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Polyglycerin – PEG-drug conjugates


05.01.2010 | Ref.Nr. 09059
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Life Science › Pharma&Biotech › Drug delivery

A novel drug polymer conjugate consisting of a dendritic polyglycerin (PG) core of 3-5 or more glycerol units and a polyethylene glycol shell has been developed. The pharmaceutically or diagnostically compound is covalently bound to a glycerol unit through a cleavable linker (and optionally an additional spacer). Dependently on the used linker, the compound can be cleaved physically or chemically e.g. by light, heat, or by hydrolysis, pH-dependent cleavage or cleavage by enzymes. As there are multiple glycerol units, more than one binding site exists, so that more than one active compound can be coupled to the same carrier molecule. Moreover, one carrier molecule also enables the loading of different pharmaceutically compounds (combinational therapy).

These carriers are suitable for conjugation of various drug agents or diagnostically compounds such as e.g. cytostatic agents, cytokines, immunosuppressants, virostatics, radioactive agents, light-emitting or light absorbing substance, which allows the application in therapies of various diseases. The polymer drug conjugate may be in any form suitable for the patient, for example in an injectable form, as a tablette or a capsule, or as composition for inhalation.

 

IP Rights
A European patent application has been filed on February, 6, 2009. International patent application (PCT) has been filed on March, 31, 2009.

Origin
The invention was made at the Freie Universität Berlin and the KTB
Tumorforschungsgesellschaft mbH Freiburg.

Application Area:
Pharma, Diagnostic
Development Stage: In vivo test (xenograft)
Type of Collaboration: License
Schlagworte: Cleavable Linker, Conjugate, Dendritic, Drug agent, Drug Polymer, Glycerol, Polyglycerin,
Weitere Kategorien: Diagnostics, Life Science, Pharma & Biotech, Drug delivery
Bild des Benutzers Dr. Bettina Büttner
Licensing Manager: Dr. Bettina Büttner
T +49 30 2125 4835
F +49 30 2125 4822
bettina.buettner@ipal.de
Market Potential: Worldwide
Benefits:
  • Carrier allows high loading with active compounds due to multiple binding sites
  • Design of prodrugs comprising advantageous combination of different pharmaceutically active compounds –> individualized modes of treatment
  • Dendritic polyglycerols can be functionalized with various reactive groups
  • PG-drug conjugate preparation in three steps - Shown with the cytostatic agent doxorubicin (derivatives) and the folic acid antagonist methotrexate
  • pH stability studies (cleavage studies) with four Doxorubicin conjugates; Cytotoxity tests in two human tumor cell lines
  • Cleavage study of PG-Phe-Lys-PABC-Doxorubicin with cathepsin B
  • Successfull in vivo studies with four Doxorubicin conjugates in the ovarian carcinoma A2780 xenograft model (mouse) -> tumor growth inhibition