| Name | Tebipenem Pivoxil |
| Description | Tebipenem Pivoxil (Orapenem) , an orally activity carbapenem antibiotic, is utilized in treating 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] |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | Ethanol : 81 mg/mL (162.8 mM)
DMSO : 92 mg/mL (184.9 mM)
H2O : < 1 mg/mL (insoluble or slightly soluble)
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| Keywords | Antibiotic | broad antibacterial spectrum | L 084 | penicillin-binding protein | inhibit | L-084 | Inhibitor | orally active | ME-1211 | Haemophilus influenza | L084 | Bacterial | Tebipenem Pivoxil | Erythromycin-resistant Streptococcus pneumonia | Streptococcus pneumonia | ME 1211 |
| Inhibitors Related | Neomycin sulfate | Dehydroacetic acid sodium | Ampicillin sodium | Methyl anthranilate | Kanamycin sulfate | G-418 disulfate | Sulfamethoxazole sodium | Metronidazole | Doxycycline | EDTA copper(II) disodium salt | Dimethyl sulfoxide | Crystal Violet |
| Related Compound Libraries | Bioactive Compound Library | Endoplasmic Reticulum Stress Compound Library | Approved Drug Library | Pediatric Drug Library | Drug Repurposing Compound Library | Orally Active Compound Library | Clinical Compound Library | Bioactive Compounds Library Max | Preclinical Compound Library | Human Metabolite Library |
United States
