Skip to main content
. 2021 Apr 21;13(5):592. doi: 10.3390/pharmaceutics13050592

Table 1.

TB drugs in clinical trials [101].

Chemical Class Compound Progress Mode of Action Reference(s)
Fluoroquinolone Levofloxacin Phase 2 DNA gyrase inhibitor [102,103]
Rifamycin Rifampicin (high dose) Phase 2 RpoB inhibitor [37]
Oxazolidinone Delpazolid Phase 2 Inhibition of protein synthesis [104,105]
Sutezolid Phase 2 Inhibition of protein synthesis [47]
TBI-223 Phase 1 Inhibits the binding of N-formylmethionyl tRNA to ribosome [106]
Nitroimidazole Delamanid Phase 3—approved Inhibits cell wall synthesis [107]
Pretomanid Phase 3—approved Inhibits cell wall synthesis [108]
Diarylquinoline Bedaquiline Phase 3—accepted Inhibits mycobacterial ATP synthase [109]
TBAJ-587 Preclinical trial Inhibits mycobacterial ATP synthase and hERG potassium channel [110]
TBAJ-876 Preclinical trial Inhibits mycobacterial ATP synthase [73,111]
Benzothiazinone Macozinone Phase 2 DprE1 inhibitor [112,113]
BTZ-043 Phase 1 DprE1 inhibitor [74]
Other classes Telacebec (imidazopyridine) Phase 2 QcrB inhibitor [84]
Nitazoxanide (nitrothiazolyl-salicylamide derivate) Phase 2 Disruption of membrane potential and pH homeostasis [114,115]
SQ109 (ethylenediamine) Phase 2 MmpL3 inhibitor [37,94]
TBA-7371 (1,4-azaindole) Phase 2 DprE1 inhibitor [116]
OPC-167832 (3,4-dihydrocarbostyril derivate) Phase 2 DprE1 inhibitor [117]
SPR-720 (ethyl urea benzimidazole) Phase 1 GyrB inhibitor [98]
TBI-166 (riminophenazine) Phase 1 Membrane destabilization [99]
Sanfetrinem (beta-lactam) Preclinical trial Inhibits peptidoglycan synthesis [118]
Spectinamide-1810 (spectinamide) Preclinical trial Selective ribosomal inhibition [100]