Abstract
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.
Keywords: Ethionamide, ETH-SO, EthA, EthR, ETH-NAD, metabolism, tuberculosis, mycobacterium tuberculosis, multidrug resistance
Current Drug Metabolism
Title:Metabolism of the Antituberculosis Drug Ethionamide
Volume: 14 Issue: 1
Author(s): Nuno Vale, Paula Gomes and Helder A. Santos
Affiliation:
Keywords: Ethionamide, ETH-SO, EthA, EthR, ETH-NAD, metabolism, tuberculosis, mycobacterium tuberculosis, multidrug resistance
Abstract: 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.
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Cite this article as:
Vale Nuno, Gomes Paula and A. Santos Helder, Metabolism of the Antituberculosis Drug Ethionamide, Current Drug Metabolism 2013; 14 (1) . https://dx.doi.org/10.2174/1389200211309010151
DOI https://dx.doi.org/10.2174/1389200211309010151 |
Print ISSN 1389-2002 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5453 |
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