- Molecular NameIndinavir
- SynonymCompound J; Indinavir sulfate
- Weight613.803
- Drugbank_IDDB00224
- ACS_NO150378-17-9
- Show 3D model
- LogP (experiment)3.49
- LogP (predicted, AB/LogP v2.0)3.35
- pka3.7; 5.9
- LogD (pH=7, predicted)3.27
- Solubility (experiment)0.015 mg/ml
- LogS (predicted, ACD/Labs)(ph=7)-3.36
- LogSw (predicted, AB/LogsW2.0)0.04
- Sw (mg/ml) (predicted, ACD/Labs)0.26
- No.of HBond Donors4
- No.of HBond Acceptors9
- No.of Rotatable Bonds12
- TPSA118.03
- StatusFDA approved
- AdministrationN/A
- PharmacologyA protease inhibitor used as a component of highly active antiretroviral therapy (HAART) to treat HIV infection and AIDS.
- Absorption_valueN/A
- Absorption (description)Indinavir is rapidly absorbed after oral administration and peak plasma concentrations are reached within 0.8 h. Absorption is reduced when administration occurs with a high fat meal.
- Caco_2N/A
- Bioavailability65.0
- Protein binding60.0
- Volume of distribution (VD)195 L
- Blood/Plasma Partitioning ratio (D_blood)N/A
- MetabollsmThe drug is metabolised by oxidation by the CYP3A4 isoenzyme in the liver and also glucuronidation, para-hydroxylation, 3′-hydroxylation and N-depyridomethylation. Seven metabolites have been isolated and identified; minor product identified as a 2′,3′-trans-dihydroxyindan analogue.
- Half life1.8 h; 0.77 h (children).
- ExcretionLess than 20% of the absorbed dose is excreted in urine, with about half being the unchanged drug. The rest is excreted in faeces.
- Urinary ExcretionN/A
- Clerance110 L/h
- ToxicityIn a study of 11 children undergoing treatment with 500 mg/m2 indinavir every 8 h (with stavudine or lamivudine), toxicity was observed as renal side effects ranging from mild to severe. This included kidney stones, renal cholic and acute renal failure (serum creatinine level greater than 5 mg/L above the base-line) [G. Gatti et al.,Antimicrob. Agents Chemother.,2000, 44(3), 752–755].
- LD50 (rat)N/A
- LD50 (mouse)N/A