Table 2.
Drug classification | Groups | Anti-TB drugs | Mechanism of action | Target TB | Efficacy | Mechanism of resistance | References |
---|---|---|---|---|---|---|---|
Cell envelope synthesis inhibitor | Peptidoglycan | Cycloserine | Inhibit 2 enzymes forming D-alanine residues | MDR, XDR | High | Mutations in alrA | Patel et al., 2012 |
Terizidone | Cycloserine derivative | MDR, XDR | High | Non | Galietti et al., 1991 | ||
Arabinogalactan | Ethambutol | Inhibiting arabinosyltransferase, arabinose acceptor | Active | Low | embCAB operon | Telenti et al., 1997; Wolucka, 2008 | |
Mycolic acid | Isoniazid | Activation katG enzyme and inhibits inhA gene | Active, latent | High | Mutations in katG and inhA genes | Vilche‘ze and Jacobs, 2007; Riccardi et al., 2009 | |
Triclosan | Inhibits the inhA enzyme without activation katG | MDR | Low | – | Wang et al., 2004; Freundlich et al., 2009 | ||
Pyridomycin | Inhibits the inhA enzyme | MDR, XDR | High | Mutations in inha | Hartkoorn et al., 2012 | ||
Ethionamide | Inhibits InhA by enzyme ethA | MDR, XDR | High | Mutations in inha, etha | Wolff and Nguyen, 2012 | ||
Prothionamide | Inhibits InhA by enzyme ethA | MDR, XDR | High | Mutations in etha | Wang et al., 2007 | ||
Thiocarlide | Inhibiting synthesis of oleic acid | MDR, XDR | High | Mutations in ethA | Phetsuksiri et al., 2003 | ||
Delamanid | Releasing Nitric oxide by Ddn enzyme | Active, latent, MDR, XDR | High | Non | Gler et al., 2012; Zhang et al., 2013 | ||
SQ109 | Membrane transporter MmpL3 | Active, latent | High | Non | Owens et al., 2013 | ||
Protein synthesis inhibitor | Aminoglycosides | Streptomycin | Bind to 30S subunit of ribosome | MDR, XDR | High | Mutation in rpsl | Honort and Cole, 1994 |
Amikacin | Bind to 30S subunit of ribosome | MDR, XDR | High | Mutation in rrs | Sowajassatakul et al., 2014 | ||
Kanamycin | Bind to 30S subunit of ribosome | MDR, XDR | High | Mutation in rrs | Sowajassatakul et al., 2014 | ||
Oxazolidone | Linezolid | Bind to 50S subunit of ribosome | MDR, XDR | High | Mutation in G2576T(23S) | Scheetz et al., 2008 | |
Sutezolid | Bind to 50S subunit of ribosome | MDR, XDR | High | Non | Zumla et al., 2015 | ||
Peptidoglycan | Capreomycin | Peptidoglycan Breakdown | MDR, XDR | High | Mutation in tlyA | Chen et al., 2003 | |
Nucleic acid inhibitor | Rifamycins | Rifampicin | RNA polymerase inhibitor | Active, latent | Low | Mutations in rpoB gene | Sensi, 1983; Telenti et al., 1993 |
Rifapentine | RNA polymerase inhibitor (b-subunit) | Active, latent/HIV | High | Mutations in rpoB gene | Chan et al., 2014 | ||
Rifabutin | RNA polymerase inhibitor (b-subunit) | Active, latent/HIV | High | Mutations in rpoB gene | Yan et al., 2015 | ||
Rifalazil | RNA polymerase inhibitor (b-subunit) | Active, latent/HIV | High | Mutations in rpoB gene | Saribaş et al., 2003 | ||
PAS | PAS | Folic acid synth inhibitor | MDR, XDR | High | Mutations in thyA | Patel et al., 2012 | |
Quinolones | Levofloxacin | DNA gyrase inhibitor | MDR, XDR | High | Mutations in gyrA | Pranger et al., 2011 | |
Moxifloxacin | DNA gyrase inhibitor | MDR, XDR | High | Mutations in gyrA | Pranger et al., 2011 | ||
New drugs | Bedaquiline | Inhibiting ATP synthase enzyme | Active, MDR, dorment,XDR | High | Mutations in atpE gene | Chan et al., 2013; Chahine et al., 2014 | |
Pyrazinamide | Interferes with binding to mRNA | Active,MDR | High | Mutations in RpsA, pncA | Zhang et al., 2003; Shi et al., 2011 | ||
Clofazimine | Inhibits DNA replication | MDR, XDR/HIV | High | Mutations in rv0678 | Arbiser and Moschella, 1995 |
PAS:para-aminosalicylic acid.