Tebipenem pivoxil hydrobromide  (Synonyms: L084 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 (K_m = 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^[1][2][3][4].

Tebipenem pivoxil (2.5-1000 μM; 60 min) hydrobromide is a substrate for human OATP1A2 which has high affinity (K_m = 41.1 μM), while human OATP2B1 has low affinity for the compound (K_m > 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 (5 mg/kg; p.o.; single dose) hydrobromide achieves a peak plasma Tebipenem (HY-A0076) concentration of 2.88 μg/mL and an AUC₀-inf of 1.52 μg·h/mL in fasted male Sprague-Dawley rats^[1].
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.

578.54

C₂₂H₃₂BrN₃O₆S₂

1381788-20-0

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

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [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.

  [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.

  [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.