SAN DIEGO, June 30, 2026
Contineum Therapeutics, Inc. announced the publication of its scientific manuscript describing the discovery and characterization of PIPE-791 in the Journal of Medicinal Chemistry, highlighting the company’s internally developed lysophosphatidic acid receptor 1 (LPAR1) antagonist as a potentially best-in-class therapeutic candidate for fibrotic and neuroinflammatory diseases. The peer-reviewed publication, titled “Discovery of PIPE-791, a Potent and Brain-Penetrant Lysophosphatidic Acid Receptor 1 (LPAR1) Antagonist with Slow Tight Binding Characteristics for the Treatment of Neuroinflammatory Disorders,” details the medicinal chemistry, structural optimization, and pharmacological properties that differentiate PIPE-791 from earlier LPAR1 inhibitors. The publication represents an important scientific milestone for Contineum Therapeutics, reinforcing the company’s expertise in developing innovative oral small-molecule therapies targeting neuroscience, inflammation, and immunology (NI&I) disorders with significant unmet medical needs.
Novel LPAR1 Antagonist Demonstrates Differentiated Drug Design
According to the publication, extensive structure-activity relationship (SAR) studies enabled researchers to identify a unique molecular scaffold responsible for the compound’s slow but tight receptor-binding characteristics, providing prolonged inhibition of LPAR1, a receptor involved in multiple fibrotic and inflammatory signaling pathways. Researchers further optimized the compound to improve brain penetration and ADME (absorption, distribution, metabolism, excretion) properties, ultimately creating PIPE-791, the first reported LPAR1 antagonist capable of efficiently crossing the blood-brain barrier while maintaining sustained target engagement at a low once-daily oral dose. The company believes these pharmacokinetic advantages may support improved therapeutic activity across both central nervous system (CNS) disorders and systemic fibrotic diseases driven by abnormal LPA-LPAR1 signaling.
Preclinical Research Supports Broad Therapeutic Potential
The published research demonstrated that PIPE-791 produced encouraging activity across multiple preclinical disease models, supporting its potential application in both neurological and fibrotic disorders. By blocking LPAR1, the investigational therapy inhibits key biological pathways involved in fibrosis, inflammation, and tissue remodeling, making it a promising candidate for diseases characterized by excessive scar tissue formation and chronic inflammation. Company scientists noted that the compound’s combination of high receptor occupancy, brain penetration, and once-daily oral administration differentiates it from previous LPAR1-targeting molecules. Daniel Lorrain, Ph.D., Chief Scientific Officer of Contineum Therapeutics, stated that the discovery reflects years of research focused on unlocking the full therapeutic potential of LPAR1 inhibition, with the unique chemical properties of PIPE-791 providing the opportunity to pursue a potentially best-in-class treatment across multiple inflammatory and fibrotic indications.
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PIPE-791 Advances Across Fibrotic and Neurological Diseases
Building on its preclinical foundation, PIPE-791 is currently being evaluated in a global Phase 2 clinical trial for idiopathic pulmonary fibrosis (IPF), a progressive and life-threatening lung disease with limited treatment options. In addition to IPF, Contineum Therapeutics is investigating the molecule’s potential in chronic pain and other diseases linked to dysregulated LPAR1 signaling, reflecting the broad applicability of its mechanism of action. The publication of the discovery research provides external scientific validation of the company’s proprietary drug discovery platform while strengthening confidence in its broader pipeline of internally developed oral therapies. As Contineum Therapeutics continues advancing PIPE-791 alongside other clinical-stage programs, the company aims to expand treatment options for patients affected by serious inflammatory, neurological, and fibrotic diseases where significant unmet medical needs remain.
Source: Contineum Therapeutics, press release
