Oliceridine

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

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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.

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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

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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.

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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

Soergel D, Subach RA, Burnham N, Lark MW, James IE, Sadler BM, Skobieranda F, Violin JD, Webster LR. Pain. 2014 Sep;155(9):1829-35

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TRV130- First clinical experience, pharmacokinetics and pharmacodynamics (analgesic and VRH response)

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

Soergel DG, Subach RA, Sadler B, Connell J, Marion AS, Cowan CL, Violin JD, Lark MW. J Clin Pharmacol. 2014 Mar;54(3):351-7.

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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

Chen XT, Pitis P, Liu G, Yuan C, Gotchev D, Cowan CL, Rominger DH, Koblish M, Dewire SM, Crombie AL, Violin JD, Yamashita DS. J Med Chem. 2013 Oct 24;56(20):8019-31.

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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

DeWire SM, Yamashita DS, Rominger DH, Liu G, Cowan CL, Graczyk TM, Chen XT, Pitis PM, Gotchev D, Yuan C, Koblish M, Lark MW, Violin JD. J Pharmacol Exp Ther. 2013 Mar;344(3):708-17.

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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

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Discovery Innovations

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

Violin JD, Crombie AL, Soergel DG, Lark MW. Trends Pharmacol Sci. 2014 Jul;35(7):308-16.

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

Kenakin T, Christopoulos A. Nat Rev Drug Discov. 2013 Mar;12(3):205-16.

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

Allen JA, Yost JM, Setola V, Chen X, Sassano MF, Chen M, Peterson S, Yadav PN, Huang XP, Feng B, Jensen NH, Che X, Bai X, Frye SV, Wetsel WC, Caron MG, Javitch JA, Roth BL, Jin J. Proc Natl Acad Sci U S A. 2011 Nov 8;108(45):18488-93.

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Structural features for functional selectivity at serotonin receptors

Wacker D, Wang C, Katritch V, Han GW, Huang XP, Vardy E, McCorvy JD, Jiang Y, Chu M, Siu FY, Liu W, Xu HE, Cherezov V, Roth BL, Stevens RC. Science. 2013 May 3;340(6132):615-9.

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Quantifying ligand bias at seven-transmembrane receptors

Rajagopal S, Ahn S, Rominger DH, Gowen-MacDonald W, Lam CM, Dewire SM, Violin JD, Lefkowitz RJ. Mol Pharmacol. 2011 Sep;80(3):367-77.

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Beta-arrestin-biased ligands at seven-transmembrane receptors

Violin JD, Lefkowitz RJ. Trends Pharmacol Sci. 2007 Aug;28(8):416-22.

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Beta-arrestins and cell signaling

DeWire SM, Ahn S, Lefkowitz RJ, Shenoy SK. Annu Rev Physiol. 2007;69:483-510.

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Biased ligands: pathway validation for novel GPCR therapeutics

Rominger DH, Cowan CL, Gowen-MacDonald W, Violin JD. Curr Opin Pharmacol. 2014 Jun;16:108-15

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TRV734

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.

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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.

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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.

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