oral QD sGC stimulator
Ph. I in healthy volunteers completed
from HTS + optimization
J. Med. Chem., April 11, 2023
Bayer, Wuppertal, DE
Potential for an improved sGC stimulator for resistant hypertension. BAY 1165747 (BAY-747) is a new, structurally distinct, soluble guanylate cyclase (sGC) stimulator with potential in the treatment of resistant hypertension. Identified through ultrahigh-throughput screening, it features an imidazo[1,2-a]pyridine core, distinct from the previously described 2-(1-benzyl-1H-pyrazol-3-yl) pyrimidine sGC stimulators. The property-based design led to an improved human PK profile compared to Bayer’s approved sGC stimulator, riociguat (2013). As Drug Hunter has highlighted previously, treatment-resistant hypertension remains an area with high unmet need, with up to 15M Americans not adequately treated after 3 or more medications. current oral sGC stimulators Current sGC stimulators for hypertension require frequent dosing. To date the only sGC stimulator approved for treatment of hypertension is riociguat, with…