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FB-1083 is a potent and selective, orally bioavailable small molecule antagonist of Faun269g, a ligand-gated ion channel. Discovered by Fauna Bio using its proprietary platform, the target Faun269g was identified for its role in protecting hibernating thirteen-lined ground squirrels from hypoxia/reperfusion injury. FB-1083 is currently in preclinical development for the treatment of heart failure with preserved ejection fraction (HFpEF) and pulmonary hypertension (PH). In preclinical studies, FB-1083 demonstrated sub-nanomolar potency (IC50 of 0.179 nM) and high selectivity (>5,000-fold) over related receptors. It has shown efficacy in rodent models of PH and HFpEF, significantly reducing mean right ventricular systolic pressure (RVSP), improving diastolic function, and attenuating adverse cardiac remodeling.
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