Drug intelligence / Profile preview

solengepras

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

Overview

CVN424 (solengepras) is a first-in-class, orally available, brain-penetrant small molecule developed for the treatment of Parkinson’s disease. It acts as a selective inverse agonist of G protein-coupled receptor 6 (GPR6), an orphan G-protein coupled receptor predominantly expressed in dopamine D2-type medium spiny neurons within the striatum. By inhibiting GPR6 activity, CVN424 modulates the indirect (striatopallidal) pathway implicated in motor dysfunction in Parkinson’s disease. This non-dopaminergic mechanism allows for improvement of motor symptoms without directly affecting D1-dependent pathways or causing dyskinesia associated with traditional dopaminergic therapies. The drug is being developed both as monotherapy and as an adjunct to levodopa therapy[1][2][5][6][8].

Other names
1-[2-[4-(2,4-difluorophenoxy)piperidin-1-yl]-3-[[(3r)-oxolan-3-yl]amino]-7,8-dihydro-5h-pyrido[3,4-b]pyrazin-6-yl]ethanone1-(2-(4-(2,4-difluorophenoxy)piperidin-1-yl)-3-(((R)-tetrahydrofuran-3-yl)amino)-7,8-dihydropyrido[3,4-b]pyrazin-6(5H)-yl)ethan-1-one
02

Targets

GPR6 (G protein-coupled receptor 6)

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