德拉马尼 (Deltyba)

概览

Delamanid is an antibiotic used to treat multidrug resistant tuberculosis.

作用机制

Delamanid is a prodrug that requires biotransformation via via the mycobacterial F420 coenzyme system, including the deazaflavin dependent nitroreductase (Rv3547), to mediate its antimycobacterial activity against both growing and nongrowing mycobacteria . Mutations in one of five coenzyme F420 genes, fgd, Rv3547, fbiA, fbiB, and fbiC has been proposed as the mechanism of resistance to delamanid . Upon activation, the radical intermediate formed between delamanid and desnitro-imidazooxazole derivative is thought to mediate antimycobacterial actions via inhibition of methoxy-mycolic and keto-mycolic acid synthesis, leading to depletion of mycobacterial cell wall components and destruction of the mycobacteria . Nitroimidazooxazole derivative is thought to generate reactive nitrogen species, including nitrogen oxide (NO). However unlike isoniazid, delamanid does not alpha-mycolic acid .

适应症

Indicated for use as part of an appropriate combination regimen for pulmonary multi-drug resistant tuberculosis (MDR-TB) in adult patients when an effective treatment regimen cannot otherwise be composed for reasons of resistance or tolerability .

• Pulmonary Multi-Drug Resistant Tuberculosis (MDR-TB)