posted on 2018-10-08, 00:00authored byEric M. Gordon, Matthew A. J. Duncton, Mark A. Gallop
Only one FDA-approved
β-lactamase inhibitor has ever been
orally available: clavulanic acid, approved in 1984. Avibactam, approved
by FDA in 2015, is the first of a new class of BLIs called diazabicyclooctanes,
or “DBOs”. This class has much broader coverage than
clavulanic acid but can only be administered by intravenous injection.
Herein, we describe the synthesis and testing of the first approved
BLI to be rendered orally bioavailable since clavulanic acid (1984).