Drug intelligence / Profile preview

rilpivirine + raltegravir

Development stage
Preclinical
Lead developer
Janssen Pharmaceutical
Modality
Small Molecules
Administration
Oral
01

Overview

TMC278 + raltegravir is a combination of two antiretroviral agents for HIV-1 treatment. Rilpivirine (TMC278) is a next-generation non-nucleoside reverse transcriptase inhibitor (NNRTI) with potent anti-HIV-1 activity and a high barrier to resistance. It inhibits HIV-1 reverse transcriptase, preventing viral DNA synthesis[2]. Raltegravir is an integrase strand transfer inhibitor that blocks HIV-1 integrase, preventing the integration of viral DNA into the host genome[1][5]. Used together, these drugs target separate essential steps of HIV replication: reverse transcription and genome integration. The combination is investigated for nucleoside-sparing regimens or multi-class resistant HIV.

Other names
rilpivirineTMC278TMC-278TMC 278raltegravir
02

Targets

Human immunodeficiency virus type 1 reverse transcriptaseIntegrase allosteric pocket (HIV)

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