| 词条 | Oliceridine |
| 释义 |
| drug_name = | IUPAC_name = N-[(3-Methoxythiophen-2-yl)methyl]-2-[(9R)-9-pyridin-2-yl-6-oxaspiro[4.5]decan-9-yl]ethanamine | image = TRV130.svg | width = 200 | alt = | caption = | tradename = Olinvo | Drugs.com = | MedlinePlus = | pregnancy_AU = | pregnancy_US = | pregnancy_category= | legal_AU = | legal_CA = | legal_UK = | legal_US = Investigational New Drug | legal_status = | routes_of_administration = Intravenous | bioavailability = | protein_bound = | metabolism = | elimination_half-life = | excretion = | CAS_number = 1401028-24-7 | ATCvet = | ATC_prefix = none | ATC_suffix = | PubChem = 66553195 | DrugBank = | ChemSpiderID = 30841043 | UNII = MCN858TCP0 | KEGG = D11214 | ChEMBL = 2443262 | synonyms = TRV-130 | C=22 | H=30 | N=2 | O=2 | S=1 | smiles = COc1ccsc1CNCC[C@]2(CCOC3(CCCC3)C2)c4ccccn4 | StdInChI = 1S/C22H30N2O2S/c1-25-18-7-15-27-19(18)16-23-13-10-21(20-6-2-5-12-24-20)11-14-26-22(17-21)8-3-4-9-22/h2,5-7,12,15,23H,3-4,8-11,13-14,16-17H2,1H3/t21-/m1/s1 | StdInChIKey = DMNOVGJWPASQDL-OAQYLSRUSA-N }}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] Society and cultureAn 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
References1. ^{{cite journal|year=October 2013|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=Journal of Medicinal Chemistry|volume=56|issue=20|pages=8019–31|doi=10.1021/jm4010829|pmid=24063433|subscription=yes|author=|month=|vauthors=Chen XT, Pitis P, Liu G, Yuan C, Gotchev D, Cowan CL, Rominger DH, Koblish M, Dewire SM, Crombie AL, Violin JD, Yamashita DS}} 2. ^{{cite journal|date=March 2013|title=A G protein-biased ligand at the μ-opioid receptor is potently analgesic with reduced gastrointestinal and respiratory dysfunction compared with morphine|journal=Journal of Pharmacology and Experimental Therapeutics|volume=344|issue=3|pages=708–17|doi=10.1124/jpet.112.201616|pmid=23300227|author=|vauthors=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}} 3. ^{{cite journal|date=October 2013|title=First clinical experience with TRV130: Pharmacokinetics and pharmacodynamics in healthy volunteers|journal=The Journal of Clinical Pharmacology|volume=54|issue=3|pages=351–7|doi=10.1002/jcph.207|pmid=24122908|subscription=yes|author=|vauthors=Soergel DG, Subach RA, Sadler B, Connell J, Marion AS, Cowan C, Violin JD, Lark MW}} 4. ^{{Cite journal|last=Staff|first=|date=1 October 2015|title=Acute Postoperative Pain|url=|journal=Genetic Engineering & Biotechnology News|type=Paper|volume=35|issue=17|page=40|doi=|pmid=|access-date=}} 5. ^{{cite journal |last1=Waldman |first1=SA |title=Does potency predict clinical efficacy? Illustration through an antihistamine model. |journal=Annals of allergy, asthma & immunology : official publication of the American College of Allergy, Asthma, & Immunology |date=July 2002 |volume=89 |issue=1 |pages=7-11; quiz 11-2, 77 |doi=10.1016/S1081-1206(10)61904-7 |pmid=12141724 }} 6. ^{{cite web |title=FDA Panel Votes Against Analgesic Oliceridine |url=https://www.medpagetoday.com/painmanagement/opioids/75668 |website=www.medpagetoday.com |publisher=MedPage Today, LLC |accessdate=23 December 2018 |language=en |date=11 October 2018}} 7. ^{{cite web |title=FDA rejects Trevena’s painkiller oliceridine {{!}} FierceBiotech |url=https://www.fiercebiotech.com/biotech/fda-rejects-trevena-s-painkiller-oliceridine |website=www.fiercebiotech.com |publisher=Questex LLC |accessdate=23 December 2018 |language=en}} External links
7 : Analgesics|Biased ligands|Experimental drugs|Mu-opioid agonists|Pyridines|Spiro compounds|Thiophenes |
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