Corporate Banner
Satellite Banner
Biomolecular Screening
Scientific Community
 
Become a Member | Sign in
Home>News>This Article
  News
Return

Trevena GPCR Platform Yields a Novel Mu-Opioid Biased Ligand Analgesic with Side Effect Benefits

Published: Thursday, January 24, 2013
Last Updated: Thursday, January 24, 2013
Bookmark and Share
JPET publication describes the discovery and activity of TRV130.

Trevena, Inc. announced that an article has been published describing the discovery and characterization of TRV130, a novel mu-opioid receptor biased ligand in development for the treatment of severe acute pain. The article illustrates how Trevena is able to translate the biased ligand hypothesis for the mu-opioid receptor, based on mouse knock-out data, into a differentiated molecule with a unique and beneficial profile. As a biased ligand, TRV130 stimulates the mu-opioid G-protein coupling to produce analgesia, without stimulating the β-arrestin pathway, thereby minimizing many opioid side effects. In preclinical studies, TRV130 was powerfully analgesic with an improved safety and tolerability profile when compared directly to morphine.

The article, entitled “A G protein-biased ligand at the μ-opioid receptor is potently analgesic with reduced gastrointestinal and respiratory dysfunction compared to morphine” was published online on January 8th, 2013 in the Journal of Pharmacology and Experimental Therapeutics.

Michael Lark, Ph.D., Chief Scientific Officer of Trevena commented, “It is very exciting to have successfully validated the theory of biased GPCR ligands by designing molecules with the desired pharmacology that translate so well into preclinical studies. If we can demonstrate a similar therapeutic index advantage over morphine in humans, TRV130 has the potential to redefine the use of intravenous opioids for the management of severe post-operative pain.”

TRV130 is a first-in-class biased ligand that targets the mu-opioid receptor and optimizes analgesia while minimizing receptor-mediated adverse effects on gastrointestinal motility and respiratory effort. The drug recently completed a phase 1 first-in-human study, in which it was safe and generally well-tolerated. The next clinical study of TRV130 will investigate analgesic efficacy and tolerability in a direct comparison with intravenous morphine, a gold-standard post-operative analgesic.


Further Information

Join For Free

Access to this exclusive content is for Technology Networks Premium members only.

Join Technology Networks Premium for free access to:

  • Exclusive articles
  • Presentations from international conferences
  • Over 3,500+ scientific posters on ePosters
  • More than 5,000+ scientific videos on LabTube
  • 35 community eNewsletters


Sign In



Forgotten your details? Click Here
If you are not a member you can join here

*Please note: By logging into TechnologyNetworks.com you agree to accept the use of cookies. To find out more about the cookies we use and how to delete them, see our privacy policy.


Scientific News
Mass Spec Technology Drives Innovation Across the Biopharma Workflow
With greater resolving power, analytical speed, and accuracy, new mass spectrometry technology and techniques are infiltrating the biopharmaceuticals workflow.
One Step Closer to Precision Medicine for Chronic Lung Disease Sufferers
A study led by University of North Carolina at Chapel Hill, and National Jewish Health, has provided evidence of links between SNPs and known COPD blood protein biomarkers.
New Therapeutic Target for Crohn’s Disease
A promising new target for drugs that treat IBD has been identified along with a possible biomarker for IBD severity.
Researchers Find Fungus-Fighting Compound
A compound has been identifed that blocks growth of a fungus responsible for lung infections and allergic reactions.
Analysing 10,000 Cells Simultaneously
New techniquethat traps 10,000 cells on a single chip has potential for cancer screening for individuals.
Peer Reviewed Study Demonstrates Mass Spec Technique
The peer reviewed study demonstrates MS workflow, TMTCalibrator workflow, which dramatically enhances detection of key early stage Alzheimer’s biomarkers.
Small Molecules Lead to a Big Change in Reaction Outcomes
Scientists have changed the behaviour of a group of molecules involved in carbon-oxygen bond synthesis.
Enhancing Antibiotics to Defeat Resistant Bacteria
Scientists enhance ability of antibiotics to defeat resistant types of bacteria using molecules called PPMOs
Sanger Institute, St Jude Data-Sharing Agreement
Childhood cancer targeted by Sanger Institute and St Jude Children’s Research Hospital exchanges of cancer data
Over Two-Thirds of Cervical Cancer Deaths Prevented
Cervical screening prevents 70% of cervical cancer deaths and if all eligible women regularly attended screening this would rise to 83%.
SELECTBIO

Skyscraper Banner
Go to LabTube
Go to eposters
 
Access to the latest scientific news
Exclusive articles
Upload and share your posters on ePosters
Latest presentations and webinars
View a library of 1,800+ scientific and medical posters
3,500+ scientific and medical posters
A library of 2,500+ scientific videos on LabTube
5,000+ scientific videos
Close
Premium CrownJOIN TECHNOLOGY NETWORKS PREMIUM FOR FREE!