Table 2.
Promising new β-lactams or β-lactamase inhibitors in preclinical development
| β-Lactamase Inhibitor Name | Partner β-Lactam | Company | Type of β-Lactamase Inhibitor |
|---|---|---|---|
| FPI-1465 | Aztreonam or ceftazidime | Fedora | DBO (also inhibits PBP activity) |
| WCK 4234 | Meropenem | Wockhardt, Ltd | DBO |
| WO2013/030735 | Not necessary? | Wockhardt, Ltd | DBO (also inhibits PBP activity) |
| WCK 5153 | Not necessary? | Wockhardt, Ltd | DBO (also inhibits PBP activity) |
| Benzo(b)thiophene-2-boronic acid | Ceftazidime | Therabor and Regents of the University of California | Boronate |
| Sulfonamide boronates (CR161, compound 4, and compound 9) | Ceftazidime or cefotaxime | Therabor and Regents of the University of California | Boronate |
| S02030 | Cefepime | Case Western Reserve University and Università degli Studi di Modena e Reggio Emilia | Boronate |
| 3,4-dihydro-2H-benzo[e][1,2] oxaborinine-8-carboxylic acids | Ceftazidime or meropenem | VenatoRx Pharmaceuticals | Boronate |
| α-Aminoboronic acids | Ceftazidime | VenatoRx Pharmaceuticals | Boronate |
| 3,4-Dihydro-2H-benzo[e][1,2] oxaborinine-8-carboxylic acids | Carbapenem | Rempex Pharmaceuticals (The Medicines Company) | Boronate |
| AA101 | Cefepime | Allecra Therapeutics | Sulfone |
| Sulfone derivatives | Meropenem or imipenem | Orchid Pharmaceuticals | Sulfone |
| Sulfone derivatives | Meropenem or imipenem | Dr John D. Buynak (Southern Methodist University) | Sulfone |
| Clavam derivatives | Ceftazidime | Nabriva Therapeutics | Clavam |
| MG96077 | Imipenem | Mirati Therapeutics | Phosphonate |
| BAL30072 | Meropenem or no β-lactam required | Basilea Pharmaceuticals | Siderophore monobactam |
| BAL30376 (BAL19764, BAL29880, & clavulanic acid) | No β-lactam required | Basilea Pharmaceuticals | Siderophore monobactam, bridged monobactam, and a clavam |
| MK-8712 | Imipenem | Merck Sharp & Dohme Corporation | Bridged monobactam |
| Siderophore monobactams | Aztreonam or meropenem | Pfizer | Siderophore monobactam |
| Syn2190 | Ceftazidime | Taiho Pharmaceuticals Co | Siderophore monobactam |
| 3′-Thiobenzoyl cephalosporins | Meropenem | University of Waterloo, Wilfrid Laurier University | β-Lactam |
| FSI-1686 and FSI-1671 | No β-lactam required | FOB Synthesis Inc | β-Lactam |
| BTZs | Imipenem | Universidad de la República, Montevideo, Uruguay | Bisthiazolidine |
| ME1071 | Ceftazidime or biapenem | Meiji Seika Kaisha Ltd | Maleic acid derivative |