Delamanid

Delamanid is a small-molecule antibiotic in the nitro-dihydro-imidazooxazole class developed specifically to treat multidrug-resistant (MDR) and extensively drug-resistant (XDR) tuberculosis. It operates as a prodrug which, upon activation by the mycobacterial enzyme deazaflavin-dependent nitroreductase (Ddn), inhibits the synthesis of methoxy- and keto-mycolic acid, key components of the mycobacterial cell wall. Delamanid is approved under the brand name Deltyba and is distinguished by its role in modern MDR-TB regimens, where it is often combined with other agents such as bedaquiline, linezolid, and fluoroquinolones. Its use is limited by safety concerns (notably QT prolongation), the potential for emergent resistance, and the need for combination therapy with other drugs due to TB’s propensity for resistance development[1][2][3][4][5][6][7][9]. For research on the actual molecular target of delamanid, refer to “deazaflavin-dependent nitroreductase” (Ddn), a mycobacterial enzyme responsible for delamanid’s bioactivation and inhibition of mycolic acid synthesis[3][4][6][9].

Other names

DeltybaOPC-67683

Delamanid is activated by mycobacterial deazaflavin-dependent nitroreductase (Ddn) using the reduced F420 cofactor and inhibits the synthesis of methoxy and keto-mycolic acids, disrupting mycobacterial cell wall formation[3][4][6][9]. Its selectivity for mycobacteria is due to bioactivation restricted to bacterial enzymes, not host enzymes[9].