Drug intelligence / Profile preview

vilaprisan

Development stage
Discontinued
Lead developer
Bayer
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Oral
01

Overview

Vilaprisan is a synthetic and steroidal selective progesterone receptor modulator (SPRM) developed by Bayer for the treatment of symptomatic uterine fibroids and endometriosis. It acts as a highly potent antagonist at the progesterone receptor (PR), exhibiting strong binding affinity with no agonistic activity. By competitively binding to PR in progesterone-responsive tissues, vilaprisan inhibits PR-mediated gene expression and interferes with progesterone activity in the reproductive system. This mechanism suppresses ovulation and may inhibit proliferation of endometrial tissue or uterine fibroid formation. Vilaprisan is orally administered and has been evaluated in multiple phase I–III clinical trials for gynecological conditions such as uterine fibroids (leiomyoma) and endometriosis[1][2][3][4][5][6][7].

Other names
17β-Hydroxy-11β-[4-(methylsulfonyl)phenyl]-17α-(1,1,2,2,2-pentafluoroethyl)estra-4,9-dien-3-one
02

Targets

PR (Progesterone receptor)

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