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] |