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TD-0714 is an orally active, potent, and highly selective small molecule inhibitor of human neprilysin (NEP), also known as CD10. It was developed for the treatment of chronic heart failure. The drug acts by inhibiting NEP, leading to increased levels of natriuretic peptides and sustained elevations in plasma cyclic guanosine monophosphate (cGMP), a biomarker of NEP target engagement. This mechanism supports vasodilation and natriuresis, which are beneficial in heart failure management. TD-0714 demonstrates high oral bioavailability, dose-proportional pharmacokinetics, minimal accumulation with once-daily dosing, negligible renal elimination (less than 1% excreted via kidneys), and a favorable safety profile in healthy volunteers. Its pharmacological properties suggest potential advantages over existing NEP inhibitors for patients with compromised renal function[1][2][5][6].
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