Contineum drug compound PIPE-791 published in medicinal chemistry journal
Contineum Therapeutics (NASDAQ: CTNM) announced the publication of a manuscript describing the discovery and characterization of its LPAR1 antagonist compound PIPE-791 in the Journal of Medicinal Chemistry on June 29, 2026.
The article, authored by Chen et al., details how structural-activity relationship studies led to the identification of a scaffold responsible for slow but tight binding to the LPAR1 receptor. The compound was further optimized for brain-penetration and ADME properties, resulting in a once-daily oral dose formulation.
According to the company, PIPE-791 is described as the first LPAR1 antagonist capable of crossing the blood-brain barrier and fully occupying the target receptor at a low, once-daily oral dose. The compound demonstrated activity in multiple preclinical disease models targeting both central nervous system and peripheral disorders associated with LPA-LPAR1 signaling.
Daniel Lorrain, Ph.D., Chief Scientific Officer at Contineum Therapeutics, said the compound's chemical structure "facilitates a slow on-off rate," along with "differentiated pharmacokinetics and sustained, high target coverage."
PIPE-791 is currently enrolled in a global Phase 2 clinical trial for the treatment of idiopathic pulmonary fibrosis (IPF), identified by trial registration number NCT07284459. The company also lists chronic pain as an additional development indication for the compound.
Contineum Therapeutics is a clinical-stage biopharmaceutical company based in San Diego. Its pipeline includes PIPE-307, a selective M1 receptor inhibitor in clinical development for relapsing-remitting multiple sclerosis and major depressive disorder, being developed under a license agreement with Janssen Pharmaceutica NV, a Johnson & Johnson company.
