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Peptide-Derived Orally-Active Kappa-Opioid Receptor Agonists for Peripheral Pain

Award Information
Agency: Department of Health and Human Services
Branch: National Institutes of Health
Contract: 1R43DA036398-01A1
Agency Tracking Number: R43DA036398
Amount: $224,893.00
Phase: Phase I
Program: SBIR
Solicitation Topic Code: NIDA
Solicitation Number: PA13-234
Timeline
Solicitation Year: 2014
Award Year: 2014
Award Start Date (Proposal Award Date): N/A
Award End Date (Contract End Date): N/A
Small Business Information
300 West Coleman Blvd. Suite 203
MOUNT PLEASANT, SC 29464-3429
United States
DUNS: 831342022
HUBZone Owned: No
Woman Owned: No
Socially and Economically Disadvantaged: No
Principal Investigator
 THOMAS DIX
 (843) 876-5092
 dixta@musc.edu
Business Contact
 GAUTAM GHATNEKAR
Phone: (843) 860-8785
Email: ghatnekar@firststringresearch.com
Research Institution
 Stub
Abstract

DESCRIPTION (provided by applicant): Treatment of peripheral pain of various origins remains a major unmet medical need, affecting tens to hundreds of millions of people nationwide at some time during their lives. Kappa-opioid agonists have been shown in peripheral pain models to be particularly efficacious but suffer from centrally mediated effects that have limited their development. Perhaps the most promising kappa-agonists under development are derivatives of the tetrapeptide D-Phe-D-Phe-D-Nle-D-Arg-NH2such as CR665, which exhibits high (but not absolute) peripheral to central (CNS) selectivity when administered IV. Clinical studies have shown significant benefit in patients with visceral and neuropathic pain; however, the compound is not active when administered orally which significantly limits its potential use as an analgesic for peripheral pain. As proof of concept, application of the Halimed Pharmaceuticals non- natural amino acid technology to CR665 produced derivatives that exhibit oral acti

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

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