Tebipenem pivoxil(L-084) is a novel oral carbapenem antibiotic with an IC50 of 100 μg/ml for human CYP isoforms. In mouse, rat, dog and monkey, TBPM-PI were absorbed quickly, and the bioavailability was (71.4, 59.1, 34.8 and 44.9%, respectively. There was
Tebipenem Pivoxil is an oral carbapenem antibiotic. Tebipenem Pivoxil is absorbed and metabolized into Tebipenem, its active metabolite which showed excellent bactericidal activity against β-lactamase-nonproducing, ampicillin-resistant isolates.
ChEBI: Tebipenem pivoxil is a member of carbapenems and a pivaloyloxymethyl ester.
Tebipenem pivoxil (L-084I; ME1211; SPR994; Tebi-pivoxil; TBM-PI) corresponds to the orally bioavailable pivalyl ester prodrug form of the carbapenem class broad-spectrum β-lactam antibiotic Tebipenem (LJC 11,036; SPR859; TBM). TBM is potent against both gram-positive and gram-negative bacteria, including penicillin-resistant S. pneumoniae (PRSP) and many β-lactamase-producing strains, while being less effective against methicillin-resistant S. aureus (MRSA), S. marcescens, and P. aeruginosa. TBM is 2- to 64-fold more potent than imipenem, cefdinir, and faropenem against clinical isolates from respiratory and urinary-tract infections.
Tebipenem pivoxil (L084) (0-4.00 g/kg; p.o.; once) 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) 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. |
