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Peripheral FAAH inhibitor, URB937, as an opioid-sparing analgesic for chronic pain.

Award Information
Agency: Department of Health and Human Services
Branch: National Institutes of Health
Contract: 1R41NS106999-01A1
Agency Tracking Number: R41NS106999
Amount: $225,000.00
Phase: Phase I
Program: STTR
Solicitation Topic Code: 101
Solicitation Number: PA17-303
Timeline
Solicitation Year: 2017
Award Year: 2018
Award Start Date (Proposal Award Date): 2018-09-30
Award End Date (Contract End Date): 2019-09-29
Small Business Information
751 GRANT PL
Boulder, CO 80302-7412
United States
DUNS: 080790077
HUBZone Owned: No
Woman Owned: No
Socially and Economically Disadvantaged: No
Principal Investigator
 DANIELE PIOMELLI
 (949) 824-6180
 piomelli@uci.edu
Business Contact
 SOREN MOGELSVANG
Phone: (720) 261-1109
Email: soren@aspirebioscience.com
Research Institution
 UNIVERSITY OF CALIFORNIA-IRVINE
 
141 INNOVATION DRIVE, SUITE 250
IRVINE, CA 92617-3213
United States

 Nonprofit college or university
Abstract

PROJECT SUMMARY
Opioid drugs are powerful analgesicsbut their side effect profile strongly limits their useIndeedtheir
addictive properties have led to an epidemic of abuse in the US that accounts forof the global
utilization of prescription opioid analgesics in the USwith a market of over $billion per yearPrevious
studies have shown that the endocannabinoid neurotransmitteranandamidecontrols nociception in
mammals through a predominantly peripheral mechanismThe biological actions of anandamide are
terminated by the enzyme fatty acid amide hydrolaseFAAHWe have recently discovered a novel class of
small molecule inhibitors that block FAAH activity exclusively outside the central nervous systemCNSThe prototype member of this classURBexerts profound and long lasting analgesic effects in a variety
of animal modelssuggesting that peripheral FAAH inhibition may offer a transformative approach to pain
therapy by providing a means to reduce the need for opioid analgesicsPrevious selectivitysafety and
pharmacokinetics studies have identified URBas a lead candidate for preclinical developmentThe
present proposal will assess the pharmacodynamics interactions between URBand opioids in two sets
of mouse and rat modelsChronic pain modelsWe will compare the analgesic effects of different
dosages of URBand two commonly abused opioid analgesicshydrocodone and oxycodonein two
preclinical models of chronic neuropathic and inflammatory painSub effective and median effectiveEDdoses of each compound will be selected and combined to investigate potential synergistic effectsPotential
sex specific differences will also be exploredModels of opiate addiction and constipationWe will
examine the effects of URBon three unwanted effects caused by the administration of opioid
analgesicswhich could be affected by the combination of both drugsself administrationwithdrawaland
constipationIf the proposed activities show thatithe analgesic actions of URBare synergistic with
those of oxycodone and hydrocodoneandiiURBdoes not aggravate the side effects of these opioid
drugswe will seek further funding in the private or public financial market for the preclinical development of
URBas an opioid sparing analgesic for chronic pain PROJECT NARRATIVE
Prescription opioids are potent painkillersbut their use can cause addiction and other serious side effectsHerewe propose a series of preclinical experiments to determine whether the compound URBa drug
that boosts the actions of natural cannabis like substances outside the brainmight be used to replace or
complement opioids in the clinic

* Information listed above is at the time of submission. *

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