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Pharmacokinetic/Pharmacodynamic Determination and Preclinical Pharmacokinetics of the β-Lactamase Inhibitor ETX1317 and Its Orally Available Prodrug ETX0282.
ACS Infectious Diseases ( IF 4.0 ) Pub Date : 2020-05-07 , DOI: 10.1021/acsinfecdis.0c00019 John O'Donnell 1 , Angela Tanudra 1 , April Chen 1 , Daniel Hines 1 , Ruben Tommasi 1 , John Mueller 1
ACS Infectious Diseases ( IF 4.0 ) Pub Date : 2020-05-07 , DOI: 10.1021/acsinfecdis.0c00019 John O'Donnell 1 , Angela Tanudra 1 , April Chen 1 , Daniel Hines 1 , Ruben Tommasi 1 , John Mueller 1
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Increasingly resistant Enterobacteriaceae have emerged as a health threat in both hospital and community settings. Infections of the urinary tract, once often treated with oral agents in the community, are requiring increased hospitalization and use of intravenously administered agents for effective treatment. These isolates often carry extended spectrum β-lactamases (ESBLs) and carbapenemases that necessitate the need for an inhibitor to cover a broad range of β-lactamases. ETX1317 is a novel diazabicyclooctane class serine β-lactamase inhibitor that restores the antibacterial activity of several classes of β-lactams, including third-generation cephalosporins such as cefpodoxime. ETX1317 is currently being developed as an orally available prodrug, ETX0282, to be administered with cefpodoxime proxetil (CPDP). The combination has demonstrated oral efficacy in murine models of infection. Pharmacokinetics established in preclinical species and pharmacokinetic/pharmacodynamic attributes suggest the orally administered combination ETX0282 + CPDP could serve as an effective treatment option against contemporary ESBL and carbapenemase-producing Enterobacteriaceae.
中文翻译：
β-内酰胺酶抑制剂 ETX1317 及其口服前药 ETX0282 的药代动力学/药效学测定和临床前药代动力学。
耐药性日益增强的肠杆菌科细菌已成为医院和社区环境中的健康威胁。泌尿道感染曾经在社区中经常使用口服药物治疗，但现在需要增加住院治疗和使用静脉注射药物才能有效治疗。这些分离株通常携带超广谱 β-内酰胺酶 (ESBL) 和碳青霉烯酶，因此需要抑制剂来覆盖广泛的 β-内酰胺酶。 ETX1317是一种新型二氮杂双环辛烷类丝氨酸β-内酰胺酶抑制剂，可恢复几类β-内酰胺的抗菌活性，包括第三代头孢菌素如头孢泊肟。 ETX1317 目前正在开发为口服前药 ETX0282，与头孢泊肟普塞酯 (CPDP) 一起给药。该组合已在小鼠感染模型中证明了口服功效。临床前物种建立的药代动力学和药代动力学/药效学属性表明，口服组合 ETX0282 + CPDP 可以作为针对当代 ESBL 和产碳青霉烯酶肠杆菌科细菌的有效治疗选择。
更新日期：2020-05-07
中文翻译：
β-内酰胺酶抑制剂 ETX1317 及其口服前药 ETX0282 的药代动力学/药效学测定和临床前药代动力学。
耐药性日益增强的肠杆菌科细菌已成为医院和社区环境中的健康威胁。泌尿道感染曾经在社区中经常使用口服药物治疗，但现在需要增加住院治疗和使用静脉注射药物才能有效治疗。这些分离株通常携带超广谱 β-内酰胺酶 (ESBL) 和碳青霉烯酶，因此需要抑制剂来覆盖广泛的 β-内酰胺酶。 ETX1317是一种新型二氮杂双环辛烷类丝氨酸β-内酰胺酶抑制剂，可恢复几类β-内酰胺的抗菌活性，包括第三代头孢菌素如头孢泊肟。 ETX1317 目前正在开发为口服前药 ETX0282，与头孢泊肟普塞酯 (CPDP) 一起给药。该组合已在小鼠感染模型中证明了口服功效。临床前物种建立的药代动力学和药代动力学/药效学属性表明，口服组合 ETX0282 + CPDP 可以作为针对当代 ESBL 和产碳青霉烯酶肠杆菌科细菌的有效治疗选择。
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