Terzi Irene, Panagopoulos Periklis, Rafailidis Petros
University General Hospital of Alexandroupolis, Alexandroupolis, Greece.
Department of Medicine, Democritus University of Thrace, Alexandroupolis, Greece.
Infez Med. 2025 Jun 1;33(2):175-181. doi: 10.53854/liim-3302-3. eCollection 2025.
Carbapenem-resistant (CRAB) poses a critical global health threat, particularly among hospitalized and critically ill patients, due to its association with severe, difficult-to-treat infections. Its high resistance stems from genomic plasticity, biofilm formation, and environmental persistence, leading to limited treatment options and high mortality. Existing treatments often rely on sulbactam-based combinations, yet resistance continues to rise and new agents remain limited.
This review aims to highlight the therapeutic potential of zosurabalpin, a first-in-class lipopolysaccharide (LPS) transport inhibitor with selective activity against , by summarizing preclinical and early clinical data on its efficacy, mechanism of action, pharmacokinetics, and safety.
Peer-reviewed publications from PubMed and Scopus, clinical data from ClinicalTrials.gov, and relevant conference materials ECCMID and IDWeek.
Zosurabalpin inhibits the LptB-FGC complex, blocking LPS transport and causing lethal intracellular accumulation. Preclinical data demonstrate potent in vitro and in vivo activity against CRAB, with high selectivity and favorable pharmacokinetics. Phase 1 studies report good tolerability and a promising safety profile.Its novel mechanism makes zosurabalpin a strong candidate for treating CRAB.
With rising resistance and limited effective treatments, zosurabalpin offers a new, targeted therapeutic approach. Continued clinical development could help close a critical gap in the management of multidrug-resistant .
耐碳青霉烯类鲍曼不动杆菌（CRAB）对全球健康构成严重威胁，尤其在住院患者和重症患者中，因其与严重的、难以治疗的感染相关。其高耐药性源于基因组可塑性、生物膜形成和环境持久性，导致治疗选择有限且死亡率高。现有治疗方法通常依赖基于舒巴坦的联合用药，但耐药性仍在上升，新药物仍然有限。
本综述旨在通过总结关于佐苏巴平疗效、作用机制、药代动力学和安全性的临床前和早期临床数据，突出其作为首个对[具体对象]具有选择性活性的脂多糖（LPS）转运抑制剂的治疗潜力。
来自PubMed和Scopus的同行评审出版物、ClinicalTrials.gov的临床数据以及相关会议资料ECCMID和IDWeek。
佐苏巴平抑制LptB-FGC复合物，阻断LPS转运并导致致命的细胞内积累。临床前数据表明其对CRAB具有强大的体外和体内活性，具有高选择性和良好的药代动力学。1期研究报告了良好的耐受性和有前景的安全性。其新颖机制使佐苏巴平成为治疗CRAB的有力候选药物。
随着耐药性上升和有效治疗方法有限，佐苏巴平提供了一种新的、有针对性的治疗方法。持续的临床开发可能有助于填补多重耐药菌管理方面的关键空白。
