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 3,200+ scientific posters on ePosters
  • More than 4,600+ 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
Platelets are the Pathfinders for Leukocyte Extravasation During Inflammation
Findings from the study could help in the prevention and treatment of inflammatory pathologies.
Benchtop Automation Trends
Gain a better understanding of current interest in and future deployment of benchtop automated systems.
Molecular Map Provides Clues To Zinc-Related Diseases
Mapping the molecular structure where medicine goes to work is a crucial step toward drug discovery against deadly diseases.
Genetic Research Can Significantly Improve Drug Development
With drug development costs topping $1.2bn (£850 million) to get a single treatment to the point it can be sold and used in the clinic, could genetic analysis save hundreds of millions of dollars?
New Method Opens Door to Development of Many New Medicines
Findings from TSRI reveal human proteins are better drug targets than previously thought.
Diagnosing Systemic Infections Quickly, Reliably
Team develop rapid and specific diagnostic assay that could help physicians decide within an hour whether a patient has a systemic infection and should be hospitalized for aggressive intervention therapy.
What Makes a Good Scientist?
It’s the journey, not just the destination that counts as a scientist when conducting research.
Blood Test That Detects Early Alzheimer’s Disease
A research team, led by Dr. Robert Nagele from Rowan University School of Osteopathic Medicine and Durin Technologies, Inc., has announced the development of a blood test that leverages the body’s immune response system to detect an early stage of Alzheimer’s disease – referred to as the mild cognitive impairment (MCI) stage – with unparalleled accuracy.
A New Approach to Chemical Synthesis
Communesins, originally found in fungus, could hold potential as cancer drugs.
Angina Drug Could Inform A New Strategy To Fight Cryptococcosis
A drug, more commonly used in the treatment of angina, could be the focus of a new strategy in fighting the fatal fungal infection cryptococcosis.
SELECTBIO

SELECTBIO Market Reports
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
3,200+ scientific and medical posters
A library of 2,500+ scientific videos on LabTube
4,600+ scientific videos
Close
Premium CrownJOIN TECHNOLOGY NETWORKS PREMIUM FOR FREE!