Drug intelligence / Profile preview

Obicetrapib + evolocumab

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

Overview

Obicetrapib + evolocumab is a combination of two lipid-lowering agents with complementary mechanisms of action, both under investigation or in use for the management of hypercholesterolemia and reduction of cardiovascular risk. Obicetrapib is a highly selective small molecule inhibitor of cholesteryl ester transfer protein (CETP), which reduces low-density lipoprotein cholesterol (LDL-C) by decreasing hepatic cholesterol and upregulating LDL receptor expression, thereby increasing LDL clearance. Evolocumab is a fully human monoclonal antibody that inhibits proprotein convertase subtilisin/kexin type 9 (PCSK9), preventing PCSK9-mediated degradation of LDL receptors on hepatocytes and thus enhancing removal of LDL-C from circulation. Obicetrapib is being developed primarily for patients with atherosclerotic cardiovascular disease or familial hypercholesterolemia as an adjunct to maximally tolerated lipid-lowering therapy[1][4][7]. Evolocumab, marketed as Repatha by Amgen, is approved for use in adults and children with primary hyperlipidemia or familial hypercholesterolemia to reduce LDL-C levels and lower the risk of major adverse cardiovascular events[3][5][6].

02

Targets

CETPPCSK9 (Proprotein convertase subtilisin/kexin type 9)

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