Drug resistance which is at present the main impendence to global tuberculosis (TB) control and drug- resistant (DR) activity of Mycobacterium tuberculosis in various strains have become the major challenge worldwide. Nowadays, many researchers use different antibiotics for treatment of DR-TB which are often not well tolerated and not adequately efficient. A large group study from various research published in different time described a treatment regimen for multidrug-resistant tuberculosis (MDR-TB) including Clofazimine (CFZ) as high incidence against MDR-TB; whereas the therapeutic ways are still limited, the main strategy for treatment of DR-TB is to repurpose existing anti- mycobacterial agents. CFZ is one such drug that has recently devoted interest against DR-TB. CFZ is a fat-soluble riminophenazine dye used in the treatment of TB, HIV, and leprosy co-infected people worldwide. Clofazimine has shown action against MDR TB and which is now recommended by the WHO to treat drug resistant tuberculosis as a therapeutic agent with “unclear efficacy”. Although the mode of action and molecular mechanism of CFZ are not yet entirely understood, it has been exposed that outer membrane is its primary action site, an extensive number of mutant resistant to clofazimine and found mutations in rv0678 to be the most prominent mechanism of clofazimine resistance and the respiratory chain and ion transporters are the putative targets. This study discussed the comprehensive report, action and molecular reactivity of CFZ, and provides new acuteness into the clinical conduct of this drug. Key words: Clofazimine, background, mode of action, molecular mechanism.
