Trevena, Inc. GPCR Platform Yields a Novel Mu-opioid Biased Ligand Analgesic With Side Effect Benefits
Published: Jan 23, 2013
KING OF PRUSSIA, Pa.--(BUSINESS WIRE)--Trevena, Inc., the leader in discovery and development of G-protein coupled receptor (GPCR) biased ligands, today 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 ß-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.