Oliceridine significantly reduced risk of vomiting and rescue antiemetic use compared to IV morphine in a retrospective analysis

Oliceridine is Associated with Reduced Risk of Vomiting and Need for Rescue Antiemetics Compared to Morphine: Exploratory Analysis from Two Phase 3 Randomized Placebo and Active Controlled Trials

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Benefit and Risk Evaluation of Biased μ-Receptor Agonist Oliceridine versus Morphine.

Albert Dahan, C. Jan van Dam, Marieke Niesters, Monique van Velzen, Michael J. Fossler, Mark A. Demitrack, Erik Olofsen. Anesthesiology 2020. doi:

Incidence of Opioid-Induced Respiratory Depression Associated with Oliceridine and Morphine as Measured by the Frequency and Average Cumulative Duration of Dosing Interruption in Patients Treated for Acute Postoperative Pain: Findings indicate improved safety with oliceridine.

Evaluating the Incidence of Opioid-Induced Respiratory Depression Associated with Oliceridine and Morphine as Measured by the Frequency and Average Cumulative Duration of Dosing Interruption in Patients Treated for Acute Postoperative Pain.

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Oliceridine Monograph

Oliceridine, a G protein-selective ligand at the μ-opioid receptor, for the management of moderate to severe acute pain

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Phase 3 “Real World” Safety Study for Oliceridine

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The Influence of Renal or Hepatic Impairment on the Pharmacokinetics, Safety, and Tolerability of Oliceridine

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Oliceridine (TRV130) Phase-3 Pivotal trial in soft-tissue (abdominoplasty) acute pain

APOLLO-2: A Randomized, Placebo and Active-Controlled Phase III Study Investigating Oliceridine (TRV130), a G Protein-Biased Ligand at the μ-Opioid Receptor, for Management of Moderate to Severe Acute Pain Following Abdominoplasty

Neil K. Singla, Franck Skobieranda, David G. Soergel, Monica Salamea, David A. Burt, Mark A. Demitrack, Eugene R. Viscusi Pain Pract. 2019 Sep;19(7):715-731

Oliceridine (TRV130) Phase-3 Pivotal trial in hard-tissue (bunionectomy) acute pain

APOLLO-1: a randomized placebo and active-controlled phase III study investigating oliceridine (TRV130), a G protein-biased ligand at the µ-opioid receptor, for management of moderate-to-severe acute pain following bunionectomy

Eugene R Viscusi, Franck Skobieranda, David G Soergel,Emily Cook, David A Burt, and Neil Singla. J Pain Res. 2019; 12: 927–943.

Oliceridine (TRV130) Phase 2b trial in soft-tissue (abdominoplasty) acute pain

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

Neil Singla, Harold S Minkowitz, David G Soergel, David A Burt, Ruth Ann Subach, Monica Y Salamea, Michael J Fossler, and Franck Skobieranda. J Pain Res. 2017; 10: 2413–2424

Oliceridine (TRV130) Phase 2 trial in hard-tissue (bunionectomy) acute pain

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

Viscusi ER, Webster L, Kuss M, Daniels S, Bolognese JA, Zuckerman S, Soergel DG, Subach RA, Cook E, Skobieranda F. Pain. 2016 Jan;157(1):264-72.

TRV130- phase I study in healthy volunteers

Biased agonism of the μ-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

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TRV130 – analgesia and ventilatory response to hypercapnia vs. morphine in healthy volunteers

Biased agonism of the μ-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

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TRV130- First clinical experience, pharmacokinetics and pharmacodynamics

First clinical experience with TRV130: pharmacokinetics and pharmacodynamics in healthy volunteers

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TRV130-Concept of biased ligand

Structure-activity relationships and discovery of a G protein biased μ opioid receptor ligand, [(3-methoxythiophen-2-yl)methyl]({2-[(9R)-9-(pyridin-2-yl)-6-oxaspiro-[4.5]decan-9-yl]ethyl})amine (TRV130), for the treatment of acute severe pain

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TRV-130 preclinical safety results

A G protein-biased ligand at the μ-opioid receptor is potently analgesic with reduced gastrointestinal and respiratory dysfunction compared with morphine

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Reduced Incidence of Postoperative Vomiting with Oliceridine than with Morphine at Equianalgesic Conditions

Timothy L Beard, Cathy Michalsky, Keith A Candiotti, Paul Rider, Linda Wase, Ashraf S Habib, Mark A Demitrack, Michael J Fossler, Eugene R Viscusi

Annual Meeting of the American Society of Anesthesiologists (ASA); 2020

Evaluating Predictive Value of Postoperative O2 Saturation Levels to Rate of Respiratory Safety Events In Oliceridine Trials

Sabry Ayad, Ashish K Khanna, Cathy Michalsky, Linda Wase, Mark A Demitrack, Michael J Fossler, Kit N Simpson

Annual Meeting of the American Society of Anesthesiologists (ASA); 2020

Improved Tolerability with Oliceridine Compared to Morphine at Equianalgesic Conditions

Gregory B Hammer, Cathy Michalsky, Linda Wase, Mark A Demitrack, Roderick Little, Sabry Ayad, Ashish K Khanna, Michael J Fossler

Annual Meeting of the American Society of Anesthesiologists (ASA); 2020

Improved Safety of Opioid Analgesic Oliceridine Compared to Morphine Assessed by Utility Function Analysis

Albert Dahan, Marieke Niesters, Michael J. Fossler, Mark A. Demitrack, Erik Olofsen.

Annual Meeting of the American Society of Anesthesiologists (ASA); 2019

Biased ligands at G-protein-coupled receptors: promise and progress

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

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

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Quantifying ligand bias at seven-transmembrane receptors

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TRV250 – Phase 1 Study in Healthy Volunteers

A Phase I, Randomized, Single Blind, Placebo Controlled, Single Ascending Dose Study of the Safety, Tolerability, and Pharmacokinetics of Subcutaneous and Oral TRV250, a G Protein-Selective Delta Receptor Agonist, in Healthy Subjects.

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A Phase 1 Healthy Volunteer Study of the Safety, Tolerability and Pharmacokinetics of TRV250, a G Protein-Selective Delta Receptor Agonist

Mark A. Demitrack, Michael S. Kramer, Kelly Arscott, Ian E. James, Michael J.Fossler.

A First-in-Human Clinical Study With TRV734, an Orally Bioavailable G-Protein-Biased Ligand at the μ-Opioid Receptor

James IE, Skobieranda F, Soergel DG, Ramos KA, Ruff D, Fossler MJ. Clin Pharmacol Drug Dev. 2019 Jul 8.

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

Franck Skobieranda, Ian E. James, Michael J. Fossler, Gregory Alcorn, David G. Soergel.

An orally available µ-opioid receptor biased ligand is analgesic with reduced constipation in rodents

Jonathan D. Violin, Scott M. DeWire, Mike Koblish, Daniel Chen, Aimee L. Crombie, Dennis Yamashita, Ruth Ann Subach, David G. Soergel, Michael W. Lark.

β-Arrestin-Biased Angiotensin II Receptor Agonists for COVID-19

Manglik A, Wingler LM, Rockman HA, Lefkowitz RJ. Circulation. 15 May 2020.

TRV045, a novel, selective S1PR1 modulator, is efficacious in reversing neuropathic pain without affecting lymphocyte trafficking

Michael S. Kramer, Stefania Risso, Michael J.Fossler, Mark A. Demitrack.

American College of Neuropsychopharmacology 59th Annual Meeting; 2020

TRV045, a novel, selective S1P1 receptor modulator that is not an immunosuppressant, is efficacious in rodent models of epilepsy

Stefania Risso, Michael S. Kramer, Michael J.Fossler, Mark A. Demitrack

American College of Neuropsychopharmacology 59^th Annual Meeting; 2020