Messing with Cannabinoid Receptors Can be Fatal

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In January, the University Hospital of Rennes in France released a statement indicating that one person had died and five others were hospitalized following a drug trial. In the weeks that have followed, it has been discovered that the drug being tested was designed to block necessary processes in the human Endocannabinoid Signaling (ECS) system. Instead of embracing a natural, plant-based medicine that has been shown to work for many conditions, researchers hell-bent on synthesizing cannabinoid therapy to ensure massive corporate profits accidentally killed one and disabled several others.

The drug trial’s Phase 1 began on January 7th, 2016, with 128 healthy volunteers (each paid roughly $2,000 USD) involved, ninety of whom were taking varying doses of the medication.  Phase 1 is how companies establish that the drug, which has already been tested on animals, is safe on humans. In this case, it proved to not be as safe as its creators had hoped.

Within three days, several participants were reporting severe, adverse reactions. Six of the participants were hospitalized, and one died after being declared brain dead. Of the five survivors, four are expected to likely suffer permanent disability due to neurological damage. That means that the drug created permanent brain damage in a small but substantial portion of volunteers who were involved in the drug trial. The fifth, who appears to have avoided the same fate, was hospitalized and monitored for some time. Others who were given the drug have been screened, but none appear to be manifesting the same devastating responses.

The medication being tested was intended to work on the ECS, but researchers have insisted from the beginning that the compound is not cannabis-derived or a synthetic cannabinoid. So what is BIA 10-2427? It’s a drug called a fatty acid amide hydrolase (FAAH) inhibitor.  In layman’s terms, the drug was meant to block the process by which the human body breaks down naturally-occurring cannabinoid compounds in the body, theoretically leading to an increase in cannabinoid levels and thus a decrease in the perception of pain and anxiety, as well as produce a possible improvement in motor function for those who struggle with disorders that impact motor function. Many other companies have developed similar drugs in the past, but none have ever been proved effective in clinical trials, so none are on the market.

The recent French trials were conducted by Biotrial International, and investigations so far have indicated the facility and practices involved with the trial were safe, as such things go. The drug itself, BIA 10-2427, was developed by Bial, a Portuguese science group, who stated the compounds was meant to be a painkiller, anxiety reducer, and aid for motor disorders. The company has stated that they have no explanation for the severe adverse reactions of the patients in the study.

Some researchers analyzing brain scans of those adversely affected have posited the theory that the drug BIA 10-2427 is operating “off-target,” preventing other, necessary proteins in the human body and brain from being properly processed. There is no known antidote for the drug. Because there has been much secrecy regarding the actual molecular composition of the drug BIA 10-2427, scientists and researchers are left grasping at straws, trying to figure out how a drug meant to manipulate the ECS could have caused catastrophic brain damage and death.

Research companies have had very negative results in the past when attempting to block cannabinoid receptors, as evidenced by the studies on Rimonabant (SR141716), a drug developed to block the CB-1 cannabinoid receptor to decrease appetite. Like BIA 10-2427, Rimonabant caused unexpected, severe side effects: it led to extreme depression and suicidal ideation in some taking the drug. There is also anecdote to indicate there were increased rates of cancer in people who took CB-1 blocking drugs. Rimonabant was never approved by the FDA because of this effect and was eventually taken off the market in Europe as well, less than two years after it was approved for sale in the EU.

Whether the tragic outcome of this study was the result of “off-target” function by the drug or by the synthetic blocking of cannabinoid receptors, there is little question that there is already known, safe substances that could produce the exact desired effects of this deadly drug trial: natural state cannabis and well-made cannabis extracts.

Instead of continuing to attempt to fully block or selectively block cannabinoid receptors or ECS function in humans, medical scientists and research chemists should focus instead on better understanding the function of the ECS and cannabinoids in the human body. With the incredibly rare exception of those with cannabis allergies, naturally-derived cannabinoids are known to be safe, with few negative side effects.


For previous Ladybud articles about the endocannabinoid system, click here.
Photo Credit: GerryShaw under CC BY -SA 3.0 via Wikimedia Commons