Vaborbactam - CAS 1360457-46-0
Catalog number: 1360457-46-0
Category: Inhibitor
Please be kindly noted products are not for therapeutic use. We do not sell to patients.
Molecular Formula:
C12H16BNO5S
Molecular Weight:
297.14
COA:
Inquire
Targets:
Antibacterial
Description:
Vaborbactam is a selective beta-lactamase inhibitor under the development of Rempex Pharmaceuticals. Vaborbactam is a broad-spectrum inhibitor, especially restoring the activity of carbapenems against KPC-producing strains. Combined with a carbapenem, Vaborbactam can be a promising product for the treatment of multidrug resistant Gram-negative bacteria. Phase III clinical trials for the treatment of Bacteraemia, Gram-negative infections, Pneumonia, Pyelonephritis and Urinary tract infections are on-going.
Purity:
98%
Appearance:
Powder
Synonyms:
RPX 7009; MP-7009; REBO-07; MP-7;Meropenem;2-((3R,6S)-2-hydroxy-3-(2-(thiophen-2-yl)acetamido)-1,2-oxaborinan-6-yl)acetic acid
Solubility:
Soluble in DMSO
Storage:
-20°C Freezer
MSDS:
Inquire
Application:
Bacteraemia, Gram-negative infections, Pneumonia, Pyelonephritis and Urinary tract infections
Quality Standard:
In-house standard
Shelf Life:
2 month in rt, long time
Quantity:
Milligrams-Grams
InChIKey:
IOOWNWLVCOUUEX-WPRPVWTQSA-N
InChI:
1S/C12H16BNO5S/c15-11(7-9-2-1-5-20-9)14-10-4-3-8(6-12(16)17)19-13(10)18/h1-2,5,8,10,18H,3-4,6-7H2,(H,14,15)(H,16,17)/t8-,10-/m0/s1
Canonical SMILES:
B1([C@H](CC[C@H](O1)CC(=O)O)NC(=O)Cc2cccs2)O
Current Developer:
Rempex Pharmaceuticals; The Medicines Company; US Department of Health and Human Services
1.Effect of Meropenem-Vaborbactam vs Piperacillin-Tazobactam on Clinical Cure or Improvement and Microbial Eradication in Complicated Urinary Tract Infection: The TANGO I Randomized Clinical Trial.
Kaye KS;Bhowmick T;Metallidis S;Bleasdale SC;Sagan OS;Stus V;Vazquez J;Zaitsev V;Bidair M;Chorvat E;Dragoescu PO;Fedosiuk E;Horcajada JP;Murta C;Sarychev Y;Stoev V;Morgan E;Fusaro K;Griffith D;Lomovskaya O;Alexander EL;Loutit J;Dudley MN;Giamarellos-Bourboulis EJ JAMA. 2018 Feb 27;319(8):788-799. doi: 10.1001/jama.2018.0438.
Importance: ;Meropenem-vaborbactam is a combination carbapenem/beta-lactamase inhibitor and a potential treatment for severe drug-resistant gram-negative infections.;Objective: ;To evaluate efficacy and adverse events of meropenem-vaborbactam in complicated urinary tract infection (UTI), including acute pyelonephritis.;Design, Setting, and Participants: ;Phase 3, multicenter, multinational, randomized clinical trial (TANGO I) conducted November 2014 to April 2016 and enrolling patients (≥18 years) with complicated UTI, stratified by infection type and geographic region.;Interventions: ;Eligible patients were randomized 1:1 to receive meropenem-vaborbactam (2g/2g over 3 hours; n = 274) or piperacillin-tazobactam (4g/0.5g over 30 minutes; n = 276) every 8 hours. After 15 or more doses, patients could be switched to oral levofloxacin if they met prespecified criteria for improvement, to complete 10 days of total treatment.;Main Outcomes and Measures: ;Primary end point for FDA criteria was overall success (clinical cure or improvement and microbial eradication composite) at end of intravenous treatment in the microbiologic modified intent-to-treat (ITT) population. Primary end point for European Medicines Agency (EMA) criteria was microbial eradication at test-of-cure visit in the microbiologic modified ITT and microbiologic evaluable populations.
2.Game Changers: New β-Lactamase Inhibitor Combinations Targeting Antibiotic Resistance in Gram-Negative Bacteria.
Bush K ACS Infect Dis. 2018 Feb 9;4(2):84-87. doi: 10.1021/acsinfecdis.7b00243. Epub 2017 Dec 12.
Recent regulatory approvals for the β-lactam inhibitor combinations of ceftazidime-avibactam and meropenem-vaborbactam have provided two novel therapeutic options for the treatment of multidrug-resistant infections caused by Gram-negative bacteria. Most importantly, these combination agents have satisfied an important medical need related to antibiotic-resistant Klebsiella pneumoniae that produce serine carbapenemases, especially the Klebsiella pneumoniae carbapenemase (KPC) enzymes. Both combinations contain non-β-lactam β-lactamase inhibitors of novel chemical classes not previously developed as antibacterial agents, the diazabicyclooctanes and cyclic boronic acid derivatives. Their rapid development and approval programs have spurred a number of similar inhibitor combinations that will need to differentiate themselves for commercial success. Gaps still exist for the treatment of infections caused by multidrug-resistant Pseudomonas aeruginosa, Acinetobacter spp., and metallo-β-lactamase-producing pathogens. Overall, the new β-lactamase inhibitor combinations have infused new life into the search for new antibacterial agents to treat multidrug-resistant bacteria.
3.Physical Compatibility of Meropenem and Vaborbactam With Select Intravenous Drugs During Simulated Y-site Administration.
Kidd JM;Avery LM;Asempa TE;Nicolau DP;Kuti JL Clin Ther. 2018 Feb;40(2):261-269. doi: 10.1016/j.clinthera.2017.12.007. Epub 2017 Dec 28.
PURPOSE: ;Meropenem/vaborbactam is a novel intravenous antibiotic combining the carbapenem, meropenem, with a novel β-lactamase inhibitor, vaborbactam. Meropenem/vaborbactam is administered as a 3-hour infusion given every 8 hours, thereby potentially restricting an intravenous line for 9 h/d. Intravenous medications may be given concurrently via Y-site when compatibility data are available. Herein, physical compatibility was determined for the identification which medications can be coadministered with meropenem/vaborbactam via Y-site.;METHODS: ;Y-site administration was simulated in vitro by admixing 5 mL of meropenem 8 mg/mL and vaborbactam 8 mg/mL with an equal volume of 88 other diluted intravenous medications, including 34 antimicrobials. All other medications were diluted with 0.9% sodium chloride to the upper range of concentrations considered standard for intravenous infusion. Visual inspection, turbidity measurement, and pH measurement were performed prior to admixture, directly after admixture, and at time points up to 3 hours after admixture.;FINDINGS: ;Of the 88 medications tested, meropenem/vaborbactam was compatible with 73 (83%), including many antibiotics such as aminoglycosides (amikacin, gentamicin, and tobramycin), colistin, fosfomycin, linezolid, tedizolid, tigecycline, and vancomycin.
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