Edaravone

Identification

Summary

Edaravone is a free radical scavenger used to delay the progression of ALS.

Brand Names
Radicava
Generic Name
Edaravone
DrugBank Accession Number
DB12243
Background

Edaravone is a free radical scavenger and neuroprotective agent with antioxidant properties.5 It has three tautomers.3 Edaravone works to scavenge reactive oxygen species, which have been implicated in neurological disorders, such as amyotrophic lateral sclerosis (ALS) and cerebral ischemia.3,11,5

The intravenous formulation of edaravone was first approved in Japan in 2001 for the treatment of acute ischemic stroke.11 It was later approved for the treatment of amyotrophic lateral sclerosis (ALS) in Japan and South Korea in 2015, followed by the FDA approval in May 2017 6 and Health Canada approval in October 2018.11 The oral suspension formulation of edaravone was approved by the FDA in May 2022 and by Health Canada in November 2022.13

Edaravone was initially granted orphan designation by the European Medicines Agency on June 19, 2015 11 and was under regulatory review in Europe. However, the drug manufacturer, Mitsubishi Tanabe Pharma, withdrew the Marketing Authorization Application (MAA) for edaravone from the European market on May 24, 2019, in response to the request made by the Committee for Medicinal Products for Human Use (CHMP) for a long-term study demonstrating the long-term efficacy and safety of edaravone.10,12 Edaravone was also investigated in other disorders, such as Alzheimer's disease,1 neuropathic pain, and ischemia-induced nerve injury.2

Type
Small Molecule
Groups
Approved, Investigational
Structure
Weight
Average: 174.203
Monoisotopic: 174.07931295
Chemical Formula
C10H10N2O
Synonyms
  • 1-phenyl-3-methyl-5-oxo-2-pyrazoline
  • 2,4-dihydro-5-methyl-2-phenyl-3H-pyrazol-3-one
  • 3-methyl-1-phenyl-2-pyrazolin-5-one
  • 3-methyl-1-phenyl-5-pyrazolone
  • 3-methyl-1-phenylpyrazol-5-one
  • Edaravone
  • Methylphenylpyrazolone
  • Norphenazone
  • Phenyl methyl pyrazolone
  • Phenylmethylpyrazolone
External IDs
  • MCI-186
  • NSC-12
  • NSC-26139
  • NSC-2629
  • TW001

Pharmacology

Indication

Edaravone is indicated for the treatment of amyotrophic lateral sclerosis (ALS) in the US and Canada.6,7 It is also indicated to treat acute ischemic stroke in Japan.3,4,11

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Associated Conditions
Indication TypeIndicationCombined Product DetailsApproval LevelAge GroupPatient CharacteristicsDose Form
Management ofAmyotrophic lateral sclerosis••••••••••••
Contraindications & Blackbox Warnings
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Pharmacodynamics

Edaravone works to delay the disease progression of neurological disorders such as ischemic stroke and ALS by limiting the extent of neuronal damage or death.3

Mechanism of action

Oxidative stress and reactive oxygen species (ROS) production have been implicated in various neurological disorders, such as amyotrophic lateral sclerosis (ALS) and cerebral ischemia.3,11,5 Oxidative stress caused by excess ROS damages endothelial cells in the cerebral vasculature as well as neuronal cell membranes, leading to neuronal cell death.3

Edaravone is a free radical scavenger that scavenges and suppresses the generation of hydroxyl radicals and peroxynitrite radicals.3 The exact mechanism of action of edaravone in ALS has not been fully elucidated; however, edaravone is thought to mediate therapeutic effects via its antioxidant properties. Since oxidative stress has been implicated in the pathophysiology of ALS and cerebral ischemia, inhibiting lipid peroxidation, suppressing endothelial cell damage induced by lipid peroxides, and scavenging free radicals may lead to neuroprotective effects.2 Edaravone has no effect on superoxide production.2,3 It is suggested that edaravone may also possess anti-inflammatory properties, as it inhibited neutrophil activation and suppressed inducible nitric oxide synthase (iNOS) and neuronal nitric oxide synthase (nNOS) expression in animal models. It was also shown to ameliorate ROS-induced inflammatory oxidative stress after ischemic brain reperfusion.3

Absorption

One study investigated the absorption of edaravone in healthy adults, who either received a single oral (105 mg/mL) or intravenous (60 mg/60 min) dose. The mean Cmax (CV%) and Tmax were 1656 (44.3) ng/mL and 0.5 hours, respectively, following oral administration.7 The absolute oral bioavailability is about 57% because of first-pass metabolism.6

The mean Cmax (CV%) and Tmax were 1253 (18.3) ng/mL and one hour, respectively, following intravenous administration.7 When intravenously administered, the maximum plasma concentration (Cmax) of edaravone was reached by the end of infusion.6

The Cmax and area under the concentration-time curve (AUC) of edaravone increases more than dose-proportional over the dose range of 30 to 300 mg. Edaravone does not accumulate in plasma with once-daily or multiple-dose administration. The Cmax and AUC decreased when the oral suspension formulation of edaravone was administered with a high-fat meal.7

Volume of distribution

After intravenous administration, edaravone has a mean volume of distribution of 63.1 L, suggesting substantial tissue distribution. Edaravone has an apparent volume of distribution of 164 L following oral administration.7 Edaravone readily crosses the blood-brain barrier.4

Protein binding

Edaravone is 92% bound to human serum proteins, mainly to albumin, with no concentration dependence in the range of 0.1 to 50 micromol/L.6

Metabolism

The metabolites of edaravone have not been fully characterized. Edaravone is metabolized to a sulfate conjugate and a glucuronide conjugate, which are not pharmacologically active. The glucuronide conjugation of edaravone involves multiple uridine diphosphate glucuronosyltransferase (UGT) isoforms (UGT1A1, UGT1A6, UGT1A7, UGT1A8, UGT1A9, UGT1A10, UGT2B7, and UGT2B17). In human plasma, edaravone is mainly detected as the sulfate conjugate, which is presumed to be formed by sulfotransferases. Oral edaravone results in 1.3- and 1.7-fold higher exposures for both sulfate and glucuronide metabolites, respectively, when compared to intravenously-administered edaravone because of first-pass metabolism.6

Route of elimination

In Japanese and Caucasian healthy volunteer studies, edaravone was excreted mainly in the urine as its glucuronide conjugate (60-80% of the dose up to 48 hours). Approximately 6-8% of the dose was recovered in the urine as the sulfate conjugate, and <1% of the dose was recovered in the urine as the unchanged drug. _In vitro_ studies suggest that the sulfate conjugate of edaravone is hydrolyzed back to edaravone, which is then converted to the glucuronide conjugate in the kidney before excretion into the urine.6

Half-life

The mean terminal elimination half-life of edaravone is approximately 4.5 to nine hours. The half-lives of its metabolites range from three to six hours.6

Clearance

Following intravenous administration, the total clearance of edaravone is estimated to be 35.9 L/h.6 The apparent total clearance of edaravone is estimated to be 67.9L/h following oral administration.7

Adverse Effects
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Toxicity

Oral and intravenous LD50 in rats are 1915 mg/kg and 631 mg/kg, respectively.9 There is limited information on the acute toxicity of edaravone.

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.
Not Available
Food Interactions
  • Take on an empty stomach. RADICAVA ORS should be taken in the morning on an empty stomach after overnight fasting. Food should not be consumed for 1 hour after administration except water. The higher the fat content of the previous meal, the longer the fasting time before taking RADICAVA ORS will be.

Products

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International/Other Brands
Arone (Edinburgh Pharmaceuticals (India)) / Radicut (Mitsubishi Tanabe Pharma Corporation)
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
RadicavaInjection30 mg/100mLIntravenousMitsubishi Tanabe Pharma America, Inc.2017-05-05Not applicableUS flag
RadicavaSolution30 mg / 100 mLIntravenousMitsubishi Tanabe Pharma Corporation2019-10-29Not applicableCanada flag
RadicavaSuspension105 mg / 5 mLOralMitsubishi Tanabe Pharma Corporation2023-02-09Not applicableCanada flag
RadicavaInjection60 mg/100mLIntravenousMitsubishi Tanabe Pharma America, Inc.2020-05-05Not applicableUS flag
Radicava OrsKit; Suspension735 mg/35mLOralMitsubishi Tanabe Pharma America, Inc.2022-05-12Not applicableUS flag

Categories

ATC Codes
N07XX14 — Edaravone
Drug Categories
Chemical TaxonomyProvided by Classyfire
Description
This compound belongs to the class of organic compounds known as pyrazolones. These are compounds containing a pyrazole ring which bears a ketone.
Kingdom
Organic compounds
Super Class
Organoheterocyclic compounds
Class
Azolines
Sub Class
Pyrazolines
Direct Parent
Pyrazolones
Alternative Parents
Benzene and substituted derivatives / Carboxylic acids and derivatives / Azacyclic compounds / Organopnictogen compounds / Organonitrogen compounds / Organic oxides / Hydrocarbon derivatives / Carbonyl compounds
Substituents
Aromatic heteromonocyclic compound / Azacycle / Benzenoid / Carbonyl group / Carboxylic acid derivative / Hydrocarbon derivative / Monocyclic benzene moiety / Organic nitrogen compound / Organic oxide / Organic oxygen compound
Molecular Framework
Aromatic heteromonocyclic compounds
External Descriptors
ring assembly (CHEBI:31530)
Affected organisms
Not Available

Chemical Identifiers

UNII
S798V6YJRP
CAS number
89-25-8
InChI Key
QELUYTUMUWHWMC-UHFFFAOYSA-N
InChI
InChI=1S/C10H10N2O/c1-8-7-10(13)12(11-8)9-5-3-2-4-6-9/h2-6H,7H2,1H3
IUPAC Name
3-methyl-1-phenyl-4,5-dihydro-1H-pyrazol-5-one
SMILES
CC1=NN(C(=O)C1)C1=CC=CC=C1

References

General References
  1. Jiao SS, Yao XQ, Liu YH, Wang QH, Zeng F, Lu JJ, Liu J, Zhu C, Shen LL, Liu CH, Wang YR, Zeng GH, Parikh A, Chen J, Liang CR, Xiang Y, Bu XL, Deng J, Li J, Xu J, Zeng YQ, Xu X, Xu HW, Zhong JH, Zhou HD, Zhou XF, Wang YJ: Edaravone alleviates Alzheimer's disease-type pathologies and cognitive deficits. Proc Natl Acad Sci U S A. 2015 Apr 21;112(16):5225-30. doi: 10.1073/pnas.1422998112. Epub 2015 Apr 6. [Article]
  2. Li H, Xu K, Wang Y, Zhang H, Li T, Meng L, Gong X, Zhang H, Ou N, Ruan J: Phase I clinical study of edaravone in healthy Chinese volunteers: safety and pharmacokinetics of single or multiple intravenous infusions. Drugs R D. 2012 Jun 1;12(2):65-70. doi: 10.2165/11634290-000000000-00000. [Article]
  3. Watanabe T, Tahara M, Todo S: The novel antioxidant edaravone: from bench to bedside. Cardiovasc Ther. 2008 Summer;26(2):101-14. doi: 10.1111/j.1527-3466.2008.00041.x. [Article]
  4. Kikuchi K, Uchikado H, Miyagi N, Morimoto Y, Ito T, Tancharoen S, Miura N, Miyata K, Sakamoto R, Kikuchi C, Iida N, Shiomi N, Kuramoto T, Kawahara K: Beyond neurological disease: new targets for edaravone (Review). Int J Mol Med. 2011 Dec;28(6):899-906. doi: 10.3892/ijmm.2011.795. Epub 2011 Sep 15. [Article]
  5. Cruz MP: Edaravone (Radicava): A Novel Neuroprotective Agent for the Treatment of Amyotrophic Lateral Sclerosis. P T. 2018 Jan;43(1):25-28. [Article]
  6. FDA Approved Drug Products: RADICAVA (edaravone) intravenous injection and RADICAVA ORS (edaravone) oral suspension [Link]
  7. Health Canada Approved Drug Products: RADICAVA (edaravone) oral suspension [Link]
  8. Cayman Chemical: Edaravone MSDS [Link]
  9. CymitQuimica: Edaravone MSDS [Link]
  10. EMA: Radicava; Withdrawal of the marketing authorisation application [Link]
  11. EMA Withdrawal assessment report: Radicava [Link]
  12. The Pharma Letter: Mitsubishi Tanabe pulls Radicava MAA for ALS in the Europe [Link]
  13. Newswire: MITSUBISHI TANABE PHARMA CANADA ANNOUNCES CANADIAN AUTHORIZATION OF RADICAVA® (EDARAVONE) ORAL SUSPENSION FOR THE TREATMENT OF PATIENTS WITH ALS [Link]
Human Metabolome Database
HMDB0251697
KEGG Drug
D01552
KEGG Compound
C13008
PubChem Compound
4021
PubChem Substance
347828521
ChemSpider
3881
BindingDB
50200541
RxNav
1921877
ChEBI
31530
ChEMBL
CHEMBL290916
ZINC
ZINC000018203737
PDBe Ligand
W1P
Wikipedia
Edaravone
PDB Entries
5s3i / 5s52 / 7gp5

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4CompletedTreatmentCerebral Infarctions1
4CompletedTreatmentMyocardial Infarction / Reperfusion Injury1
4CompletedTreatmentStroke1
4RecruitingTreatmentAcute Ischemic Stroke1
3CompletedTreatmentAcute Ischemic Stroke1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
FormRouteStrength
InjectionIntravenous30 mg/100mL
InjectionIntravenous60 mg/100mL
Injection, solution, concentrateIntravenous
SolutionIntravenous30 mg / 100 mL
SuspensionOral105 mg / 5 mL
Kit; suspensionOral1050 mg/50mL
Kit; suspensionOral735 mg/35mL
SolutionIntravenous30 mg/20mL
Prices
Not Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)Region
US6933310No2005-08-232020-11-13US flag
US11241416No2019-11-012039-11-01US flag
US10987341No2021-04-272039-11-01US flag
US11478450No2019-11-012039-11-01US flag
US11826352No2019-11-012039-11-01US flag

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)129.7https://www.accessdata.fda.gov/drugsatfda_docs/label/2022/215446s000lbl.pdf
boiling point (°C)287https://cdn.caymanchem.com/cdn/msds/13320m.pdf
logP1.12https://static.cymitquimica.com/products/04/pdf/sds-C13105000.pdf
pKa7.0Watanabe T, Tahara M, Todo S: The novel antioxidant edaravone: from bench to bedside. Cardiovasc Ther. 2008 Summer;26(2):101-14. doi: 10.1111/j.1527-3466.2008.00041.x. [A19140]
Predicted Properties
PropertyValueSource
Water Solubility0.939 mg/mLALOGPS
logP0.53ALOGPS
logP1.53Chemaxon
logS-2.3ALOGPS
pKa (Strongest Acidic)13.45Chemaxon
pKa (Strongest Basic)-1.5Chemaxon
Physiological Charge0Chemaxon
Hydrogen Acceptor Count2Chemaxon
Hydrogen Donor Count0Chemaxon
Polar Surface Area32.67 Å2Chemaxon
Rotatable Bond Count1Chemaxon
Refractivity49.49 m3·mol-1Chemaxon
Polarizability18.61 Å3Chemaxon
Number of Rings2Chemaxon
Bioavailability1Chemaxon
Rule of FiveYesChemaxon
Ghose FilterYesChemaxon
Veber's RuleYesChemaxon
MDDR-like RuleNoChemaxon
Predicted ADMET Features
Not Available

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
LC-MS/MS Spectrum - LC-ESI-qTof , PositiveLC-MS/MSsplash10-004i-1900000000-9c17dd936441a10926dc
MS/MS Spectrum - , positiveLC-MS/MSsplash10-004i-1900000000-9c17dd936441a10926dc
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSsplash10-004i-0900000000-9ea4a99e078ec22e7294
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSsplash10-0059-1900000000-598bc7ef4795e7eeb9c5
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSsplash10-00di-0900000000-5c654330cb1d8b0bb0a8
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSsplash10-00di-0900000000-b02a76446b5f1692841f
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSsplash10-066r-9400000000-447b6dc4369b77dbb4cc
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSsplash10-0ab9-2900000000-c020b59970cb3fb90e51
Predicted 1H NMR Spectrum1D NMRNot Applicable
Predicted 13C NMR Spectrum1D NMRNot Applicable
Chromatographic Properties
Collision Cross Sections (CCS)
AdductCCS Value (Å2)Source typeSource
[M-H]-142.99
predicted
DarkChem Lite v0.1.0
[M-H]-143.0470834
predicted
DarkChem Lite v0.1.0
[M-H]-133.77623
predicted
DeepCCS 1.0 (2019)
[M+H]+143.49
predicted
DarkChem Lite v0.1.0
[M+H]+143.5318834
predicted
DarkChem Lite v0.1.0
[M+H]+136.1718
predicted
DeepCCS 1.0 (2019)
[M+Na]+143.59
predicted
DarkChem Lite v0.1.0
[M+Na]+143.06975
predicted
DeepCCS 1.0 (2019)

Enzymes

Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Substrate
General Function
Steroid binding
Specific Function
UDPGT is of major importance in the conjugation and subsequent elimination of potentially toxic xenobiotics and endogenous compounds. This isoform glucuronidates bilirubin IX-alpha to form both the...
Gene Name
UGT1A1
Uniprot ID
P22309
Uniprot Name
UDP-glucuronosyltransferase 1-1
Molecular Weight
59590.91 Da
References
  1. FDA Approved Drug Products: RADICAVA (edaravone) intravenous injection and RADICAVA ORS (edaravone) oral suspension [Link]
Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Substrate
General Function
Protein homodimerization activity
Specific Function
UDPGT is of major importance in the conjugation and subsequent elimination of potentially toxic xenobiotics and endogenous compounds. This isoform has specificity for phenols. Isoform 3 lacks trans...
Gene Name
UGT1A6
Uniprot ID
P19224
Uniprot Name
UDP-glucuronosyltransferase 1-6
Molecular Weight
60750.215 Da
References
  1. FDA Approved Drug Products: RADICAVA (edaravone) intravenous injection and RADICAVA ORS (edaravone) oral suspension [Link]
Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Substrate
General Function
Retinoic acid binding
Specific Function
UDPGT is of major importance in the conjugation and subsequent elimination of potentially toxic xenobiotics and endogenous compounds. Isoform 2 lacks transferase activity but acts as a negative reg...
Gene Name
UGT1A7
Uniprot ID
Q9HAW7
Uniprot Name
UDP-glucuronosyltransferase 1-7
Molecular Weight
59818.315 Da
References
  1. FDA Approved Drug Products: RADICAVA (edaravone) intravenous injection and RADICAVA ORS (edaravone) oral suspension [Link]
Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Substrate
General Function
Steroid binding
Specific Function
UDPGT is of major importance in the conjugation and subsequent elimination of potentially toxic xenobiotics and endogenous compounds. Isoform 2 lacks transferase activity but acts as a negative reg...
Gene Name
UGT1A8
Uniprot ID
Q9HAW9
Uniprot Name
UDP-glucuronosyltransferase 1-8
Molecular Weight
59741.035 Da
References
  1. FDA Approved Drug Products: RADICAVA (edaravone) intravenous injection and RADICAVA ORS (edaravone) oral suspension [Link]
Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Substrate
General Function
Retinoic acid binding
Specific Function
UDPGT is of major importance in the conjugation and subsequent elimination of potentially toxic xenobiotics and endogenous compounds. This isoform has specificity for phenols. Isoform 2 lacks trans...
Gene Name
UGT1A9
Uniprot ID
O60656
Uniprot Name
UDP-glucuronosyltransferase 1-9
Molecular Weight
59940.495 Da
References
  1. FDA Approved Drug Products: RADICAVA (edaravone) intravenous injection and RADICAVA ORS (edaravone) oral suspension [Link]
Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Substrate
General Function
Protein kinase c binding
Specific Function
UDPGT is of major importance in the conjugation and subsequent elimination of potentially toxic xenobiotics and endogenous compounds. Isoform 2 lacks transferase activity but acts as a negative reg...
Gene Name
UGT1A10
Uniprot ID
Q9HAW8
Uniprot Name
UDP-glucuronosyltransferase 1-10
Molecular Weight
59809.075 Da
References
  1. FDA Approved Drug Products: RADICAVA (edaravone) intravenous injection and RADICAVA ORS (edaravone) oral suspension [Link]
Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Substrate
General Function
Glucuronosyltransferase activity
Specific Function
UDPGT is of major importance in the conjugation and subsequent elimination of potentially toxic xenobiotics and endogenous compounds.Its unique specificity for 3,4-catechol estrogens and estriol su...
Gene Name
UGT2B7
Uniprot ID
P16662
Uniprot Name
UDP-glucuronosyltransferase 2B7
Molecular Weight
60694.12 Da
References
  1. FDA Approved Drug Products: RADICAVA (edaravone) intravenous injection and RADICAVA ORS (edaravone) oral suspension [Link]
Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Substrate
General Function
Glucuronosyltransferase activity
Specific Function
UDPGT is of major importance in the conjugation and subsequent elimination of potentially toxic xenobiotics and endogenous compounds. The major substrates of this isozyme are eugenol > 4-methylumbe...
Gene Name
UGT2B17
Uniprot ID
O75795
Uniprot Name
UDP-glucuronosyltransferase 2B17
Molecular Weight
61094.915 Da
References
  1. FDA Approved Drug Products: RADICAVA (edaravone) intravenous injection and RADICAVA ORS (edaravone) oral suspension [Link]
Kind
Protein group
Organism
Humans
Pharmacological action
No
Actions
Substrate
General Function
Sulfotransferase activity
Specific Function
Sulfotransferase that utilizes 3'-phospho-5'-adenylyl sulfate (PAPS) as sulfonate donor to catalyze the sulfonation of steroids and bile acids in the liver and adrenal glands.

Components:
References
  1. FDA Approved Drug Products: RADICAVA (edaravone) intravenous injection and RADICAVA ORS (edaravone) oral suspension [Link]

Carriers

Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Binder
General Function
Toxic substance binding
Specific Function
Serum albumin, the main protein of plasma, has a good binding capacity for water, Ca(2+), Na(+), K(+), fatty acids, hormones, bilirubin and drugs. Its main function is the regulation of the colloid...
Gene Name
ALB
Uniprot ID
P02768
Uniprot Name
Serum albumin
Molecular Weight
69365.94 Da
References
  1. FDA Approved Drug Products: RADICAVA (edaravone) intravenous injection and RADICAVA ORS (edaravone) oral suspension [Link]

Transporters

Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Substrate
Curator comments
Substrate profile was investigated in vitro using HEK293 cells.
General Function
Sodium-independent organic anion transmembrane transporter activity
Specific Function
Involved in the renal elimination of endogenous and exogenous organic anions. Functions as organic anion exchanger when the uptake of one molecule of organic anion is coupled with an efflux of one ...
Gene Name
SLC22A6
Uniprot ID
Q4U2R8
Uniprot Name
Solute carrier family 22 member 6
Molecular Weight
61815.78 Da
References
  1. VanWert AL, Gionfriddo MR, Sweet DH: Organic anion transporters: discovery, pharmacology, regulation and roles in pathophysiology. Biopharm Drug Dispos. 2010 Jan;31(1):1-71. doi: 10.1002/bdd.693. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Substrate
Curator comments
Substrate activity was demonstrated in vitro using HEK293 cells.
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. VanWert AL, Gionfriddo MR, Sweet DH: Organic anion transporters: discovery, pharmacology, regulation and roles in pathophysiology. Biopharm Drug Dispos. 2010 Jan;31(1):1-71. doi: 10.1002/bdd.693. [Article]

Drug created at October 20, 2016 21:42 / Updated at August 03, 2023 15:04