Drug intelligence / Profile preview

aliskiren + irbesartan

Development stage
Preclinical
Lead developer
Novartis
Modality
Small Molecules
Administration
Oral
01

Overview

Aliskiren + irbesartan is an oral combination of two antihypertensive agents: **aliskiren**, a direct renin inhibitor, and **irbesartan**, an angiotensin II receptor blocker (ARB). This combination aims to provide dual blockade of the renin-angiotensin-aldosterone system (RAAS)—aliskiren inhibits renin, preventing the conversion of angiotensinogen to angiotensin I, while irbesartan selectively blocks angiotensin II receptors, reducing downstream vasoconstriction and aldosterone effects. The combination has shown a greater antiproteinuric effect in type 2 diabetic patients with hypertension and albuminuria compared to monotherapy with either agent[1][2]. However, evidence and regulatory guidance warn of increased risks, including renal impairment, hypotension, and hyperkalemia in patients (particularly those with diabetes or renal impairment), and this combination is generally not recommended or approved for use in these populations due to safety concerns[3][7].

02

Targets

REN (Renin)AGTR1 (Angiotensin II Type-1 receptor)

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