First Light-activated Analgesic May Change How Pain Disorders Are Treated, Study Suggests

First Light-activated Analgesic May Change How Pain Disorders Are Treated, Study Suggests

Scientists at the Institute of Neurosciences of the University of Barcelona helped develop the first light-activated drug, called JP-NP-26, for the treatment of pain. This novel strategy may revolutionize how we treat pain disorders such as fibromyalgia.

The study, “Optical control of pain in vivo with a photoactive mGlu5 receptor negative allosteric modulator,” was published in the journal eLife.

The development of drugs according to existing pharmacology is often impaired by constrains such as the difficulty in following the drug in time once delivered, the time required to assess the correct dosages, and cases where the drug is slow or affects multiple tissues.

A new field in pharmacology called optopharmacology was developed to overcome some of these constrains. This new discipline uses light to control drug activity. This means that if a drug is developed to be light-sensitive, then scientists can actually control the drug’s activity in a spatial and temporal manner.

The study reports the development of a “photo-drug” – called JF-NP-26 – that demonstrated a potent therapeutic value for treating pain.

“In the clinical field, there is not any precedent of the uses of optopharmacology to improve pain treatment or any disease associated with the nervous system. This is the first light-activated drug designed for the treatment of pain in vivo with animal models,” Prof. Francisco Ciruela at the University of Barcelona and the study’s co-lead author, said in a press release.

In this new optopharmacology approach, scientists can use an analgesic for which the mechanism of action is known, and turn it into a photosensitive and inactive drug. Using light with a certain wavelength, the drug can be activated in a targeted and precise region, such as the brain or skin.

JF-NP-26 is also called photocaged, since it only exerts its activity when activated by light. Without light, it remains inactive.

In fact, when compared to other photosensitive compounds, JF-NP-26 shows no effect inside an animal until a specific beam of light (in this case, 405 nm wave length) hits the target tissue. Of note, JF-NP-26 showed no toxic or unwanted effects even in high dosages.

The strategy is based on the release of the active molecule called raseglurant when the drug receives light. This molecule is then free to block the metabotropic glutamate type 5 (mGlu5) receptor, responsible for propagating neuronal pain.

“The molecule created by the action of the light, the raseglurant, does not belong to any group of drugs from the classic anti-pain list of drugs: non-steroidal anti-inflammatory drugs or NSAID (paracetamol, ibuprofen, etc.) and opioids (morphine, phentanyl),” Ciruela said. “Consequently, this study describes an analgesic mechanism which has not been explored enough so far.”

“Actually, the raseglurant was examined in clinical trials as an analgesic to treat migraine but it was ruled out due its hepatoxicity,” he added. “This new optopharmacology of the raseglurant can stop adverse effects in the liver and opens a new path to start using it as an analgesic.”

Optopharmacology may represent a potential new strategy for redefining the way we treat pain in fibromyalgia and other diseases. It may also help reduce the unwanted effects of several of the current drugs, such as morphine, and its high risk of addiction.

“If we compare natural biological molecules that act in living beings with drugs, we can see that the former can work with great precision, acting in centralized areas and with regulated doses, with defined lengths,” said second co-lead author Amadeu Llebaria, from the Medicinal Chemistry & Synthesis group of the Institute of Advanced Chemistry of Catalonia.

“However, the drugs we have act in all areas and without a strict control. The use of light-controlled molecules tries to complete these spaces to get more precise drugs that can act like biological molecules,” LLebaria said.

8 comments

  1. Sandra says:

    Um…how can you use something that needs to be light activated when the pain is all over your entire body? They still really don’t get Fibro.

    • Mary says:

      I was actually just thinking the same thing. On my “good days” the pain stays in my legs and lower back. On my “bad days” it spider webs through my whole body. So if they only have it activated for my legs what am I suppose to do on a bad day??

  2. StevefromMA says:

    I think it is blocking glutamate in the brain and therefore blocking the wrongful stimulation of our nerves at the brain level. It bypasses the blood brain barrier apparently, not clear, and I’m at the limits of my biology here. Why does most fibro research seem to be coming out of SA and Europe not here, where Big Pharma keeps running studies with the same crap meds until one finally shows they are wonderful?

  3. NOLA says:

    Problem with a lot of drugs on the market today is the side effects they may cause. This sounds very promising but appears is only tested so far in animals, not as yet human trials. It appears for example if one’s neck and shoulders were in spasm/pain…they could take an EXISTING opioid drug like morphine and turn it into a photosensitive and inactive drug. SO when the drug is taken it remains inactive in the body UNTIL a SPECIFIC BEAM of light HITs or Targets SPECIFIC TISSUE (so in this example if targeting neck and shoulders specifically, the drug taken lays inactive in the body until that specific tissue receives the specified beam of light. Using drugs in this process may mean a substantial reduction of the unwanted side effects you get when taking the original morphine opioid! Wouldn’t that be great!!

  4. Kim cousins says:

    I wonder if the powers that be realise that Fibromalgia is often triggered with light in the eyes? And answer would be very welcomed ☺️

    • Alison says:

      I have to agree With you Kim. I wear glasses but they have tinted lenses for three glare. But this research sounds promising. ?

  5. Caprice Whitmire says:

    This sounds very promising. I’m assuming that the drug that is made photosensitive is dispersed throughout the whole body via the bloodstream, so if you have pain in certain areas more than others, the beam of light would be targeted to those areas. It would be more advantageous if the physician that prescribes the medication gives you a device that emits the correct frequency of the light. Then you could target whichever areas are a problem for you. It also sounds like it would solve much of the “Opioid Crisis” that has been touted so much in the US lately. If a person stole or purchased the photosensitive medication, they would be unable to get the effects from it without having the light frequency needed to activate it.

    As far as the forward-thinking research coming from Europe and South America, it’s because Big Pharma doesn’t want new drugs and treatments developed because their pets they developed for fibromyalgia would then be unused by the patients who don’t get the effects from those that are promised. Also, fibromyalgia is still not a “real disease” to many physicians in the US because there is no definitive blood test to diagnose it. Instead, it’s what’s left when all the other diseases that can be detected from a blood test are negative.

    • Tim Bossie says:

      Thank you for sharing your thoughts Caprice. You’re right, many doctors in the US will not diagnose Fibro as there is no “test” to make sure. We hope that these light activated therapies will become available in all areas so that people who suffer with this disease can finally get some relief.

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