AM095

AM095 is an LPA? receptor antagonist with good oral exposure and antifibrotic activity in rodent models. In vitro, AM095 inhibited GTPγS binding to Chinese hamster ovary (CHO) cell membranes overexpressing recombinant human or mouse LPA? with IC?? values of 0.98 and 0.73 μM, respectively, and exhibited no LPA? agonism. In functional assays, AM095 inhibited LPA-driven chemotaxis of CHO cells overexpressing mouse LPA? (IC??= 778 nM) and human A2058 melanoma cells (IC?? = 233 nM). Another study showed that LPA/LPA? pathway inhibition has the potential to be an effective new therapeutic strategy for systemic sclerosis (SSc), and that LPA? is an attractive pharmacologic target in dermal fibrosis.