Drug intelligence / Profile preview

aliskiren + enalapril + valsartan

Development stage
Phase 4
Lead developer
Novartis
Modality
Small Molecules
Administration
Oral
01

Overview

This refers to a research regimen consisting of three distinct classes of renin-angiotensin system (RAS) inhibitors: the direct renin inhibitor **aliskiren**, the angiotensin-converting enzyme (ACE) inhibitor **enalapril**, and the angiotensin receptor blocker (ARB) **valsartan**. This specific triad was evaluated by the **University Hospital, Basel** in a Phase 1 clinical trial (NCT02141971) to characterize the "RAS-peptide-profile" (also known as the RAS-fingerprint) in healthy male subjects. The study utilized advanced mass spectrometry-based profiling to quantify the equilibrium concentrations of various angiotensin peptides, including Angiotensin I, Angiotensin II, Angiotensin 1-7, and Angiotensin 1-5. By inhibiting the RAS at three different levels—renin activity, ACE-mediated conversion, and the AT1 receptor—researchers aimed to map the systemic biochemical impact of these inhibitors and correlate peptide levels with pharmacokinetic and pharmacodynamic outcomes such as aldosterone suppression and blood pressure changes.

Other names
ACEI + ARB + RITriple RAS Blockade
02

Targets

AGTR1 (Angiotensin II Type-1 receptor)ACE (Angiotensin Converting Enzyme)REN (Renin)

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