Identification
NameEluxadoline
Accession NumberDB09272
TypeSmall Molecule
GroupsApproved
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
Product Ingredients Not Available
Approved 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
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International BrandsNot Available
Brand mixturesNot Available
Categories
UNII45TPJ4MBQ1
CAS number864821-90-9
WeightAverage: 569.662
Monoisotopic: 569.263819247
Chemical FormulaC32H35N5O5
InChI KeyQFNHIDANIVGXPE-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
PharmacodynamicsNot 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.

TargetKindPharmacological actionActionsOrganismUniProt ID
Mu-type opioid receptorProteinyes
agonist
HumanP35372 details
Delta-type opioid receptorProteinyes
antagonist
HumanP41143 details
Kappa-type opioid receptorProteinyes
agonist
HumanP41145 details
Related Articles
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 distributionNot 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.

ClearanceNot Available
Toxicity

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

Affected organismsNot Available
PathwaysNot Available
Pharmacogenomic Effects/ADRs Not Available
Interactions
Drug Interactions
DrugInteractionDrug group
AclidiniumAclidinium may increase the constipating activities of Eluxadoline.Approved
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
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
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
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, 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, Withdrawn
DezocineDezocine may increase the constipating activities of Eluxadoline.Approved
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
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
FentanylFentanyl may increase the constipating activities of Eluxadoline.Approved, Illicit, Investigational, Vet Approved
FesoterodineFesoterodine may increase the constipating activities of Eluxadoline.Approved
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
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
Levomethadyl AcetateLevomethadyl Acetate may increase the constipating activities of Eluxadoline.Approved
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
MecamylamineMecamylamine may increase the constipating activities of Eluxadoline.Approved
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
MethylnaltrexoneThe risk or severity of adverse effects can be increased when Methylnaltrexone is combined with 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
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
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
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.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
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
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 InteractionsNot 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
ATC CodesNot Available
AHFS Codes
  • 56:92
PDB EntriesNot Available
FDA labelDownload (503 KB)
MSDSNot Available
Clinical Trials
Clinical Trials
PhaseStatusPurposeConditionsCount
2CompletedTreatmentIrritable Bowel Syndrome (IBS)1
3CompletedTreatmentIrritable Bowel Syndrome (IBS)2
4RecruitingTreatmentDiarrhoea Predominant Irritable Bowel Syndrome1
Pharmacoeconomics
ManufacturersNot Available
PackagersNot Available
Dosage forms
FormRouteStrength
TabletOral100 mg
TabletOral75 mg
Tablet, film coatedOral100 mg/1
Tablet, film coatedOral75 mg/1
PricesNot Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US9115091 No2008-07-072028-07-07Us
US9205076 No2005-03-142025-03-14Us
US8691860 No2008-07-072028-07-07Us
US8344011 No2005-03-142025-03-14Us
US8609709 No2005-03-142025-03-14Us
US7741356 No2008-03-252028-03-25Us
US7786158 No2005-03-142025-03-14Us
US9364489 No2008-07-072028-07-07Us
US8772325 No2005-03-142025-03-14Us
Properties
StateSolid
Experimental PropertiesNot 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 featuresNot Available
Spectra
Mass Spec (NIST)Not Available
Spectra
Spectrum TypeDescriptionSplash Key
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, NegativeNot Available
Taxonomy
DescriptionThis 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.
KingdomOrganic compounds
Super ClassOrganic acids and derivatives
ClassCarboxylic acids and derivatives
Sub ClassAmino acids, peptides, and analogues
Direct ParentPhenylalanine and derivatives
Alternative ParentsAlpha amino acid amides / Phenylimidazoles / O-methoxybenzoic acids and derivatives / Amphetamines and derivatives / Benzamides / Benzoic acids / m-Xylenes / Benzoyl derivatives / Benzylamines / Anisoles
SubstituentsPhenylalanine or derivatives / Alpha-amino acid amide / O-methoxybenzoic acid or derivatives / 5-phenylimidazole / 4-phenylimidazole / Amphetamine or derivatives / Benzamide / Benzoic acid or derivatives / Benzoic acid / Phenoxy compound
Molecular FrameworkAromatic heteromonocyclic compounds
External Descriptorsamino 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. Agonist binding to the receptor induces coupling to an inactive GDP-bound heterotrimeric G-protein complex and subsequent exchange of GDP for GTP in the G-protein alpha subunit leading to dissociati...
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 nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors, such as adenylate cyclase. Signaling leads to the inhibition of adenylate cyclase activity. Inhibits neurot...
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 synthetic opioids and for the psychoactive diterpene salvinorin A. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates th...
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
substrateinhibitor
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, prostaglandin E2, thromboxane B2, leukotriene C3, leukotriene E4, thyroxine and triiodothyronine. Involved in the clearance of bile acids and organic anions from the liver.
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, fexofenadine. Transports benzylpenicillin (PCG), estrone-3-sulfate (E1S), cimetidine (CMD), 2,4-dichloro-phenoxyacetate (2,4-D), p-amino-hippurate (PAH), acyclovir (ACV) and ochratoxin (OTA).
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 September 01, 2017 12:04