Clofazimine

Clofazimine
Clinical data
ATC code	J04BA01 (WHO) ;
Pharmacokinetic data
Elimination half-life	70 days
Identifiers
	IUPAC name N,5-bis(4-chlorophenyl)-3- (1-methylethylimino)-5H-phenazin-2-amine;
CAS Number	2030-63-9;
PubChem CID	2794;
DrugBank	APRD00278;
E number	{{#property:P628}}
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Chemical and physical data
Formula	C27H22Cl2N4
Molar mass	473.396 g/mol

Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]

Overview

Clofazimine is a 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. Clofazimine also has a marked anti-inflammatory effect and is given to control the leprosy reaction, erythema nodosum leprosum (ENL).^[1]

US Brand Names

LAMPRENE^® (DISCONTINUED)

Historical Perspective

Clofazimine, initially known as B663, was first synthesised in 1954 by a team led by Dr Vincent Barry at Trinity College, Dublin as an anti-tuberculosis drug. The drug proved ineffective against tuberculosis but in 1959 a researcher named Chang identified its effectiveness against leprosy. After clinical trials in Nigeria and elsewhere during the 1960s, some sponsored by the Swiss pharmaceutical company Geigy (today member of the Novartis group of drug producers), the product was launched in 1969 as Lamprene.

The U.S. government named Clofazimine an orphan drug in June 1986. Geigy gained FDA approval for the drug in December 1986.

Supply

Clofazimine is marketed under the trade name Lamprene^® by Novartis. One of the only suppliers of Clofazimine Active Pharmaceutical Ingredient in the world is Sangrose Laboratories, located at Mavelikara in the southern Indian state of Kerala.

Metabolism

Clofazimine has a very long half life of about 70 days. Clofazimine produces pink to brownish skin pigmentation in 75-100% of patients within a few weeks.

Mechanism of Action

Clofazimine exerts a slow bactericidal effect on Mycobacterium leprae. It inhibits mycobacterial growth and binds preferentially to mycobacterial DNA. It also exerts anti-inflammatory properties in controlling erythema nodosum leprosum reactions. However, its precise mechanisms of action are unknown.

External links

↑ LastName, FirstName (1992). Drug evaluations annual 1993. Chicago, Ill: American Medical Association. ISBN 0899704980.

[1] LastName, FirstName (1992). Drug evaluations annual 1993. Chicago, Ill: American Medical Association. ISBN 0899704980.

[1]