Tebipenem pivoxil (L084) hydrochloride is an orally active antibiotic against a variety of pathogenic bacteria. Tebipenem pivoxil hydrochloride binds penicillin-binding protein (PBP), thereby inhibiting cell wall synthesis[1].
in vivo
Tebipenem pivoxil (L084) (0-4.00 g/kg; p.o.; once) hydrochloride shows minimal lethal dosage (MLD) of 4.00 g/kg and the maximum tolerance dosage (MTD) of 3.40 g/kg in mice[1].
Tebipenem pivoxil (50 and 100 mg/kg; p.o.; once) hydrochloride significantly protects the sepsis mice challenged with various pathogenic bacteria[1].
Animal Model:
KM mice weighing 18–22 g[1]
Dosage:
2.89, 3.40 and 4.00 g/kg
Administration:
Oral administration (tablet), once
Result:
Within the 14-day observation period, only one mouse was dead in the maximum oral dosage (4.00 g/kg). The minimal lethal dosage (MLD) was 4.00 g/kg and the maximum tolerance dosage (MTD) in the mice was 3.40 g/kg. Showed dose-dependent liver and kidney damage.
Animal Model:
ICR mice, sepsis mouse models[1]
Dosage:
50 and 100 mg/kg
Administration:
Oral administration (tablet), once
Result:
Significantly increased the survival number of the sepsis mice within a 168 h observation period.
IC 50
β-lactam
References
[1] 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. 2016 Jan 6;21(1):62. DOI:10.3390/molecules21010062
