Polyglycerin – PEG-drug conjugates


A novel drug polymer conjugate consisting of a dendritic polyglycerine (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 addi-tional 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, immune-suppressants, virostatics and radioactive agents, light-emitting or light absorbing substance, which allows the application in therapies of various diseases. The polymer drug conjugate may be suitable for the patient in an injectable form, as a tablet or a capsule, or as composition for inhalation. </p> <p><strong>Benefits</strong> <ul> <li>Carrier allows high loading with active compounds due to multiple binding sites and divers functionalizing with various reactive groups </li> <li>Design of prodrugs comprising advantageous combination of different pharmaceutically active compounds-> individualized modes of treatment</li> <li>Easy drug conjugate preparation in three steps with high yield </li> <li>Very high biocompatibility of branched polyglycerol </li> <li>Controlled loading and release of the drugs by in vivo stimuli at the site of action (e.g. by pH changes or enzyme)</li> <li>Tumor growth inhibition in the ovarian carcinoma A2780 xenograft model by the application of Doxorubicin</li> </ul> <p><strong>IP Rights</strong><br> European Patent Applic. (02/2009)<br> US Application (03/2009) <br> <br> <strong>Origin</strong><br> The invention was made at the Freie Universität Berlin and the KTB Tumorforschungsgesellschaft mbH Freiburg.</p>

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