Opioid compositions resistant to overdose and abuse
AssigneeElysium Therapeutics, Inc.
InventorThomas E. JENKINS
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Abstract
The invention provides pharmaceutical compositions comprising macromolecular gastrointestinal enzyme-labile opioid prodrugs, co-formulated with small-molecule and/or macromolecular gastrointestinal enzyme inhibitors. The macromolecular constructs are minimally absorbed from the GI tract, and can produce non-linear pharmacokinetic profiles of the delivered opioid agonist following oral ingestion. An optional macromolecular opioid antagonist may also be present in compositions of the invention to discourage tampering by potential abusers.
Claims36
A composition comprising:
- a gastrointestinal enzyme inhibitor, or a pharmaceutically acceptable salt thereof, and
- a therapeutically-effective amount of a macromolecule of formula:
- or a pharmaceutically acceptable salt thereof, wherein:
- PD is a gastrointestinal enzyme-labile opioid agonist prodrug;
- X is a linker group that covalently joins PD to a polymer;
- P is a polymer;
- and
- n is 1 or 2.
The composition of claim 36, wherein D is
- AA is a side chain of lysine or arginine;
- and
- R is independently hydrogen, methyl, ethyl, or a natural or unnatural amino acid.
A method for treating a condition, the method comprising administering to a subject in need thereof a therapeutically effective amount of a macromolecule of formula
- and a macromolecule of formula:
- wherein:
- PD is a gastrointestinal enzyme-labile opioid against prodrug;
- I is a gastrointestinal enzyme inverse substrate;
- each X1 and X2 is independently a linker group that covalently joins I to a polymer;
- P1 and P2 are a polymer, wherein each P1 and P2 is independently selected to provide less than 20% absorption of the macromolecule from the gastrointestinal tract of a subject following oral administration;
- and
- n is from 1 to 1000.
Dependencies are inferred from the claim text.