Drug intelligence / Profile preview

ezetimibe + efavirenz

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

Overview

Ezetimibe + efavirenz is a combination therapy used in HIV-infected patients with hyperlipidemia. Ezetimibe is a cholesterol absorption inhibitor that reduces the absorption of cholesterol from foods and the production of cholesterol in the body. Efavirenz is a non-nucleoside reverse transcriptase inhibitor (NNRTI) used as part of highly active antiretroviral therapy (HAART) for the treatment of HIV type 1. Clinical studies have shown that ezetimibe may be a safe and efficient therapeutic option in patients with HIV infection on efavirenz-containing regimens, as ezetimibe had no effect on the disposition of efavirenz, and efavirenz did not significantly impact the lipid-lowering effects of ezetimibe.

02

Targets

Human immunodeficiency virus type 1 reverse transcriptaseABCC2 (ATP-binding cassette sub-family C member 2)CYP46A1 (Cholesterol 24-hydroxylase)ABCB1 (P-glycoprotein)NPC1L1 (Niemann-pick C1-Like 1 transporter)

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