| Description | Taniborbactam is a reversible and selective boronic acid-containing pan-spectrum β-lactamase inhibitor (IC50s: 8-530 nM). Taniborbactam has IC50s of 30 nM, 32 nM, 42 nM, 20 nM for KPC-2, AmpC, OXA-48, and VIM-2. |
| In vitro | Both cefepime/Taniborbactam (10 μg/mL) and meropenem/Taniborbactam combinations are highly active against all six of the NDM-1-producing clinical isolates from K.pneumoniae and E.coli (MIC: ranges of 16-0.25 and 1-0.125 μg/mL, respectively). Taniborbactam has IC50s of 0.5 nM, 2 nM, 0.5 nM, 0.06 nM for KPC-2, OXA-48, VIM-4 of K.pneumoniae strain and VIM-2 of P.aeruginosa strain [1][2]. |
| In vivo | Taniborbactam has a T1/2 of 0.16 hours, a CL of 618 mL/h/kg, and a Vss of 143 mL/kg for mice. Combination of Cefepime (16 mg/kg) and Taniborbactam (16 mg/kg; s.c.; twice-a-day for 7 days) shows >2 log10 reductions in viable bacterial counts in the kidney of the ascending urinary tract infection model against a CTX-M-15-producing strain of E.coli. A single dose of cefepime (32 mg/kg)/Taniborbactam (16 mg/kg; s.c.) achieves >4 log10 reductions in viable bacterial counts in the neutropenic mouse lung infection model against a CTX-M-14-producing strain of K.pneumoniae [2]. |
| Synonyms | VNRX-5133 |
| molecular weight | 389.25 |
| Molecular formula | C19H28BN3O5 |
| CAS | 1613267-49-4 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| References | 1. Krajnc A, et al. Bicyclic Boronate VNRX-5133 Inhibits Metallo- and Serine-β-Lactamases. J Med Chem. 2019 Sep 26;62(18):8544-8556. 2. Liu B ,et al. Discovery of Taniborbactam (VNRX-5133): A Broad-Spectrum Serine- and Metallo-β-lactamase Inhibitor for Carbapenem-Resistant Bacterial Infections. J Med Chem. 2019 Dec 16. |