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.
Claims35
A compound of the formula:
- OP-X-POLY
- wherein OP is an opioid compound, X is a linker, and POLY is a small water-soluble oligomer.
A method of reducing, but not substantially eliminating, the rate of crossing the blood brain barrier of an opioid compound comprising conjugating the compound to a small water-soluble oligomer.
A prodrug comprising a mu, kappa, or delta opioid agonist reversibly attached via a covalent bond to a releasable moiety, wherein a given molar amount of the prodrug administered to a patient exhibits a rate of accumulation and a Cmax of the mu, kappa, or delta opioid agonist in the central nervous system in the mammal that is less than the rate of accumulation and the Cmax of an equal molar amount of the mu, kappa, or delta opioid agonist had the mu, kappa, or delta opioid agonist not been administered as part of a prodrug.
Use of a prodrug comprising a mu, kappa, or delta opioid agonist reversibly attached via a covalent bond to a releasable moiety for achieving a rate of accumulation and a Cmax of the mu, kappa, or delta opioid agonist in the central nervous system of a mammal to whom a given molar amount of prodrug is administered that is less than the rate of accumulation and the Cmax of an equal molar amount of the mu, kappa, or delta opioid agonist when administered to the mammal in non-prodrug form.
Dependencies are inferred from the claim text.