TY - JOUR T1 - Metabolism and hepatotoxicity of pyrazinamide, an anti-tuberculosis drug JF - Drug Metabolism and Disposition JO - Drug Metab Dispos DO - 10.1124/dmd.121.000389 SP - DMD-MR-2021-000389 AU - Zahir Hussain AU - Junjie Zhu AU - Xiaochao Ma Y1 - 2021/01/01 UR - http://dmd.aspetjournals.org/content/early/2021/06/01/dmd.121.000389.abstract N2 - Pyrazinamide (PZA) is an important component of a standard combination therapy against tuberculosis. However, PZA is hepatotoxic and the underlying mechanisms are poorly understood. Biotransformation of PZA in the liver was primarily suggested behind its hepatoxicity. This review summarizes the knowledge of the key enzymes involved in PZA metabolism and discusses their contributions to PZA hepatotoxicity. Significance Statement This review outlines the current understanding of PZA metabolism and hepatotoxicity. This work also highlights the gaps in this field, which can be used to guide the future studies on PZA-induced liver injury. ER -