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 4,800+ 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
Liquid Biopsies: Miracle Diagnostic or Next New Fad?
Thanks to the development of highly specific gene-amplification and sequencing technologies liquid biopsies access more biomarkers relevant to more cancers than ever before.
Drug Candidates Reduce Abnormal Protein Production
New drug candidates improve cell ability to catch miss-folded proteins that could cause deadly diseases.
Supercomputing and Drug Discovery
New biotech company uses supercomputer simulations to speed up drug discovery and biotech molecule development.
Preventing Breast Cancer with Hops
Study of hops extract suggests prevention of breast cancer through chemical pathway activation.
Treatment Advancement for Gaucher and Parkinson's Diseases
NIH scientists identify molecule that may act as a possible treatment of neurological diseases.
Biomunex Confirms Optimal Properties and Activity of BiXAb® Antibodies
Biomunex‘s Plug-and-Play bispecific antibodies demonstrated excellent in vitro properties and in vivo activity positively differentiating their BiXAb platform from competing formats.
Liquid Biopsy Predicts Colon Cancer Recurrence
Scientists have used a genetic test that spots bits of cancer-related DNA circulating in the blood to accurately predict the likelihood of the disease’s return in some — but not all — of a small group of patients with early-stage colon cancer.
New Treatment for Rare Blood Cancers
Drug called midostaurin showed promise in an international clinical trial led by a Stanford physician.
Biomarker for Parkinson's Disease Found in Urine Samples
Protein identified as Parkinson's biomarker sourced from patient's stored frozen urine samples.
Testing for Malaria or Cancer at Home
Chemist develops tech to save lives in rural Africa.
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
4,800+ scientific videos
Close
Premium CrownJOIN TECHNOLOGY NETWORKS PREMIUM FOR FREE!