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Musculoskeletal disease


Lysophosphatidic acid receptor 1 (LPAR1; EDG2; LPA1)

In vitro and mouse studies suggest LPAR1 antagonists could help treat osteoporosis. In mouse models of the indication, bone levels of Lpar1 were higher than those in healthy control mice, and LPAR1 antagonists decreased bone loss compared with vehicle. In bone marrow cells from normal mice, Lpar1 levels correlated with markers of osteoclast differentiation, and Lpar1 deficiency or inhibition decreased osteoclast differentiation compared with normal Lpar1 expression or vehicle. Planned work includes testing bone levels of LPAR1 in patients with osteoporosis.
Bristol-Myers Squibb Co.'s BMS-986202 (formerly AM152), an oral LPAR1 antagonist, is in Phase I testing to treat pulmonary fibrosis. The company also has another oral LPAR1 antagonist, AM095, in preclinical testing to treat scleroderma.
Kyowa Hakko Kirin Co. Ltd. and Debiopharm Group have Debio 0719, a selective inhibitor of LPAR1 and LPAR3 (EDG7; LPA3), in preclinical testing to treat cancer.

SciBX 7(6); doi:10.1038/scibx.2014.177
Published online Feb. 13, 2014

Unpatented; unlicensed; available for partnering

David, M. et al. J. Biol. Chem.; published online Jan. 15, 2014;
Contact: Olivier Peyruchaud, Institut National de la Santé et de la Recherche Médicale (INSERM) U1033, Lyon, France