Skip to main content
. 2017 Sep 26;8:689. doi: 10.3389/fphar.2017.00689

Table 2.

Classification of anti-tuberculosis (anti-TB) drugs according to the site of action and its respective mechanism of resistance.

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.