Drug intelligence / Profile preview

sitokiren

Development stage
Phase 3
Lead developer
Shanghai Pharmaceuticals
Modality
Small Molecules
Administration
Oral
01

Overview

SPH3127 (sitokiren) is an orally active small molecule direct renin inhibitor developed for the treatment of hypertension and related cardiovascular and renal diseases. It is a non-peptide compound with improved oral bioavailability and greater antihypertensive potency compared to aliskiren in preclinical models. The drug acts by inhibiting renin—the rate-limiting enzyme in the renin-angiotensin-aldosterone system (RAAS)—thereby reducing blood pressure and potentially offering benefits in conditions such as essential hypertension, diabetic nephropathy, and ulcerative colitis. Sitokiren has reached phase III clinical trials for hypertension and phase II trials for diabetic nephropathies and ulcerative colitis[2][3][5][6].

Other names
CARBAMIC ACID N-(3-(3-((1R)-1-(CYCLOPROPYL((2R)-2-MORPHOLINYLCARBONYL)AMINO)ETHYL)-6-METHYL-1H-PYRAZOLO(3,4-B)PYRIDIN-1-YL)PROPYL)- METHYL ESTER
02

Targets

REN (Renin)

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