Biased Ligands. Better Drugs.

Publications

TRV027 Publications

Article - Molecular mechanisms of biased AT1R ligand pharmacology, a collaboration with J. Solaro

The β-arrestin-Biased Ligand TRV120023 Inhibits Angiotensin II-Induced Cardiac Hypertrophy While Preserving Enhanced Myofilament Response to Calcium

Poster - TRV027 Phase 2a hemodynamics study summary

TRV027, a β-arrestin biased ligand at the angiotensin 2 type 1 receptor, produces rapid, reversible changes in hemodynamics in patients with stable systolic heart failure. Presented at 2013 American College of Cardiology meeting

Article - Review of biased ligands in heart failure

GPCR biased ligands as novel heart failure therapeutics. Article in Press. Available online March 15th 2013

Poster - TRV027 Phase 1 FTIH study summary

First human dosing experience with TRV027, a novel therapy for acute heart failure. Presented at 2012 Heart Failure of America Society meeting

Article - Cardioprotective properties of biased AT1R ligands

β-Arrestin-biased AT1R stimulation promotes cell survival during acute cardiac injury. Am J Physiol Heart Circ Physiol 303:H1001-H1010, 2012. First published 10 August 2012

Article - TRV027 in normal and heart failure canines, a collaboration with J. Burnett

Cardiorenal Actions of TRV120027, a Novel, β-Arrestin-Biased Ligand at the Angiotensin II Type I Receptor, in Healthy and Heart Failure Canines: A Novel Therapeutic Strategy for Acute Heart Failure. Circ Heart Fail. 2011 Aug. PubMed PMID: 21835984.

Article - Review of biased ligands for cardiovascular disease

Biased ligands for better cardiovascular drugs:dissecting G protein-coupled receptor pharmacology. Circ Res. 2011 Jul. PubMed PMID: 21737816.

Article - The discovery, in vitro profile, & rodent pharmacology of TRV027

Selectively engaging Beta-arrestins at the angiotensin II type 1 receptor reduces blood pressure and increases cardiac performance. J Pharmacol Exp Ther 2010 Dec.

Poster - TRV027 in-vitro and in-vivo pharmacology summary

TRV120027, a Beta-arrestin biased ligand at the angiotensin II type 1 receptor, produces unique pharmacology and is a novel potential therapy for heart failure. Presented at the 2010 Heart Failure of Society of America meeting

Presentation - 14th Annual Scientific Meeting of The Heart Failure Society of America - TRV027 improves hemodynamics in a heart failure dog model

Cardiorenal Actions of TRV120027, a Novel, Beta-Arrestin-Biased Ligand at the Angiotensin II Type I Receptor, in Healthy and Heart Failure Canines: A Novel Therapeutic Strategy for Acute Heart Failure

TRV130 Publications

Article - Discovery and development of TRV130, a muopioid biased ligand

A G Protein-Biased Ligand at the mu opioid Receptor is Potently Analgesic with Reduced Gastrointestinal and Respiratory Dysfunction Compared with Morphine. J Pharmacol Exp Ther 344:708-717, March 2013.

Poster - TRV130 FTIH study summary

First human dosing experience with TRV130, a G protein biased ligand at the mu opioid receptor. Presented at 2013 American Academy of Neurology meeting

Poster - TRV130 efficacy and tolerability in rodents

A G protein biased mu opioid receptor ligand elicits potent analgesia but reduced constipation & respiratory depression compared to morphine in rodents. Presented at the 2012 American Association of Pain Medicine Meeting

Biased Ligand Publications

Poster - TRV734 - An orally available mu-opioid receptor biased ligand is analgesic with reduced constipation in rodents

This poster introduces TRV734, a G protein-biased mu-opioid receptor ligand that is analgesic with improved gastrointestinal effects compared to morphine and oxycodone in rodents. TRV734 displays promising pharmacokinetics in non-human primates; together these data suggest that oral TRV734 may deliver powerful analgesia with better tolerability than currently used oral opioids for acute and chronic pain.

Article - Signalling bias in new drug discovery: detection, quantification and therapeutic impact

Nat Rev Drug Discov. 2013 Mar;12(3):205-16

Article - Discovery of β-arrestin-biased dopamine D2 ligands for probing signal transduction pathways essential for antipsychotic efficacy

Proc Natl Acad Sci U S A. 2011 Nov 8;108(45):18488-93

Review - Introduction to Novel Aspects of Cardiovascular GPCR Signaling

AHA Journals Free Article

Article - Structural Features for Functional Selectivity at Serotonin Receptors

Science. 2013 Mar 21 (online)

Article - The quantification of ligand bias, a collaboration with R. Lefkowitz

Quantifying ligand bias at seven-transmembrane receptors. Mol Pharmacol. 2011 Sep. PubMed Central PMCID: PMC3164332

Article - A review of biased ligands

β-arrestin-biased ligands at seven-transmembrane receptors. Trends Pharmacol Sci. 2007 Aug

Article - A comprehensive review of β-arrestin functions

β-arrestins and cell signaling. Annu Rev Physiol. 2007

Copyright © Trevena, Inc.