Nucleotide-based prodrugs
AssigneeGilead Sciences, Inc.
InventorStephen Warren
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AssigneeGilead Sciences, Inc.
InventorStephen Warren
Estimating the term…
This invention relates to nucleotide-based prodrugs and their drug-delivery applications. The nucleotide-based prodrugs of the present invention comprise a drug component covalently attached via junctional ester bond(s) to one or more nucleotide components. Release and activation of the drug component of a nucleotide-based prodrug arises from hydrolysis of the junctional ester bond joining the nucleotide component to the drug component. The active drug component may be a nucleoside analog, a nucleic acid ligand, or a non-nucleoside drug. The nucleotide component provides a means of targeting and/or anchoring the nucleotide-based prodrug to the desired tissue compartment and/or a mechanism of sustained release of the active drug, thereby providing for a more effective drug delivery system with reduced toxicity. The targeting and/or anchoring of the nucleotide-based prodrugs to the desired tissue can be achieved through several methods, including employing a nucleic acid ligand as the nucleotide component, and/or by incorporating photocrosslinkable bases into the nucleotide component, and/or by covalently bonding the nucleotide component to a macromolecular support. The invention further includes lipid constructs comprising a nucleotide-based prodrug.
A nucleotide-based prodrug comprising a nucleotide component covalently bonded via a physiologically hydrolyzable junctional ester bond to a drug component;
A nucleotide-based prodrug comprising a nucleotide component covalently bonded via a physiologically hydrolyzable junctional ester bond to a drug component;
A method of preparing a nucleotide-based prodrug;
A method of preparing a nucleotide-based prodrug;
Dependencies are inferred from the claim text.