Polysubunit opioid prodrugs resistant to overdose and abuse
AssigneeElysium Therapeutics, Inc.
InventorThomas E. Jenkins
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Abstract
The invention provides compositions and methods for the treatment or prevention of pain. The invention provides constructs whereby hydrolysis of the construct by a specified gastrointestinal enzyme directly, or indirectly, releases an opioid when taken orally as prescribed. The gastrointestinal enzyme mediated release of opioid from constructs of the invention is designed to be attenuated in vivo via a saturation or inhibition mechanism when overdoses are ingested. The invention further provides constructs that are highly resistant to oral overdose, chemical tampering, and abuse via non-oral routes of administration.
Claims35
A compound represented by the structure of Formula (I):
- or a salt thereof, wherein:
- Q is independently selected from optionally substituted heteroalkyl and optionally substituted alkyl;
- L1 is independently at each occurrence absent or a cleavable or non-cleavable linker;
- L2 is independently at each occurrence absent or a cleavable or non-cleavable linker;
- R1 is independently selected at each occurrence from a GI enzyme substrate, a GI enzyme inhibitor, and an opioid antagonist;
- R2 is an opioid agonist covalently bound to a GI enzyme substrate;
- and
- m and n are independently selected at each occurrence from 1 to 1,000,000.
Dependencies are inferred from the claim text.