Drug intelligence / Profile preview

fimasartan + atorvastatin + ezetimibe

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

Overview

**Fimasartan + atorvastatin + ezetimibe** is a fixed-dose combination drug designed to target both *essential hypertension* and *primary hypercholesterolemia*, commonly coexisting cardiovascular risk factors[1]. - **Fimasartan** is an angiotensin II receptor blocker (ARB) that lowers blood pressure via selective antagonism of the angiotensin II type 1 receptor, decreasing vasoconstriction. - **Atorvastatin** is a statin that inhibits HMG-CoA reductase, reducing cholesterol biosynthesis primarily by lowering LDL cholesterol. - **Ezetimibe** inhibits the Niemann-Pick C1-Like 1 (NPC1L1) protein, reducing intestinal absorption of cholesterol. Combined therapy is shown to be superior to dual or monotherapy in reducing both blood pressure and LDL cholesterol levels in patients with both hypertension and dyslipidemia, with comparable safety and tolerability to its individual components[1]. Mechanistically, this combination provides complementary approaches to cardiovascular risk reduction: inhibiting cholesterol biosynthesis, cholesterol absorption, and angiotensin II-driven vascular tone.

Other names
fimasartan + ezetimibe + atorvastatin
02

Targets

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

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