Professor developing cocaine overdose drug

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UK pharmaceutical sciences professor Chang-Guo Zhan is working on the first FDA-approved drugs to treat cocaine overdoses and addiction in the Molecular Modeling and Biopharmaceutical Center, according to information specialist senior Keith Hautala in an article for UKNow.

There is currently no approved treatment for potentially deadly cocaine overdose. Zhan’s drugs, funded by grant money from the National Institutes of Health, are currently in clinical human trials, Zhan told Hautala.

Using an enzyme from bacteria found in the soil where coca, the source of cocaine, is grown, Zhan hopes to use one drug to neutralize cocaine in the bloodstream and another to remain in the body to nullify the effects of drug use, which should help break the cycle of addiction, he told Hautala.

The enzyme, called bacterial cocaine esterase, helps break down cocaine into less-harmful products. In nature, the enzyme decays too quickly to be of use in medicine, with a half-life of about 12 minutes at human body temperature.

Zhan and a team of researchers from UK, Columbia University and University of Michigan introduced mutations to the enzyme in an attempt to keep the qualities they wanted while rooting out any problems that would make it unusable as a drug, Zhan told Hautala.

By using the enzyme, the number of possible treatments has been narrowed down to a few efficable options, instead of the work that would go in to testing thousands of compounds.

The team introduced two mutations that have made the enzyme stable for up to six hours and increased its ability to chemically break down cocaine 4,000 times.

Both drugs should neutralize the effects of cocaine, Zhan told Hautala, but the overdose treatment will have to work quickly to save patients’ lives, while the goal of the other is to remain in effect for a longer period of time so that a patient who takes more of the drug will not feel those effects either and may stop the addiction cycle.

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