DESCOVY Film-coated tablet Ref.[10515] Active ingredients: Emtricitabine Emtricitabine and Tenofovir alafenamide Tenofovir alafenamide

Emtricitabine is a synthetic nucleoside analogue of cytidine with activity that is specific to HIV-1, HIV-2 and HBV. Emtricitabine is phosphorylated by cellular enzymes to form emtricitabine 5'-triphosphate, which competitively inhibits HIV-1 reverse transcriptase, resulting in DNA chain termination. Emtricitabine is a weak inhibitor of mammalian DNA polymerase α, β and ε and mitochondrial DNA polymerase γ.

Emtricitabine is a nucleoside reverse transcriptase inhibitor (NRTI) and nucleoside analogue of 2'-deoxycytidine. Tenofovir alafenamide is a nucleotide reverse transcriptase inhibitor (NtRTI) and phosphonamidate prodrug of tenofovir (2'-deoxyadenosine monophosphate analogue). They both inhibit HIV replication through incorporation into viral DNA by the HIV RT, which results in DNA chain-termination. They have activity against HIV-1, HIV-2, and HBV.

Tenofovir alafenamide is a phosphonamidate prodrug of tenofovir. Tenofovir alafenamide enters primary hepatocytes by passive diffusion and by the hepatic uptake transporters OATP1B1 and OATP1B3. Tenofovir alafenamide is primarily hydrolysed to form tenofovir by carboxylesterase 1 in primary hepatocytes. Intracellular tenofovir is subsequently phosphorylated to the pharmacologically active metabolite tenofovir diphosphate. Tenofovir diphosphate inhibits HBV replication through incorporation into viral DNA by the HBV reverse transcriptase, which results in DNA chain termination. Tenofovir has activity that is specific to HBV and HIV (HIV-1 and HIV-2).