr.3516

Source DB:  PubMed          Journal:  J Labelled Comp Radiopharm        ISSN: 0362-4803            Impact factor:   1.921


  3 in total

1.  A Phase I dose-escalation, pharmacokinetics and food-effect study of oral donafenib in patients with advanced solid tumours.

Authors:  Xiaoyu Li; Meng Qiu; Li Zheng; ShengJun Wang; Hong Zhu; Bi Feng
Journal:  Cancer Chemother Pharmacol       Date:  2020-02-01       Impact factor: 3.333

2.  Phase I clinical trial of HC-1119 soft capsule in Chinese healthy adult male subjects: Pharmacokinetics and safety of single-dose proportionality and effects of food.

Authors:  Haiping Ma; Weidong Xu; Jin Ni; Naping Zhao; Shouyan Tang; Song Li; Tingting Cai; Jianping Xiu; Xin Kang; Shen Gao; Li Zhang; Tie Zhou
Journal:  Prostate       Date:  2021-11-22       Impact factor: 4.012

Review 3.  Recent Updates on the Development of Deuterium-Containing Drugs for the Treatment of Cancer.

Authors:  Tafere Mulaw Belete
Journal:  Drug Des Devel Ther       Date:  2022-10-04       Impact factor: 4.319

  3 in total

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