Trevena GPCR Platform Yields a Novel Mu-Opioid Biased Ligand Analgesic with Side Effect Benefits
News Jan 24, 2013
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.
Boyds Acquires New Cambridge Office to Support Rapid GrowthNews
Boyds, the drug development consultancy which helps pharmaceutical companies translate great science into marketable medicines for patient benefit, has relocated into new premises in Cambridge.READ MORE
Anti-Inflammatory Pill Could Make Vaccines More Effective for the ElderlyNews
By identifying why skin immunity declines in old age, a UCL-led research team has found that an anti-inflammatory pill could help make vaccines more effective for elderly people.READ MORE
Combination Chemotherapy Could Significantly Improve Deadly Brain Tumor TreatmentNews
A team led by Massachusetts General Hospital (MGH) investigators has found that adding the chemotherapy drug hydroxyurea to the current chemotherapy protocol for glioblastoma significantly increased survival in animal models.READ MORE