- Molecular NameHalofantrine
- SynonymHalofantrina [INN-Spanish]; Halofantrine [Usan]; Halofantrinum [INN-Latin]
- Weight500.432
- Drugbank_IDDB01218
- ACS_NO69756-53-2
- Show 2D model
- LogP (experiment)N/A
- LogP (predicted, AB/LogP v2.0)7.43
- pkaN/A
- LogD (pH=7, predicted)4.93
- Solubility (experiment)N/A
- LogS (predicted, ACD/Labs)(ph=7)-5.59
- LogSw (predicted, AB/LogsW2.0)0.0
- Sw (mg/ml) (predicted, ACD/Labs)0.0
- No.of HBond Donors1
- No.of HBond Acceptors2
- No.of Rotatable Bonds11
- TPSA23.47
- StatusFDA approved
- AdministrationN/A
- PharmacologyA drug used to treat malaria. Halofantrine's structure contains a substituted phenanthrene, and is related to the antimalarial drugs quinine and lumefantrine.
- Absorption_valueN/A
- Absorption (description)After oral administration, halofantrine is slowly and erratically absorbed and the drug enters systemic circulation within 1 h. The rate and extent of absorption are increased in the presence of food.
- Caco_2N/A
- Bioavailability6.3
- Protein binding65.0
- Volume of distribution (VD)73 L/kg (patients with malaria); 8572 L (healthy individuals).
- Blood/Plasma Partitioning ratio (D_blood)N/A
- MetabollsmHepatic (CYP3A4-mediated). The major metabolite is N-desbutylhalofantrine which is active and has a longer half-life than halofantrine. Peak concentrations of the metabolite are observed after 12 to 20 h and are 2 to 4 times lower than the drug levels.
- Half life38 h in healthy volunteers and 91~113 h in patients with malaria (halofantrine); 103 h in healthy individuals and 79 to 118 h in those with malaria (N-desbutylhalofantrine).
- ExcretionThe main route of elimination is in faeces as the unchanged drug.
- Urinary ExcretionN/A
- Clerance0.58 L/h/kg
- ToxicitySide effects incldue coughing noisy, rattling, troubled breathing, loss of appetite, aches and pain in joints, indigestion,and skin itching or rash.
- LD50 (rat)N/A
- LD50 (mouse)N/A