Drug intelligence / Profile preview

evolocumab + ezetimibe

Development stage
Unknown
Lead developer
Amgen
Modality
Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
Administration
Subcutaneous, Oral
01

Overview

Evolocumab + ezetimibe is a combination therapy consisting of evolocumab, a monoclonal antibody that inhibits proprotein convertase subtilisin/kexin type 9 (PCSK9), and ezetimibe, a small molecule that inhibits intestinal cholesterol absorption. Evolocumab increases hepatic LDL receptor (LDLR) availability by preventing PCSK9-mediated degradation of LDLR, thereby enhancing LDL cholesterol clearance from the blood. Ezetimibe blocks the Niemann-Pick C1-Like 1 (NPC1L1) protein in the small intestine, reducing dietary and biliary cholesterol absorption. Together, these agents provide additive LDL cholesterol lowering, primarily used for hypercholesterolemia, especially in high-risk cardiovascular disease patients who are statin-intolerant or inadequately controlled on statins. Both agents have proven efficacy in reducing LDL cholesterol and improving additional lipid parameters, and can be used in combination with statins or as adjuncts when statins are insufficient or contraindicated[1][2][3][4].

02

Targets

NPC1L1 (Niemann-pick C1-Like 1 transporter)

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