2016年10月18日星期二

Tigecycline




Tigecycline (INN) is an antibiotic used to treat a number of bacterial infections. It is a first-in-class glycylcycline that is administered intravenously. It was developed in response to the growing rate of antibiotic resistance in bacteria such as Staphylococcus aureus, Acinetobacter baumannii, and E. coli. As a tetracycline derivative antibiotic, its structural modifications has expanded its therapeutic activity to include Gram-positive and Gram-negative organisms, including those of multi-drug resistance. It is approved to treat complicated skin and soft tissue infections (cSSTI), complicated intra-abdominal infections (cIAI), and community-acquired bacterial pneumonia (CAP) in individuals 18 years and older.
Medical uses

Tigecycline is used to treat different kinds of bacterial infections, including complicated skin and structure infections, complicated intra-abdominal infections and community-acquired bacterial pneumonia. The spectrum of activity of tigecycline is discussed below.

Tigecycline can treat complicated skin and structure infections caused by; Escherichia coli, vancomycin-susceptible Enterococcus faecalis, methicillin-resistant Staphylococcus aureus (MRSA), Streptococcus agalactiae, Streptococcus anginosus grp., Streptococcus pyogenes, Enterobacter cloacae, Klebsiella pneumoniae, and Bacteroides fragilis.
Tigecycline is indicated for treatment of complicated intra-abdominal infections caused by; Citrobacter freundii, Enterobacter cloacae, Escherichia coli, Klebsiella oxytoca, Klebsiella pneumoniae, vancomycin-susceptible Enterococcus faecalis, methicillin-resistant Staphylococcus aureus (MRSA), Streptococcus anginosus grp., Bacteroides fragilis, Bacteroides thetaiotaomicron, Bacteroides uniformis, Bacteroides vulgatus, Clostridium perfringens, and Peptostreptococcus micros.
Tigecycline may be used for treatment of community-acquired bacterial pneumonia caused by; penicillin susceptible Streptococcus pneumoniae, Haemophilus influenzae that does not produce Beta-lactamase and Legionella pneumophila.
Tigecycline is given intravenously and has activity against a variety of Gram-positive and Gram-negative bacterial pathogens, many of which are resistant to existing antibiotics. Tigecycline successfully completed phase III trials in which it was at least equal to intravenous Vancomycin and Aztreonam to treat complicated skin and skin structure infections, and to intravenous imipenem and cilastatian to treat complicated intra-abdominal infections. Tigecycline is active against many Gram-positive bacteria, Gram-negative bacteria and anaerobes – including activity against methicillin-resistant Staphylococcus aureus (MRSA), Stenotrophomonas maltophilia, Haemophilus influenzae, and Neisseria gonorrhoeae (with MIC values reported at 2 µg/mL) and multi-drug resistant strains of Acinetobacter baumannii. It has no activity against Pseudomonas spp. or Proteus spp. The drug is licensed for the treatment of skin and soft tissue infections as well as intra-abdominal infections.

The European Society of Clinical Microbiology and Infection recommends tigecycline as a potential salvage therapy for severe and/or complicated or refractory Clostridium difficile infection.

Tigecycline can also be used in vulnerable populations such as immunocompromised patients or patients with cancer. Tigecycline may also have potential for use in Acute myeloid leukemia

Product Description
Product:Tigecycline
CAS No.:220620-09-7
Product
Product nameTigecycline
Synonyms(4S,4aS,5aR,12aS)-4,7-Bis(dimethylamino)-9-[(tert-butylamino)acetamido]-3,10,12,12a-tetrahydroxy-1,11-dioxo-1,4,4a,5,5a,6,11,12a-octahydrotetracen-2-carboxamide
CAS NO.220620-09-7
Molecular formulaC29H39N5O8
Molecular weight585.65
Specifications
AppearanceOff-white powder
Density 1.455 g/cm3
Boiling point890.9 ºC at 760 mmHg
Assay99%
Others
Packing1Kg;5Kg;10Kg;25Kg or as demand
ApplicationPharmaceutical intermidiates

Specifications

1.Tigecycline
2.Pharmaceutical Intermediates
3.CAS NO.:220620-09-7
4.High quality
5.competetive price

Iterm

SPECIFICATIONS

Product Name

Tigecycline

CAS No.

220620-09-7

Appearance

Orange crystalline powder

Solubility

Freely soluble in water,sparingly soluble in diethyl ether,slightly soluble in methanol and ethanol

Identification

A)IR:Conforms

B)HPLC:The retention time of the major peak in the chromatogram of the sample solution corresponds to that of the standard solution as obtained in the assay

Water

5.0%

pH

7.0~8.0

Residue on ignition

0.1%

Heavy metals

10ppm

C-4 epimer

1.0%

Other single impurity

1.0%

Total impurities

2.0%

Residual solvents

Methanol3000ppm

Isopropyl alcohol2000ppm

Acetone3000ppm

Methylene chloride300ppm

Purity(HPLC)

99.0%

Assay(On dried basis)

98.0~105.0%


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Notice: This product is only suitable for laboratory use, or the use of animals. It can not be used directly on the human body

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