The historical classification (1993) of anti-tuberculosis drugs included three (I-III) lines that were subdivided into five groups (2006). The duration of treatment of drug-sensitive (DS) tuberculosis (TB) with first-line drugs is 6 – 12 months; of multidrug-resistant (MDR) TB and extensively drug-resistant (XDR) TB with second-line drugs, 18 months and longer. The Directly Observed Treatment Short course (DOTS) and DOTS-Plus therapies are measures of world TB control. Based on the need for more effective treatment of MDR and XDR TB, the classification of 2016 introduced six groups (A-C and D1-D3) in connection with the development of new anti-TB drugs. The present review presents first-line preparations and their new derivatives possessing activity against DS and drug-resistant (DR) M. tuberculosis strains.