Oliceridine

Oliceridine
Clinical data
Trade names Olinvo
Synonyms TRV-130
Routes of
administration		 Intravenous
ATC code
  • none
Legal status
Legal status
Identifiers
CAS Number
PubChem CID
ChemSpider
UNII
ChEMBL
Chemical and physical data
Formula C22H30N2O2S
Molar mass 386.55 g·mol−1
3D model (JSmol)

Oliceridine (developmental code name TRV-130; tentative brand name Olinvo) is an opioid drug that is under evaluation in human clinical trials for the intravenous treatment of severe acute pain. It is a μ-opioid receptor biased agonist developed by Trevena. In cell-based (in vitro) research, oliceridine elicits robust G protein signaling, with potency and efficacy similar to that of morphine, but with less β-arrestin 2 recruitment and receptor internalization—thus, it may have fewer adverse effects than morphine.[1][2][3][4] In general, in vitro potency does not guarantee any clinical relevance in humans.[5]

See also

References

  1. ↑ Chen XT, Pitis P, Liu G, Yuan C, Gotchev D, Cowan CL, Rominger DH, Koblish M, Dewire SM, Crombie AL, Violin JD, Yamashita DS (October 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". Journal of Medicinal Chemistry. 56 (20): 8019–31. doi:10.1021/jm4010829. PMID 24063433. (Subscription required (help)).
  2. ↑ 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". Journal of Pharmacology and Experimental Therapeutics. 344 (3): 708–17. doi:10.1124/jpet.112.201616. PMID 23300227.
  3. ↑ 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". The Journal of Clinical Pharmacology. 54 (3): 351–7. doi:10.1002/jcph.207. PMID 24122908. (Subscription required (help)).
  4. ↑ Staff (1 October 2015). "Acute Postoperative Pain". Genetic Engineering & Biotechnology News (Paper). 35 (17): 40.
  5. ↑ Waldman, SA (July 2002). "Does potency predict clinical efficacy? Illustration through an antihistamine model". Annals of allergy, asthma & immunology : official publication of the American College of Allergy, Asthma, & Immunology. 89 (1): 7–11, quiz 11-2, 77. doi:10.1016/S1081-1206(10)61904-7. PMID 12141724.



This article is issued from Wikipedia. The text is licensed under Creative Commons - Attribution - Sharealike. Additional terms may apply for the media files.