Abandeh Foad I, Drew Mark E, Sopirala Madhuri M
Division of Infectious Diseases, Department of Medicine, The Ohio State University Medical Center, Columbus, Ohio, USA.
Recent Pat Antiinfect Drug Discov. 2012 Apr;7(1):19-27. doi: 10.2174/157489112799829675.
Multidrug resistant gram-negative bacteria are an increasing therapeutic challenge. The beta-lactamases are a group of enzymes that confer resistance to the beta-lactam antibiotics. The carbapenems have been in wide use to treat beta-lactamase producing, multidrug resistant gram-negative bacterial infections. However, the emergence of carbapenemases, enzymes capable of hydrolyzing the carbapenems, has limited our therapeutic options. In the recent years, there has been some development in the discovery of new agents such as boronic acid derivatives, ME1071 and Ca-EDTA that may enhance the activity of existing antibiotics, CTC-96 which reverses antibiotic resistance and polymyxin derivatives with decreased renal toxicity. While global efforts towards new drug development should continue, appropriate use of currently available antibiotics is equally important. In this review, we will discuss the general characteristics of carbapenemases, recent patents with drugs under development and current treatment options.
耐多药革兰氏阴性菌对治疗构成的挑战日益增加。β-内酰胺酶是一类使细菌对β-内酰胺类抗生素产生耐药性的酶。碳青霉烯类药物已被广泛用于治疗产β-内酰胺酶的耐多药革兰氏阴性菌感染。然而，能够水解碳青霉烯类药物的碳青霉烯酶的出现，限制了我们的治疗选择。近年来，在新型药物的研发方面取得了一些进展，例如可能增强现有抗生素活性的硼酸衍生物、ME1071和Ca-EDTA，具有逆转抗生素耐药性的CTC-96，以及肾毒性降低的多粘菌素衍生物。虽然全球在新药研发方面的努力应继续，但合理使用现有抗生素同样重要。在本综述中，我们将讨论碳青霉烯酶的一般特性、正在研发的药物的近期专利以及当前的治疗选择。
