RTN-001

RTN-001 is a first-in-class, potent, and selective second-generation small molecule inhibitor of phosphodiesterase type 5 (PDE5), developed to preferentially target and distribute to cardiovascular tissues—especially the aorta and higher vasculature—to treat uncontrolled and resistant hypertension. This compound enhances nitric oxide (NO) signaling by preventing the breakdown of cyclic guanosine monophosphate (cGMP), which is essential for vasodilation and blood pressure regulation. Unlike earlier PDE5 inhibitors, RTN-001 was specifically optimized for central cardiovascular action rather than erectile dysfunction, leading to a sustained antihypertensive effect and clinically significant reductions in blood pressure in phase 2 studies. It is being developed in an oral, modified-release formulation for once-daily dosing to improve 24-hour blood pressure control. RTN-001 is Retension Pharmaceuticals’ lead clinical candidate and is in-licensed from Sanofi.

Other names

RTN 001RTN001RTN-001