Doripenem
doripenem
CAS: 148016-81-3
Molecular Formula: C15H24N4O6S2
Doripenem - Names and Identifiers
Doripenem - Physico-chemical Properties
| Molecular Formula | C15H24N4O6S2 |
| Molar Mass | 420.5 |
| Density | 1.59±0.1 g/cm3(Predicted) |
| Melting Point | >186°C dec. |
| Boling Point | 694.8±65.0 °C(Predicted) |
| Solubility | In water, not known, in DMSO 20 mg/ml, in pBS 3 mg/ml |
| Appearance | Solid |
| Color | White to Light Beige |
| pKa | 4.27±0.60(Predicted) |
| Storage Condition | Sealed in dry,Store in freezer, under -20°C |
| Stability | Hygroscopic |
| Refractive Index | 1.68 |
Doripenem - Reference Information
| Overview | Donipenem was developed by Japan's Shiono Yoshio Company under the trade name Finibax. Johnson & Johnson obtained the right to develop and market the drug from Japan's Shiano Yoshinoshi Company. In 2007, the United States approved Doribax (Donipem) injection for the treatment of complex intra-abdominal infections and complex urinary tract infections including pyelonephritis. |
| application | donipenem has a wide antibacterial spectrum and is stable to most daily phenolamine enzymes. its nephrotoxicity is low and central nervous toxicity is extremely small. these characteristics will become the biggest selling point of the product's market promotion. In addition, donipenem can be used to treat difficult hospital-acquired pneumonia (NP), and the effective rate is as high as 81%, which greatly exceeds the clinical anti-NP effect of other existing antibiotics. |
| new carbapenem antibiotics | donipenem is a new carbapenem antibiotic developed by Japan's Shiano Yoshiki Company. It has a wide antibacterial spectrum and is resistant to most β-lactamases. Stable, including penicillinase, cephalosporin enzyme and ultra-broad-spectrum β-lactamases (ESBLs). Human dehydropeptidase (DHP-1) is stable, is not hydrolyzed by DHP-1 in the body, and can be used alone. Strong antibacterial activity against both anaerobic or aerobic Gram-positive and Gram-negative bacteria. Overall, the antibacterial activity of donipenem is equivalent to that of imipenem, meropenem and ertapenem. However, the activity of Staphylococcus aureus, Pseudomonas aeruginosa and penicillin-resistant Streptococcus pneumoniae was significantly stronger than that of meropenem. In vitro studies show that the activity of donipenem against methicillin-resistant Staphylococcus and Streptococcus is equivalent to that of imipenem, and the MIC90 value is 0.5 mg/ml or lower; it has high activity against Enterobacter, Haemophilus influenzae and Moraxella catarrhalis bacteria, and the MIC90 value is 0.032~0.5 mg/ml; it also has a good antibacterial effect against imipenem-resistant Pseudomonas aeruginosa, MIC90 value is 8 mg/ml, which is stronger than meropenem, biapenem, cefpirome, and donipenem also have good antibacterial effects against ceftazidime, ciprofloxacin and gentamicin-resistant bacteria. Donipenem has a good antibacterial effect on clinically isolated common gynecological and obstetric infection bacteria. MIC50 and MIC90 are 0.25 and 1 mg/ml respectively. Donipenem has a good therapeutic effect on rats infected with uterus of these bacteria, suggesting the prospect of Donipenem application in clinical gynecology and obstetrics. Donipenem is stable to DHP-1 from humans, dogs, pigs, guinea pigs, rats, mice and rabbits. Animal model studies show that mice can reach a high blood level after subcutaneous injection of Donipenem, which has a good protective effect on Gram-positive and Gram-negative bacteria (including drug-resistant bacteria) infection in mouse models. Clinical studies of donipenem show that this product is stable in human body and is not affected by human DHP-1 enzymes. The half-life (t1/2) of 125mg intravenous injection is 0.85h, which is mainly excluded by urine. The drug recovery rate in 24h urine is 75%. Its pharmacokinetic characteristics are similar to those of meropenem and are not affected by multiple doses. 250mg ~ 1000mg, administered once, twice or three times a day, the effective rate of complex urinary tract infection and chronic respiratory tract infection is 93.8% ~ 95.2, and the bacterial clearance rate is 87.5% ~ 98.2%, showing good antibacterial effect of this product. |
| countries approve treatable diseases | on October 15, 2007, the U.S. food and drug administration (FDA) approved Johnson & Johnson's donipenem (doripenem,Doribax) injection for the treatment of complicated intra-abdominal infections and complicated urinary tract infections, including pyelonephritis caused by sensitive bacteria, with a specification of 500mg. The drug is currently approved in Europe for the treatment of hospital-acquired pneumonia. This product has antibacterial effects on Gram-positive bacteria and Gram-negative bacteria, including Pseudomonas, which can cause serious infections. Johnson & Johnson obtained the right to develop and market the drug from Japan's Shiono Yoshinoshi Company. Donipenem was listed in Japan in September 2005 under the trade name Finibax. At present, the application of this product for the treatment of NP including VAP is under review. In Europe, the European Union Medical Products Committee (CHMP) has given positive opinions on the treatment of cIAI, cUTI, NP, including VAP. On July 16, 2008, Johnson & Johnson Pharmaceutical Research and Development Company announced that the voting results of the FDA Anti-infective Drugs Advisory Committee affirmed the therapeutic and safety data of donipenem injection (doripenem for injection, Doribax) for the treatment of hospital-acquired pneumonia (NP) and ventilator-associated pneumonia (VAP). This product is a carbapenem antibiotic, which is used in hospitals and administered by intravenous injection. The committee voted that the 500mg donipenem 1-hour and 4-hour infusion regimens are safe and effective. On August 21, 2008, the U.S. Food and Drug Administration submitted to Johnson & Johnson that the current research data are not sufficient to support the inclusion of hospital-acquired pneumonia as an indication for donipenem (Doribax). |
| biological activity | Doripenem is a broad-spectrum β-lactam antibiotic, which is effective against gram-positive bacteria, negative bacteria and anaerobic bacteria. |
Last Update：2024-04-09 21:21:28
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Product Name: Doripenem Request for quotationCAS: 148016-81-3
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Mobile: 18916960931
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Tel: +86-400-900-4166
Email: product@acmec-e.com
Mobile: +86-18621343501
QQ: 2881950922
Wechat: 18621343501
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View History
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