Identification

Name
Eluxadoline
Accession Number
DB09272
Type
Small Molecule
Groups
Approved
Description

Eluxadoline is a mixed mu-opioid receptor agonist, kappa-opioid receptor agonist, and a-delta opioid receptor antagonist indicated for use in diarrhea-predominant irritable bowel syndrome (IBS-D). The mu-, kappa-, and delta-opioid receptors mediate endogenous and exogenous opioid response in the central nervous system and peripherally in the gastrointestinal system. Agonism of peripheral mu-opioid receptors results in reduced colonic motility, while antagonism of central delta-opioid receptors results in improved analgesia, making eluxadoline usable for the symptoms of both pain and diarrhea characteristic of IBS-D.

Marketed under the tradename Viberzi (FDA), eluxadoline is an antimotility agent that decreases bowel contractions, inhibits colonic transit, and reduces fluid/ion secretion resulting in improved symptoms of abdominal pain and reductions in the Bristol Stool Scale.

Structure
Thumb
Synonyms
  • 5-({(4-carbamoyl-2,6-dimethyl-L-phenylalanyl)[(1S)-1-(4-phenyl-1H-imidazol-2-yl)ethyl]amino}methyl)-2-methoxybenzoic acid
External IDs
JNJ 27018966 / JNJ-27018966 / JNJ27018966
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
ViberziTablet, film coated75 mg/1OralAllergan2015-10-01Not applicableUs
ViberziTablet100 mgOralAllergan Pharma Co.2017-04-24Not applicableCanada
ViberziTablet, film coated100 mg/1OralAllergan2015-10-01Not applicableUs
ViberziTablet75 mgOralAllergan Pharma Co.2017-04-24Not applicableCanada
Categories
UNII
45TPJ4MBQ1
CAS number
864821-90-9
Weight
Average: 569.662
Monoisotopic: 569.263819247
Chemical Formula
C32H35N5O5
InChI Key
QFNHIDANIVGXPE-FNZWTVRRSA-N
InChI
InChI=1S/C32H35N5O5/c1-18-12-23(29(34)38)13-19(2)24(18)15-26(33)31(39)37(17-21-10-11-28(42-4)25(14-21)32(40)41)20(3)30-35-16-27(36-30)22-8-6-5-7-9-22/h5-14,16,20,26H,15,17,33H2,1-4H3,(H2,34,38)(H,35,36)(H,40,41)/t20-,26-/m0/s1
IUPAC Name
5-{[(2S)-2-amino-3-(4-carbamoyl-2,6-dimethylphenyl)-N-[(1S)-1-(4-phenyl-1H-imidazol-2-yl)ethyl]propanamido]methyl}-2-methoxybenzoic acid
SMILES
COC1=CC=C(CN([[email protected]@H](C)C2=NC(=CN2)C2=CC=CC=C2)C(=O)[[email protected]@H](N)CC2=C(C)C=C(C=C2C)C(N)=O)C=C1C(O)=O

Pharmacology

Indication

For the treatment of irritable bowel syndrome with diarrhea (IBS-D).

Structured Indications
Pharmacodynamics
Not Available
Mechanism of action

Eluxadoline is a mu-opioid receptor agonis, kappa opioid receptor agonist and a delta opioid receptor antagonist. Eluxadoline is used for diarrhea predominant IBS because it reduces intestinal contractility and normalizes stress-induced acceleration of upper GI transit. Antagonistic activity at the delta receptor minimizes the constipating effect usually seen by mu-opioid receptor agonists alone. Because of it's limited systemic bioavailability, there may be less side effects associated with the use of eluxadoline in comparison with other therapies used to treat diarrhea predominant IBS.

TargetActionsOrganism
AMu-type opioid receptor
agonist
Human
ADelta-type opioid receptor
antagonist
Human
AKappa-type opioid receptor
agonist
Human
Absorption

The oral absorption of eluxadoline is poor - estimated to be 1.02%, this could be attributed to poor in vitro GI permeability, and its zwitterionic nature leading to a negatively charged molecule across the GI pH range.

Volume of distribution
Not Available
Protein binding

81%

Metabolism

The metabolism of eluxadoline is currently unclear, however evidence suggests limited glucoronidation forms an acyl glucuronide metabolite that is then excreted into urine.

Route of elimination

82% excreted in feces, <1% excreted in urine.

Half life

The mean plasma elimination half-life ranged from 3.7 hours to 6 hours.

Clearance
Not Available
Toxicity

The most common adverse reactions (>5%) are constipation, nausea and abdominal pain.

Affected organisms
Not Available
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteractionDrug group
AclidiniumAclidinium may increase the constipating activities of Eluxadoline.Approved
AlcuroniumAlcuronium may increase the constipating activities of Eluxadoline.Experimental
AlfentanilAlfentanil may increase the constipating activities of Eluxadoline.Approved, Illicit
AlosetronAlosetron may increase the constipating activities of Eluxadoline.Approved, Withdrawn
AlphacetylmethadolAlphacetylmethadol may increase the constipating activities of Eluxadoline.Experimental, Illicit
AlphaprodineAlphaprodine may increase the constipating activities of Eluxadoline.Illicit
Anisotropine MethylbromideAnisotropine Methylbromide may increase the constipating activities of Eluxadoline.Approved
AtazanavirThe serum concentration of Eluxadoline can be increased when it is combined with Atazanavir.Approved, Investigational
AtracuriumAtracurium may increase the constipating activities of Eluxadoline.Experimental, Investigational
Atracurium besylateAtracurium besylate may increase the constipating activities of Eluxadoline.Approved
AtropineAtropine may increase the constipating activities of Eluxadoline.Approved, Vet Approved
BenactyzineBenactyzine may increase the constipating activities of Eluxadoline.Withdrawn
BenzatropineBenzatropine may increase the constipating activities of Eluxadoline.Approved
BezitramideBezitramide may increase the constipating activities of Eluxadoline.Experimental, Illicit, Withdrawn
BiperidenBiperiden may increase the constipating activities of Eluxadoline.Approved, Investigational
BornaprineBornaprine may increase the constipating activities of Eluxadoline.Experimental
BuprenorphineBuprenorphine may increase the constipating activities of Eluxadoline.Approved, Illicit, Investigational, Vet Approved
ButorphanolButorphanol may increase the constipating activities of Eluxadoline.Approved, Illicit, Vet Approved
CarfentanilCarfentanil may increase the constipating activities of Eluxadoline.Illicit, Investigational, Vet Approved
ChlorphenoxamineChlorphenoxamine may increase the constipating activities of Eluxadoline.Withdrawn
CodeineCodeine may increase the constipating activities of Eluxadoline.Approved, Illicit
CyclopentolateCyclopentolate may increase the constipating activities of Eluxadoline.Approved
CyclosporineThe serum concentration of Eluxadoline can be increased when it is combined with Cyclosporine.Approved, Investigational, Vet Approved
DarifenacinDarifenacin may increase the constipating activities of Eluxadoline.Approved, Investigational
DesloratadineDesloratadine may increase the constipating activities of Eluxadoline.Approved, Investigational
DexetimideDexetimide may increase the constipating activities of Eluxadoline.Withdrawn
DextromoramideDextromoramide may increase the constipating activities of Eluxadoline.Experimental, Illicit
DextropropoxypheneDextropropoxyphene may increase the constipating activities of Eluxadoline.Approved, Illicit, Investigational, Withdrawn
DezocineDezocine may increase the constipating activities of Eluxadoline.Approved, Investigational
DicyclomineDicyclomine may increase the constipating activities of Eluxadoline.Approved
DihydrocodeineDihydrocodeine may increase the constipating activities of Eluxadoline.Approved, Illicit
DihydroetorphineDihydroetorphine may increase the constipating activities of Eluxadoline.Experimental, Illicit
DihydromorphineDihydromorphine may increase the constipating activities of Eluxadoline.Experimental, Illicit
DiphenoxylateDiphenoxylate may increase the constipating activities of Eluxadoline.Approved, Illicit
DPDPEDPDPE may increase the constipating activities of Eluxadoline.Investigational
EltrombopagThe serum concentration of Eluxadoline can be increased when it is combined with Eltrombopag.Approved
EmeproniumEmepronium may increase the constipating activities of Eluxadoline.Experimental
EtanautineEtanautine may increase the constipating activities of Eluxadoline.Experimental
EthanolThe risk or severity of adverse effects can be increased when Ethanol is combined with Eluxadoline.Approved
EthopropazineEthopropazine may increase the constipating activities of Eluxadoline.Approved
EthylmorphineEthylmorphine may increase the constipating activities of Eluxadoline.Approved, Illicit
EtorphineEtorphine may increase the constipating activities of Eluxadoline.Illicit, Vet Approved
EtybenzatropineEtybenzatropine may increase the constipating activities of Eluxadoline.Experimental
FentanylFentanyl may increase the constipating activities of Eluxadoline.Approved, Illicit, Investigational, Vet Approved
FesoterodineFesoterodine may increase the constipating activities of Eluxadoline.Approved
GallamineGallamine may increase the constipating activities of Eluxadoline.Experimental
Gallamine TriethiodideGallamine Triethiodide may increase the constipating activities of Eluxadoline.Approved
GemfibrozilThe serum concentration of Eluxadoline can be increased when it is combined with Gemfibrozil.Approved
GlycopyrroniumGlycopyrronium may increase the constipating activities of Eluxadoline.Approved, Investigational, Vet Approved
HeroinHeroin may increase the constipating activities of Eluxadoline.Approved, Illicit, Investigational
HexamethoniumHexamethonium may increase the constipating activities of Eluxadoline.Experimental
HomatropineHomatropine may increase the constipating activities of Eluxadoline.Approved
HydrocodoneHydrocodone may increase the constipating activities of Eluxadoline.Approved, Illicit
HydromorphoneHydromorphone may increase the constipating activities of Eluxadoline.Approved, Illicit
HyoscyamineHyoscyamine may increase the constipating activities of Eluxadoline.Approved
Ipratropium bromideIpratropium bromide may increase the constipating activities of Eluxadoline.Approved
KetobemidoneKetobemidone may increase the constipating activities of Eluxadoline.Approved, Investigational
Levomethadyl AcetateLevomethadyl Acetate may increase the constipating activities of Eluxadoline.Approved, Investigational
LevorphanolLevorphanol may increase the constipating activities of Eluxadoline.Approved
LofentanilLofentanil may increase the constipating activities of Eluxadoline.Illicit
LopinavirThe serum concentration of Eluxadoline can be increased when it is combined with Lopinavir.Approved
MazaticolMazaticol may increase the constipating activities of Eluxadoline.Experimental
MecamylamineMecamylamine may increase the constipating activities of Eluxadoline.Approved
MeptazinolMeptazinol may increase the constipating activities of Eluxadoline.Experimental
MethadoneMethadone may increase the constipating activities of Eluxadoline.Approved
Methadyl AcetateMethadyl Acetate may increase the constipating activities of Eluxadoline.Approved, Illicit
MethanthelineMethantheline may increase the constipating activities of Eluxadoline.Approved, Investigational
MethylnaltrexoneThe risk or severity of adverse effects can be increased when Methylnaltrexone is combined with Eluxadoline.Approved
Methylscopolamine bromideMethylscopolamine bromide may increase the constipating activities of Eluxadoline.Approved
MetixeneMetixene may increase the constipating activities of Eluxadoline.Approved
MorphineMorphine may increase the constipating activities of Eluxadoline.Approved, Investigational
NalbuphineNalbuphine may increase the constipating activities of Eluxadoline.Approved
NaloxegolThe risk or severity of adverse effects can be increased when Eluxadoline is combined with Naloxegol.Approved
NicomorphineNicomorphine may increase the constipating activities of Eluxadoline.Experimental
NormethadoneNormethadone may increase the constipating activities of Eluxadoline.Approved, Illicit
OpiumOpium may increase the constipating activities of Eluxadoline.Approved, Illicit
OrphenadrineOrphenadrine may increase the constipating activities of Eluxadoline.Approved
OtiloniumOtilonium may increase the constipating activities of Eluxadoline.Experimental, Investigational
OxitropiumOxitropium may increase the constipating activities of Eluxadoline.Investigational
OxybutyninOxybutynin may increase the constipating activities of Eluxadoline.Approved, Investigational
OxycodoneOxycodone may increase the constipating activities of Eluxadoline.Approved, Illicit, Investigational
OxymorphoneOxymorphone may increase the constipating activities of Eluxadoline.Approved, Investigational, Vet Approved
OxyphenoniumOxyphenonium may increase the constipating activities of Eluxadoline.Approved
PancuroniumPancuronium may increase the constipating activities of Eluxadoline.Approved
PentazocinePentazocine may increase the constipating activities of Eluxadoline.Approved, Vet Approved
PentoliniumPentolinium may increase the constipating activities of Eluxadoline.Approved
PethidinePethidine may increase the constipating activities of Eluxadoline.Approved
PhenazocinePhenazocine may increase the constipating activities of Eluxadoline.Experimental
PhenglutarimidePhenglutarimide may increase the constipating activities of Eluxadoline.Experimental
PhenoperidinePhenoperidine may increase the constipating activities of Eluxadoline.Experimental
PipecuroniumPipecuronium may increase the constipating activities of Eluxadoline.Approved
PirenzepinePirenzepine may increase the constipating activities of Eluxadoline.Approved
PiritramidePiritramide may increase the constipating activities of Eluxadoline.Investigational
ProcyclidineProcyclidine may increase the constipating activities of Eluxadoline.Approved
PropanthelinePropantheline may increase the constipating activities of Eluxadoline.Approved
PropiverinePropiverine may increase the constipating activities of Eluxadoline.Approved, Investigational
QuinidineQuinidine may increase the constipating activities of Eluxadoline.Approved
RemifentanilRemifentanil may increase the constipating activities of Eluxadoline.Approved
RifampicinThe serum concentration of Eluxadoline can be increased when it is combined with Rifampicin.Approved
RitonavirThe serum concentration of Eluxadoline can be increased when it is combined with Ritonavir.Approved, Investigational
RosuvastatinThe serum concentration of Rosuvastatin can be increased when it is combined with Eluxadoline.Approved
SaquinavirThe serum concentration of Eluxadoline can be increased when it is combined with Saquinavir.Approved, Investigational
ScopolamineScopolamine may increase the constipating activities of Eluxadoline.Approved
Scopolamine butylbromideScopolamine butylbromide may increase the constipating activities of Eluxadoline.Approved, Vet Approved
SolifenacinSolifenacin may increase the constipating activities of Eluxadoline.Approved
SufentanilSufentanil may increase the constipating activities of Eluxadoline.Approved, Investigational
TapentadolTapentadol may increase the constipating activities of Eluxadoline.Approved
TeriflunomideThe serum concentration of Eluxadoline can be increased when it is combined with Teriflunomide.Approved
TilidineTilidine may increase the constipating activities of Eluxadoline.Experimental
TiotropiumTiotropium may increase the constipating activities of Eluxadoline.Approved
TipranavirThe serum concentration of Eluxadoline can be increased when it is combined with Tipranavir.Approved, Investigational
TolterodineTolterodine may increase the constipating activities of Eluxadoline.Approved, Investigational
TramadolTramadol may increase the constipating activities of Eluxadoline.Approved, Investigational
TrihexyphenidylTrihexyphenidyl may increase the constipating activities of Eluxadoline.Approved
TrimethaphanTrimethaphan may increase the constipating activities of Eluxadoline.Approved, Investigational
TropatepineTropatepine may increase the constipating activities of Eluxadoline.Experimental
TropicamideTropicamide may increase the constipating activities of Eluxadoline.Approved
TrospiumTrospium may increase the constipating activities of Eluxadoline.Approved
TubocurarineTubocurarine may increase the constipating activities of Eluxadoline.Approved
UmeclidiniumUmeclidinium may increase the constipating activities of Eluxadoline.Approved
VecuroniumVecuronium may increase the constipating activities of Eluxadoline.Approved
Food Interactions
Not Available

References

Synthesis Reference

Breslin HJ, Diamond CJ, Kavash RW, Cai C, Dyatkin AB, Miskowski TA, Zhang SP, Wade PR, Hornby PJ, He W: Identification of a dual delta OR antagonist/mu OR agonist as a potential therapeutic for diarrhea-predominant Irritable Bowel Syndrome (IBS-d). Bioorg Med Chem Lett. 2012 Jul 15;22(14):4869-72. doi: 10.1016/j.bmcl.2012.05.042. Epub 2012 May 24. Pubmed

General References
  1. Garnock-Jones KP: Eluxadoline: First Global Approval. Drugs. 2015 Jul;75(11):1305-10. doi: 10.1007/s40265-015-0436-4. [PubMed:26149369]
  2. Nee J, Zakari M, Lembo AJ: Current and emerging drug options in the treatment of diarrhea predominant irritable bowel syndrome. Expert Opin Pharmacother. 2015 Dec;16(18):2781-92. doi: 10.1517/14656566.2015.1101449. Epub 2015 Nov 11. [PubMed:26558923]
  3. Dove LS, Lembo A, Randall CW, Fogel R, Andrae D, Davenport JM, McIntyre G, Almenoff JS, Covington PS: Eluxadoline benefits patients with irritable bowel syndrome with diarrhea in a phase 2 study. Gastroenterology. 2013 Aug;145(2):329-38.e1. doi: 10.1053/j.gastro.2013.04.006. Epub 2013 Apr 9. [PubMed:23583433]
  4. Davenport JM, Covington P, Bonifacio L, McIntyre G, Venitz J: Effect of uptake transporters OAT3 and OATP1B1 and efflux transporter MRP2 on the pharmacokinetics of eluxadoline. J Clin Pharmacol. 2015 May;55(5):534-42. doi: 10.1002/jcph.442. Epub 2015 Jan 14. [PubMed:25491493]
  5. Fujita W, Gomes I, Dove LS, Prohaska D, McIntyre G, Devi LA: Molecular characterization of eluxadoline as a potential ligand targeting mu-delta opioid receptor heteromers. Biochem Pharmacol. 2014 Dec 1;92(3):448-56. doi: 10.1016/j.bcp.2014.09.015. Epub 2014 Sep 28. [PubMed:25261794]
External Links
KEGG Drug
D10403
PubChem Compound
11250029
PubChem Substance
310265167
ChemSpider
9425062
BindingDB
50393720
ChEBI
85980
ChEMBL
CHEMBL2159122
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Eluxadoline
AHFS Codes
  • 56:92.00 — Miscellaneous GI Drugs
FDA label
Download (503 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
2CompletedTreatmentIrritable Bowel Syndrome (IBS)1
2Not Yet RecruitingTreatmentIrritable Bowel Syndrome (IBS)1
3CompletedTreatmentIrritable Bowel Syndrome (IBS)2
4RecruitingTreatmentDiarrhoea Predominant Irritable Bowel Syndrome1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage forms
FormRouteStrength
TabletOral100 mg
TabletOral75 mg
Tablet, film coatedOral100 mg/1
Tablet, film coatedOral75 mg/1
Prices
Not Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US9115091No2008-07-072028-07-07Us
US9205076No2005-03-142025-03-14Us
US8691860No2008-07-072028-07-07Us
US8344011No2005-03-142025-03-14Us
US8609709No2005-03-142025-03-14Us
US7741356No2008-03-252028-03-25Us
US7786158No2005-03-142025-03-14Us
US9364489No2008-07-072028-07-07Us
US8772325No2005-03-142025-03-14Us
US9675587No2013-03-142033-03-14Us
US9700542No2005-03-142025-03-14Us

Properties

State
Solid
Experimental Properties
Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.00268 mg/mLALOGPS
logP1.08ALOGPS
logP1.8ChemAxon
logS-5.3ALOGPS
pKa (Strongest Acidic)3.66ChemAxon
pKa (Strongest Basic)7.99ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count7ChemAxon
Hydrogen Donor Count4ChemAxon
Polar Surface Area164.63 Å2ChemAxon
Rotatable Bond Count11ChemAxon
Refractivity160.38 m3·mol-1ChemAxon
Polarizability61.86 Å3ChemAxon
Number of Rings4ChemAxon
Bioavailability0ChemAxon
Rule of FiveNoChemAxon
Ghose FilterNoChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleYesChemAxon
Predicted ADMET features
Not Available

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available

Taxonomy

Description
This compound belongs to the class of organic compounds known as phenylalanine and derivatives. These are compounds containing phenylalanine or a derivative thereof resulting from reaction of phenylalanine at the amino group or the carboxy group, or from the replacement of any hydrogen of glycine by a heteroatom.
Kingdom
Organic compounds
Super Class
Organic acids and derivatives
Class
Carboxylic acids and derivatives
Sub Class
Amino acids, peptides, and analogues
Direct Parent
Phenylalanine and derivatives
Alternative Parents
Alpha amino acid amides / Phenylimidazoles / O-methoxybenzoic acids and derivatives / Amphetamines and derivatives / Benzamides / Benzoic acids / m-Xylenes / Benzoyl derivatives / Anisoles / Imidazolyl carboxylic acids and derivatives
show 16 more
Substituents
Phenylalanine or derivatives / Alpha-amino acid amide / O-methoxybenzoic acid or derivatives / 5-phenylimidazole / 4-phenylimidazole / Amphetamine or derivatives / Benzoic acid / Benzoic acid or derivatives / Benzamide / Imidazolyl carboxylic acid derivative
show 35 more
Molecular Framework
Aromatic heteromonocyclic compounds
External Descriptors
amino acid amide, imidazoles, benzamides, L-phenylalanine derivative, methoxybenzoic acid (CHEBI:85980)

Targets

Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Agonist
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. Fujita W, Gomes I, Dove LS, Prohaska D, McIntyre G, Devi LA: Molecular characterization of eluxadoline as a potential ligand targeting mu-delta opioid receptor heteromers. Biochem Pharmacol. 2014 Dec 1;92(3):448-56. doi: 10.1016/j.bcp.2014.09.015. Epub 2014 Sep 28. [PubMed:25261794]
  2. Dove LS, Lembo A, Randall CW, Fogel R, Andrae D, Davenport JM, McIntyre G, Almenoff JS, Covington PS: Eluxadoline benefits patients with irritable bowel syndrome with diarrhea in a phase 2 study. Gastroenterology. 2013 Aug;145(2):329-38.e1. doi: 10.1053/j.gastro.2013.04.006. Epub 2013 Apr 9. [PubMed:23583433]
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Antagonist
General Function
Opioid receptor activity
Specific Function
G-protein coupled receptor that functions as receptor for endogenous enkephalins and for a subset of other opioids. Ligand binding causes a conformation change that triggers signaling via guanine n...
Gene Name
OPRD1
Uniprot ID
P41143
Uniprot Name
Delta-type opioid receptor
Molecular Weight
40368.235 Da
References
  1. Fujita W, Gomes I, Dove LS, Prohaska D, McIntyre G, Devi LA: Molecular characterization of eluxadoline as a potential ligand targeting mu-delta opioid receptor heteromers. Biochem Pharmacol. 2014 Dec 1;92(3):448-56. doi: 10.1016/j.bcp.2014.09.015. Epub 2014 Sep 28. [PubMed:25261794]
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Agonist
General Function
Opioid receptor activity
Specific Function
G-protein coupled opioid receptor that functions as receptor for endogenous alpha-neoendorphins and dynorphins, but has low affinity for beta-endorphins. Also functions as receptor for various synt...
Gene Name
OPRK1
Uniprot ID
P41145
Uniprot Name
Kappa-type opioid receptor
Molecular Weight
42644.665 Da

Transporters

Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
Inhibitor
General Function
Sodium-independent organic anion transmembrane transporter activity
Specific Function
Mediates the Na(+)-independent uptake of organic anions such as pravastatin, taurocholate, methotrexate, dehydroepiandrosterone sulfate, 17-beta-glucuronosyl estradiol, estrone sulfate, prostagland...
Gene Name
SLCO1B1
Uniprot ID
Q9Y6L6
Uniprot Name
Solute carrier organic anion transporter family member 1B1
Molecular Weight
76447.99 Da
References
  1. Davenport JM, Covington P, Bonifacio L, McIntyre G, Venitz J: Effect of uptake transporters OAT3 and OATP1B1 and efflux transporter MRP2 on the pharmacokinetics of eluxadoline. J Clin Pharmacol. 2015 May;55(5):534-42. doi: 10.1002/jcph.442. Epub 2015 Jan 14. [PubMed:25491493]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Organic anion transmembrane transporter activity
Specific Function
Mediates hepatobiliary excretion of numerous organic anions. May function as a cellular cisplatin transporter.
Gene Name
ABCC2
Uniprot ID
Q92887
Uniprot Name
Canalicular multispecific organic anion transporter 1
Molecular Weight
174205.64 Da
References
  1. Davenport JM, Covington P, Bonifacio L, McIntyre G, Venitz J: Effect of uptake transporters OAT3 and OATP1B1 and efflux transporter MRP2 on the pharmacokinetics of eluxadoline. J Clin Pharmacol. 2015 May;55(5):534-42. doi: 10.1002/jcph.442. Epub 2015 Jan 14. [PubMed:25491493]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Sodium-independent organic anion transmembrane transporter activity
Specific Function
Plays an important role in the excretion/detoxification of endogenous and exogenous organic anions, especially from the brain and kidney. Involved in the transport basolateral of steviol, fexofenad...
Gene Name
SLC22A8
Uniprot ID
Q8TCC7
Uniprot Name
Solute carrier family 22 member 8
Molecular Weight
59855.585 Da
References
  1. Davenport JM, Covington P, Bonifacio L, McIntyre G, Venitz J: Effect of uptake transporters OAT3 and OATP1B1 and efflux transporter MRP2 on the pharmacokinetics of eluxadoline. J Clin Pharmacol. 2015 May;55(5):534-42. doi: 10.1002/jcph.442. Epub 2015 Jan 14. [PubMed:25491493]

Drug created on October 28, 2015 13:50 / Updated on November 19, 2017 20:34