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E12-7Fc-M3 demonstrates efficacy as treatment for cocaine overdose

Posted: 10 November 2015 | Victoria White

E12-7Fc-M3 not only demonstrated a significantly improved efficiency against cocaine, but also had a considerably prolonged biological half-life in animal models…

A long-acting enzyme that rapidly and safely metabolises cocaine in the blood stream is currently being investigated in animal models as a possible treatment for cocaine overdose.

A research team from the University of Kentucky previously designed and tested CocH1, an enzyme that specifically breaks down cocaine without producing harmful by-products in the body as a result. The researchers are currently evaluating a novel enzyme, E12-7Fc-M3 for its ability to neutralise cocaine in the blood stream using molecular modelling technology. E12-7Fc-M3 was tested in vivo to examine its activity against cocaine – following injection of cocaine into mice and rats, scientists gave the cocaine-metabolising enzyme to the animals intravenously.

E12-7Fc-M3 demonstrated a prolonged biological half-life in animal models

E12-7Fc-M3 not only demonstrated a significantly improved efficiency against cocaine, but also had a considerably prolonged biological half-life in mice and rats of roughly 110 hours, compared to the half-life of CocH1-HSA (a pharmaceutical formulation of CocH1), which was only about eight hours. A single administration of 0.25 mg/kg E12-7Fc-M3 followed by multiple doses of 5 mg/kg E12-7Fc-M3 was shown to accelerate cocaine hydrolysis in mice and rats for at least 20 days. A single dose of 2.5 mg/kg E12-7Fc-M3 was also found to completely eliminate 25 mg/kg of cocaine in mice and rats for at least seven days.

“This next stage of our research is promising, showing that the enzyme has extended function in small animal models and potentially even longer in humans,” said Chang-Guo Zhan, Ph.D, College of Pharmacy at the University of Kentucky. “We envision that this therapy could eventually become a viable treatment option in emergency rooms for people who overdose on cocaine.”

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