• Molecular NameTenofovir
  • SynonymD,L-Tenofovir; PMPA; TDF; Tenofovir disoproxil; Tenofovir disoproxil fumarate
  • Weight287.216
  • Drugbank_IDDB00300
  • ACS_NO147127-20-6
  • Show 2D model
  • LogP (experiment)N/A
  • LogP (predicted, AB/LogP v2.0)-1.62
  • pka3.75
  • LogD (pH=7, predicted)-6.02
  • Solubility (experiment)13.4 mg/ml
  • LogS (predicted, ACD/Labs)(ph=7)0.54
  • LogSw (predicted, AB/LogsW2.0)3.74
  • Sw (mg/ml) (predicted, ACD/Labs)3.15
  • No.of HBond Donors4
  • No.of HBond Acceptors9
  • No.of Rotatable Bonds5
  • TPSA146.19
  • StatusFDA approved
  • AdministrationN/A
  • PharmacologyA class of antiretroviral drugs known as nucleotide analogue reverse transcriptase inhibitors (nRTIs), which block reverse transcriptase, an enzyme crucial to viral production in HIV-infected people.
  • Absorption_valueN/A
  • Absorption (description)The oral bioavailability in fasted patients is approximately 25%. Administration of food (high fat meal containing 40 to 50% fat) increases the oral bioavailability, with an increase in the AUC of approximately 40%.
  • Caco_2N/A
  • Bioavailability25.0
  • Protein binding4.0
  • Volume of distribution (VD)1.3 L/kg
  • Blood/Plasma Partitioning ratio (D_blood)N/A
  • MetabollsmNeither tenofovir disoproxil nor tenofovir are substrates of CYP450 enzymes.
  • Half life8.1 h (Longer apparent plasma t1/2 (17 hours) reported for steady-state oral dosing; this may reflect a longer duration of blood sampling; also, phosphorylated 'active' metabolite exhibits a longer intracellular t1/2 (60 hours.))
  • ExcretionRenal
  • Urinary Excretion82
  • Clerance2.6 ml/min/kg
  • ToxicityLimited clinical experience at doses higher than the therapeutic dose of tenofovir 300 mg is available. In Study 901 tenofovir disoproxil fumarate 600 mg was administered to 8 patients orally for 28 days. No severe adverse reactions were reported. The effects of higher doses are not known.
  • LD50 (rat)N/A
  • LD50 (mouse)N/A