A new class of penicillin-binding protein inhibitors to address drug-resistant Neisseria gonorrhoeae.
Uehara T, Zulli AL, Miller B, Avery LM, Boyd SA, Chatwin CL, Chu GH, Drager AS, Edwards M, Emeigh Hart SG, Line NJ, Myers CL, Rongala G, Stevenson A, Uehara K, Yi F, Wang B, Liu Z, Wang M, Zhao Z, Zhou X, Zhao H, Stratton CM, Bala S, Davies C, Tkavc R, Jerse AE, Pevear DC, Burns CJ, Daigle DM, Condon SM. Nat Microbiol. Apr 8:2026. doi.org/10.1038/s41564-026-02309-3.
Exploring the activity of a novel orally bioavailable β-lactam-β-lactamase inhibitor combination, ceftibuten-ledaborbactam, against Enterobacterales-carrying blaOXA-48.
Mojica MF, Zeiser ET, Becka SA, Six DA, Moeck G, Bonomo RA, Papp-Wallace KM. Microbiol Spectr. 2026 Feb 3;14(2):e0314825. doi: 10.1128/spectrum.03148-25. Epub 2025 Dec 23. PMID: 41432447.
Burkholderia pseudomallei PenI β-lactamase and variants are potently inhibited by taniborbactam.
Mojica MF, Becka SA, Edwards M, Myers C, Uehara K, Uehara T, Hoshino T, Zeiser ET, Chatwin CL, Six DA, Bonomo RA, Papp-Wallace KM, Nukaga M. Antimicrob Agents Chemother. 2025 Oct;69(10):e0078725. doi: 10.1128/aac.00787-25. Epub 2025 Sep 12. PMID: 40938351.
Establishing the reference broth microdilution MIC method for cefepime-taniborbactam.
Belley A, Cusick SM, Pevear DC, Koeth L, DiFranco-Fisher J, Kothari N, Hawser S, Moeck G. J Clin Microbiol. 2025 Sep 10;63(9):e0066125. doi: 10.1128/jcm.00661-25. Epub 2025 Aug 19. PMID: 40827922.
Assessment of human exposures of cefepime-taniborbactam against cefepime-resistant Enterobacterales and Pseudomonas aeruginosa in a 7-day hollow fiber infection model.
Avery LM, Edwards M, Yi F, Moeck G, Uehara T, Pevear DC. Antimicrob Agents Chemother. 2025 Sep 3;69(9):e0001725. doi: 10.1128/aac.00017-25. Epub 2025 Jul 31. PMID: 40741958.
Structure and mechanism of taniborbactam inhibition of the cefepime-hydrolyzing, partial R2-loop deletion Pseudomonas-derived cephalosporinase variant PDC-88.
Mack AR, Kumar V, Bethel CR, Taracila MA, Miller BA, Uehara T, Six DA, Papp-Wallace KM, van den Akker F, Bonomo RA. Antimicrob Agents Chemother. 2025 Jul 2;69(7):e0007825. doi: 10.1128/aac.00078-25. Epub 2025 Jun 12. PMID: 40503958.
Discovery of VNRX-9945, a Potent, Broadly Active Capsid Assembly Modulator as a Clinical Candidate for the Treatment of Chronic Hepatitis B Virus Infection.
Liu B, Yao J, Haimowitz T, Benetatos CA, Boyd SA, Condon SM, Burns CJ, White A, Lakshminarasimhan D, Suto RK, Cakici O, Drager AS, Hart SGE, Pevear DC, Coburn GA. ACS Med Chem Lett. 2025 Jun 20;16(7):1209-1216. doi: 10.1021/acsmedchemlett.5c00315. eCollection 2025 Jul 10. PMID: 40666476.
Impact of porin deletions on cefepime-taniborbactam activity against Klebsiella pneumoniae.
Uehara T, Chatwin CL, Miller B, Edwards M, Stevenson A, Colombo J, Uehara K, Daigle DM. Antimicrob Agents Chemother. 2025 May 7;69(5):e0167224. doi: 10.1128/aac.01672-24. Epub 2025 Apr 2. PMID: 40172193.
Spectrum of cefepime-taniborbactam coverage against 190 β-lactamases defined in engineered isogenic Escherichia coli strains.
Uehara T, Chatwin CL, Miller B, Edwards M, Stevenson A, Colombo J, Six DA, Daigle DM, Moeck G, Boyd SA, Pevear DC. Antimicrob Agents Chemother. 2025 May 7;69(5):e0169924. doi: 10.1128/aac.01699-24. Epub 2025 Apr 1. PMID: 40167371.
Cefepime-taniborbactam and ceftibuten-ledaborbactam maintain activity against KPC variants that lead to ceftazidime-avibactam resistance.
Myers CL, Stevenson A, Miller B, Daigle DM, Uehara T, Pevear DC. Antimicrob Agents Chemother. 2025 Mar 5;69(3):e0151124. doi: 10.1128/aac.01511-24. Epub 2025 Feb 10. PMID: 39927783.
ARGONAUT-IV: susceptibility of carbapenemase-producing Klebsiella pneumoniae to the oral bicyclic boronate β-lactamase inhibitor ledaborbactam combined with ceftibuten.
Jacobs MR, Good CE, Abdelhamed AM, Mack AR, Bethel CR, Marshall SH, Hujer AM, Hujer KM, Patel R, van Duin D, Fowler VG, Rhoads DD, Six DA, Moeck G, Uehara T, Papp-Wallace KM, Bonomo RA. Antimicrob Agents Chemother. 2024 Dec 5;68(12):e0112724. doi: 10.1128/aac.01127-24. Epub 2024 Oct 30. PMID: 39475259.
Cefepime-taniborbactam activity against antimicrobial-resistant clinical isolates of Enterobacterales and Pseudomonas aeruginosa: GEARS global surveillance programme 2018-22.
Karlowsky JA, Wise MG, Hackel MA, Six DA, Uehara T, Daigle DM, Pevear DC, Moeck G, Sahm DF. J Antimicrob Chemother. 2024 Dec 2;79(12):3116-3131. doi: 10.1093/jac/dkae329. PMID: 39287999.
Cefepime-taniborbactam demonstrates potent in vitro activity vs Enterobacterales with blaOXA-48.
Mojica MF, Zeiser ET, Becka SA, Six DA, Moeck G, Papp-Wallace KM. Microbiol Spectr. 2024 Nov 5;12(11):e0114424. doi: 10.1128/spectrum.01144-24. Epub 2024 Sep 24. PMID: 39315842.
ARGONAUT-III and -V: susceptibility of carbapenem-resistant Klebsiella pneumoniae and multidrug-resistant Pseudomonas aeruginosa to the bicyclic boronate β-lactamase inhibitor taniborbactam combined with cefepime.
Jacobs MR, Abdelhamed AM, Good CE, Mack AR, Bethel CR, Marshall S, Hujer AM, Hujer KM, Patel R, van Duin D, Fowler VG, Rhoads DD, Six DA, Moeck G, Uehara T, Papp-Wallace KM, Bonomo RA. Antimicrob Agents Chemother. 2024 Sep 4;68(9):e0075124. doi: 10.1128/aac.00751-24. Epub 2024 Aug 12. PMID: 39133021.
Examining the activity of cefepime-taniborbactam against Burkholderia cepacia complex and Burkholderia gladioli isolated from cystic fibrosis patients in the United States.
Mojica MF, Zeiser ET, Becka SA, LiPuma JJ, Six DA, Moeck G, Papp-Wallace KM. Antimicrob Agents Chemother. 2023 Nov 15;67(11):e0049823. doi: 10.1128/aac.00498-23. Epub 2023 Sep 28. PMID: 37768313.
In Vitro Activity of Cefepime-Taniborbactam and Comparators against Clinical Isolates of Gram-Negative Bacilli from 2018 to 2020: Results from the Global Evaluation of Antimicrobial Resistance via Surveillance (GEARS) Program.
Karlowsky JA, Hackel MA, Wise MG, Six DA, Uehara T, Daigle DM, Cusick SM, Pevear DC, Moeck G, Sahm DF. Antimicrob Agents Chemother. 2023 Jan 24;67(1):e0128122. doi: 10.1128/aac.01281-22. Epub 2022 Dec 21. PMID: 36541767.
In vivo pharmacokinetics and pharmacodynamics of ceftibuten/ledaborbactam, a novel oral β-lactam/β-lactamase inhibitor combination.
Fratoni AJ, Avery LM, Nicolau DP, Asempa TE. J Antimicrob Chemother. 2022 Dec 23;78(1):93-100. doi: 10.1093/jac/dkac359. PMID: 36272135.
Ceftibuten-Ledaborbactam Activity against Multidrug-Resistant and Extended-Spectrum-β-Lactamase-Positive Clinical Isolates of Enterobacterales from a 2018-2020 Global Surveillance Collection.
Karlowsky JA, Wise MG, Hackel MA, Pevear DC, Moeck G, Sahm DF. Antimicrob Agents Chemother. 2022 Nov 15;66(11):e0093422. doi: 10.1128/aac.00934-22. Epub 2022 Oct 26. PMID: 36286518.
Fluorescent sensors of siderophores produced by bacterial pathogens.
Kumar A, Yang T, Chakravorty S, Majumdar A, Nairn BL, Six DA, Marcondes Dos Santos N, Price SL, Lawrenz MB, Actis LA, Marques M, Russo TA, Newton SM, Klebba PE. J Biol Chem. 2022 Mar;298(3):101651. doi: 10.1016/j.jbc.2022.101651. Epub 2022 Jan 29. PMID: 35101443.
The Next-Generation β-Lactamase Inhibitor Taniborbactam Restores the Morphological Effects of Cefepime in KPC-Producing Escherichia coli.
Roach EJ, Uehara T, Daigle DM, Six DA, Khursigara CM. Microbiol Spectr. 2021 Oct 31;9(2):e0091821. doi: 10.1128/Spectrum.00918-21. Epub 2021 Sep 8. PMID: 34494877.
Discovery of VNRX-7145 (VNRX-5236 Etzadroxil): An Orally Bioavailable β-Lactamase Inhibitor for Enterobacterales Expressing Ambler Class A, C, and D Enzymes.
Trout RE, Zulli A, Mesaros E, Jackson RW, Boyd S, Liu B, Hamrick J, Daigle D, Chatwin CL, John K, McLaughlin L, Cusick SM, Weiss WJ, Pulse ME, Pevear DC, Moeck G, Xerri L, Burns CJ. J Med Chem. 2021 Jul 22;64(14):10155-10166. doi: 10.1021/acs.jmedchem.1c00437. Epub 2021 Jun 30. PMID: 34191513.
Microbiological Characterization of VNRX-5236, a Broad-Spectrum β-Lactamase Inhibitor for Rescue of the Orally Bioavailable Cephalosporin Ceftibuten as a Carbapenem-Sparing Agent against Strains of Enterobacterales Expressing Extended-Spectrum β-Lactamases and Serine Carbapenemases.
Chatwin CL, Hamrick JC, Trout REL, Myers CL, Cusick SM, Weiss WJ, Pulse ME, Xerri L, Burns CJ, Moeck G, Daigle DM, John K, Uehara T, Pevear DC. Antimicrob Agents Chemother. 2021 Jul 16;65(8):e0055221. doi: 10.1128/AAC.00552-21. Epub 2021 Jul 16. PMID: 34001510.
Iron Acquisition Systems of Gram-negative Bacterial Pathogens Define TonB-Dependent Pathways to Novel Antibiotics.
Klebba PE, Newton SMC, Six DA, Kumar A, Yang T, Nairn BL, Munger C, Chakravorty S. Chem Rev. 2021 May 12;121(9):5193-5239. doi: 10.1021/acs.chemrev.0c01005. Epub 2021 Mar 16. PMID: 33724814.
Discovery of Taniborbactam (VNRX-5133): A Broad-Spectrum Serine- and Metallo-β-lactamase Inhibitor for Carbapenem-Resistant Bacterial Infections.
Liu B, Trout REL, Chu GH, McGarry D, Jackson RW, Hamrick JC, Daigle DM, Cusick SM, Pozzi C, De Luca F, Benvenuti M, Mangani S, Docquier JD, Weiss WJ, Pevear DC, Xerri L, Burns CJ. J Med Chem. 2020 Mar 26;63(6):2789-2801. doi: 10.1021/acs.jmedchem.9b01518. Epub 2019 Dec 16. PMID: 31765155.
VNRX-5133 (Taniborbactam), a Broad-Spectrum Inhibitor of Serine- and Metallo-β-Lactamases, Restores Activity of Cefepime in Enterobacterales and Pseudomonas aeruginosa.
Hamrick JC, Docquier JD, Uehara T, Myers CL, Six DA, Chatwin CL, John KJ, Vernacchio SF, Cusick SM, Trout REL, Pozzi C, De Luca F, Benvenuti M, Mangani S, Liu B, Jackson RW, Moeck G, Xerri L, Burns CJ, Pevear DC, Daigle DM. Antimicrob Agents Chemother. 2020 Feb 21;64(3):e01963-19. doi: 10.1128/AAC.01963-19. Print 2020 Feb 21. PMID: 31871094.