Jump to content

Oliceridine: Difference between revisions

From Wikipedia, the free encyclopedia
Browse history interactively
← Previous editNext edit →
Content deleted Content added
VisualWikitext
Navira (talk | contribs)
12 edits
No edit summary
Tags: Mobile edit Mobile web edit
Navira (talk | contribs)
12 edits
No edit summary
Tags: Mobile edit Mobile web edit
Line 43: Line 43:
It is a [[functional selectivity|functionally selective]] [[Mu-opioid receptor|μ-opioid receptor]] [[agonist]] developed by [[Trevena Inc]]. TRV130 elicits robust [[G protein]] [[signal transduction|signaling]], with [[Potency (pharmacology)|potency]] and [[Intrinsic activity|efficacy]] similar to [[morphine]], but with far less [[Arrestin beta 2|β-arrestin 2]] recruitment and [[receptor internalization]], it displays less [[adverse effect]]s than morphine.
It is a [[functional selectivity|functionally selective]] [[Mu-opioid receptor|μ-opioid receptor]] [[agonist]] developed by [[Trevena Inc]]. TRV130 elicits robust [[G protein]] [[signal transduction|signaling]], with [[Potency (pharmacology)|potency]] and [[Intrinsic activity|efficacy]] similar to [[morphine]], but with far less [[Arrestin beta 2|β-arrestin 2]] recruitment and [[receptor internalization]], it displays less [[adverse effect]]s than morphine.


On August 31, 2014 [[Trevena]] announced positive data from its randomized, double-blind, placebo- and active-controlled phase 2b trial of TRV130 in moderate to severe acute postoperative pain after abdominoplasty surgery[1]
On August 31, 2014 [[Trevena]] announced positive data from its randomized, double-blind, placebo- and active-controlled phase 2b trial of TRV130 in moderate to severe acute postoperative pain after abdominoplasty surgery[ref needed]


<ref name="pmid24063433">{{cite journal | author = Chen XT, Pitis P, Liu G, Yuan C, Gotchev D, Cowan CL, Rominger DH, Koblish M, Dewire SM, Crombie AL, Violin JD, Yamashita DS | title = 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 | journal = J. Med. Chem. | volume = 56| issue = 20| pages = 8019–31| year = 2013 | month = October | pmid = 24063433 | doi = 10.1021/jm4010829 }}</ref><ref name="pmid23300227">{{cite journal | author = 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 | title = A G protein-biased ligand at the μ-opioid receptor is potently analgesic with reduced gastrointestinal and respiratory dysfunction compared with morphine | journal = J. Pharmacol. Exp. Ther. | volume = 344 | issue = 3 | pages = 708–17 |date=March 2013 | pmid = 23300227 | doi = 10.1124/jpet.112.201616 }}</ref><ref name="pmid24122908">{{cite journal | author = Soergel DG, Subach RA, Sadler B, Connell J, Marion AS, Cowan C, Violin JD, Lark MW | title = First clinical experience with TRV130: Pharmacokinetics and pharmacodynamics in healthy volunteers | journal = J Clin Pharmacol | volume = 54| issue = 3| pages = 351–7|date=October 2013 | pmid = 24122908 | doi = 10.1002/jcph.207 }}</ref>
<ref name="pmid24063433">{{cite journal | author = Chen XT, Pitis P, Liu G, Yuan C, Gotchev D, Cowan CL, Rominger DH, Koblish M, Dewire SM, Crombie AL, Violin JD, Yamashita DS | title = 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 | journal = J. Med. Chem. | volume = 56| issue = 20| pages = 8019–31| year = 2013 | month = October | pmid = 24063433 | doi = 10.1021/jm4010829 }}</ref><ref name="pmid23300227">{{cite journal | author = 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 | title = A G protein-biased ligand at the μ-opioid receptor is potently analgesic with reduced gastrointestinal and respiratory dysfunction compared with morphine | journal = J. Pharmacol. Exp. Ther. | volume = 344 | issue = 3 | pages = 708–17 |date=March 2013 | pmid = 23300227 | doi = 10.1124/jpet.112.201616 }}</ref><ref name="pmid24122908">{{cite journal | author = Soergel DG, Subach RA, Sadler B, Connell J, Marion AS, Cowan C, Violin JD, Lark MW | title = First clinical experience with TRV130: Pharmacokinetics and pharmacodynamics in healthy volunteers | journal = J Clin Pharmacol | volume = 54| issue = 3| pages = 351–7|date=October 2013 | pmid = 24122908 | doi = 10.1002/jcph.207 }}</ref>

Revision as of 21:02, 31 August 2015

TRV130
Clinical data
Routes of
administration		IV
ATC code
  • none
Legal status
Legal status
Identifiers
  • [(3-Methoxythiophen-2-yl)methyl]({2-[(9R)-9-(pyridin-2-yl)-6-oxaspiro-[4.5]decan-9-yl]ethyl})amine
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC22H30N2O2S
Molar mass386.55 g·mol−1

TRV130 is an opioid drug that is under evaluation by Trevena in human clinical trials for the treatment of acute severe pain. It is a functionally selective μ-opioid receptor agonist developed by Trevena Inc. TRV130 elicits robust G protein signaling, with potency and efficacy similar to morphine, but with far less β-arrestin 2 recruitment and receptor internalization, it displays less adverse effects than morphine.

On August 31, 2014 Trevena announced positive data from its randomized, double-blind, placebo- and active-controlled phase 2b trial of TRV130 in moderate to severe acute postoperative pain after abdominoplasty surgery[ref needed]

[2][3][4]

References

  1. ^ "FDA-sourced list of all drugs with black box warnings (Use Download Full Results and View Query links.)". nctr-crs.fda.gov. FDA. Retrieved 22 Oct 2023.
  2. ^ Chen XT, Pitis P, Liu G, Yuan C, Gotchev D, Cowan CL, Rominger DH, Koblish M, Dewire SM, Crombie AL, Violin JD, Yamashita DS (2013). "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". J. Med. Chem. 56 (20): 8019–31. doi:10.1021/jm4010829. PMID 24063433. {{cite journal}}: Unknown parameter |month= ignored (help)CS1 maint: multiple names: authors list (link)
  3. ^ 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 (March 2013). "A G protein-biased ligand at the μ-opioid receptor is potently analgesic with reduced gastrointestinal and respiratory dysfunction compared with morphine". J. Pharmacol. Exp. Ther. 344 (3): 708–17. doi:10.1124/jpet.112.201616. PMID 23300227.{{cite journal}}: CS1 maint: multiple names: authors list (link)
  4. ^ Soergel DG, Subach RA, Sadler B, Connell J, Marion AS, Cowan C, Violin JD, Lark MW (October 2013). "First clinical experience with TRV130: Pharmacokinetics and pharmacodynamics in healthy volunteers". J Clin Pharmacol. 54 (3): 351–7. doi:10.1002/jcph.207. PMID 24122908.{{cite journal}}: CS1 maint: multiple names: authors list (link)



Stub icon

This analgesic-related article is a stub. You can help Wikipedia by expanding it.

Retrieved from "https://en.wikipedia.org/w/index.php?title=Oliceridine&oldid=678823174"