Clofazimine: current status and future prospects.
Clofazimine, a lipophilic riminophenazine antibiotic, possesses both antimycobacterial and anti-inflammatory activities. However, its efficacy has been demonstrated only in the treatment of leprosy, not in human tuberculosis, despite the fact that this agent is impressively active in vitro against multidrug-resistant strains of Mycobacterium tuberculosis. Recent insights into novel targets and mechanisms of antimicrobial and anti-inflammatory activity coupled with the acquisition of innovative drug delivery technologies have, however, rekindled interest in clofazimine as a potential therapy for multidrug- and extensively multidrug-resistant tuberculosis in particular, as well as several autoimmune diseases. The primary objective of this review is to critically evaluate these recent developments and to assess their potential impact on improving the therapeutic efficacy and versatility of clofazimine.
Medical Research Council Unit for Inflammation and Immunity, Department of Immunology, Faculty of Health Sciences, University of Pretoria and Tshwane Academic Division of the National Health Laboratory Service, Pretoria, South Africa. moloko.cholo@mrc.ac.za
Moloko C
MC
Cholo
Helen C
HC
Steel
P B
PB
Fourie
Willem A
WA
Germishuizen
Ronald
R
Anderson
D000893:Anti-Inflammatory Agents / Q000737:chemistry / Q000627:therapeutic use*; D000995:Antitubercular Agents / Q000737:chemistry / Q000627:therapeutic use*; D002991:Clofazimine / Q000737:chemistry / Q000627:therapeutic use*; D024901:Drug Resistance, Multiple, Bacterial; D006801:Humans; D007918:Leprosy / Q000188:drug therapy*; D009169:Mycobacterium tuberculosis / Q000187:drug effects; D014376:Tuberculosis / Q000188:drug therapy*
D000893:Anti-Inflammatory Agents; D000995:Antitubercular Agents; D002991:Clofazimine