Drug intelligence / Profile preview

zilebesiran + olmesartan

Development stage
Phase 2
Lead developer
Alnylam Pharmaceuticals
Modality
Chemically Modified siRNA → Small Interfering RNA (siRNA) → Small RNA Therapeutics → RNA Therapeutics → Nucleic Acid Therapeutics, Conjugated siRNA → Small Interfering RNA (siRNA) → Small RNA Therapeutics → RNA Therapeutics → Nucleic Acid Therapeutics, Small Molecules
Administration
Subcutaneous, Oral
01

Overview

A combination of **zilebesiran**, an investigational small interfering RNA (siRNA) targeting hepatic angiotensinogen, and **olmesartan**, an angiotensin II receptor blocker (ARB), primarily evaluated for the treatment of hypertension. Zilebesiran works by silencing hepatic angiotensinogen mRNA, directly reducing levels of angiotensinogen, suppressing the entire renin–angiotensin–aldosterone system (RAAS) upstream and leading to blood pressure reduction[1][4][6]. Olmesartan selectively blocks the angiotensin II type 1 receptor (AT1) and inhibits the vasoconstrictor and blood pressure-elevating actions of angiotensin II[2]. Their combination targets the RAAS at different points and has been studied in clinical trials for enhanced antihypertensive efficacy, though the BP-lowering effect when combined with olmesartan may be less pronounced and possibly shorter in duration versus other antihypertensive agents[1][3][5][7].

02

Targets

AGTR1 (Angiotensin II Type-1 receptor)AGT (O6-methylguanine-DNA methyltransferase)

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