- Molecular NameClofazimine
- SynonymChlofazimine; Clofazimina [INN-Spanish]; Clofaziminum [INN-Latin]
- Weight473.407
- Drugbank_IDDB00845
- ACS_NO2030-63-9
- Show 2D model
- LogP (experiment)7.48
- LogP (predicted, AB/LogP v2.0)7.59
- pka8.5
- LogD (pH=7, predicted)5.97
- Solubility (experiment)0.00075 mg/ml
- LogS (predicted, ACD/Labs)(ph=7)-5.5
- LogSw (predicted, AB/LogsW2.0)0.0
- Sw (mg/ml) (predicted, ACD/Labs)0.0
- No.of HBond Donors1
- No.of HBond Acceptors4
- No.of Rotatable Bonds4
- TPSA39.99
- StatusFDA approved
- AdministrationN/A
- PharmacologyA fat-soluble riminophenazine dye used in combination with rifampicin and dapsone as multidrug therapy (MDT) for the treatment of leprosy. It has been used investigationally in combination with other antimycobacterial drugs to treat Mycobacterium avium infections in AIDS patients and Mycobacterium avium paratuberculosis infection in Crohn's disease patients.
- Absorption_valueN/A
- Absorption (description)Incompletely absorbed after oral administration.
- Caco_2N/A
- Bioavailability57.0
- Protein bindingN/A
- Volume of distribution (VD)N/A
- Blood/Plasma Partitioning ratio (D_blood)N/A
- MetabollsmAutopsies performed on clofazimine patients have found crystallized clofazimine in the intestinal mucosa, liver, spleen, and lymph nodes.
- Half life10 days following a single dose, 70 days after long-term, high-dose therapy.
- ExcretionIt is stored in body tissues and only very slowly excreted in the urine. 3-(p-Hydroxy)clofazimine and a 3-glucuronide conjugate have been detected in the urine, each accounting for less than 0.5% of a daily dose.
- Urinary ExcretionN/A
- CleranceN/A
- ToxicitySevere abdominal symptoms have necessitated exploratory laparotomies in some patients on clofazimine therapy. Rare reports have included splenic infarction, bowel obstruction, and gastrointestinal bleeding. Deaths have been reported, following severe abdominal symptoms.
- LD50 (rat)N/A
- LD50 (mouse)LD50 = > 4 g/kg.