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] |