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Ezetimibe + Atorvastatin

Organon and Co · FDA-approved active Small molecule

This combination reduces cholesterol by blocking intestinal cholesterol absorption (ezetimibe) and inhibiting HMG-CoA reductase to decrease hepatic cholesterol synthesis (atorvastatin).

This combination reduces cholesterol by blocking intestinal cholesterol absorption (ezetimibe) and inhibiting HMG-CoA reductase to decrease hepatic cholesterol synthesis (atorvastatin). Used for Hypercholesterolemia and mixed dyslipidemia, Cardiovascular risk reduction in patients requiring LDL-C lowering.

At a glance

Generic nameEzetimibe + Atorvastatin
Also known asSCH 58235, Zetia, Lipitor
SponsorOrganon and Co
Drug classCholesterol absorption inhibitor + HMG-CoA reductase inhibitor (statin combination)
TargetNPC1L1 (ezetimibe); HMG-CoA reductase (atorvastatin)
ModalitySmall molecule
Therapeutic areaCardiovascular
PhaseFDA-approved

Mechanism of action

Ezetimibe selectively inhibits Niemann-Pick C1-like 1 (NPC1L1) protein in the intestinal brush border, reducing dietary and biliary cholesterol absorption. Atorvastatin is an HMG-CoA reductase inhibitor (statin) that blocks the rate-limiting enzyme in hepatic cholesterol synthesis. Together, they provide complementary mechanisms to lower LDL cholesterol and reduce cardiovascular risk.

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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