Drug intelligence / Profile preview

remikiren

Development stage
Discontinued
Lead developer
Roche
Modality
Covalent Small Molecules → Small Molecules, Classical Binding Small Molecules → Small Molecules
Administration
Oral
01

Overview

Remikiren is an orally active small molecule renin inhibitor developed for the treatment of hypertension and heart failure. It acts by specifically inhibiting human renin (IC50 ≈ 0.7 nM), thereby blocking the conversion of angiotensinogen to angiotensin I in the renin-angiotensin system, which leads to a reduction in blood pressure. Remikiren was first developed by Hoffmann–La Roche and demonstrated potent antihypertensive effects in preclinical and clinical studies; however, its development was discontinued before approval[1][2][3][4][5][6][7].

Other names
remikiren
02

Targets

REN (Renin)

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