Basic Information
ID DDInter1329
Drug Type small molecule
Molecular Formula C22H30N2O2S
Molecular Weight 386.550
CAS Number 1401028-24-7
Description Severe acute pain occurs through nociceptive signalling involving both ascending and descending spinal pathways, in which nerve conductance is mediated in part by the action of opioid receptors.[A218041, A218046] Opioid receptors are seven-transmembrane G-protein-coupled receptors (GPCRs), of which the μ-opioid receptor subtype is predominantly targeted by and is responsible for the effects of opioid agonists.[A218031, A218046] However, due to the ability of some opioid agonists to bind to other targets, as well as activation of additional downstream pathways from opioid receptors such as those involving β-arrestin, the beneficial analgesic effects of opioids are coupled with severe adverse effects such as constipation and respiratory depression.[A218026, A218031, A218036, A218041, A218046] Oliceridine (formerly known as TRV130) is a "biased agonist" at the μ-opioid receptor by preferentially activating the G-protein pathway with minimal receptor phosphorylation and recruitment of β-arrestin.[A218026, A218031] By acting as a biased agonist, oliceridine provides comparable analgesia compared with traditional opioids such as [morphine] at a comparable or decreased risk of opioid-related adverse effects such as constipation and respiratory depression.[A218026, A218031, A218051, A218056, A218061, A218066, A218071, L15516] Oliceridine was first reported in 2013,[A218026, A218086] but was initially not approved by the FDA due to concerns raised by the Anesthetic and Analgesic Drug Products Advisory Committee.[A218041] Oliceridine gained FDA approval on August 7, 2020, and is currently marketed by Trevena Inc as OLINVYK™.[L15516]
ATC Classification N02AX07
IUPAC Name [(3-methoxythiophen-2-yl)methyl]({2-[(9R)-9-(pyridin-2-yl)-6-oxaspiro[4.5]decan-9-yl]ethyl})amine
InChI DMNOVGJWPASQDL-OAQYLSRUSA-N
Canonical SMILES COC1=C(CNCC[C@]2(CCOC3(CCCC3)C2)C2=NC=CC=C2)SC=C1
Useful Links DrugBank ChemSpider BindingDB Wikipedia ChEMBL ZINC
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