Drug intelligence / Profile preview

clofazimine

Development stage
Approved
Lead developer
Novartis
Modality
Light/Condition-Responsive Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules
Administration
Oral
01

Overview

Clofazimine is a riminophenazine antimycobacterial agent primarily used in combination with other drugs to treat leprosy (Hansen's disease), especially the multibacillary and dapsone-resistant forms, as well as lepromatous leprosy complicated by erythema nodosum leprosum[1][2][5][7]. It is also being investigated for use in multidrug-resistant tuberculosis and has shown immunosuppressive effects that may be relevant for autoimmune diseases such as multiple sclerosis, rheumatoid arthritis, and type 1 diabetes[5][6]. Clofazimine acts mainly by interfering with mycobacterial cell membranes. Its mechanism involves competing with menaquinone at the bacterial electron transport chain enzyme NDH-2 (type 2 NADH dehydrogenase), leading to reduced ATP production and generation of reactive oxygen species that contribute to bactericidal activity[6][7][8]. Additionally, it destabilizes bacterial membranes through lysophospholipid accumulation. In humans, clofazimine exhibits anti-inflammatory properties by inhibiting T-lymphocyte activation—partly via antagonism of the potassium voltage-gated channel subfamily A member 3 (Kv1.3)[5][7]. **Developers:** Novartis

Brand names
Lamprene
Other names
riminophenazineCZM
02

Targets

NDH-2 (Type II NADH-quinone oxidoreductase)KCNA3 (Potassium voltage-gated channel subfamily A member 3)Neuraminidase

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