Polyheterocyclic uncharged bisoxime antidotes for organophosphate poisoning and methods for making and using them

Polyheterocyclic uncharged bisoximes overcome the limitations of existing antidotes by diffusing across biological membranes to rapidly and completely reactivate AChE in both peripheral and central nervous systems, providing faster and more effective recovery from organophosphate poisoning.

WO2026043719A1 Publication Date: 2026-02-26RGT UNIV OF CALIFORNIA
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Patent Information

Application Number
PCT/US2025/042060
Authority / Receiving Office
WO · WO
Patent Type
Applications
Current Assignee / Owner
Priority Date
2024-08-19
Filing Date
2025-08-14
Publication Date
2026-02-26

AI Technical Summary

Technical Problem

Current antidotes for organophosphate poisoning, such as pralidoxime, obidoxime, and asoxime, are unable to cross the blood-brain barrier and effectively reactivate brain acetylcholinesterase (AChE), leading to incomplete recovery from organophosphate intoxication.

Method used

Development of polyheterocyclic uncharged bisoxime compounds that can spontaneously diffuse across biological membranes, including the blood-brain barrier, to rapidly reactivate both peripheral and central nervous system AChE, offering faster and more complete recovery from organophosphate poisoning.

Benefits of technology

The polyheterocyclic bisoximes provide several-fold faster and more complete reactivation of inhibited AChE compared to existing antidotes, enabling life-saving recovery at lower doses and allowing for oral administration, thereby addressing the limitations of current antidotes.

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Abstract

In alternative embodiments, provided are polyheterocyclic uncharged bisoxime antidotes, including polyheterocyclic uncharged bisoximes, and methods for treating, preventing or ameliorating excessive acetylcholine stimulation in the brain comprising administering to an individual in need thereof a polyheterocyclic uncharged bisoxime antidote as provided herein. In alternative embodiments, provided are methods for treating, preventing or ameliorating excessive acetylcholine stimulation in the brain; or, treating, ameliorating or protecting (preventing) an organophosphate toxicity or poisoning or toxic exposure, or for treating, ameliorating or protecting (preventing) organophosphate inhibition of an acetylcholinesterase (AChE) comprising administering to an individual in need thereof a polyheterocyclic uncharged bisoxime antidote as provided herein.
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