Centro de Investigação em Química da Universidade do Porto, Department of Chemistry and Biochemistry, Faculty of Sciences, University of Porto, R. Campo Alegre, 687, P- 4169-007 Porto, Portugal.
Curr Drug Metab. 2013 Jan;14(1):151-8.
Ethionamide (ETH) is an important second-line antituberculosis drug used for the treatment of patients infected with multidrug-resistant Mycobacterium. Although ETH is a structural analogue of isoniazid (INH), both are pro-drugs that need to be activated by mycobacterial enzymes to exert their antimicrobial activity. ETH mechanism of action is thought to be identical to INH although the pathway of activation is distinct from that of INH. ETH is activated by an EthA enzyme, leading to the formation of an Soxide metabolite that has considerably better activity than the parent drug. This review comprehensively examines the aspects related with the metabolism of ETH since its discovery up to today.
乙硫异烟胺（ETH）是一种重要的二线抗结核药物，用于治疗感染耐多药分枝杆菌的患者。尽管乙硫异烟胺（ETH）是异烟肼（INH）的结构类似物，但两者都是前药，需要被分枝杆菌酶激活才能发挥其抗菌活性。尽管激活途径与异烟肼不同，但乙硫异烟胺的作用机制被认为与异烟肼相同。乙硫异烟胺由 EthA 酶激活，导致形成 S 氧化物代谢物，其活性比母体药物好得多。本综述全面考察了乙硫异烟胺自发现至今的代谢相关方面。
