Tenofovir disoproxil fumarate is a nucleotide reverse transcriptase inhibitor employed in the treatment of HIV and chronic hepatitis B.

Tenofovir exhibits cytotoxic effects on cell viability in HK-2 cells with IC50 values of 9.21 and 2.77 μM at 48 and 72 hours in the MTT assay, respectively. It diminishes ATP levels, increases oxidative stress and protein carbonylation (3.0 to 28.8 μM), and induces apoptosis via mitochondrial damage in HK-2 cells. Tenofovir and M48U1, formulated in 0.25% HEC, inhibit the replication of both R5-tropic HIV-1 BaL and X4-tropic HIV-1 IIIb in activated PBMCs and various laboratory strains and patient-derived HIV-1 isolates, with the combined formulation exhibiting synergistic antiretroviral activity against R5-tropic HIV-1 BaL and showing no toxicity to PBMCs [1][2].

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