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Rosuvastatin and Ezetimibe

Hanmi Pharmaceutical Company Limited · FDA-approved active Small molecule

Rosuvastatin inhibits HMG-CoA reductase to lower LDL cholesterol, while ezetimibe blocks intestinal cholesterol absorption, providing dual lipid-lowering action.

Rosuvastatin inhibits HMG-CoA reductase to lower LDL cholesterol, while ezetimibe blocks intestinal cholesterol absorption, providing dual lipid-lowering action. Used for Hypercholesterolemia and dyslipidemia, Cardiovascular risk reduction in patients requiring additional LDL-C lowering.

At a glance

Generic nameRosuvastatin and Ezetimibe
Also known asCrestor and Ezetrol
SponsorHanmi Pharmaceutical Company Limited
Drug classStatin and ezetimibe combination
TargetHMG-CoA reductase and NPC1L1 transporter
ModalitySmall molecule
Therapeutic areaCardiovascular
PhaseFDA-approved

Mechanism of action

Rosuvastatin is a statin that reduces cholesterol synthesis in the liver by inhibiting HMG-CoA reductase, the rate-limiting enzyme in cholesterol production. Ezetimibe selectively inhibits cholesterol absorption in the small intestine by blocking the Niemann-Pick C1-like 1 (NPC1L1) transporter. Together, they provide complementary mechanisms to reduce both endogenous cholesterol production and dietary cholesterol uptake, resulting in greater LDL-C lowering than either agent alone.

Approved indications

Common side effects

Key clinical trials

Primary sources

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SourceUsed for
ClinicalTrials.govTrial enrolment, design, endpoints, results

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