Drug intelligence / Profile preview

GSK2248761 + darunavir + ritonavir

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

Overview

GSK2248761 + darunavir + ritonavir is a combination of three orally administered small molecules for the treatment of HIV infection. GSK2248761 is an investigational non-nucleoside reverse transcriptase inhibitor (NNRTI) developed by GSK. Darunavir is an HIV-1 protease inhibitor, and ritonavir is used as a pharmacokinetic enhancer (booster) to increase plasma concentrations of darunavir. Darunavir and ritonavir are widely used together in antiretroviral therapy and are generally co-administered with an additional antiretroviral agent. This triple combination would be expected to provide potent suppression of HIV replication by inhibiting two critical viral enzymes: reverse transcriptase (via GSK2248761) and protease (via darunavir, boosted by ritonavir).

02

Targets

Human immunodeficiency virus type 1 reverse transcriptaseCYP3A7 (Cytochrome P450 3A7)PR (Progesterone receptor)

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