Tenofovir hydrate is a nucleotide reverse transcriptase inhibitor used in the treatment of HIV and chronic Hepatitis B.

Tenofovir demonstrates cytotoxic effects on HK-2 cell viability, with IC 50 values of 9.21 μM at 48 h and 2.77 μM at 72 h in an MTT assay, respectively. It also reduces ATP levels and induces oxidative stress and protein carbonylation within these cells, in concentrations ranging from 3.0 to 28.8 μM. Moreover, tenofovir triggers apoptosis through mitochondrial damage in HK-2 cells. Additionally, tenofovir, alongside M48U1 in a 0.25% HEC formulation, effectively inhibits the replication of both R5-tropic HIV-1 BaL and X4-tropic HIV-1 IIIb in activated PBMCs, as well as several laboratory strains and patient-derived HIV-1 isolates. This combination achieves synergistic antiretroviral effects against R5-tropic HIV-1 BaL infection without causing toxicity to PBMCs.

Tenofovir Disoproxil fumarate (20, 50, 140, or 300 mg/kg) administered to BLT mice, displays dose dependent activity during vaginal HIV challenge in BLT humanized mice. Tenofovir Disoproxil fumarate (50, 140, 300 mg/kg) significantly decreases HIV transmission in BLT mice [3]. Tenofovir Disoproxil fumarate (0.5, 1.5, or 5.0 mg/kg/day, p.o.) induces a dose-dependent decline in serum viremia in woodchucks chronically infected with WHV. Tenofovir Disoproxil fumarate administration is safe and effective in the woodchuck model of chronic HBV infection [4].