Both isoniazid (INH) and rifampicin (RIF) are widely used drugs in antituberculosis therapy recommended by World Health Organization (WHO) and the main reason of acute drug-induced liver injury in China. INH and RIF has been known to be hepatotoxic but the mechanism of Isoniazid- and rifampicin- induced hepatotoxicity and the interaction between INH and RIF is still not entirely clear. The present study summaries the incidence,Pathology and Clinical characteristic of soniazid- and rifampicin- induced hepatotoxicity, illustrates metabolism process and hepatotoxicity mechanism of the two First-line antitubercular drugs, provides theoretical basis for clinical drugs’ rational use.