Drug intelligence / Profile preview

rezvilutamide

Development stage
Phase 3
Lead developer
Hengrui Pharmaceutical
Modality
Small Molecules
Administration
Oral
01

Overview

Rezvilutamide is an oral, second-generation small molecule androgen receptor (AR) antagonist developed for the treatment of prostate cancer. It competitively binds to the androgen receptor in target tissues and prevents androgen-induced activation by inhibiting AR nuclear translocation and DNA binding. This results in reduced transcription of AR-mediated genes that drive prostate cancer cell proliferation. Rezvilutamide has demonstrated efficacy in delaying disease progression and improving patient-reported outcomes compared to bicalutamide when combined with androgen deprivation therapy (ADT). It was developed by Jiangsu Hengrui Medicine Co., Ltd., and is marketed under the brand name 艾瑞恩 in China for metastatic hormone-sensitive prostate cancer (mHSPC) with high tumor burden[1][3][5][6].

Brand names
艾瑞恩
Other names
4-(3-(4-((S)-2,3-dihydroxypropoxy)phenyl)-4,4-dimethyl-5-oxo-2-thioxoimidazolidin-1-yl)-2-(trifluoromethyl)benzonitrileBenzonitrile, 4-(3-(4-((2S)-2,3-dihydroxypropoxy)phenyl)-4,4-dimethyl-5-oxo-2-thioxoimidazolidinyl)-2-(trifluoromethyl)
02

Targets

AR (Adrenergic receptors)

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