ATC Group: J04AK Other drugs for treatment of tuberculosis

Bedaquiline is a diarylquinoline. Bedaquiline specifically inhibits mycobacterial ATP (adenosine 5'-triphosphate) synthase, an essential enzyme for the generation of energy in Mycobacterium tuberculosis. The inhibition of ATP synthase leads to bactericidal effects for both replicating and non-replicating tubercle bacilli.

The pharmacological mode of action of delamanid involves inhibition of the synthesis of the mycobacterial cell wall components, methoxy-mycolic and keto-mycolic acid. The identified metabolites of delamanid do not show anti-mycobacterial activity.

Ethambutol is bacteriostatic. It is effective against Mycobacterium tuberculosi and M.bovis with an MIC of 0.5–8µg per ml. The exact mechanism of action is unknown. While it has activity against some atypical mycobacteria including M.Kansasii, activity against other micro-organisms has not yet been reported.

The mechanism of action of pretomanid is thought to involve inhibition of the synthesis of cell wall lipids under aerobic conditions and generation of reactive nitrogen species under anaerobic conditions. Reductive activation of pretomanid by a mycobacterial deazaflavin (F420)-dependent nitro-reductase is required for activity under both aerobic and anaerobic conditions.

Pyrazinamide exhibits tuberculostatic activity. Pyrazinamide is active only at an acid pH, and it is therefore active mainly on the tubercle bacilli located within the cell.