SAN DIEGO, December 14, 2016 /PRNewswire/ — Abide Therapeutics, a developer of innovative pharmaceuticals, announced today initiation of dosing in a Phase 1b study to evaluate the effects of ABX-1431, a first-in-class investigational monoacylglycerol lipase (MGLL) inhibitor, on gastric accommodation in patients with functional dyspepsia (FD), a gastrointestinal disorder characterized by altered gut motility and pain.
“MGLL inhibitors have the potential to improve impaired gastric function as well as central nervous system dysfunction in patients with FD, one of the most common gastrointestinal disorders encountered in clinical practice,” said Alan Ezekowitz, MBChB, DPhil, CEO and President of Abide Therapeutics. “With this study, which is the first investigation of ABX-1431 in patients, we hope to show the potential for treatment of FD via endocannabinoid modulation.”
The Phase 1b FD study that is now underway will assess the effect of a single dose of ABX-1431 on gastric accommodation (relaxation of the stomach during food intake), satiety, epigastric symptoms, and psychological state in FD patients undergoing a nutrient volume tolerance test. ABX-1431 is an orally available small molecule that helps regulate the activity of the endocannabinoid system. The endocannabinoid system is believed to play a role in gastric motility and the perception of gastrointestinal-associated pain. Thus, ABX-1431 may be useful for the treatment of disorders of the gastrointestinal system characterized by altered gut motility or abdominal pain.
“Our previous work suggests endocannabinoid levels play a role in the pathophysiology of FD. We are excited to determine if ABX-1431 can improve the gastrointestinal abnormalities that underlie symptoms of this common disorder,” said Prof. Jan Tack, MD, PhD, Head of Clinic in the Department of Gastroenterology and Professor in Internal Medicine at the University of Leuven, Belgium. Prof. Tack is the Principal Investigator for this study.
ABX-1431 has successfully completed dosing in a first-in-human, placebo-controlled, Phase 1a study. The drug was well tolerated and there were no serious adverse events. Preliminary data from an ongoing PET occupancy study indicate dose-dependent brain penetrance of orally-administered ABX-1431 using [18F]ABX-1488, an Abide proprietary, MGLL-specific PET ligand. Furthermore, an fMRI study aimed at assessing the patterns of neural activity in the brain associated with ABX-1431 administration is scheduled to start in the fourth quarter of 2016.
About the Endocannabinoid System
MGLL is an enzyme that catalyzes the breakdown of the endocannabinoid 2-arachidonoylglycerol (2-AG), an endogenous ligand of the cannabinoid receptors CB1 and CB2, which are the molecular targets of the psychoactive component of cannabis, delta-9 tetrahydrocannabinol (THC). MGLL is the major regulator of 2-AG levels available to signal through CB1 and CB2. CB1 is the primary cannabinoid receptor in the nervous system, and its activation accounts for most of the neurobehavioral effects of THC. CB2 is found primarily on immune cells and mediates the immunosuppressive effects of cannabinoids. Direct activation of cannabinoid receptors by medicinal cannabis preparations elicits therapeutically beneficial effects on pain, spasticity, sleep, appetite, and nausea. ABX-1431 is expected to produce similar beneficial therapeutic effects through amplification of endogenous cannabinoid signaling.
About Abide Therapeutics
Abide Therapeutics is focused on developing innovative medicines that target serine hydrolases, one of the largest enzyme classes in nature with validated but mostly untapped therapeutic potential. Serine hydrolases play important regulatory roles in human physiology and disease. Abide has created a proprietary platform, based on technology developed at The Scripps Research Institute by Professors Ben Cravatt and Dale Boger, that specifically targets serine hydrolases with selective small molecules. The ability to target and modulate serine hydrolases has potential to develop new medicines in many therapeutic areas. Abide is located in San Diego. To learn more, visit www.abidetx.com.
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