Biased Ligands. Better Drugs.


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OLINVO™ (oliceridine) Publications

Poster - 2016 ASRA Meeting

Presentations from the 41st Annual Regional Anesthesiology and Acute Pain Medicine Meeting, 2016.

Article - TRV130 Phase 2 bunionectomy full results

A randomized, phase 2 study investigating TRV130, a biased ligand of the μ-opioid receptor, for the intravenous treatment of acute pain

Poster - TRV130 Phase 2 bunionectomy trial

TRV130, a G Protein-biased Ligand of the µ-opioid Receptor, Demonstrates Analgesic Efficacy Following Bunionectomy in an Adaptive Phase 2 Study

Article - TRV130 Phase 1b full results

Biased agonism of the mu-opioid receptor by TRV130 increases analgesia and reduces on-target adverse effects versus morphine: A randomized, double-blind, placebo-controlled, crossover study in healthy volunteers. Pain 155(9):1829-35, September 2014.

Review - Advances in biased ligand drug discovery

Biased ligands at G protein-coupled receptors: promise and progress. Trends in Pharmacological Sciences 35(7):308-16, July 2014

Poster - TRV130 Phase 1b study summary

A comparison of the pharmacokinetics and pharmacodynamics of TRV130 vs. morphine in healthy volunteers. Presented at the 2014 American Pain Society meeting.

Article - TRV130 FTIH study

First Clinical Experience With TRV130: Pharmacokinetics and Pharmacodynamics in Healthy Volunteers. The Journal of Clinical Pharmacology 54(3) 351–357. March 2014.

Article - TRV130 Journal of Medicinal Chemistry Publication

Structure-Activity Relationships and Discovery of a G Protein Biased Mu Opioid Receptor Ligand, TRV130, for the Treatment of Acute Severe Pain.

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

TRV027 Publications

Article - BLAST-AHF trial design

Heart Failure Therapeutics on the Basis of a Biased Ligand of the Angiotensin-2 Type 1 Receptor : Rationale and Design of the BLAST-AHF Study (Biased Ligand of the Angiotensin Receptor Study in Acute Heart Failure). JACC Heart Fail. 2015 Mar;3(3):193-201. doi: 10.1016/j.jchf.2014.09.008. Epub 2015 Jan 28.

Poster - TRV027 Phase 2b trial design

Rationale and Design of the TRV027 Biased Ligand at the Angiotensin Receptor Study in Acute Heart Failure (BLAST-AHF). Presented at the 2014 European Society for Cardiology – Heart Failure meeting.

Article - Angiotensin receptor biased ligands and Acute Heart Failure

Beta-arrestin-biased ligands at the AT1R: a novel approach to the treatment of acute heart failure. Drug Discovery Today: Therapeutic Strategies.

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

Biased Ligand Publications

Poster - TRV250 preclinical studies

TRV250: a novel biased ligand at the delta receptor for the potential treatment of migraine

Poster - TRV734 Phase 1 clinical studies

TRV734, a G Protein-biased Ligand of the µ-opioid Receptor, Demonstrates Oral Bioavailability, Displays Predictable Pharmacokinetics and Pharmacodynamics, and Provides Analgesia in Healthy Adults

Poster - TRV734 Phase 1 formulation study

Formulation and Food Effect Studies of TRV734, an Oral, G Protein-biased Ligand of the µ-opioid Receptor

Review - Biased Ligand research

Biased ligands: pathway validation for novel GPCR therapeutics. Current Opinions in Pharmacology 2014 16: 108-115.

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

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