Vaborbactam (INN)[1] is a non-
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Clinical data | |
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Routes of administration | IV |
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ECHA InfoCard | 100.235.136 |
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Formula | C12H16BNO5S |
Molar mass | 297.13 g·mol−1 |
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In the United States, the combination drug meropenem/vaborbactam (Vabomere) is approved by the Food and Drug Administration for complicated urinary tract infections and pyelonephritis.[3]
Biochemistry
editVaborbactam is a boronic acid
Carbapenemases can be broadly divided into two different categories based on the mechanism they use to hydrolyze the lactam ring in their substrates: Metallo-
Given their mechanism of action, the possibility of off-target effects brought about through inhibition of endogenous serine hydrolases is an obvious possible concern in the development of boronic acid
References
edit- ^ "International Nonproprietary Names for Pharmaceutical Substances (INN). Recommended International Nonproprietary Names: List 75" (PDF). World Health Organization. pp. 161–2. Archived from the original (PDF) on February 2, 2017.
- ^ a b c d Hecker SJ, Reddy KR, Totrov M, Hirst GC, Lomovskaya O, Griffith DC, et al. (May 2015). "Discovery of a Cyclic Boronic Acid
β -Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases". Journal of Medicinal Chemistry. 58 (9): 3682–92. doi:10.1021/acs.jmedchem.5b00127. PMID 25782055. - ^ "FDA approves new antibacterial drug" (Press release). Food and Drug Administration. August 29, 2017.
- ^ Burgos RM, Biagi MJ, Rodvold KA, Danziger LH (October 2018). "Pharmacokinetic evaluation of meropenem and vaborbactam for the treatment of urinary tract infection". Expert Opinion on Drug Metabolism & Toxicology. 14 (10): 1007–1021. doi:10.1080/17425255.2018.1511702. PMID 30106599. S2CID 52006261.
- ^ a b Queenan AM, Bush K (July 2007). "Carbapenemases: the versatile beta-lactamases". Clinical Microbiology Reviews. 20 (3): 440–58, table of contents. doi:10.1128/CMR.00001-07. PMC 1932750. PMID 17630334.
- ^ Lamotte-Brasseur J, Knox J, Kelly JA, Charlier P, Fonzé E, Dideberg O, Frére JM (December 1994). "The structures and catalytic mechanisms of active-site serine beta-lactamases". Biotechnology & Genetic Engineering Reviews. 12 (1): 189–230. doi:10.1080/02648725.1994.10647912. PMID 7727028.
- ^ Griffith DC, Loutit JS, Morgan EE, Durso S, Dudley MN (October 2016). "Phase 1 Study of the Safety, Tolerability, and Pharmacokinetics of the
β -Lactamase Inhibitor Vaborbactam (RPX7009) in Healthy Adult Subjects". Antimicrobial Agents and Chemotherapy. 60 (10): 6326–32. doi:10.1128/AAC.00568-16. PMC 5038296. PMID 27527080.