Identification

Name
Oliceridine
Accession Number
DB14881
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.4,5 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.2,5 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.1,2,3,4,5

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.1,2 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.1,2,6,7,8,9,10,15

Oliceridine was first reported in 2013,1,14 but was initially not approved by the FDA due to concerns raised by the Anesthetic and Analgesic Drug Products Advisory Committee.4 Oliceridine gained FDA approval on August 7, 2020, and is currently marketed by Trevena Inc as OLINVYK™.15

Type
Small Molecule
Groups
Approved, Investigational
Structure
Thumb
Weight
Average: 386.55
Monoisotopic: 386.202799388
Chemical Formula
C22H30N2O2S
Synonyms
  • Oliceridine
External IDs
  • TRV 130
  • TRV-130
  • TRV130

Pharmacology

Indication

Oliceridine is indicated for the management of acute pain in adults severe enough to require intravenous opioid analgesics and for whom no acceptable alternative treatments exist.15

Associated Conditions
Contraindications & Blackbox Warnings
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Pharmacodynamics

Oliceridine is a biased μ-opioid receptor agonist that acts through downstream signalling pathways to exert antinociceptive analgesia in patients experience severe acute pain.1,2,3,4,5,15 Results from multiple clinical studies6,7,8,9,10,15 and simulation data11,12 demonstrate that oliceridine exerts significant analgesic benefits within 5-20 minutes following administration but dissipates quickly with a half-life between one and three hours.6,7,8,9,10,15 Despite an improved adverse effect profile over conventional opioids6,7,8,9,10,15, oliceridine carries important clinical warnings. Oliceridine has the potential to cause severe respiratory depression, especially in patients who are elderly, cachectic, debilitated, or who otherwise have chronically impaired pulmonary function. In addition, severe respiratory depression or sedation may occur in patients with increased intracranial pressure, head injury, brain tumour, or impaired consciousness. Patients with adrenal insufficiency or severe hypotension may require treatment alterations or discontinuation. Finally, oliceridine has been demonstrated to prolong the QTc interval and has not been properly evaluated beyond a maximum daily dose of 27 mg; it is recommended not to exceed 27 mg per day.15

Mechanism of action

Pain perception follows a complex pathway initiated in primary sensory neurons, subsequently transmitted to the spinal cord dorsal horn and through ascending axons to multiple regions within the thalamus, brainstem, and midbrain, and finally relayed through descending signals that either inhibit or facilitate the nociceptive signalling.4,5 Opioid receptors are seven-transmembrane G-protein-coupled receptors (GPCRs) that can be divided into μ, κ, δ, and opioid-like-1 (ORL1) subtypes,2,5. However, the μ-opioid receptor is predominantly targeted by and is responsible for the effects of traditional opioids.5 GPCRs in the inactive state are bound intracellularly by a complex consisting of a Gα, β, and γ subunit together with guanosine diphosphate (GDP). Activation of the GPCR through extracellular agonist binding catalyzes the replacement of GDP with guanosine triphosphate (GTP), dissociation of both Gα-GTP and a βγ heterodimer, and subsequent downstream effects.5

In the case of the μ-opioid receptor, the Gα-GTP directly interacts with the potassium channel Kir3 while the dissociated Gβγ subunit directly binds to and occludes the pore of P/Q-, N-, and L-type Ca2+ channels. Furthermore, opioid receptor activation inhibits adenylyl cyclase, which in turn reduces cAMP-dependent Ca2+ influx. By altering membrane ion conductivity, these effects modulate nociceptive signalling and produce an analgesic effect.3,4,5 In addition to the G-protein pathway, μ-opioid receptor activation can also result in downstream signalling through β-arrestin, which results in receptor internalization and is associated with negative effects of opioid use including respiratory depression, gastrointestinal effects, and desensitization/tolerance.1,2,3,4,5

Oliceridine acts as a "biased agonist" at the μ-opioid receptor by preferentially activating the G-protein pathway with minimal receptor phosphorylation and recruitment of β-arrestin.1,2 Competetive binding assays and structural modelling suggest that the binding site for oliceridine on the μ-opioid receptor is the same as for classical opioids.1,13 However, molecular modelling supports a model whereby oliceridine binding induces a different intracellular conformation of the μ-opioid receptor, specifically due to a lack of coupling with transmembrane helix six, which confers the specificity for G-protein over β-arrestin interaction.13 Numerous in vitro, in vivo, and clinical studies support the view that this biased agonism results in comparable analgesia compared with traditional opioids at a comparable or decreased risk of opioid-related adverse effects such as constipation and respiratory depression.1,2,6,7,8,9,10,15

TargetActionsOrganism
AMu-type opioid receptor
agonist
Humans
Absorption

Oliceridine administered as a single intravenous injection of 1.5, 3, or 4.5 mg in healthy male volunteers had a corresponding Cmax of 47, 76, and 119 ng/mL and a corresponding AUC0-24 of 43, 82, and 122 ng*h/mL.6 Simulations of single doses of oliceridine between 1-3 mg suggest that the expected median Cmax is between 43 and 130 ng/mL while the expected median AUC is between 22 and 70 ng*h/mL.12

Volume of distribution

Oliceridine has a mean steady-state volume of distribution of 90-120 L.15

Protein binding

Oliceridine is approximately 77% bound to plasma proteins.15

Metabolism

Oliceridine is primarily metabolized hepatically by CYP3A4 and CYP2D6 in vitro, with minor contributions from CYP2C9 and CYP2C19.15 None of oliceridine's metabolites are known to be active.5,15 Metabolic pathways include N-dealkylation, glucuronidation, and dehydrogenation.15

Hover over products below to view reaction partners

Route of elimination

Approximately 70% of oliceridine is eliminated via the renal route, of which only 0.97-6.75% of an initial dose is recovered unchanged. The remaining 30% is eliminated in feces.15

Half-life

Oliceridine has a half-life of 1.3-3 hours while its metabolites, none of which are known to be active, have a substantially longer half-life of 44 hours.15

Clearance

Healthy volunteers given doses of oliceridine between 0.15 and 7 mg had mean clearance rates between 34 and 59.6 L/h.11,12

Adverse Effects
Learn about our commercial Adverse Effects data.
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Toxicity

Symptoms of oliceridine overdose are variable but can include respiratory depression, airway obstruction, pulmonary edema, bradycardia, hypotension, muscle flaccidity, cold skin, and somnolence progressing to either stupor or coma. Miosis is commonly observed but in cases of severe hypoxia, mydriasis may be observed instead. Oliceridine overdose may be fatal. In case of overdose, the establishment of a protected airway followed by the institution of assisted or controlled ventilation is a high priority; in case of cardiac arrhythmias or arrest, additional supportive measures may be immediately required. Supportive treatment, including oxygen, vasopressors, and the administration of an opioid antagonist such as naloxone may be applied but should be tailored to the individual patient's condition.15

Affected organisms
  • Humans and other mammals
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
DrugInteraction
AbametapirThe serum concentration of Oliceridine can be increased when it is combined with Abametapir.
AbataceptThe metabolism of Oliceridine can be increased when combined with Abatacept.
AbirateroneThe serum concentration of Oliceridine can be increased when it is combined with Abiraterone.
AcebutololThe metabolism of Oliceridine can be decreased when combined with Acebutolol.
AcetaminophenThe serum concentration of Oliceridine can be decreased when it is combined with Acetaminophen.
AcetazolamideThe risk or severity of hypotension, sedation, death, somnolence, and respiratory depression can be increased when Acetazolamide is combined with Oliceridine.
AcetophenazineThe risk or severity of hypotension, sedation, death, somnolence, and respiratory depression can be increased when Acetophenazine is combined with Oliceridine.
AclidiniumThe risk or severity of urinary retention, reduced gastrointestinal motility, and constipation can be increased when Aclidinium is combined with Oliceridine.
AdalimumabThe metabolism of Oliceridine can be increased when combined with Adalimumab.
AgomelatineThe risk or severity of hypotension, sedation, death, somnolence, and respiratory depression can be increased when Agomelatine is combined with Oliceridine.
Additional Data Available
  • Extended Description
    Extended Description

    Extended description of the mechanism of action and particular properties of each drug interaction.

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  • Severity
    Severity

    A severity rating for each drug interaction, from minor to major.

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  • Evidence Level
    Evidence Level

    A rating for the strength of the evidence supporting each drug interaction.

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  • Action
    Action

    An effect category for each drug interaction. Know how this interaction affects the subject drug.

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Food Interactions
No interactions found.

Products

International/Other Brands
Olinvo / Olinvyk
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
OlinvykInjection, solution2 mg/2mLIntravenousTrevena, Inc.2020-08-07Not applicableUS flag
OlinvykInjection, solution1 mg/1mLIntravenousTrevena, Inc.2020-08-07Not applicableUS flag
OlinvykInjection, solution30 mg/30mLIntravenousTrevena, Inc.2020-08-07Not applicableUS flag
Additional Data Available
  • Application Number
    Application Number

    A unique ID assigned by the FDA when a product is submitted for approval by the labeller.

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  • Product Code
    Product Code

    A governmentally-recognized ID which uniquely identifies the product within its regulatory market.

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Categories

Drug Categories
Classification
Not classified

Chemical Identifiers

UNII
MCN858TCP0
CAS number
1401028-24-7
InChI Key
DMNOVGJWPASQDL-OAQYLSRUSA-N
InChI
InChI=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
IUPAC Name
[(3-methoxythiophen-2-yl)methyl]({2-[(9R)-9-(pyridin-2-yl)-6-oxaspiro[4.5]decan-9-yl]ethyl})amine
SMILES
COC1=C(CNCC[[email protected]]2(CCOC3(CCCC3)C2)C2=NC=CC=C2)SC=C1

References

Synthesis Reference

Chen XT, Pitis P, Liu G, Yuan C, Gotchev D, Cowan CL, Rominger DH, Koblish M, Dewire SM, Crombie AL, Violin JD, Yamashita DS: Structure-activity relationships and discovery of a G protein biased mu opioid receptor ligand, (3-methoxythiophen-2-yl)methylamine (TRV130), for the treatment of acute severe pain. J Med Chem. 2013 Oct 24;56(20):8019-31. doi: 10.1021/jm4010829.

General References
  1. 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: A G protein-biased ligand at the mu-opioid receptor is potently analgesic with reduced gastrointestinal and respiratory dysfunction compared with morphine. J Pharmacol Exp Ther. 2013 Mar;344(3):708-17. doi: 10.1124/jpet.112.201616. Epub 2013 Jan 8. [PubMed:23300227]
  2. Manglik A, Lin H, Aryal DK, McCorvy JD, Dengler D, Corder G, Levit A, Kling RC, Bernat V, Hubner H, Huang XP, Sassano MF, Giguere PM, Lober S, Da Duan, Scherrer G, Kobilka BK, Gmeiner P, Roth BL, Shoichet BK: Structure-based discovery of opioid analgesics with reduced side effects. Nature. 2016 Sep 8;537(7619):185-190. doi: 10.1038/nature19112. Epub 2016 Aug 17. [PubMed:27533032]
  3. Ok HG, Kim SY, Lee SJ, Kim TK, Huh BK, Kim KH: Can oliceridine (TRV130), an ideal novel micro receptor G protein pathway selective (micro-GPS) modulator, provide analgesia without opioid-related adverse reactions? Korean J Pain. 2018 Apr;31(2):73-79. doi: 10.3344/kjp.2018.31.2.73. Epub 2018 Apr 2. [PubMed:29686804]
  4. Azzam AAH, McDonald J, Lambert DG: Hot topics in opioid pharmacology: mixed and biased opioids. Br J Anaesth. 2019 Jun;122(6):e136-e145. doi: 10.1016/j.bja.2019.03.006. Epub 2019 Apr 19. [PubMed:31010646]
  5. Urits I, Viswanath O, Orhurhu V, Gress K, Charipova K, Kaye AD, Ngo A: The Utilization of Mu-Opioid Receptor Biased Agonists: Oliceridine, an Opioid Analgesic with Reduced Adverse Effects. Curr Pain Headache Rep. 2019 Mar 18;23(5):31. doi: 10.1007/s11916-019-0773-1. [PubMed:30880365]
  6. Soergel DG, Subach RA, Burnham N, Lark MW, James IE, Sadler BM, Skobieranda F, Violin JD, Webster LR: Biased agonism of the mu-opioid receptor by TRV130 increases analgesia and reduces on-target adverse effects versus morphine: A randomized, double-blind, placebo-controlled, crossover study in healthy volunteers. Pain. 2014 Sep;155(9):1829-35. doi: 10.1016/j.pain.2014.06.011. Epub 2014 Jun 19. [PubMed:24954166]
  7. Viscusi ER, Webster L, Kuss M, Daniels S, Bolognese JA, Zuckerman S, Soergel DG, Subach RA, Cook E, Skobieranda F: A randomized, phase 2 study investigating TRV130, a biased ligand of the mu-opioid receptor, for the intravenous treatment of acute pain. Pain. 2016 Jan;157(1):264-72. doi: 10.1097/j.pain.0000000000000363. [PubMed:26683109]
  8. Singla N, Minkowitz HS, Soergel DG, Burt DA, Subach RA, Salamea MY, Fossler MJ, Skobieranda F: A randomized, Phase IIb study investigating oliceridine (TRV130), a novel micro-receptor G-protein pathway selective (mu-GPS) modulator, for the management of moderate to severe acute pain following abdominoplasty. J Pain Res. 2017 Oct 6;10:2413-2424. doi: 10.2147/JPR.S137952. eCollection 2017. [PubMed:29062240]
  9. Singla NK, Skobieranda F, Soergel DG, Salamea M, Burt DA, Demitrack MA, Viscusi ER: APOLLO-2: A Randomized, Placebo and Active-Controlled Phase III Study Investigating Oliceridine (TRV130), a G Protein-Biased Ligand at the mu-Opioid Receptor, for Management of Moderate to Severe Acute Pain Following Abdominoplasty. Pain Pract. 2019 Sep;19(7):715-731. doi: 10.1111/papr.12801. Epub 2019 Jun 24. [PubMed:31162798]
  10. Viscusi ER, Skobieranda F, Soergel DG, Cook E, Burt DA, Singla N: APOLLO-1: a randomized placebo and active-controlled phase III study investigating oliceridine (TRV130), a G protein-biased ligand at the micro-opioid receptor, for management of moderate-to-severe acute pain following bunionectomy. J Pain Res. 2019 Mar 11;12:927-943. doi: 10.2147/JPR.S171013. eCollection 2019. [PubMed:30881102]
  11. Fossler MJ, Sadler BM, Farrell C, Burt DA, Pitsiu M, Skobieranda F, Soergel DG: Oliceridine, a Novel G Protein-Biased Ligand at the mu-Opioid Receptor, Demonstrates a Predictable Relationship Between Plasma Concentrations and Pain Relief. II: Simulation of Potential Phase 3 Study Designs Using a Pharmacokinetic/Pharmacodynamic Model. J Clin Pharmacol. 2018 Jun;58(6):762-770. doi: 10.1002/jcph.1075. Epub 2018 Feb 2. [PubMed:29393971]
  12. Fossler MJ, Sadler BM, Farrell C, Burt DA, Pitsiu M, Skobieranda F, Soergel DG: Oliceridine (TRV130), a Novel G Protein-Biased Ligand at the mu-Opioid Receptor, Demonstrates a Predictable Relationship Between Plasma Concentrations and Pain Relief. I: Development of a Pharmacokinetic/Pharmacodynamic Model. J Clin Pharmacol. 2018 Jun;58(6):750-761. doi: 10.1002/jcph.1076. Epub 2018 Feb 7. [PubMed:29412458]
  13. Schneider S, Provasi D, Filizola M: How Oliceridine (TRV-130) Binds and Stabilizes a mu-Opioid Receptor Conformational State That Selectively Triggers G Protein Signaling Pathways. Biochemistry. 2016 Nov 22;55(46):6456-6466. doi: 10.1021/acs.biochem.6b00948. Epub 2016 Nov 7. [PubMed:27778501]
  14. Chen XT, Pitis P, Liu G, Yuan C, Gotchev D, Cowan CL, Rominger DH, Koblish M, Dewire SM, Crombie AL, Violin JD, Yamashita DS: Structure-activity relationships and discovery of a G protein biased mu 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. 2013 Oct 24;56(20):8019-31. doi: 10.1021/jm4010829. Epub 2013 Oct 14. [PubMed:24063433]
  15. FDA Approved Drug Products: Olinvyk (oliceridine) injection [Link]
  16. FDA Briefing Document: Oliceridine [Link]
ChemSpider
30841043
RxNav
2392230
ChEMBL
CHEMBL2443262
ZINC
ZINC000096940334
Wikipedia
Oliceridine

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
3CompletedTreatmentPain, Acute3
2CompletedTreatmentPain1
2CompletedTreatmentPain, Acute1
2TerminatedTreatmentPain1
1CompletedTreatmentHealthy Volunteers2
1CompletedTreatmentPain, Acute1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
FormRouteStrength
Injection, solutionIntravenous1 mg/1mL
Injection, solutionIntravenous2 mg/2mL
Injection, solutionIntravenous30 mg/30mL
Prices
Not Available
Patents
Not Available

Properties

State
Solid
Experimental Properties
PropertyValueSource
logP3.19DeWire 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: A G protein-biased ligand at the mu-opioid receptor is potently analgesic with reduced gastrointestinal and respiratory dysfunction compared with morphine. J Pharmacol Exp Ther. 2013 Mar;344(3):708-17. doi: 10.1124/jpet.112.201616.
Predicted Properties
PropertyValueSource
Water Solubility0.00131 mg/mLALOGPS
logP3.88ALOGPS
logP3.96ChemAxon
logS-5.5ALOGPS
pKa (Strongest Basic)9.12ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count4ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area43.38 Å2ChemAxon
Rotatable Bond Count7ChemAxon
Refractivity108.97 m3·mol-1ChemAxon
Polarizability42.65 Å3ChemAxon
Number of Rings4ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleYesChemAxon
Predicted ADMET Features
Not Available

Spectra

Mass Spec (NIST)
Not Available
Spectra
Not Available

Targets

Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Agonist
Curator comments
Oliceridine is approximately 400-fold selective for the mu-type opioid receptor over all other opioid receptor subtypes in cell-based assays.
General Function
Voltage-gated calcium channel activity
Specific Function
Receptor for endogenous opioids such as beta-endorphin and endomorphin. Receptor for natural and synthetic opioids including morphine, heroin, DAMGO, fentanyl, etorphine, buprenorphin and methadone...
Gene Name
OPRM1
Uniprot ID
P35372
Uniprot Name
Mu-type opioid receptor
Molecular Weight
44778.855 Da
References
  1. Schneider S, Provasi D, Filizola M: How Oliceridine (TRV-130) Binds and Stabilizes a mu-Opioid Receptor Conformational State That Selectively Triggers G Protein Signaling Pathways. Biochemistry. 2016 Nov 22;55(46):6456-6466. doi: 10.1021/acs.biochem.6b00948. Epub 2016 Nov 7. [PubMed:27778501]
  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: A G protein-biased ligand at the mu-opioid receptor is potently analgesic with reduced gastrointestinal and respiratory dysfunction compared with morphine. J Pharmacol Exp Ther. 2013 Mar;344(3):708-17. doi: 10.1124/jpet.112.201616. Epub 2013 Jan 8. [PubMed:23300227]
  3. Manglik A, Lin H, Aryal DK, McCorvy JD, Dengler D, Corder G, Levit A, Kling RC, Bernat V, Hubner H, Huang XP, Sassano MF, Giguere PM, Lober S, Da Duan, Scherrer G, Kobilka BK, Gmeiner P, Roth BL, Shoichet BK: Structure-based discovery of opioid analgesics with reduced side effects. Nature. 2016 Sep 8;537(7619):185-190. doi: 10.1038/nature19112. Epub 2016 Aug 17. [PubMed:27533032]
  4. Urits I, Viswanath O, Orhurhu V, Gress K, Charipova K, Kaye AD, Ngo A: The Utilization of Mu-Opioid Receptor Biased Agonists: Oliceridine, an Opioid Analgesic with Reduced Adverse Effects. Curr Pain Headache Rep. 2019 Mar 18;23(5):31. doi: 10.1007/s11916-019-0773-1. [PubMed:30880365]
  5. FDA Approved Drug Products: Olinvyk (oliceridine) injection [Link]

Enzymes

Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Substrate
Curator comments
In vitro studies suggest that oliceridine is primarily metabolized by CYP3A4 and CYP2D6.
General Function
Vitamin d3 25-hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
Gene Name
CYP3A4
Uniprot ID
P08684
Uniprot Name
Cytochrome P450 3A4
Molecular Weight
57342.67 Da
References
  1. Flockhart Table of Drug Interactions [Link]
  2. FDA Drug Development and Drug Interactions: Table of Substrates, Inhibitors and Inducers [Link]
  3. FDA Approved Drug Products: Olinvyk (oliceridine) injection [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
Curator comments
In vitro studies suggest that oliceridine is primarily metabolized by CYP3A4 and CYP2D6.
General Function
Steroid hydroxylase activity
Specific Function
Responsible for the metabolism of many drugs and environmental chemicals that it oxidizes. It is involved in the metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic...
Gene Name
CYP2D6
Uniprot ID
P10635
Uniprot Name
Cytochrome P450 2D6
Molecular Weight
55768.94 Da
References
  1. Flockhart Table of Drug Interactions [Link]
  2. FDA Drug Development and Drug Interactions: Table of Substrates, Inhibitors and Inducers [Link]
  3. FDA Approved Drug Products: Olinvyk (oliceridine) injection [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
Curator comments
In vitro studies suggest that CYP2C9 and CYP2C19 have minor roles in the metabolism of oliceridine.
General Function
Steroid hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP2C9
Uniprot ID
P11712
Uniprot Name
Cytochrome P450 2C9
Molecular Weight
55627.365 Da
References
  1. Flockhart Table of Drug Interactions [Link]
  2. FDA Drug Development and Drug Interactions: Table of Substrates, Inhibitors and Inducers [Link]
  3. FDA Approved Drug Products: Olinvyk (oliceridine) injection [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
Curator comments
In vitro studies suggest that CYP2C9 and CYP2C19 have minor roles in the metabolism of oliceridine.
General Function
Steroid hydroxylase activity
Specific Function
Responsible for the metabolism of a number of therapeutic agents such as the anticonvulsant drug S-mephenytoin, omeprazole, proguanil, certain barbiturates, diazepam, propranolol, citalopram and im...
Gene Name
CYP2C19
Uniprot ID
P33261
Uniprot Name
Cytochrome P450 2C19
Molecular Weight
55930.545 Da
References
  1. Flockhart Table of Drug Interactions [Link]
  2. FDA Drug Development and Drug Interactions: Table of Substrates, Inhibitors and Inducers [Link]
  3. FDA Approved Drug Products: Olinvyk (oliceridine) injection [Link]

Drug created on May 20, 2019 08:32 / Updated on August 16, 2020 00:13

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