Tenofovir

Tenofovir (GS 1278; PMPA) is a nucleotide reverse transcriptase inhibitor to treat HIV and chronic Hepatitis B (HBV)^[1]. In Vitro:Tenofovir displays cytotoxicity against HK-2 cells, with IC₅₀ values of 9.21 μM at 48 h and 2.77 μM at 72 h determined by MTT assay. It reduces intracellular ATP levels, elevates oxidative stress and protein carbonylation, and triggers mitochondria-mediated apoptosis in HK-2 cells^[1].
Tenofovir formulated with M48U1 in 0.25% HEC inhibits the replication of R5-tropic HIV-1_BaL and X4-tropic HIV-1_IIIb in activated PBMCs, and suppresses a panel of laboratory HIV-1 strains and patient-derived primary HIV-1 isolates. The combined formulation of Tenofovir and M48U1 in 0.25% HEC delivers synergistic antiretroviral activity against R5-tropic HIV-1_BaL infection and exhibits no cytotoxicity toward PBMCs^[2]. In Vivo:Tenofovir Disoproxil Fumarate (20-300 mg/kg) administered to BLT mice, shows dose dependent activity during vaginal HIV challenge in BLT humanized mice^[3].
Tenofovir Disoproxil Fumarate (50-300 mg/kg) significantly reduces HIV transmission in BLT mice^[3].
Tenofovir Disoproxil Fumarate (0.5-5.0 mg/kg/day, p.o.) induces a dose-dependent decrease in serum viremia in marmots with chronic WHV infection and is safe and effective in a marmot model of chronic HBV infection^[4].