Polymer conjugates of opioid antagonists
AssigneeNektar Therapeutics
InventorsMichael James Roberts, Xiaoming Shen, Lin Cheng, Michael David Bentley
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Abstract
The invention provides polymer conjugates of opioid antagonists comprising a polymer, such as poly(ethylene glycol), covalently attached to an opioid antagonist. The linkage between the polymer and the opioid antagonist is preferably hydrolytically stable. The invention also includes a method of treating one or more side effects associated with the use of opioid analgesics, such as constipation, nausea, or pruritus, by administering a polymer conjugate of the invention.
Claims12
A method of treating constipation resulting from the administration of an opioid agonist to a patient in need thereof, said method comprising administering to the patient in need thereof a therapeutically effective amount of a polymer conjugate of the formula:
- or pharmaceutically acceptable salt thereof, wherein:
- Y is allyl;
- Z is OH;
- X is —NHC(O)—, —NH—, —OC(O)NH—, —O—, —S— or —NHC(O)NH—;
- and
- POLY is methoxy poly(ethylene glycol), wherein POLY has a molecular weight of from about 100 Da to about 2,000 Da.
A method of treating nausea resulting from the administration of an opioid agonist to a patient in need thereof, said method comprising administer to the patient in need thereof a therapeutically effective amount of a polymer conjugate of the formula:
- or pharmaceutically acceptable salt thereof, wherein:
- Y is allyl;
- Z is OH:
- X is —NHC(O)—, —NH—, —OC(O)NH—, —O—, —S— or —NHC(O)NH—;
- and
- POLY is methoxy poly(ethylene glycol), wherein POLY has a molecular weight of from about 100 Da to about 2.000 Da.
A method of treating pruritus resulting from the administration of an opioid agonist to a patient in need thereof, said method comprising administering to the patient in need thereof a therapeutically effective amount of a polymer conjugate of the formula:
- or pharmaceutically acceptable salt thereof, wherein:
- Y is allyl;
- Z is OH;
- X is —NHC(O)—, —NH—, —OC(O)NH—, —O—, —S— or —NHC(O)NH—;
- and
- POLY is methoxy poly(ethylene glycol), wherein POLY has a molecular weight of from about 100 Da to about 2,000 Da.
Dependencies are inferred from the claim text.