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

Journal of Clinical Pharmacology

Volumn 54, Issue 3, 2014, Pages 351-357

  Soergel, David G ^a   Ann Subach, Ruth ^a   Sadler, Brian ^b   Connell, John ^b   Marion, Alan S ^b   Cowan, Conrad L ^a   Violin, Jonathan D ^a   Lark, Michael W ^a  

^a TREVENA INC   (United States)

^b ICON Development Solutions   (United States)

Author keywords

analgesic; biased ligand; opioid; TRV130

Indexed keywords

AMYLASE; ANALGESIC AGENT; BILIRUBIN; CYTOCHROME P450 2D6; MU OPIATE RECEPTOR; TRV 130; UNCLASSIFIED DRUG;

ADULT; ANALGESIA; AREA UNDER THE CURVE; ARTICLE; BLOOD SAMPLING; BODY MASS; CLINICAL ARTICLE; DIZZINESS; DRUG BLOOD LEVEL; DRUG CLEARANCE; DRUG DOSE COMPARISON; DRUG HALF LIFE; DRUG METABOLISM; DRUG SAFETY; DRUG TOLERABILITY; FATIGUE; HUMAN; HUMAN EXPERIMENT; HUMAN TISSUE; HYPERHIDROSIS; INJECTION SITE PAIN; MALE; MAXIMUM PLASMA CONCENTRATION; NAUSEA AND VOMITING; NORMAL HUMAN; PRURITUS; PUPIL REFLEX; PUPILLOMETRY; SOMNOLENCE;

ANALGESIC; BIASED LIGAND; OPIOID; TRV130;

ADMINISTRATION, INTRAVENOUS; ADULT; ANALGESICS; CROSS-OVER STUDIES; DOUBLE-BLIND METHOD; HEALTHY VOLUNTEERS; HUMANS; LIGANDS; MALE; MIDDLE AGED; NAUSEA; RECEPTORS, OPIOID, MU; SPIRO COMPOUNDS; THIOPHENES; VOMITING; YOUNG ADULT;

EID: 84898655082     PISSN: 00912700     EISSN: 15524604     Source Type: Journal    
DOI: 10.1002/jcph.207     Document Type: Article

References (15)

1. Apfelbaum JL, Chen C, Mehta SS, Gan TJ., Postoperative pain experience: results from a national survey suggest postoperative pain continues to be undermanaged. Anesth Analg. 2003; 97 (2): 534-540, table of contents. (Pubitemid 36899761)
2. Lubawski J, Saclarides T., Postoperative ileus: strategies for reduction. Ther Clin Risk Manag. 2008; 4 (5): 913-917.
3. Philip BK, Reese PR, Burch SP., The economic impact of opioids on postoperative pain management. J Clin Anesth. 2002; 14 (5): 354-364.
4. Practice guidelines for acute pain management in the perioperative setting: an updated report by the American Society of Anesthesiologists Task Force on Acute Pain Management. Anesthesiology. 2004; 100 (6): 1573-1581.
5. Practice guidelines for acute pain management in the perioperative setting: an updated report by the American Society of Anesthesiologists Task Force on Acute Pain Management. Anesthesiology. 2012; 116 (2): 248-273.
6. Asgeirsson T, El-Badawi KI, Mahmood A, Barletta J, Luchtefeld M, Senagore AJ., Postoperative ileus: it costs more than you expect. J Am Coll Surg. 2010; 210 (2): 228-231.
7. DeWire SM, Yamashita DS, Rominger DH, et al. 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. 2013; 344 (3): 708-717.
8. Bohn LM, Lefkowitz RJ, Gainetdinov RR, Peppel K, Caron MG, Lin FT., Enhanced morphine analgesia in mice lacking beta-arrestin 2. Science. 1999; 286 (5449) 2495-2498.
9. Raehal KM, Walker JK, Bohn LM., Morphine side effects in beta-arrestin 2 knockout mice. J Pharmacol Exp Ther. 2005; 314 (3) 1195-1201. (Pubitemid 41205984)
10. Violin JD, Lefkowitz RJ., Beta-arrestin-biased ligands at seven-transmembrane receptors. Trends Pharmacol Sci. 2007; 28 (8) 416-422.
11. Schmid B, Bircher J, Preisig R, Kupfer A., Polymorphic dextromethorphan metabolism: co-segregation of oxidative O-demethylation with debrisoquin hydroxylation. Clin Pharmacol Ther. 1985; 38 (6) 618-624. (Pubitemid 16124372)
12. Saunders DL, Messina J, Darwish M, Xie F, Leary KJ, Cantilena LR., Assessment of the relative potency of fentanyl buccal tablet to intravenous morphine in healthy volunteers using a thermally induced hyperalgesia pain model. J Clin Pharmacol. 2012; 52 (6) 870-879.
13. Posner J, Telekes A, Crowley D, Phillipson R, Peck AW., Effects of an opiate on cold-induced pain and the CNS in healthy volunteers. Pain. 1985; 23 (1) 73-82. (Pubitemid 15236654)
14. Trescot AM, Datta S, Lee M, Hansen H., Opioid pharmacology. Pain Physician. 2008; 11 (2 Suppl): S133-S153. (Pubitemid 351682083)
15. Gaedigk A, Bradford LD, Marcucci KA, Leeder JS., Unique CYP2D6 activity distribution and genotype-phenotype discordance in black Americans. Clin Pharmacol Ther. 2002; 72 (1) 76-89. (Pubitemid 34833189)