Drug intelligence / Profile preview

ezetimibe + laropiprant

Development stage
Discontinued
Lead developer
Merck
Modality
Small Molecules
Administration
Oral
01

Overview

Ezetimibe + laropiprant is a hypothetical combination of two small molecule drugs, each with distinct mechanisms of action related to lipid management. Ezetimibe is a cholesterol absorption inhibitor that acts at the intestinal brush border by selectively blocking the Niemann-Pick C1-Like 1 protein (NPC1L1), thereby reducing the absorption of dietary and biliary cholesterol into enterocytes and ultimately lowering blood LDL cholesterol levels[1][6]. Laropiprant is a selective antagonist of the prostaglandin D2 receptor subtype DP1; it was developed to reduce niacin-induced flushing by inhibiting vasodilation mediated by prostaglandin D2 activation of DP1[3][4][8]. While both agents have been used in lipid-lowering strategies—ezetimibe as monotherapy or in combination with statins, and laropiprant primarily in fixed-dose combinations with niacin—there are no known marketed products or clinical evidence for their use together as a fixed combination. Ezetimibe is indicated for hypercholesterolemia and certain rare inherited lipid disorders, while laropiprant was previously approved (now withdrawn) only as part of niacin/laropiprant combinations for dyslipidemia.

02

Targets

NPC1L1 (Niemann-pick C1-Like 1 transporter)PTGDR (Prostanoid DP1 receptor)

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