New Non-Opioid Analgesic Offers Effective Pain Relief with Reduced Risks

Researchers at Kyoto University have announced the development of a groundbreaking pain-relief medication called ADRIANA, which operates through a novel mechanism and may serve as a promising alternative to traditional opioids. Opioids like morphine are commonly used for severe pain management but are associated with serious side effects such as respiratory depression and addiction, leading many countries, including Japan, to enforce strict prescribing regulations.

The global opioid crisis has intensified over recent years, with misuse of synthetic opioids like fentanyl resulting in over 80,000 deaths in 2023 in the United States alone. The search for safer painkillers is thus more urgent than ever.

Kyoto University’s team focused on the body's natural pain suppression pathways involving noradrenaline, which is released during critical situations to activate specific receptors (α2A-adrenoceptors). While substances mimicking noradrenaline can reduce pain, they often cause dangerous cardiovascular effects owing to interactions with other receptor subtypes.

To address this, researchers hypothesized that selectively inhibiting α2B-adrenoceptors could increase noradrenaline levels, thereby activating α2A-adrenoceptors to provide pain relief without adverse cardiovascular consequences. Using innovative screening technology, they discovered the first compound that specifically blocks α2B-adrenoceptors. This compound demonstrated safety and efficacy in animal studies.

Subsequently, clinical trials led by physicians at Kyoto University validated its potential. Phase I trials with healthy volunteers and Phase II trials involving patients post-lung cancer surgery showed promising analgesic effects. Preparations are now underway for large-scale Phase II trials in the United States in partnership with BTB Therapeutics, Inc.

As Japan’s first non-opioid analgesic, ADRIANA could significantly impact the management of severe pain worldwide. Moreover, it presents a strategic solution to the opioid crisis by offering effective pain relief without the risks of addiction and respiratory depression.

Professor Masatoshi Hagiwara emphasized the broader goal of this research: to evaluate ADRIANA’s effectiveness across various pain types and provide an accessible, safer alternative for patients suffering from chronic pain. This innovation holds promise not only for improving individual patient outcomes but also for contributing to global public health efforts against opioid dependency.

Source: Medical Xpress