Drug intelligence / Profile preview

alirocumab + ezetimibe

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

Overview

**Alirocumab + ezetimibe** is a combination of two lipid-lowering drugs: alirocumab, a fully human monoclonal antibody that inhibits proprotein convertase subtilisin/kexin type 9 (PCSK9), and ezetimibe, a small molecule that inhibits cholesterol absorption at the brush border of the small intestine via the sterol transporter Niemann-Pick C1-Like-1 (NPC1L1)[1][2][4]. Alirocumab increases the number of LDL receptors on hepatocytes, promoting LDL cholesterol clearance, while ezetimibe prevents intestinal cholesterol uptake, reducing cholesterol delivery to the liver[1][2][4]. Both drugs are indicated for lowering low-density lipoprotein cholesterol (LDL-C) in patients with hypercholesterolemia, especially those inadequately controlled by statins or who are statin-intolerant[5][6]. This combination is not available as a fixed-dose product but is used in clinical practice and trials to achieve greater reductions in LDL-C than either agent alone[5][6].

02

Targets

NPC1L1 (Niemann-pick C1-Like 1 transporter)PCSK9 (Proprotein convertase subtilisin/kexin type 9)

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