Products
Eftenla
Pharmacotherapeutic group
Antiviral for the treatment of HIV infectionsInternational name
Lamivudine + Tenofovir + EfavirenzDosage form
TabletsEfavirenz, lamivudine, and tenofovir disoproxil fumarate fixed-dose antiviral combination.
Lamivudine is a nucleoside analogue inhibiting viral DNA synthesis during the HIV reverse transcription.
Tenofovir disoproxil fumarate is a fumaric acid salt of tenofovir disoproxil pro-drug. Upon absorption, tenofovir disoproxil is converted into tenofovir, the active substance that is a nucleoside monophosphate (nucleotide) analogue. Tenofovir is then converted to the active metabolite, tenofovir diphosphate, an obligate chain terminator, by constitutively expressed cellular enzymes. Tenofovir diphosphate inhibits HIV-1 reverse transcriptase and HBV polymerase by direct binding competition with the natural deoxyribonucleotide substrate and, after incorporation into DNA, by DNA chain termination.
Efavirenz is a non-nucleoside reverse transcriptase inhibitor (NNRTI) of HIV-1. Efavirenz is a noncompetitive inhibitor of HIV-1 reverse transcriptase but it does not inhibit HIV-2 reverse transcriptase and human cellular DNA polymerases (alpha, beta, gamma, and delta).