Clofazimine

Clofazimine is an active phenazine composed of an imino group and aromatic tricyclic heterocycles that is used as an antimycobacterial, anti-inflammatory and anti-cancer compound. It has been shown to be a potent in vivo antimycobacterial agent toward Mycobacterium leprae and in vitro to Mycobacterium avium.

As an anti-inflammatory, clofazimine inhibits reactive oxygen species (ROS) formation within neutrophils by inhibiting myeloperoxidase catalyzed reactions. The formed ROS are responsible for activating tumor necrosis factor alpha (TNFα) and interleukin 8 (IL8), which are inflammatory cytokines.

Conversely, clofazimine has been shown to increase ROS production in phagocytes, enhancing cytotoxic effects of neutrophils. Clofazimine increased neutrophil in vitro efficacy against fast growing cancer cultures, but exhibited less activity toward slower growing cancers.

Clofazimine has been studied thoroughly, but its exact mechanism of action has not been elucidated. It has been shown to preferentially bind mycobacterial DNA, preventing bacterial replication and proliferation. Clofazimine has also been proposed to stimulate phospholipase A₂ activity, which inhibits potassium transport. Other studies have found data that suggests clofazimine disrupts bacterial membranes, similar to cationic peptides.

Product Specifications
Clofazimine
Lamprene
Lampren

Formula: C₂₇H₂₂Cl₂N₄

MW: 473.40 g/mol

Storage/Handling: Store at room temperature.

PubChem Chemical ID: 2794