Blue-181 molecule acts on pain receptors on the spinal cord instead of in the brain and essentially produces no narcotic or addiction side effects, despite being 50 times more potent than morphine
The National Institute on Drug Abuse estimates that over 115 people in the United States alone die of opioids overdose a day. The opioid crisis has become a public emergency and has assumed an epidemic role in the country. For decades, the line between benefit versus harm in opioid usage has been blurry - a cause of serious concern.
After countless studies and clinical experiments, scientists are moving closer to developing a revolutionary painkiller. A team of Harvard-trained researchers in Massachusetts believe that they may be on the verge of developing a painkiller that does not carry the harmful adverse effect profile that comes with an opioid. This newly engineered painkiller makes use of the active molecule Blue-181 developed by Blue Therapeutics and hopes to deliver fifty times the pain-relieving effects of morphine.
Ajay Yekkirala, co-founder and chief scientific officer at Blue Therapeutics explains the pharmacodynamics of this revolutionary molecule: Blue-181 targets the pain receptors found in the spinal cord without affecting the opioid mu-receptors in the brain that lead to the addiction and dependency side effects. Blue-181 is to begin its first clinical trial soon but Yekkirala speculates that it will take around 5 years before this painkiller completes its clinical trials.
Earlier this year Tomas Joaquin Fernandez from the University of Michigan Medical School also proposed a newly engineered painkiller that clinically proven to reduce addiction and tolerance in animal subjects.
This drug was built with peptidomimetics – agents that ‘mimicked’ peptide chains and were small enough to breach the blood-brain barrier to act on the pain receptors in the central nervous system. While these peptidomimetics acted on the mu-receptors to produce a therapeutic response, they concurrently blocked the delta opioid receptors which resulted in attenuated physical dependency and tolerance.
“We are striving to solve the opioid epidemic by working at the most fundamental problem: the effective treatment of pain,” Fernandez explained. “Our work can also provide other researchers with a better understanding of opioid receptors and interactions between receptors, which could be exploited to develop better options for pain management.” The data on opioid misuse is sobering. With these latest studies underway, there may be a hope to diminish the opioid crisis and make non-addictive painkillers available for common use.
2. Fernandez, Tomas. “A Novel Approach to Safer Analgesics: Mu Opioid Receptor Agonist & Delta Opioid Receptor Antagonist Peptidomimetics.” ENDO 2017: The 99th Annual Meeting & Expo, plan.core-apps.com/eb2018/abstract/48a02c02-0f5b-48ab-98c3-106457143168.