Among the antitubercular agents, most are defined as “prodrugs” such as isoniazid and ethionamide. Adrien Albert was the first to introduce this term in 1958. Generally, prodrugs can be utilized for improving active drug solubility and bioavailability, increasing permeability and absorption, modifying the distribution profile, prevent fast metabolism and excretion and reducing toxicity. In the past, the prodrug approach was used as a last option after all other methods were spent. Nowadays, this strategy is considered in the early stages of the drug development process, thus providing novel targets for the rational design of more effective treatments for tuberculosis.
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