product name Tebipenem Pivoxil
Description: Tebipenem pivoxil (also known as L-084, ME1211) is an orally available, broad spectrum antibiotic that belongs to carbapenem analog structurally, it is use to treat otolaryngologic and respiratory infections. It was developed as a replacement drug to combat bacteria that had acquired antibiotic resistance to commonly used antibiotics. Tebipenem is formulated as the ester tebipenem pivoxil due to the better absorption and improved bioavailability of this form. It has performed well in clinical trials for ear infection and looks likely to be further developed in future. Tebipenem Pivoxil has high intestinal apical membrane permeability due to plural intestinal transport routes, including the uptake transporters such as OATP1A2 and OATP2B1 as well as simple diffusion.
References: Mol Pharm. 2010 Oct 4;7(5):1747-56; Jpn J Antibiot. 2009 Jun;62(3):214-40; Vaccine. 2007 Mar 22;25(13):2478-84.
497.63
Formula
C22H31N3O6S2
CAS No.
161715-24-8
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 99 mg/mL (198.9 mM)
Water: <1 mg/mL
Ethanol: 87 mg/mL (174.8 mM)
Solubility (In vivo)
Synonyms
L-084, ME1211
other peoduct :
| In Vitro |
In vitro activity: Tebipenem Pivoxil has high intestinal apical membrane permeability due to plural intestinal transport routes, including the uptake transporters such as OATP1A2 and OATP2B1 as well as simple diffusion. Tebipenem Pivoxil is quickly converted to tebipenem (TBPM), an active form of Tebipenem Pivoxil. Tebipenem Pivoxil are absorbed quickly, and the bioavailability is 71.4%, 59.1%, 34.8% and 44.9%, respectively, in mouse, rat, dog and monkey. Tebipenem shows the strongest bactericidal activity as early as 2 h after exposure at two times the MIC. Tebipenem shows higher affinities for PBP 1A and PBP 2B, high-molecular-weight enzymes, and for PBP 3, a low-molecular-weight enzyme, than for PBP 2X. Tebipenem has a potent activity against Neisseria gonorrhoeae; its activity is comparable to it of cefixime that has most potent activity among oral antibiotics. Kinase Assay: Cell Assay: |
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| In Vivo | Tebipenem Pivoxil results in survival rate of 83%, compared with 25% survival for Amoxicillin and 0% survival for controls in animal model of otitis media. Tebipenem exhibits slow tight-binding inhibition at low micromolar concentrations versus the chromogenic substrate nitrocefin. Tebipenem acyl-enzyme complex remains stable for greater than 90 min and exists as mixture of the covalently bound drug and the bound retro-aldol cleavage product. |
| Animal model | |
| Formulation & Dosage | |
| References |
