Tebipenem Pivoxil a broad-spectrum orally-administered antibiotic, from the carbapenem subgroup of β-lactam antibiotics CAS NO.161715-24-8

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Product Details

Keywords

Tebipenem pivoxil
Tebipenem
Orapenem

Quick Details

ProName: Tebipenem Pivoxil a broad-spectrum or...
CasNo: 161715-24-8
Molecular Formula: C23H32N2O6S2
Appearance: white powder
Application: broad-spectrum orally-administered ant...
DeliveryTime: 7-10 Days
PackAge: 1 kgs/Tin, 25kgs/Tin
Port: Any port of China
ProductionCapacity: 1 Metric Ton/Month
Purity: 99.9%
Storage: 2-8℃ storage
Transportation: By Air, By Sea or By Courier
LimitNum: 1 Gram
Related Substances: 0.1%Max
Residue on Ignition: 0.3%Max
Heavy Metal: 5 PPM Max.
Valid Period: 36 Months
Appearance: White to off white powder
Protein binding: 95%
Legal status: Prescription-only in Japan; investigat...
CAS: 161715-24-8
Formula: C23H32N2O6S2
Molecular mass: 496
Routes of Absorption: Oral
Process: It was developed as a replacement drug...
Property: orally-administered antibiotic
Products of Degradation:: The product itself and its products of...
General Use: antibiotic
Stability: Stable

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Tebipenem pivoxil
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Service	1, Professional Techincal Guidence 2, Free Sample can be supplied before commercial purchase 3, Best price based on 100% high quality guarantee 4, Lifetime customer service since first deal 5, 24*7 hours contact
Process	Tebipenem is a broad-spectrum orally-administered antibiotic, from the carbapenem subgroup of β-lactam antibiotics. 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. It is presently only marketed in Japan.Tebipenem is the first carbapenem whose prodrug form, the pivalyl ester, is orally available. Pharmacokinetics of tebipenem pivoxil (TBPM-PI), a novel oral carbapenem antibiotic, were known in various laboratory animal. (1) In mouse, rat, dog and monkey, TBPM-PI were absorbed quickly, and the bioavailability was (71.4, 59.1, 34.8 and 44.9%, respectively. (2) TBPM-PI was quickly converted to tebipenem (TBPM), an active form of TBPM-PI. Through blood circulation, TBPM was distributed into the kidney at a high concentration and eliminated quickly. There was no other tissue than the kidney, in which TBPM was highly distributed and remained for a long time. In addition, low penetration to the central nervous system was confirmed. The penetration ratio of TBPM to ELF, that is the ratio of ELF concentration to plasma concentration of TBPM, was 21.8 +/- 14.7%. (3) Serum protein bindings of TBPM in the range of 0.1-100 microg/ml were 90.4-98.3% for mouse, 78.5-90.0% for rat, 15.7-18.7% for dog, 35.3-39.3% for monkey and 59.7-73.9% for human. In vitro metabolism was investigated in plasma, liver S9 fractions and small intestinal S9 fractions derived from infant and adult animals. TBPM-PI was transformed into TBPM quickly in any matrices. It was confirmed that absorbed TBPM-PI was quickly transformed into TBPM or LJC 11,562 (opened ring TBPM) in the plasma after oral administration of 14C-TBPM-PI to infant or adult rat and monkey. TBPM-PI and opened ring TBPM-PI was not detected in plasma and urine samples. In rat and monkey, the oral absorption, distribution, metabolite and excretion of TBPM-PI were not so much different between infant and adult animals. Liver metabolic enzyme system was little affected by 7-days repeated administration of 1-100 mg/kg TBPM-PI. IC50 values of TBPM-PI and TBPM for human CYP isoforms were estimated to be 100 microg/ml or higher. After single oral administration of 10 mg/kg 14C-TBPM-PI to rat, 36.9-42.7% and 58.3-62.2% of radioactivity was excreted to urine and feces, respectively, by 120 hours after administration. The majority of dosage was excreted out of body by 48 hours after administration. After single intravenous administration of 10 mg/kg 14C-TBPM, 87.4% and 11.4% of radioactivity was excreted in urine and bile, respectively, by 24 hours after administration. The majority of dosage was excreted out of body by 4 hours after administration.

Details

Product Details

Tebipenem is a broad-spectrum orally-administered antibiotic, from the carbapenem subgroup of β-lactam antibiotics.

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.

It is presently only marketed in Japan.Tebipenem is the first carbapenem whose prodrug form, the pivalyl ester,

is orally available.

Pharmacokinetics of tebipenem pivoxil (TBPM-PI), a novel oral carbapenem antibiotic, were known in various laboratory animal. In mouse, rat, dog and monkey, TBPM-PI were absorbed quickly, and the bioavailability was (71.4, 59.1, 34.8 and 44.9%, respectively. TBPM-PI was quickly converted to tebipenem (TBPM), an active form of TBPM-PI. Through blood circulation, TBPM was distributed into the kidney at a high concentration and eliminated quickly. There was no other tissue than the kidney, in which TBPM was highly distributed and remained for a long time. In addition, low penetration to the central nervous system was confirmed. The penetration ratio of TBPM to ELF, that is the ratio of ELF concentration to plasma concentration of TBPM, was 21.8 +/- 14.7%. (3) Serum protein bindings of TBPM in the range of 0.1-100 microg/ml were 90.4-98.3% for mouse, 78.5-90.0% for rat, 15.7-18.7% for dog, 35.3-39.3% for monkey and 59.7-73.9% for human.In vitro metabolism was investigated in plasma, liver S9 fractions and small intestinal S9 fractions derived from infant and adult animals. TBPM-PI was transformed into TBPM quickly in any matrices. It was confirmed that absorbed TBPM-PI was quickly transformed into TBPM or LJC 11,562 (opened ring TBPM) in the plasma after oral administration of 14C-TBPM-PI to infant or adult rat and monkey. TBPM-PI and opened ring TBPM-PI was not detected in plasma and urine samples. In rat and monkey, the oral absorption, distribution, metabolite and excretion of TBPM-PI were not so much different between infant and adult animals. Liver metabolic enzyme system was little affected by 7-days repeated administration of 1-100 mg/kg TBPM-PI. IC50 values of TBPM-PI and TBPM for human CYP isoforms were estimated to be 100 microg/ml or higher. After single oral administration of 10 mg/kg 14C-TBPM-PI to rat, 36.9-42.7% and 58.3-62.2% of radioactivity was excreted to urine and feces, respectively, by 120 hours after administration. The majority of dosage was excreted out of body by 48 hours after administration. After single intravenous administration of 10 mg/kg 14C-TBPM, 87.4% and 11.4% of radioactivity was excreted in urine and bile, respectively, by 24 hours after administration. The majority of dosage was excreted out of body by 4 hours after administration.

Packaging

The packaging can be customized, normally, 1kgs/Tin, or 5kgs/Tin or per drums

Company Introduction

Top Pharm Chemical Group is specialized in the New Drug Researching and Developing, and mainly manufacture Chemical Intermediates, Pharmaceutical APIs and Pilot Production. To meet customers regulatory needs, we can offer products from gram to kilo and tons scale, and we can also support our customers with the DMF and other documents to Complete the registration.

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