Tenofovir hydrate is a nucleotide reverse transcriptase inhibitor to treat HIV and chronic Hepatitis B. Tenofovir shows cytotoxic effects on cell viability in HK-2 cells, with IC50 values of 9.21 and 2.77 μM at 48 and 72 h in MTT assay, respectively. Tenofovir diminishes ATP levels in HK-2 cells. Tenofovir (3.0 to 28.8 μM) increases oxidative stress and protein carbonylation in HK-2 cells. Furthermore, Tenofovir induces apoptosis in HK-2 cells, and that apoptosis is induced via mitochondrial damage.
|Solubility (25°C)||DMSO 5 mg/mL|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
 Victoria Pilkington, et al. AIDS. Tenofovir alafenamide vs. tenofovir disoproxil fumarate: an updated meta-analysis of 14 894 patients across 14 trials
 Cheng-Hao Tseng, et al. Lancet Gastroenterol Hepatol. Hepatocellular carcinoma incidence with tenofovir versus entecavir in chronic hepatitis B: a systematic review and meta-analysis
 James Riddell 4th, et al. JAMA. HIV Preexposure Prophylaxis: A Review
 Blandine Aloy, et al. AIDS Rev. Is Tenofovir Alafenamide Safer than Tenofovir Disoproxil Fumarate for the Kidneys?
 Erik De Clercq. Biochem Pharmacol. Tenofovir alafenamide (TAF) as the successor of tenofovir disoproxil fumarate (TDF)
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