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ezetimibe + raltegravir
- Development stage
- Phase 1
- Lead developer
- Merck
- Modality
- Small Molecules
- Administration
- Oral
01
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.
- Other names
- raltegravir and ezetimibe
02
Targets
Integrase allosteric pocket (HIV)NPC1L1 (Niemann-pick C1-Like 1 transporter)ACAT1 (Acyl-coenzyme A:cholesterol O-acyltransferase 1)
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