Drug intelligence / Profile preview

ezetimibe + rosuvastatin + candesartan + amlodipine

Development stage
Phase 3
Lead developer
Merck
Modality
Small Molecules
Administration
Oral
01

Overview

This is a fixed-dose or co-administered combination therapy consisting of four active pharmaceutical ingredients: - **Ezetimibe**: a cholesterol absorption inhibitor that blocks intestinal absorption of cholesterol, reducing LDL-C levels. - **Rosuvastatin**: an HMG-CoA reductase inhibitor (statin) that reduces hepatic cholesterol synthesis and lowers LDL-C, total cholesterol, and triglycerides while increasing HDL-C[2][5]. - **Candesartan**: an angiotensin II receptor blocker (ARB) used to lower blood pressure by blocking the vasoconstrictor effects of angiotensin II. - **Amlodipine**: a calcium channel blocker that relaxes vascular smooth muscle to reduce blood pressure. The primary indication for this multi-drug regimen is in patients with both essential hypertension and hyperlipidemia to improve patient compliance and reduce cardiovascular risk[3][4]. The combination targets both lipid lowering and antihypertensive effects through complementary mechanisms. Clinical studies have evaluated the safety and efficacy of using these combinations together in patients with comorbid hypertension and dyslipidemia[3][4].

Brand names
Roszet (for ezetimibe/rosuvastatin only)[2]Twynsta (for telmisartan/amlodipine, not candesartan/amlodipine)[1]
Other names
ezetimibe + rosuvastatin + candesartan cilexetil + amlodipine besylate
02

Targets

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

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