Oliceridine

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]

Oliceridine
Clinical data
Trade namesOlinvo
Other namesTRV-130
Routes of
administration		Intravenous
ATC code
  • none
Legal status
Legal status
Identifiers
CAS Number
PubChem CID
ChemSpider
UNII
KEGG
ChEMBL
Chemical and physical data
FormulaC22H30N2O2S
Molar mass386.55 g·mol−1
3D model (JSmol)

Society and culture

An FDA advisory committee voted against the approval of oliceridine in 2018, due to concerns that the benefit of the drug did not exceed the risk. The risks of oliceridine include prolongation of the QT interval on the ECG, and depression of the respiratory drive (which could cause a person to stop breathing).[6] As a result of the committee's vote, the FDA declined to approve oliceridine, citing safety concerns.[7]

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 (subscription required) (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.CS1 maint: uses authors parameter (link)
  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.
  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. 89 (1): 7–11, quiz 11-2, 77. doi:10.1016/S1081-1206(10)61904-7. PMID 12141724.
  6. "FDA Panel Votes Against Analgesic Oliceridine". www.medpagetoday.com. MedPage Today, LLC. 11 October 2018. Retrieved 23 December 2018.
  7. "FDA rejects Trevena's painkiller oliceridine | FierceBiotech". www.fiercebiotech.com. Questex LLC. Retrieved 23 December 2018.


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