Drug intelligence / Profile preview

rosuvastatin + ezetimibe + telmisartan + amlodipine

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

Overview

This drug is a **combination product** composed of four active pharmaceutical ingredients: **rosuvastatin** (an HMG-CoA reductase inhibitor/statin), **ezetimibe** (a cholesterol absorption inhibitor), **telmisartan** (an angiotensin II receptor blocker/ARB), and **amlodipine** (a dihydropyridine calcium channel blocker). It is designed for the management of comorbid conditions such as **hypertension** and **hyperlipidemia** in patients at risk of cardiovascular disease. The goal of combining these agents is to enhance patient adherence through reduced pill burden while providing comprehensive inhibition of cholesterol synthesis and absorption (rosuvastatin, ezetimibe) as well as antihypertensive effects (telmisartan, amlodipine). All four agents act via well-characterized, distinct mechanisms of action. Pharmacokinetic studies show that the coadministration of these four agents in fixed-dose combination does not result in clinically significant drug–drug interactions, and the combination has been shown to be well tolerated in healthy subjects[1][3][5].

02

Targets

HMGCR (3-hydroxy-3-methylglutaryl-coenzyme A reductase)CACNA1C (Voltage-dependent L-type calcium channel subunit alpha-1C)AGTR1 (Angiotensin II Type-1 receptor)NPC1L1 (Niemann-pick C1-Like 1 transporter)

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