PIPE-791, a CNS penetrant, orally bioavailable LPA1 antagonist, reduces neuroinflammation and promotes functional remyelination in vivo 5 and is thus a promising treatment for multiple sclerosis.
PIPE-791 is the first orally bioavailable, brain penetrant LPA1 antagonist. We have performed extensive characterization of PIPE-791 in numerous in vitro and in vivo contexts. Here, we present data showing that PIPE-791 induces OPC differentiation, impacts neuroinflammation, and restores function in the mouse MOG-EAE model of MS. In total ...
Programs - Contineum Therapeutics
Our wholly-owned lead asset, PIPE-791, is a novel, brain penetrant, small molecule antagonist of the lysophosphatidic acid 1 receptor (LPA1R) in development for the potential treatment of progressive multiple sclerosis (Progressive MS).
Discovery of a brain penetrant small molecule antagonist ... - Nature
May 8, 2024 · We have identified and profiled PIPE-791, a potent, small molecule, brain-penetrant, LPA1 antagonist. Using a combination of in vitro and in vivo models, we show that PIPE-791 induces OPC...
Phase 1 study of MS candidate PIPE-791 in healthy volunteers set
Jun 12, 2023 · Pipeline Therapeutics will soon launch a Phase 1 clinical study to test PIPE-791, one of its candidate treatments for multiple sclerosis (MS), in healthy volunteers.
Contineum Therapeutics Initiates Patient Dosing in Phase 1b …
Mar 4, 2025 · PIPE-791 is a novel, brain penetrant, small molecule antagonist of the lysophosphatidic acid 1 receptor (LPA1R). PIPE-791 is being evaluated for the treatment of chronic pain associated with two separate indications, osteoarthritis (OA) and …
Pipeline Therapeutics Announces First Subject Dosed with PIPE-791 …
PIPE-791 is a potent, selective, brain-penetrant small molecule antagonist of the LPA1 receptor that has demonstrated activity in in vitro and in vivo models and was tolerated in IND-enabling studies.
PIPE-791 is a brain-penetrant, orally bioavailable, small molecule LPA1 receptor antagonist (Poon et al., 2024). xxx Beginning two weeks after CCI, four (4) macaques were p.o. dosed with
Discovery of a brain penetrant small molecule antagonist
May 8, 2024 · A medicinal chemistry effort identified PIPE-791, an oral, brain-penetrant, LPA1 antagonist. PIPE-791 was characterized in vitro and in vivo and was found to be a potent, selective LPA1 antagonist with slow receptor off-rate kinetics.
Contineum PIPE-791 Phase 1b PET Trial Begins Patient Dosing
Dec 17, 2024 · Contineum Therapeutics has initiated a Phase 1b positron emission tomography (PET) trial for PIPE-791, a novel brain-penetrant, small molecule antagonist of the lysophosphatidic acid 1 receptor (LPA1R).