Drug intelligence / Profile preview

lonaprisan

Development stage
Phase 2
Lead developer
Bayer HealthCare Pharmaceuticals
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Oral
01

Overview

Lonaprisan is a synthetic, steroidal antiprogestogen developed by Bayer HealthCare Pharmaceuticals. It is an orally bioavailable pentafluoroethyl derivative of a mifepristone-related steroid with potent and highly selective antagonist activity at the progesterone receptor (PR), specifically both PR-A and PR-B isoforms. Unlike some other antiprogestins such as mifepristone, lonaprisan does not convert to an agonist in the presence of protein kinase A activators. Its mechanism involves binding to progesterone receptors and inhibiting their activation and associated proliferative effects in target tissues. Lonaprisan was investigated for use in endometriosis, dysmenorrhea, and breast cancer but development was discontinued after phase II clinical trials due to limited efficacy[2][3][4][5][6].

Other names
lonaprisanumProgesterone Receptor Antagonist ZK 230211
02

Targets

PR (Progesterone receptor)

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