VTP-27999

VTP‑27999 is a highly potent and selective small molecule renin inhibitor developed for the treatment of hypertension, chronic renal disease, and end-organ protection. It acts by directly inhibiting renin, thereby suppressing the renin–angiotensin–aldosterone system (RAAS), which leads to reduced production of angiotensin II and aldosterone. Compared to aliskiren, it is approximately twice as potent on a dose basis and demonstrates excellent selectivity over related off-targets. In clinical studies, VTP‑27999 effectively suppressed angiotensin and aldosterone production in humans at doses up to 300 mg. At higher doses (>300 mg), it can cause marked increases in plasma renin that may exceed its capacity for systemic inhibition. Unlike other renin inhibitors such as aliskiren, VTP‑27999 does not induce conformational changes in prorenin[1][5][6][7].

Other names

942142-51-0UNII-254XY8NV84UNII254XY8NV84UNII 254XY8NV84Methyl N-[2-[ (R)-(3-chlorophenyl)[(3R)-1-[[(2S)-2-(methylamino)-3-(3R-tetrahydro-2H-pyran-3-yl)propyl]amino]carbonyl]-3-piperidinyl]methoxy]ethyl]carbamate