molecules of the month


oral serine _-lactamase inh. prodrug

restores ceftibuten activity in model, Ph. I

hydrolysis transition state mimetic

Journal of Medicinal Chemistry

Venatorx Pharmaceuticals, Malvern, US

1 min read

11. The Venatorx serine _-lactamase inhibitor VNRX-7145 is an orally bioavailable prodrug of the boronic acid-containing inhibitor VNRX-5236, and is currently in Ph. I. It demonstrates activity in vitro and in vivo covering Enterobacterales expressing key class A or D carbapenemases or class C cephalosporinases. In preclinical studies, the inhibitor VNRX-7145 restored ceftibuten activity in a mouse model of UTI due to ESBL- and KPC-carbapenemase-producing strains of E. coli and K. pneumoniae. A related molecule, QPX7728, was covered in Apr. 2020.

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