Biased Ligands. Better Drugs.

Publications

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OLINVO™ (oliceridine)

Publications

TRV130 Phase 2 abdominoplasty results

A randomized, Phase IIb study investigating oliceridine (TRV130), a novel μ-receptor G-protein pathway selective (μ-GPS) modulator, for the management of moderate to severe acute pain following abdominoplasty

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

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.

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.

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.

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.

Manuscripts

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

Posters

APS - APOLLO-1: TRV130 Bunionectomy Trial

APOLLO-1: A Randomized, Placebo- and Active-Controlled Phase III Study Investigating Oliceridine (TRV130), a Novel μ Receptor G Protein Pathway Selective (μ-GPS) Modulator, for Management of Moderate to Severe Acute Pain Following Bunionectomy

ASA - APOLLO-2: TRV130 Abdominoplasty Trial

APOLLO-2: A Randomized, Placebo- and Active-Controlled Phase III Study Investigating Oliceridine (TRV130), a Novel μ Receptor G Protein Pathway Selective (μ-GPS) Modulator, for Management of Moderate to Severe Acute Pain Following Abdominoplasty

ASCRS - APOLLO-1: TRV130 Bunionectomy Trial

APOLLO-1: A Randomized, Placebo- and Active-Controlled Phase III Study Investigating Oliceridine (TRV130), a Novel μ Receptor G Protein Pathway Selective (μ-GPS) Modulator, for Management of Moderate to Severe Acute Pain Following Bunionectomy

ASCRS - APOLLO-2: TRV130 Abdominoplasty Trial

APOLLO-2: A Randomized, Placebo- and Active-Controlled Phase III Study Investigating Oliceridine (TRV130), a Novel μ Receptor G Protein Pathway Selective (μ-GPS) Modulator, for Management of Moderate to Severe Acute Pain Following Abdominoplasty

The Promise of Opioids Targeting G Protein Signaling

2016 ASRA Meeting

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

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

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.

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

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 Ligands

Publications

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

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

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

Structural Features for Functional Selectivity at Serotonin Receptors

Science. 2013 Mar 21 (online)

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

A review of biased ligands

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

A comprehensive review of β-arrestin functions

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

Manuscripts

Biased Ligand research

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

Introduction to Novel Aspects of Cardiovascular GPCR Signaling

AHA Journals Free Article

Posters

TRV250 preclinical studies

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

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

TRV734 Phase 1 formulation study

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

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.

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