Tebipenem Pivoxil

For research use only.

Catalog No.S2159 Synonyms: L-084, ME1211

Tebipenem Pivoxil Chemical Structure

CAS No. 161715-24-8

Tebipenem pivoxil (L-084, ME1211) is an oral carbapenem antibiotic, use to treat otolaryngologic and respiratory infections.

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Biological Activity

Description Tebipenem pivoxil (L-084, ME1211) is an oral carbapenem antibiotic, use to treat otolaryngologic and respiratory infections.
In vitro

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. [1] 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. [2] 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. [3] Tebipenem has a potent activity against Neisseria gonorrhoeae; its activity is comparable to it of cefixime that has most potent activity among oral antibiotics. [4]

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. [5] 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. [6]

Protocol

Solubility (25°C)

In vitro DMSO 99 mg/mL (198.94 mM)
Water Insoluble
Ethanol '87 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 497.63
Formula

C22H31N3O6S2

CAS No. 161715-24-8
Storage powder
in solvent
Synonyms L-084, ME1211
Smiles CC1C2C(C(=O)N2C(=C1SC3CN(C3)C4=NCCS4)C(=O)OCOC(=O)C(C)(C)C)C(C)O

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04919954 Not yet recruiting Drug: Tebipenem Pivoxil Hydrobromide Diabetes|Wound Infection|ABSSSI|Healthy Volunteers Hartford Hospital|Spero Therapeutics Inc August 2021 Phase 1

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID