- Molecular NameEfavirenz
- Synonymefavirenz; EFV
- Weight315.678
- Drugbank_IDDB00625
- ACS_NO154598-52-4
- Show 3D model
- LogP (experiment)N/A
- LogP (predicted, AB/LogP v2.0)4.08
- pka10.2
- LogD (pH=7, predicted)4.08
- Solubility (experiment)N/A
- LogS (predicted, ACD/Labs)(ph=7)-5.78
- LogSw (predicted, AB/LogsW2.0)0.0
- Sw (mg/ml) (predicted, ACD/Labs)0.0
- No.of HBond Donors1
- No.of HBond Acceptors3
- No.of Rotatable Bonds3
- TPSA38.33
- StatusFDA approved
- AdministrationN/A
- PharmacologyA non-nucleoside reverse transcriptase inhibitor (NNRTI) and is used as part of highly active antiretroviral therapy (HAART) for the treatment of a human immunodeficiency virus (HIV) type 1.
- Absorption_valueN/A
- Absorption (description)N/A
- Caco_2N/A
- Bioavailability60.0
- Protein binding99.6
- Volume of distribution (VD)N/A
- Blood/Plasma Partitioning ratio (D_blood)N/A
- MetabollsmHepatic (CYP3A4 and CYP2B6-mediated). Efavirenz is metabolised by the cytochrome P450 system to hydroxylated metabolites, which can undergo subsequent glucuronidation to inactive metabolites.
- Half life52~76 h (single dose), and 40~55 h (multiple doses)
- Excretion14 to 34% of an administered dose can be recovered in urine as the metabolites and 16 to 61% in faeces as the parent drug. Efavirenz is known to cross the blood–brain barrier.
- Urinary Excretion<1
- Clerance3.1 ml/min/kg
- ToxicityA mild to moderate rash with blistering and shedding is the main toxicology effect. Two incidents have been noted, where two patients accidentally took a total dose of 1200 mg and showed an increase in nervous system symptoms and involuntary muscle contractions.
- LD50 (rat)N/A
- LD50 (mouse)N/A