CHOLINESTERASE REACTIVATORS AS ANTIDOTES

                                       Reaktivátory-vzorec oximu

Technology Owner
University of Hradec Králové

Intentor
Kamil Musílek

IPR Status
unpublished data

Stage of Development
In-vivo validation

Contact
Lucie Bartošová
lucie.bartosova@fnhk.cz
+420 727 802 314

CHOLINESTERASE REACTIVATORS AS ANTIDOTES

Background
Acetylcholinesterase (AChE) reactivators are used as antidotes in nerve agent (NA) or organophosphorus (OP) pesticide poisonings. Although the reactivator development started in the 50s of the 20th century, there is currently no universal reactivator able to reactivate AChE inhibited by any NA or OP pesticides. Such universal antidote could be called broad spectrum reactivator. Therefore, it is necessary to know the agent that caused the intoxication because effective treatment (specific antidote) must be given as soon as possible, but that is not realistic in the practice.

Description of the Invention
We synthesized and tested a number of new reactivators with modified structure to increase reactivation efficiency. Reactivation ability of these new nucleophiles is much higher in comparison with the standards (pralidoxime, obidoxime, methoxime) and moreover toxicity is much lower when compared with e.g. pralidoxime.

Advantages

  • completely new structures
  • broadspectrum effect
  • low toxicity
  • it is not possible to perform II and III clinical phase of testing these drugs (thus drug approval process is significantly facilitated and reduced)

Competing Technologies
Intentional poisoning with organophosphorus pesticides poses a problem particularly in developing countries and causes death of about 200,000 people annually. Unintentional poisoning kills far fewer people, but still it represents problem in places where very toxic organophosphorus pesticides (WHO toxicity class I) are used. Unfortunately the targeted medical treatment availability is poor, and in more than 15% cases poisoning has fatal consequences. Chemical weapons production and use are now strictly regulated by numerous international conventions, nevertheless their misuse cannot be avoided. Chemical weapons are surprisingly easily accessible and additionally very effective. Therefore the improving protection effect of antidotes is high topical issue, especially with respect to terrorist attacks on Japan Tokyo subway in 1995, and a year before in Matsumoto.

Download in pdf here: technology summary – REACTIVATORS ENG

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