Tebipenem Hydrate is formulated as the tetrahydrate salt of Tebipenem, a carbenapenem antibiotic. Tebipenem is a β-lactam antibiotic which inhibits β-lactamase in a concentration-dependent manner. Tebinenem, like other beta-lactams, has high specificity and low toxicity and makes th.em useful against Gram-positive and Gram-negative bacteria. Tebipenem was developed to combat bacteria that had acquired resistance to common antibiotics such as methicillin-resistant Staphylococcus aureus. The prodrug form of Tebipenem is the pivalyl ester Tebipenem pivoxil.
Tebipenem Hydrate is slightly soluble in DMSO
| Mechanism of Action |
β-lactams interfere with PBP (penicillin binding protein) activity involved in the final phase of peptidoglycan synthesis. PBP’s are enzymes which catalyze a pentaglycine crosslink between alanine and lysine residues providing additional strength to the cell wall. Without a pentaglycine crosslink, the integrity of the cell wall is severely compromised and ultimately leads to cell lysis and death. Resistance to β-lactams is commonly due to cells containing plasmid encoded β-lactamases; however, carbapenems, including Doripenem, are highly resistant to β-lactamases. |
| Spectrum | Tebipenem is active against Gram-positive and Gram-negative bacteria. It is also active against methicillin-resistant strains of S. aureus and S. epidermidis and penicillin-resistant S. pneumoniae strains. |
| Microbiology Applications | Tebipenem is commonly used in clinical in vitro microbiological antimicrobial susceptibility tests (panels, discs, and MIC strips) against Gram-positive and Gram-negative microbial isolates. Medical microbiologists use AST results to recommend antibiotic treatment options. Representative MIC values include:
Carbapenems are active against enterobacteria producing extended-spectrum beta-lactamase (ESBL) and AmpC enzymes since they are not affected by these resistance mechanisms (Jain et al, 2018). |
| Molecular Formula | HC16H21N3O4S2•4H2O |
| References |
Hazra S, Xu H, Blanchard JS (2014) Tebipenem, a new carbapenem antibiotic, is a slow substrate that inhibits the β-lactamase from Mycobacterium tuberculosis. Biochem. 53(22):3671-3678 PMID: 24846409 Jain A, Utley L, Parr TR, Zabawa T, Pucci MJ (2018) Tebipenem, the first oral carbapenem antibiotic. Expert Rev Anti Infect Ther. 16(7):513-522 PMID 30014729 Mendes RE et al (2023) Contemporary evaluation of Tebipenem in iitro activity against Enterobacterales clinical isolates causing urinary tract Iifections in US medical centers (2019-2020). Microbiol Spectr. 11(1):e0205722 PMID 36625644 |
