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ezetimibe + raltegravir

Development stage: Unknown
Lead developer: Merck
Modality: Small Molecules
Administration: Oral

Overview

A combination of ezetimibe, a cholesterol absorption inhibitor, and raltegravir, an HIV-1 integrase inhibitor. Ezetimibe selectively inhibits cholesterol absorption in the small intestine by targeting the Niemann-Pick C1-Like 1 (NPC1L1) protein. Raltegravir prevents HIV-1 viral DNA integration into the host cell genome by inhibiting the HIV-1 integrase enzyme. This combination has been studied for potential co-administration in HIV patients who also require cholesterol management.

Brand names: IsentressZetia
Other names: raltegravir and ezetimibe

Targets

ACAT1 (Acyl-coenzyme A:cholesterol O-acyltransferase 1)Integrase allosteric pocket (HIV)NPC1L1 (Niemann-pick C1-Like 1 transporter)

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