**Background**
Bacterial infections caused by a wide range of pathogenic bacteria remain a significant global health challenge, often requiring potent antimicrobial agents to prevent systemic complications such as sepsis. The development of orally active antibiotics is particularly crucial for improving patient compliance and expanding treatment options beyond hospital settings. Carbapenems are a class of highly effective β-lactam antibiotics known for their broad-spectrum activity; however, many are limited to parenteral administration. To address this need, research has focused on creating prodrugs that maintain high efficacy while being suitable for oral intake. In this context, we will introduce an orally active antibiotic – Tebipenem pivoxil.
**Definition**
Tebipenem pivoxil is an orally active carbapenem antibiotic that targets penicillin-binding proteins (PBP) to inhibit bacterial cell wall synthesis.
**In Vitro and In Vivo Studies**
According to the Tebipenem pivoxil description, this compound acts by binding to PBPs, thereby disrupting the integrity of the bacterial cell wall. In terms of Tebipenem pivoxil in vitro activity, the compound (0-128 μg/mL; 18–24 h) demonstrated excellent antibacterial properties against various Gram-positive and Gram-negative bacteria, with MIC50 values below 64 μg/mL.
Regarding Tebipenem pivoxil in vivo evaluation, studies using KM mice (18–22 g) revealed a maximum tolerance dosage (MTD) of 3.40 g/kg and a minimal lethal dosage (MLD) of 4.00 g/kg following a single oral administration of tablets, although dose-dependent liver and kidney damage was observed. Furthermore, in ICR mice sepsis models, oral administration of Tebipenem pivoxil at doses of 50 and 100 mg/kg (once) significantly increased the survival rate of the mice challenged with various pathogenic bacteria within a 168 h observation period. In conclusion, Tebipenem pivoxil is a potent oral carbapenem preparation with broad-spectrum antibacterial activity.
Keywords
Tebipenem pivoxil, 161715-24-8, L084, L 084, L-084, Penicillin-binding protein (PBP), Bacterial, Antibiotic, broad antibacterial spectrum, Streptococcus pneumonia, Erythromycin-resistant Streptococcus pneumonia, Haemophilus influenza, orally active, penicillin-binding protein, Inhibitor
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