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. 2018 Jan 31;118(4):1887–1916. doi: 10.1021/acs.chemrev.7b00602

Table 1. Current TB Drugs Approved by the FDA/EMA.

  primary protein target mechanism of action pro-drug
First-Line TB Drugs, Primarily Used for Drug-Sensitive TB Treatment
isoniazid INH, H enoyl acyl-carrier protein reductase InhA inhibits mycolic acid synthesis activated by catalase-peroxidase-peroxynitritase (KatG) to form an adduct with NAD+/NADP+
rifampicin RIF, R RNA polymerase β subunit RpoB inhibits RNA synthesis/transcription N/Aa
pyrazinamide PZA, Z pleiotropic possible targets include FAS I, QAPRTase, RpsA, PanD, Rv2783 converted by pyrazinamidase (PZase) to pyrazinoic acid
ethambutol EMB, E arabinosyl transferase EmbB inhibits arabinogalactan synthesis N/A
Second-Line TB Drugs, Primarily Used for Drug-Resistant TB Treatment
streptomycin 16S rRNA subunit inhibits protein synthesis N/A
kanamycin amikacin capreomycin 30S rRNA subunit inhibit protein synthesis N/A
ofloxacin levofloxacin moxifloxacin DNA gyrase and topoisomerase inhibit DNA synthesis N/A
p-amino salicylic acid dihydrofolate reductase inhibits DNA precursor synthesis converted by dihydropteroate synthase (DHPS) and dihydrofolate synthase (DHFS) to an antifolate metabolite
ethionamide prothionamide enoyl acyl-carrier protein reductase InhA inhibit mycolic acid biosynthesis activated by a monooxygenase (EthA) to form an adduct with NAD+/NADP+
cycloserine alanine racemase and d-alanine:d-alanine ligase inhibits cell wall biosynthesis N/A
bedaquiline ATP synthase subunit ε inhibits ATP production N/A
delamanid pretomanid not specific generates NO and inhibits energy metabolism activated by a nitroreductase (Ddn)
a

N/A: not applicable.