TD-0212

Description

TD-0212 is a potent, selective and orally active, dual AT1 antagonist/NEP inhibitor (ARNI) with At1 pKi-8.9 and NEP pIC50 = 9.2. TD-0212 produced blood pressure reductions similar to omapatrilat and combinations of AT1 receptor antagonists and NEP inhibitors. TD-0212 therefore provides the enhanced activity of dual AT1/NEP inhibition with a potentially lower risk of angioedema relative to dual ACE/NEP inhibition

Uses

TD-0212 (compound 35) is an orally active dual pharmacology angiotensin II type 1 receptor (AT1) antagonist and neprilysin (NEP) inhibitor, with a pKi of 8.9 for AT1 and a pIC50 of 9.2 for NEP[1].

in vivo

References

[1] McKinnell RM, et al. Discovery of TD-0212, an Orally Active Dual Pharmacology AT1 Antagonist and Neprilysin Inhibitor (ARNI). ACS Med Chem Lett. 2018 Dec 3;10(1):86-91. DOI:10.1021/acsmedchemlett.8b00462