Drug intelligence / Profile preview

efavirenz + tenofovir disoproxil fumarate + telaprevir

Development stage
Phase 1
Lead developer
Bristol Myers Squibb
Modality
Small Molecules
Administration
Oral
01

Overview

This is a combination of three antiviral drugs: efavirenz, tenofovir disoproxil fumarate, and telaprevir. Efavirenz is a non-nucleoside reverse transcriptase inhibitor that blocks HIV reverse transcriptase, an enzyme necessary for viral replication. Tenofovir disoproxil fumarate is a nucleotide reverse transcriptase inhibitor that also inhibits HIV reverse transcriptase by competing with natural substrates and causing DNA chain termination. Telaprevir is a protease inhibitor that targets the hepatitis C virus by reversibly binding to the NS3/4A serine protease, preventing cleavage of viral polyproteins required for HCV replication[2][6]. This combination would theoretically have activity against both HIV and hepatitis C virus if used together; however, this specific triple combination does not represent an approved or standard regimen for either infection.

Brand names
Sustiva (efavirenz)Viread (tenofovir disoproxil fumarate)Incivek (telaprevir)
Other names
EFV (efavirenz)TDF (tenofovir disoproxil fumarate)TVR (telaprevir)
02

Targets

Human immunodeficiency virus type 1 reverse transcriptaseNS3/4A (Hepatitis C virus nonstructural protein 3/4A serine protease)

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