molecules of the month


penicillin-binding protein + _-lactamase inh.

preclin. eff. at 50 mpk SC, 2,000 mpk tolerated

multitarget SBDD + opt. for porin permeability


Entasis Therapeutics

Chemical structure of molecule ETX0462
3 mins read

The Entasis broad-spectrum antibiotic, ETX0462, is both an inhibitor of penicillin-binding proteins (PBPs, the target of beta-lactams) and a beta-lactamase inhibitor (BLI). Reviewer Mike Koehler thought this was a substantial disclosure. “A number of BLIs co-formulated with carbapenems and monobactams are currently on the market. There are a number of downsides to co-formulation, not the least of which is that you have to match the PK of the BLI and your beta-lactam in order to be most effective. The diazabicyclooctane (DBO) class includes avibactam, a component of AvyCaz, one of our better options for bacterial infections. Less known is the fact that DBOs can act as single agent antibiotics as well. This stems from the fact that they can inhibit penicillin-binding proteins (PBPs).…

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