VNRX-5133

VNRX-5133 是 β-内酰胺酶抑制剂。VNRX-5133 对丝氨酸活性位点 β-内酰胺酶 (Ser-BL) 和金属-β-内酰胺酶 (MBL) 具有直接抑制活性。VNRX-5133 对多药耐药的肺炎克雷伯菌 (K. pneumonia) 和绿脓杆菌 (P. aeruginosa) 临床分离株具有高活性。

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250mg

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500mg

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Background

VNRX-5133 is a cyclic boronate β-lactamase inhibitor. VNRX-5133 has direct inhibitory activity against serine-active site β-lactamases (Ser-BL) and metallo-β-lactamases (MBL). VNRX-5133 is highly active against multidrug-resistant (MDR)-K. pneumonia and P. aeruginosa clinical isolates[1]. β-lactamase[1]

VNRX-5133 is a potent β-lactamase inhibitor (BLI) possessing a unique broad spectrum of activity, including Class A, C, and D Ser-BLs. VNRX-5133 enhances the activity of Cefepime against resistant Enterobacteriaceae and P. aeruginosa isolates in a neutropenic mouse-thigh infection model[1].

[1]. Denis Daigle, PhD, et al. 1370. Cefepime/VNRX-5133 Broad-Spectrum Activity Is Maintained Against Emerging KPC- and PDC-Variants in Multidrug-Resistant K. pneumonia and P. aeruginosa. Open Forum Infect Dis. 2018 Nov; 5(Suppl 1): S419-S420.