Taniborbactam dihydrochloride (VNRX-5133 dihydrochloride) is a selective and potent novel cyclic boronic acid β-lactamase inhibitor with antimicrobial activity and significant inhibition of Gram-negative bacteria.Taniborbactam dihydrochloride inhibits KPC Taniborbactam dihydrochloride inhibits KPC-2, AmpC, OXA-48 and VIM-2 and can be used for the study of fungal infections.

Taniborbactam dihydrochloride (VNRX-5133 dihydrochloride) exhibits IC50 values of 0.5 nM, 2 nM, 0.5 nM, and 0.06 nM against KPC-2, OXA-48, VIM-4 strains of Klebsiella pneumoniae, and VIM-2 strain of Pseudomonas aeruginosa, respectively[1].The combination of Cefepime/Taniborbactam dihydrochloride (10 μg/mL) and Meropenem/Taniborbactam dihydrochloride shows MIC ranges of 16-0.25 μg/mL and 1-0.125 μg/mL against strains derived from Klebsiella pneumoniae and Escherichia coli, respectively[2].

In a single-dose mouse lung infection model with neutropenia, a single dose of Cefepime at 32 mg/kg combined with Taniborbactam dihydrochloride (VNRX-5133 dihydrochloride) at 16 mg/kg (subcutaneous injection) results in a reduction of bacterial counts by >4 log10. This combination is effective against K. pneumoniae strains producing CTX-M-14[1].In a combination treatment in a kidney infection model, Cefepime at 16 mg/kg and Taniborbactam dihydrochloride at 16 mg/kg (subcutaneous injection, twice daily for 7 days) lead to a reduction of bacterial counts by >2 log10 in the kidneys, targeting E. coli strains producing CTX-M-15[2].The half-life (T1/2) of Taniborbactam dihydrochloride in mice is 0.16 hours, with a clearance (CL) of 618 mL/h/kg and a volume of distribution at steady state (Vss) of 143 mL/kg[1].