Shares of GB Sciences (OTCQB: GBLX) gained nearly 14% on Wednesday after the company reported that it filed a patent application for exclusive formulations to treat chronic pain based on new molecular docking simulations and functional assay data.
By combining functional testing and computational modeling, GBS has designed complex mixtures of active ingredients from the cannabis plant through simultaneously inactivating or desensitizing several of the pain-sensing, Transient Receptor Potential (TRP) Superfamily members. These formulations have the potential for enhanced pain relief.
The patent application seeks to protect these cannabinoid-containing complex mixtures and addresses GBS’ method for selecting cannabis-derived compounds based on data from high throughput screening assays, electrophysiology of the TRP channels, and molecular docking simulators.
GBS and their research partners at Chaminade University are the first to model the putative TRPV1-binding sites of myrcene and cannabidiol, two of the active ingredients in their complex mixtures for chronic pain. They have used information on the molecular interactions within these TRPV1-binding pockets to discriminate between the potential pain-relieving benefits of other cannabis-based compounds in their initial cannabis-derived mixtures.
“Unlike others who are narrowly focused on using a very limited number of cannabinoids for the treatment of pain, we embraced the complexity of whole-plant cannabis extracts and then optimized these mixtures using both functional assays and computer modeling, which has allowed us to seek patent protection for groundbreaking chronic pain therapies,” Chief Science Officer and Director Dr. Andrea Small-Howard stated.
“Our complex mixtures of cannabis-based TRP ligands were designed to desensitize multiple TRP channels simultaneously, while avoiding the neuronal cytotoxicity and numbness accompanying the harsh capsaicin-based topical pain relievers on the market today that work through hyperactivation of the TRPV1 channel in a way that kills TRPV1-containing sensory neurons,” Small-Howard added.
GBS and their partners in chronic pain research at Chaminade University have focused on the Transient Receptor Potential (TRP) superfamily ion channels because they are known to be involved in certain types of pain; for example, TRPV1 is the molecular target for capsaicin-based topical pain relievers.
Last month, GBS, Chaminade University, and the University of Hawai’i published a paper on the use of cannabinoids for pain in the journal “Channels” showing the potential analgesic effects of cannabinoids by demonstrating that a variety of specific cannabinoids differentially affect the individual pain-sensing receptors in the TRP family.
GBS is designing complex mixtures of cannabis-based ingredients based on their ability to regulate pain receptors in the TRP family located in sensory neurons.
New pain treatments are a vitally important area of research and development given the widespread rates of addiction and mortality tied to opioids. Opioid addiction affects 1.7 million Americans, kills approximately 50,000 individuals per year, and has an emerging health economic burden of $78.5 billion per year. In the U.S., chronic pain represents an estimated health burden of between $560 and $650 billion.
