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FLX-787 is a highly selective small molecule drug developed as an agonist of transient receptor potential (TRP) ion channels, specifically targeting TRPA1 and TRPV1. It was designed to treat muscle cramps and spasms associated with neurological diseases such as amyotrophic lateral sclerosis (ALS), Charcot-Marie-Tooth disease (CMT), multiple sclerosis (MS), and nocturnal leg cramps. The drug acts by stimulating the TRPA1 protein and activating the TRPV1 receptor, which are believed to modulate hyperactive nerve signals in the spinal cord that cause muscle cramping. Developed originally by Flex Pharma, later merged into Salarius Pharmaceuticals, FLX-787 was formulated primarily as an orally disintegrating tablet. Despite showing positive efficacy signals in reducing cramp frequency and pain severity in early studies—including exploratory Phase 2 trials—the development of FLX-787 was discontinued due to tolerability concerns at higher doses, particularly oral intolerability observed during clinical trials[1][5][8].
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