TD-0212 (TD0212) is a potent, orally efficacious, dual AT1 antagonist/Neprilysin (NEP) inhibitor with pKi of 8.9 (AT1) and pIC50 of 9.2 (NEP).
TD-0212 produces blood pressure reductions similar to omapatrilat and combinations of AT1 receptor antagonists and NEP inhibitors in models of renin-dependent and -independent hypertension, does not increase TPE at antihypertensive doses in rat tracheal plasma extravasation (TPE) models.
1. R. Murray McKinnell, et al. Discovery of TD-0212, an Orally Active Dual Pharmacology AT1 Antagonist and Neprilysin Inhibitor (ARNI). ACS Med. Chem. Lett. DOI: 10.1021/acsmedchemlett.8b00462
