Table 6 β-Lactam/β-lactamase inhibitor (BL/BLI) combinations in clinical trials or submitted for regulatory approval (structures in Figs. 11–13)
From: Antibiotics in the clinical pipeline as of December 2022
Name (synonym)a | Compound (lead source) | Administration; indication (developer) |
|---|---|---|
NDA/MAA | ||
durlobactam (ETX2514) (60) + sulbactam (61) | DBO BLI (S)b + clavulanic acid (NP) | IV; MDR Acinetobacter infections (Innoviva) |
Phase-III | ||
taniborbactam (62) (VNRX-5133) + cefepime (41) | bicyclic boronate BLI (S) + cephalosporin (NP) | IV; cUTI (VenatoRx Pharmaceuticals) |
enmetazobactam (63) (AAI 101) + cefepime (41) | clavulanic acid (NP) + cephalosporin (NP) | IV; UTI (Allecra Therapeutics) |
zidebactam (64) + cefepime (41) | DBO BLI (S)b & PBP2 + cephalosporin (NP) | IV; G-ve (Wockhardt) |
Phase-I | ||
nacubactam (65) (OP0595) + meropenem (66) | DBO BLI (S)b + carbapenem (NP) | IV; G-ve (NacuGen Therapeutics) |
xeruborbactam (67) (QPX7728) + QPX2014cQPX7831 (68) (prodrug) + QPX2015c | bicyclic boronate BLI (S) + BL (NP) | IV/pod; G-ve (Qpex Biopharma) |
ETX0282 (69) (prodrug) + cefpodoxime proxetil (70) (prodrug); ETX1317 (71) + cefpodoxime (72) | DBO BLI (S)b + cephalosporin (NP) | po; G-ve, UTI (Innoviva/CARB-X) |
ledaborbactam etzadroxil (73) (prodrug, VNRX-7145) + ceftibuten (74); ledaborbactam (75) | bicyclic boronate BLI (S) + cephalosporin (NP) | po; G-ve (VenatoRx Pharmaceuticals) |
funobactam (XNW-4107) (76) + imipenem (77) + cilastatin (78) | DBO BLI (S) + carbapenem (NP) | IV; G-ve (Sinovent/Evopoint Biosciences) |
PF-07612577 (CTB + AVP) [AVP (79) (prodrug, PF-07338233, ARX-006, ARX-1796) + ceftibuten (74) (PF-06264006)] | avibactam (80) DBO prodrug (S) + cephalosporin (NP) | po; G-ve (Pfizer) |
