Doctors are preparing to give patients a vaccine that blocks the effects of fentanyl.

Scientists are preparing to begin the first human trials of a pair of vaccines designed to block the effects of fentanyl and heroin.

The hope is to prevent people from accidentally consuming a lethal dose, a grim result that has become a significant risk, especially in the US. In 2021 alone, tens of thousands of people died in the country as a result of an opioid overdose, according to the National Institute on Drug Abuse. And opiate-related deaths have been on the rise since at least 1999, the numbers show.

But a simple injection that could allow the body to neutralize the fentanyl and heroin in the body could help change the situation, or at least that’s the hope.

“In principle, as a vaccine, it’s very simple,” said Jay Evans, director of the Center for Translational Medicine at the University of Montana and co-founder of Inimmune, the corporate partner tasked with ramping up production of the vaccine. futurism. “You can generate an antibody response against the drug. If that antibody binds to the drug in the bloodstream, it prevents it from crossing the blood-brain barrier.”

In simple terms, the vaccine effectively eliminates the “high” of the drug, as the drug is not able to spread to the brain. In theory, this could be a powerful weapon against addiction.

The antibody attaches to fentanyl “like a sponge,” explained Marco Pravetoni, a professor of psychiatry and behavioral sciences at the University of Washington who is also involved in the research, in a separate interview. “And that fentanyl is no longer available to reach the brain and activate the opiate receptors. So it’s essentially removed from the circulation.”

The idea is to block the effects of opioids while allowing other opioid-specific treatments, such as Narcan, the trademark for naloxone, which can reverse a life-threatening overdose via a nasal spray, to still be effective.

Another issue: The vaccine could prevent fentanyl from being used as a legitimate medicine, such as in anesthesiology.

“Several physicians, especially anesthesiologists, emailed me and said, ‘How are we going to treat patients in the operating room who get this vaccine?’” Evans said.

Fortunately, there are many other medications that healthcare professionals can still turn to once the vaccine is administered to the patient.

“The vaccine is very specific for fentanyl and fentanyl analogues,” Pravetoni told Futurism, “so you can still use anesthetics.

Preclinical studies involving animal models have also shown that vaccines spare “critical drugs such as methadone, buprenorphine, naltrexone and naloxone, which are used in the treatment of opioid dependence and overdose reversal”, as Pravetoni explained in a statement about the search.

The current opioid crisis has been in the making for decades. Fentanyl was first introduced in the 1960s as an intravenous anesthetic. It is about 100 times more potent than morphine and 50 times stronger than heroin when it comes to pain relief.

Its recreational effects have made it a particularly popular street drug. It’s notoriously easy to overdose on the drug outside of a hospital setting, especially when it comes to synthetic fentanyl sold illegally in powder form or mixed with other drugs. A few grains can be enough to be fatal.

The concept of opioid vaccines has been around “for a long time,” Pravetoni said. futurism. Literature from the 1970s showed that “essentially, you could vaccinate a non-human primate and stop it from self-administering heroin”, a line of research that was soon abandoned.

As more opiates entered the picture and became available to the public, “the concept of opioid immunotherapy, both for addiction and overdose, has been on hold,” he added. “So there was a delay in the search.”

In the 1990s and early 2000s, researchers including Pravetoni began investigating nicotine and cocaine-targeted vaccines.

While some of these vaccines made it to Phase 3 clinical trials, none of them “really made it to the market,” Pravetoni explained.

Fast forward several decades and the enthusiasm behind opioid vaccine development has picked up again, with Evans, Pravetoni and their colleagues picking up where they left off, applying what they learned from their earlier efforts.

This is largely due to the Helping to End Addiction Long-term Initiative (HEAL) initiative of the National Institutes of Health (NIH), which made tens of millions of federal dollars available for Marcetoni and Evans to investigate these vaccines.

In fact, Evanssays that his research is 100% funded by the NIH.

While it is still too early to determine the effectiveness of these vaccines in humans, there are initial reasons for optimism.

Preclinical trials, as explained in two articles published in the journal NPJ vaccines earlier this year, they showed that the vaccine was able to prevent fentanyl from reaching the brains of rats and pigs.

After vaccination, fentanyl doses “had no effect” in these animals “because they don’t reach the receptor,” explained Evans. “And then it’s recycled from the body.”

More specifically, the implication is that “the vaccine will prevent the respiratory depression or bradycardia that are associated with overdoses and fatal overdoses, but it will also prevent the euphoric or euphoric effects,” Pravetoni told us.

This could be a great solution for those “who are addicted to fentanyl or heroin and they go into rehab and want to stop and it’s really hard to stop,” Evans said.

Unfortunately, there’s always the possibility that someone might try to chase the high after being vaccinated against fentanyl and turning to other medications, something “the vaccine won’t prevent,” Evans explained.

Then there is the stigma surrounding addiction.

“You’re not afraid to tell someone if you have the flu, if you have COVID, but you’re afraid to tell someone if you’re addicted to opioids” because of “this negative stigma about it,” Evans said.

Pravetoni hopes that a vaccine could provide “broader acceptance” and “open more avenues” for people who are “not interested” in taking opioids due to existing stigmas.

Now, Evans, Pravetoni and their colleagues are starting the process of clinical trials designed to test the safety of these vaccines, the first step in what is likely to be a long, years-long process.

Phase 1 trials, which will take place at Columbia University in New York and are expected to start in early 2024, will see participants already using these drugs take increasing doses of the vaccines to ensure they are safe.

If these initial clinical trials are successful, phase 2 trials could then determine how many doses would be needed and at what intervals to be effective. Finally, phase 3 trials would allow the US Food and Drug Administration to assess whether any potential risks are outweighed by the vaccines’ benefits, recruiting much larger numbers of participants.

“It takes many years to come to an approved final product,” Evans said in the statement. “Based on the efficacy data we see in our preclinical data and the safety profile established in animal models, we are very hopeful that these vaccines will be successful.”

“But there is still a lot of work to be done,” he added.

In a perfect world, Evans said he expects the vaccine’s effects to last only a few years.

“Patients who are addicted to opioids and want to quit smoking and go through rehab, the chance of relapse in the first two years is 80 to 90 percent,” he said. “If they make it past those two years, the odds of staying clean are very good. So our goal is to protect people during those two years when they are most at risk of re-overdosing.”

“And so we want the antibody titers to stay really high for a few years and then go down over time,” explained Evans. “So if that patient, ten years later, went into surgery or had an accident and needed to use fentanyl as a pain-relieving medication, then it would be available to that person again.”

In the end, vaccines, if they ever reach the market, will only be a small part of a much larger picture.

“Essentially, you need all the help you can get, so hopefully vaccines and antibodies can provide that extra layer of protection,” Pravetoni told us.

Then there is our healthcare system’s current reliance on opioids.

“Ultimately, I would love to see non-opioid pain relievers that are as effective as opioid-based pain relievers,” Evans said, “and for all opioid-based pain relievers to basically become illegal drugs. who are becoming addicted aren’t because they’re dealing with chronic pain.”

It’s part of a much bigger and immensely complex picture, and many factors must be taken into account, from “how doctors prescribe opioids and how they educate patients about how to take these opioids to prevent addiction” to “reducing the stigma around addiction” , according to Evans.

“As long as that stigma exists, it will be difficult to get patients treated who really need it,” he added, arguing that public education is a “big part of that.”

“A toolbox is needed to help with this crisis,” Evans said. “The vaccine alone is not going to solve this.”

More about fentanyl vaccines: New vaccine blocks fentanyl in rat brains