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PIPE-791 is a novel, brain-penetrant small molecule antagonist of the lysophosphatidic acid 1 receptor (LPA1R). It is being developed by Contineum Therapeutics for the treatment of idiopathic pulmonary fibrosis (IPF), progressive forms of multiple sclerosis (MS), and chronic pain conditions such as osteoarthritis and low back pain. The drug works by selectively blocking LPA1 receptor activity, which plays a key role in fibrosis and neuroinflammation—pathological processes central to IPF and progressive MS. In chronic pain states, LPA1 activation contributes to neuropathic symptoms through demyelination of nerve fibers, increased neuronal excitability, and enhanced neuroinflammatory responses in the central nervous system. By antagonizing this receptor, PIPE-791 aims to prevent or reverse maladaptive changes that drive disease progression or persistent pain[1][2][3][5][7][10].
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