Drug intelligence / Profile preview

GSK2248761 + raltegravir

Development stage
Phase 1
Lead developer
GSK
Modality
Small Molecules
Administration
Oral
01

Overview

GSK2248761 + raltegravir is a combination of two investigational and approved antiretroviral agents for the treatment of HIV infection. GSK2248761 is a next-generation non-nucleoside reverse transcriptase inhibitor (NNRTI) developed by GSK. Raltegravir is an integrase strand transfer inhibitor (INSTI) that prevents the integration of HIV DNA into the host genome and is marketed under the brand name Isentress by Merck & Co. This combination has been studied for potential pharmacokinetic interactions and was found to have no clinically significant interaction when co-administered. Both drugs act on different stages of the HIV replication cycle—GSK2248761 inhibits reverse transcription while raltegravir blocks viral DNA integration—making them suitable for use in combination antiretroviral therapy[2][7].

Brand names
Isentress HD
02

Targets

Integrase allosteric pocket (HIV)Human immunodeficiency virus type 1 reverse transcriptase

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