- Molecular NameEnfuvirtide
- SynonymEnfuvirtide; Envelope polyprotein GP160 precursor [Contains: Exterior membrane glycoprotein; GP120; Transmembrane glycoprotein; GP41]
- Weight4491.94
- Drugbank_IDDB00109
- ACS_NO159519-65-0
- Show 3D model
- LogP (experiment)N/A
- LogP (predicted, AB/LogP v2.0)N/A
- pka4.30
- LogD (pH=7, predicted)N/A
- Solubility (experiment)N/A
- LogS (predicted, ACD/Labs)(ph=7)N/A
- LogSw (predicted, AB/LogsW2.0)N/A
- Sw (mg/ml) (predicted, ACD/Labs)N/A
- No.of HBond DonorsN/A
- No.of HBond AcceptorsN/A
- No.of Rotatable BondsN/A
- TPSAN/A
- StatusFDA approved
- AdministrationSubcutaneous
- PharmacologyAn HIV fusion inhibitor, the first of a novel class of antiretroviral drugs used in combination therapy for the treatment of HIV-1 infection.
- Absorption_valueN/A
- Absorption (description)N/A
- Caco_2N/A
- BioavailabilityN/A
- Protein binding92.0
- Volume of distribution (VD)N/A
- Blood/Plasma Partitioning ratio (D_blood)N/A
- MetabollsmAs a peptide, enfuvirtide is expected to undergo catabolism to its constituent amino acids, with subsequent recycling of the amino acids in the body pool. Mass balance studies to determine elimination pathway(s) of enfuvirtide have not been performed in humans. In vitro studies with human microsomes and hepatocytes indicate that enfuvirtide undergoes hydrolysis to form a deamidated metabolite at the C-terminal phenylalanine residue, M3. The hydrolysis reaction is not NADPH dependent. The M3 metabolite is detected in human plasma following administration of enfuvirtide, with an AUC ranging from 2.4% to 15% of the enfuvirtide AUC.
- Half life3.8 h
- ExcretionN/A
- Urinary ExcretionN/A
- CleranceN/A
- ToxicityHepatic
- LD50 (rat)N/A
- LD50 (mouse)N/A