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AT-877ER is an oral, extended-release formulation of fasudil hydrochloride, a potent Rho-kinase (ROCK) inhibitor developed by Asahi Kasei Pharma. It is currently in Phase II clinical development for the treatment of pulmonary arterial hypertension (PAH). Rho-kinase is a key effector of the small GTPase Rho and plays a critical role in regulating vascular tone and remodeling; its overactivation is associated with the increased pulmonary vascular resistance and structural changes observed in PAH. By inhibiting both ROCK1 and ROCK2 isoforms, AT-877ER promotes vasodilation and may suppress the proliferation of vascular smooth muscle cells. The extended-release formulation is designed to maintain stable therapeutic plasma concentrations with twice-daily dosing, potentially improving the efficacy and safety profile compared to immediate-release or intravenous fasudil.
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