The introduction of antibiotics for the treatment of tuberculosis (TB) represented a major advance in the fight against the disease. Drug treatment is fundamental for controlling TB, promoting the cure of the patients and breaking the chain of transmission, when the anti-tuberculosis drug regimen is followed completely and correctly. Currently, the therapy of tuberculosis is performed with first-line antituberculosis drugs and some second-line drugs. However, the increased incidence of multidrug-resistant tuberculosis strains, and the association of HIV infection for tuberculosis patients, increase the problems associated with the currently available treatment of TB. The development of new anti-tuberculosis drugs with new mechanisms of action that allows shorter treatments and more effective, less toxic, with fewer side effects, is urgently required. In this chapter, we describe the current treatment regimens for tuberculosis, together with a description of the major antituberculosis drugs, their toxicity properties and pharmacological, still presenting new substances which are in advanced stages of clinical phase.