Tebipenem pivoxil hydrobromide
Tebipenem pivoxil hydrobromide (L084 hydrobromide) is an orally active carbapenem Antibiotic. Tebipenem pivoxil hydrobromide acts as a substrate of OATP1A2 with high affinity for this transporter (Km = 41.1 μM). Tebipenem pivoxil hydrobromide achieves intestinal absorption via carrier-mediated uptake and simple diffusion. Tebipenem pivoxil hydrobromide inhibits the growth of Gram-positive bacteria, Gram-negative bacteria, multidrug-resistant bacteria, and pathogens producing extended-spectrum β-lactamases. Tebipenem pivoxil hydrobromide eliminates intestinal infection pathogens and reduces mortality in septic mice. Tebipenem pivoxil hydrobromide can be used in research related to bacterial pneumonia, severe gastrointestinal infections, bacterial sepsis, complicated urinary tract infections, and acute pyelonephritis.
For research use only. We do not sell to patients.
- CAS No.: 1381788-20-0
- Formula: C22H32BrN3O6S2
- Molecular Weight:578.54
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
Tebipenem pivoxil (2.5-1000 μM; 60 min) hydrobromide is a substrate for human OATP1A2 which has high affinity (Km = 41.1 μM), while human OATP2B1 has low affinity for the compound (Km > 1 mM)[1].
Tebipenem pivoxil hydrobromide displays excellent in vitro antibacterial activity against Gram-positive bacterial strains including MSSA, MSSE, and Pyogenic streptococcus (MIC90 ≤0.125 µg/mL), with moderate activity against MRSA (MIC90 16 µg/mL), MRSE (MIC90 8 µg/mL), and Enterococcus faecalis (MIC90 32 µg/mL), and weaker activity against Enterococcus faecium (MIC90 128 µg/mL)[3].
Tebipenem pivoxil (18-24 h) hydrobromide displays strong bactericidal activity against Escherichia coli, Staphylococcus aureus, and Klebsiella pneumoniae, with MBC ranges of 0.016-2 µg/mL, 0.063-32 µg/mL, and 0.031-32 µg/mL respectively, and MBC/MIC ratios of 1-8 for Escherichia coli and 2-8 for Staphylococcus aureus and Klebsiella pneumoniae[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Tebipenem pivoxil (50 mg/kg; p.o.; two doses at 2 and 16 hours post-infection) hydrobromide delivers a 2.3-log reduction in S. flexneri CFUs in the small intestine of infected B6 mice, showing superior efficacy compared to subcutaneous Tebipenem freebase[2].
Tebipenem pivoxil (50 mg/kg; p.o.; twice daily; 5 days, starting 18 hours post-infection) hydrobromide clears faecal S. flexneri within 24 hours and significantly reduces diarrhoea severity and intestinal pathology in infected gnotobiotic piglets[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:B6 (female, 9-10 weeks old, intraperitoneal infection with S. flexneri lux1)[2]
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Dosage:50 mg/kg
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Administration:p.o.; two doses at 2 and 16 hours post-infection
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Result:Achieved a 2.3-log reduction of S. flexneri CFUs in the small intestine compared to untreated controls.
Achieved a comparable 2.3-log reduction of S. flexneri CFUs in the large intestine compared to untreated controls.
Resulted in a significantly lower bacterial load in the small intestine than in mice treated with 39 mg/kg subcutaneous Tebipenem freebase (p < 0.05).
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Animal Model:Gnotobiotic piglets (24 hours old, oral inoculation with S. flexneri 2457T)[2]
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Dosage:50 mg/kg
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Administration:p.o.; twice daily; 5 days, starting 18 hours post-infection
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Result:Significantly reduced the severity of diarrhoea compared to untreated infected controls.
Reduced faecal S. flexneri CFU/g from 1 × 107 to undetectable levels within 24 hours after a single dose, while untreated animals maintained high bacterial counts.
Markedly reduced intestinal lesions, inflammation, and intracellular Shigella in treated piglets compared to controls.
Chemical Information
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CAS No. 1381788-20-0
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Molecular Weight 578.54
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Formula C22H32BrN3O6S2
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SMILES
CC(C)(C)C(OCOC(C1=C(SC2CN(C3=NCCS3)C2)[C@H](C)[C@@]([C@@]4([H])[C@H](O)C)([H])N1C4=O)=O)=O.Br
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Synonyms
L084 hydrobromide
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
[1]. Kato K, et al. Intestinal absorption mechanism of tebipenem pivoxil, a novel oral carbapenem: involvement of human OATP family in apical membrane transport. Molecular pharmaceutics. 2010 Oct 04;7(5):1747-56. [Content Brief]
[2]. Fernández Álvaro E, et al. The repurposing of Tebipenem pivoxil as alternative therapy for severe gastrointestinal infections caused by extensively drug-resistant spp. eLife. 2022 Mar 15;11:e69798. [Content Brief]
[3]. Yao Q, et al. Antibacterial Properties of Tebipenem Pivoxil Tablet, a New Oral Carbapenem Preparation against a Variety of Pathogenic Bacteria in Vitro and in Vivo. Molecules (Basel, Switzerland). 2016 Jan 06;21(1):62. [Content Brief]
[4]. Eckburg PB, et al. Oral Tebipenem Pivoxil Hydrobromide in Complicated Urinary Tract Infection. The New England journal of medicine. 2022 Apr 07;386(14):1327-1338. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Tebipenem pivoxil hydrobromide Related Classifications
HY-B0396B Related Classifications
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