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US 2016/0243111 A1Published application
Pegylated Opioids with Low Potential for Abuse
AssigneeNektar Therapeutics
InventorsC. Simone Jude-Fishburn, Timothy A. Riley, Alberto N. Zacarias, Hema Gursahani
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Abstract
The invention provides opioid agonists covalently bound to a water-soluble oligomer having reduced potential for substance abuse and uses thereof. The compounds of the invention possess altered pharmacokinetic profiles relative to the opioid agonists alone, but are not subject to the risk of physical tampering that allows for the recovery and abuse of the opioid agonist associated with certain alternative delivery formulations.
Claims16
An opioid agonist compound of the formula:
- OP-X-POLY
- wherein:
- OP is an opioid compound selected from the group consisting of fentanyl, hydromorphone, methadone, morphine, codeine, and oxymorphone;
- X is a stable linker;
- and
- POLY is a small PEG moiety;
- and OP-X-POLY (i) binds to an OP target receptor that is the same target receptor to which OP in its unconjugated form binds, and (ii) exhibits a less than about a 10-fold loss of affinity for the OP target receptor relative to the affinity of OP to its target receptor.
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Dependencies are inferred from the claim text.