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US 9,040,032 B2Granted
Compositions comprising enzyme-cleavable opioid prodrugs and inhibitors thereof
AssigneeSignature Therapeutics, Inc.
InventorsThomas E. Jenkins, Craig O. Husfeld, Julie D. Seroogy, Jonathan W. Wray
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Abstract
Pharmaceutical compositions and their methods of use are provided, where the pharmaceutical compositions comprise an opioid prodrug that provides enzymatically-controlled release of an opioid, and an enzyme inhibitor that interacts with the enzyme(s) that mediates the enzymatically-controlled release of the opioid from the opioid prodrug so as to attenuate enzymatic cleavage of the opioid prodrug.
Claims51
A composition comprising:
- an opioid prodrug comprising a ketone-containing opioid covalently bound to a promoiety comprising a GI enzyme-cleavable moiety wherein the hydrogen atom of the corresponding enolic group of the ketone is replaced by a covalent bond to the GI enzyme-cleavable moiety, and wherein cleavage of the GI enzyme-cleavable moiety by a GI enzyme mediates release of the opioid;
- and
- a GI enzyme inhibitor that interacts with the GI enzyme that mediates enzymatically-controlled release of the opioid from the opioid prodrug following ingestion of the composition.
Dependencies are inferred from the claim text.