Multi-arm polymer prodrugs - Patents

Multi-arm polymer prodrugs

Agent: Nektar Therapeutics - San Carlos, CA, US
Inventors: Xuan Zhao, Michael D. Bentley, Zhongxu Ren, Tacey X. Viegas
Class: 424078270 (USPTO)
Related Patents: Drug, Bio-affecting And Body Treating Compositions, Solid Synthetic Organic Polymer As Designated Organic Active Ingredient (doai), Aftertreated Polymer (e.g., Grafting, Blocking, Etc.), Polymer Derived From Ethylenic Monomers Only, Chemical Treating Agent Contains Element Other Than C, H, O, Alkali, Or Alkaline Earth Metal, Nitrogen Or Sulfur
#20050112088
05/26/05
Provided herein are water-soluble prodrugs. The prodrugs of the invention comprise a water-soluble polymer having three or more arms, at least three of which are covalently attached to an active agent, e.g., a small molecule. The conjugates of the invention provide an optimal balance of polymer size and structure for achieving improved drug loading, since the conjugates of the invention possess three or more active agents releasably attached to a multi-armed water soluble polymer. The prodrugs of the invention are therapeutically effective, and exhibit improved properties in-vivo when compared to unmodified parent drug.
FIELD OF THE INVENTION
[0002] This invention relates to multi-arm, water-soluble polymer drug conjugates, and in particular, to polymer-based prodrugs, and to methods for preparing, formulating and administering compositions comprising such prodrugs.
SUMMARY OF THE INVENTION
[0011] In one aspect, the present invention provides water-soluble prodrugs. The prodrugs of the invention comprise a water-soluble polymer having three or more arms, at least three of which are covalently attached to an active agent, e.g., a small molecule. The conjugates of the invention provide an optimal balance of polymer size and structure for achieving improved drug loading, since the conjugates of the invention possess three or more active agents attached, preferably releasably, to a water soluble polymer. In one embodiment, each of the arms of the water soluble polymer possesses an active agent covalently attached thereto, preferably by a hydrolyzable linkage.
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