Drug intelligence / Profile preview

tenofovir + emtricitabine or lamivudine

Development stage
Unknown
Lead developer
Gilead Sciences
Modality
Small Molecules
Administration
Oral
01

Overview

This refers to a combination antiretroviral therapy (cART) regimen consisting of the nucleotide analog tenofovir (typically tenofovir disoproxil fumarate, TDF) paired with a nucleoside analog, either emtricitabine (FTC) or lamivudine (3TC). These agents are nucleoside/nucleotide reverse transcriptase inhibitors (NRTIs) that target the HBV DNA polymerase (reverse transcriptase), effectively blocking the replication of the hepatitis B virus (HBV) by inhibiting the reverse transcription of pregenomic HBV RNA to HBV DNA. This specific regimen was utilized as the standard-of-care background therapy in a randomized, open-label pilot study led by researchers at the University of California, San Francisco (UCSF) to evaluate the efficacy of entecavir intensification for persistent HBV viremia in HIV-HBV coinfected individuals. While tenofovir and emtricitabine are often administered as a fixed-dose combination (e.g., Truvada), the regimen described here allows for the substitution of emtricitabine with lamivudine, both of which are cytosine analogs with similar mechanisms of action against HBV and HIV-1.

Brand names
TruvadaCimduoTemixysVireadEmtrivaEpivir-HBV
Other names
TDF + FTCTDF + 3TCtenofovir disoproxil fumarate + emtricitabinetenofovir disoproxil fumarate + lamivudine
02

Targets

Human immunodeficiency virus type 1 reverse transcriptaseHBV Pol (Hepatitis B virus polymerase)

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