Drug intelligence / Profile preview

olmesartan + rosuvastatin + ezetimibe

Development stage
Preclinical
Lead developer
Daewoong Pharmaceutical
Modality
Small Molecules
Administration
Oral
01

Overview

This is an oral **fixed-dose combination drug** consisting of **olmesartan**, **rosuvastatin**, and **ezetimibe**. - **Olmesartan**: An angiotensin II receptor blocker (ARB) used for lowering blood pressure by selectively blocking angiotensin II type 1 receptors, leading to vasodilation and decreased aldosterone effects. - **Rosuvastatin**: A statin (HMG-CoA reductase inhibitor) that reduces cholesterol synthesis in the liver, used for lowering LDL cholesterol and reducing cardiovascular risk[6]. - **Ezetimibe**: A cholesterol absorption inhibitor that blocks the absorption of cholesterol at the brush border of the small intestine by inhibiting the Niemann-Pick C1-Like 1 (NPC1L1) protein, lowering plasma LDL cholesterol levels[7]. The combination targets both hypertension (via olmesartan) and hyperlipidemia/dyslipidemia (via rosuvastatin and ezetimibe), addressing cardiovascular risk factors in a single pill. It is administered as a tablet by mouth[4][7]. This specific three-drug combination does not yet have a unique brand name and is in clinical development, as a component of a four-drug fixed-dose combination (often also including amlodipine) being developed by Daewoong Pharmaceutical[4][7].

02

Targets

NPC1L1 (Niemann-pick C1-Like 1 transporter)HMGCR (3-hydroxy-3-methylglutaryl-coenzyme A reductase)AGTR1 (Angiotensin II Type-1 receptor)

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