Schematic Diagram & Description

The URB937 drug is excluded from the brain by a transporter with a pharmacology resembling BCRP, but is free to act on peripheral FAAH. The site of analgesic action is most likely peripheral pain-sensing nerve endings (red circle). Expanded red circle shows the predicted molecular mechanism of drug action, inhibition of FAAH-catalyzed metabolism of anandamide (AEA), which allows for persistent AEA activation of peripheral CB1 receptors on peripheral nerve endings. Activation of CB1 receptors ultimately reduces transmission of pain signals to the spinal cord, preventing pain sensation (Modified from Nature Neuroscience).

A transformative therapy for non-addictive management of chronic and acute pain

Based on preclinical efficacy data, mechanism of action and a significant unmet medical need, Exxel Pharma is developing URB937 as a transformative therapy for non-addictive management of chronic neuropathic pain. The clinical lead indication is Chronic Neuropathic Pain of Peripheral Neuropathy, representing a market that has been estimated to reach $3.6 billion by 2020 (Nature Reviews), and which is ripe for disruption by novel, safe, non-addictive therapies such as URB937.

Summary of recent preclinical studies showing efficacy of URB937 in different pain models

Animal model Species Gender Comparative analgesic efficacy Reference
Inflammatory Pain
Carrageenan Mouse Male Superior to URB597 Clapper et al., 2010
Mouse Male Superior to Indomethacin and Gabapentin Sasso et al., 2012
Synergistic with Indomethacin
Rat Female Superior to Indomethacin Moreno-Sanz et al., 2012
Formalin model Rat Male Clapper et al., 2010
Complete Freud’s adjuvant (CFA) Mouse Male Superior to URB597, PF-04457845 and Sasso et al., 2012
Dexamethasone
Neuropathic Pain
Chronic constriction injury (CCI) Mouse Male Comparable to URB597 Clapper et al., 2010
Mouse Male Superior to Indomethacin and Gabapentin Sasso et al., 2012
Synergistic with Indomethacin
Chemotherapy-induced neuropathy Rat Male Comparable to URB597 and Morphine Guindon et al., 2013
Superior to Gabapentin
Paclitaxel induced Mice Male Synergistic with Morphine Slivicki et al., 2018
Potential as opioid sparing therapy
Diabetes induced neuropathy Rat Male STZ induced Sasso et al., 2015
Postoperative Pain
Brennan model Mouse Male Synergistic with Ankle Joint Mobilization (AJM) Martins et al., 2013
Mouse Male Superior to URB597, PF-04457845, Indomethacin, Sasso et al., Unpublished
Gabapentic and Morphine
Accelerates wound healing
Visceral Pain
Acetic acid-induced writhing Mouse Male Comparable to URB597 and Indomethacin Clapper et al., 2010
Mouse Female Comparable to Indomethacin Moreno-Sanz et al., 2012

Key Publications

A list of published URB937 data, including work from international, academic research laboratories, can be foundĀ here.

For more information, pleaseĀ contact us.