Opicapone
Identification
- Summary
Opicapone is a catechol-O-methyltransferase inhibitor used as an adjunct treatment for Parkinson's Disease in adults currently receiving levodopa and a dopa decarboxylase inhibitor.
- Brand Names
- Ongentys
- Generic Name
- Opicapone
- DrugBank Accession Number
- DB11632
- Background
Opicapone is a potent, reversible, and peripherally-acting third-generation inhibitor of catechol-o-methyltransferase (COMT), an enzyme involved in the breakdown of various catecholamines including dopamine.4,5 Many patients with Parkinson’s disease treated with levodopa plus a dopa decarboxylase (DDC) inhibitor (eg carbidopa) experience motor complications over time, which calls for the management of these symptoms through the use of a dopamine agonist, a monoamine oxidase B inhibitor (selegiline, rasagiline), a catechol-O-methyl transferase (COMT) inhibitor, or amantadine, or using a modified-release formulation of levodopa.6
Opicapone is used for adjunct therapy to levodopa and carbidopa in adult patients with Parkinson's disease and end-of-dose motor fluctuations. Opicapone was approved for use by the European Commission in June 2016 7 and the FDA in April 2020.13 It is marketed under the brand name Ongentys as once-daily oral capsules. Exhibiting a long duration of action that exceeds 24 hours, opicapone can be administered once-daily 6 and demonstrates the lowest risk for cytotoxicity compared to other catechol-O-methyltransferase inhibitors.5
- Type
- Small Molecule
- Groups
- Approved, Investigational
- Structure
- Weight
- Average: 413.17
Monoisotopic: 411.9977395 - Chemical Formula
- C15H10Cl2N4O6
- Synonyms
- Opicapona
- Opicapone
- External IDs
- BIA 9-1067
- BIA-9-1067
- BIA-91067
Pharmacology
- Indication
Opicapone is indicated as adjunctive therapy in adults with Parkinson’s disease and end-of-dose motor fluctuations or “off” episodes whose symptoms cannot be stabilized on the combination therapy of levodopa and DOPA decarboxylase inhibitor (e.g., carbidopa).10,13
Reduce drug development failure ratesBuild, train, & validate machine-learning modelswith evidence-based and structured datasets.Build, train, & validate predictive machine-learning models with structured datasets.- Associated Conditions
Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Adjunct therapy in management of Parkinson's disease •••••••••••• ••••• ••• •• •••• ••••• •••••••••••• •••• •••••• •• •••••••••• ••••••• Adjunct therapy in management of Parkinson's disease (pd) •••••••••••• ••••• ••• •••••••• •• ••••••••• ••••••• ••••••• - Contraindications & Blackbox Warnings
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- Pharmacodynamics
Opicapone is a COMT inhibitor that serves to improve the availability and duration of action of levodopa (L-Dopa), a standard pharmacological treatment for Parkinson's Disease. Opicapone works by blocking the peripheral degradation of L-Dopa mediated by COMT.1 Opicapone has a long duration of action: following administration of a 50 mg dose, COMT inhibition lasted for more than 24 hours.10 In clinical trials, opicapone as adjunct therapy to L-Dopa plus a dopa decarboxylase inhibitor significantly improved motor fluctuations than placebo, and the effects were comparable to entacapone.1
- Mechanism of action
Levodopa (L-Dopa) is the gold standard for managing motor and some non-motor symptoms associated with Parkinson's Disease; however, only a small fraction of administered L-Dopa actually crosses the blood-brain barrier to exert its therapeutic action and patients face the risk of developing end-of-dose motor fluctuations, which reflects the rapid peripheral metabolism of L-dopa by aromatic L-amino acid decarboxylase and catechol-O-methyltransferase (COMT).1
Opicapone is a peripheral, selective, and reversible catechol-O-methyltransferase (COMT) inhibitor. It displays a high binding affinity that is in sub-picomolar ranges, resulting in a slow complex dissociation rate constant and long duration of action in vivo.10 When opicapone is added to the treatment regimen that contains L-Dopa and DOPA decarboxylase inhibitor, opicapone helps to increase the plasma levels and enhance the therapeutic efficacy of L-Dopa.1
Target Actions Organism ACatechol O-methyltransferase inhibitorHumans - Absorption
Orally administered opicapone demonstrates a linear, dose-dependent absorption profile.5 Opicapone is rapidly absorbed,2 with an oral bioavailability of about 20%.10 Following administration of a single 50 mg dose of opicapone, the median Tmax was two hours, ranging from one to four hours. A moderate fat or moderate calorie meal was shown to decrease the Cmax by 62%, the mean overall plasma exposure (AUC) by 31%, and the Tmax by 4 hours.13
- Volume of distribution
Following oral administration, the apparent Vd of opicapone at a dose of 50 mg was 29 L with an inter-subject variability of 36%.10 One study showed small systemic accumulation after multiple-dosing.2
- Protein binding
Opicapone is >99% bound to plasma proteins, which is independent of the drug concentration.13
- Metabolism
According to clinical and in vitro studies, sulphation is the primary metabolic pathway of opicapone, forming the inactive metabolite. Opicapone can also undergo glucuronidation, COMT-mediated methylation, reduction, and glutathione conjugation.10,13
As two major circulating metabolites, BIA 9-1103 (3-O-sulphated opicapone) accounts for 67.1% of the total radioactivity and BIA 9-1104 (4-O-methylated opicapone) accounts for 20.5% of the total radioactivity. Other metabolites are generally unquantifiable in plasma samples.8,10 Opicapone can undergo N-oxide reduction to form BIA 9-1079, which was shown to be an active metabolite in non-clinical studies;3 however, it is generally undetectable in humans.8 Other inactive metabolites include BIA 9-1100, BIA 9-1101, and BIA 9-1106.3
Hover over products below to view reaction partners
- Route of elimination
Following administration of a single 100 mg dose of radiolabeled opicapone in healthy subjects, about 70% of the total dose was recovered in feces, where 22% of the recovered dose was excreted as an unchanged parent drug. About 20% of the total dose was recovered in exhaled air and about 5% was recovered in the urine, where less than 1% of the recovered dose was in an unchanged form.13 The primary detectable metabolite in the urine was the glucuronide metabolite.10
- Half-life
The mean elimination half-life of opicapone is one to two hours.13 Despite the short half-life, the observed half-life of opicapone-induced COMT inhibition in human red blood cells was 61.6 hours with a standard deviation of 37.6 hours.3
- Clearance
Following oral administration of 50 mg opicapone, the apparent total body clearance was 22 L/h, with an inter-subject variability of 45%.10
- Adverse Effects
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- Toxicity
There is no reported LD50 data of opicapone. As there is no known antidote for opicapone overdose, overdosage should be managed with symptomatic and supportive treatment. Removal of the drug through gastric lavage and/or inactivation by administering activated charcoal should be considered.10,13
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs Browse all" title="About SNP Mediated Effects/ADRs" id="snp-actions-info" class="drug-info-popup" href="javascript:void(0);">
- Not Available
Interactions
- Drug Interactions Learn More" title="About Drug Interactions" id="structured-interactions-info" class="drug-info-popup" href="javascript:void(0);">
- 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.
Drug Interaction Integrate drug-drug
interactions in your softwareAbaloparatide The risk or severity of adverse effects can be increased when Abaloparatide is combined with Opicapone. Acebutolol The risk or severity of adverse effects can be increased when Acebutolol is combined with Opicapone. Aldesleukin The risk or severity of adverse effects can be increased when Aldesleukin is combined with Opicapone. Aliskiren The risk or severity of adverse effects can be increased when Aliskiren is combined with Opicapone. Ambrisentan Opicapone may increase the hypotensive activities of Ambrisentan. - Food Interactions
- Take separate from meals. Take opicapone at least one hour before or after eating, as a moderate calorie meal decreases Cmax and overall plasma exposure to the drug, and delays Tmax.
Products
- Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Ongentys Capsule 50 mg Oral Bial Portela Cª, s.a. 2016-09-08 Not applicable EU Ongentys Capsule 25 mg/1 Oral Neurocrine Biosciences, Inc. 2020-04-24 Not applicable US Ongentys Capsule 25 mg Oral Bial Portela Cª, s.a. 2016-09-08 Not applicable EU Ongentys Capsule 50 mg Oral Bial Portela Cª, s.a. 2016-09-08 Not applicable EU Ongentys Capsule 50 mg Oral Bial Portela Cª, s.a. 2016-09-08 Not applicable EU
Categories
- ATC Codes
- N04BX04 — Opicapone
- Drug Categories
- Anti-Dyskinesia Agents
- Anti-Parkinson Drugs
- BCRP/ABCG2 Substrates
- Central Nervous System Agents
- COMT Inhibitors
- Cytochrome P-450 CYP1A2 Inhibitors
- Cytochrome P-450 CYP1A2 Inhibitors (strength unknown)
- Cytochrome P-450 CYP1A2 Inhibitors (weak)
- Cytochrome P-450 CYP2B6 Inhibitors
- Cytochrome P-450 CYP2B6 Inhibitors (strength unknown)
- Cytochrome P-450 CYP2B6 Inhibitors (weak)
- Cytochrome P-450 CYP2C19 Inducers
- Cytochrome P-450 CYP2C19 Inducers (strength unknown)
- Cytochrome P-450 CYP2C8 Inhibitors
- Cytochrome P-450 CYP2C8 Inhibitors (strength unknown)
- Cytochrome P-450 CYP2C8 Inhibitors (weak)
- Cytochrome P-450 CYP2C9 Inhibitors
- Cytochrome P-450 CYP2C9 Inhibitors (strength unknown)
- Cytochrome P-450 Enzyme Inducers
- Cytochrome P-450 Enzyme Inhibitors
- Dopamine Agents
- Enzyme Inhibitors
- Hypotensive Agents
- Nervous System
- OATP1B1/SLCO1B1 Inhibitors
- OATP1B3 substrates
- OATP2B1/SLCO2B1 substrates
- Oxazoles
- P-glycoprotein substrates
- Chemical TaxonomyProvided by Classyfire
- Description
- This compound belongs to the class of organic compounds known as phenyloxadiazoles. These are polycyclic aromatic compounds containing a benzene ring linked to a 1,2,4-oxadiazole ring through a CC or CN bond.
- Kingdom
- Organic compounds
- Super Class
- Organoheterocyclic compounds
- Class
- Azoles
- Sub Class
- Oxadiazoles
- Direct Parent
- Phenyloxadiazoles
- Alternative Parents
- Nitrophenols / Nitrobenzenes / Catechols / Nitroaromatic compounds / Polyhalopyridines / 1-hydroxy-2-unsubstituted benzenoids / Methylpyridines / 1-hydroxy-4-unsubstituted benzenoids / 2-halopyridines / Aryl chlorides show 12 more
- Substituents
- 1-hydroxy-2-unsubstituted benzenoid / 1-hydroxy-4-unsubstituted benzenoid / 2-halopyridine / Aromatic heteromonocyclic compound / Aryl chloride / Aryl halide / Azacycle / Benzenoid / C-nitro compound / Catechol show 24 more
- Molecular Framework
- Aromatic heteromonocyclic compounds
- External Descriptors
- Not Available
- Affected organisms
- Humans and other mammals
Chemical Identifiers
- UNII
- Y5929UIJ5N
- CAS number
- 923287-50-7
- InChI Key
- ASOADIZOVZTJSR-UHFFFAOYSA-N
- InChI
- InChI=1S/C15H10Cl2N4O6/c1-5-10(13(17)20(24)6(2)11(5)16)14-18-15(27-19-14)7-3-8(21(25)26)12(23)9(22)4-7/h3-4,22-23H,1-2H3
- IUPAC Name
- 2,5-dichloro-3-[5-(3,4-dihydroxy-5-nitrophenyl)-1,2,4-oxadiazol-3-yl]-4,6-dimethylpyridin-1-ium-1-olate
- SMILES
- CC1=C(C2=NOC(=N2)C2=CC(=C(O)C(O)=C2)[N+]([O-])=O)C(Cl)=[N+]([O-])C(C)=C1Cl
References
- General References
- Scott LJ: Opicapone: A Review in Parkinson's Disease. Drugs. 2016 Sep;76(13):1293-1300. doi: 10.1007/s40265-016-0623-y. [Article]
- Goncalves D, Alves G, Fortuna A, Soares-da-Silva P, Falcao A: Pharmacokinetics of opicapone, a third-generation COMT inhibitor, after single and multiple oral administration: A comparative study in the rat. Toxicol Appl Pharmacol. 2017 May 15;323:9-15. doi: 10.1016/j.taap.2017.03.013. Epub 2017 Mar 16. [Article]
- Almeida L, Rocha JF, Falcao A, Palma PN, Loureiro AI, Pinto R, Bonifacio MJ, Wright LC, Nunes T, Soares-da-Silva P: Pharmacokinetics, pharmacodynamics and tolerability of opicapone, a novel catechol-O-methyltransferase inhibitor, in healthy subjects: prediction of slow enzyme-inhibitor complex dissociation of a short-living and very long-acting inhibitor. Clin Pharmacokinet. 2013 Feb;52(2):139-51. doi: 10.1007/s40262-012-0024-7. [Article]
- Bonifacio MJ, Palma PN, Almeida L, Soares-da-Silva P: Catechol-O-methyltransferase and its inhibitors in Parkinson's disease. CNS Drug Rev. 2007 Fall;13(3):352-79. doi: 10.1111/j.1527-3458.2007.00020.x. [Article]
- Svetel M, Tomic A, Kresojevic N, Kostic V: Pharmacokinetic drug evaluation of opicapone for the treatment of Parkinson's disease. Expert Opin Drug Metab Toxicol. 2018 Mar;14(3):353-360. doi: 10.1080/17425255.2018.1430138. Epub 2018 Jan 24. [Article]
- Opicapone:once-daily adjunctive therapy for Parkinson’s disease [Link]
- Clinical pharmacology review of opicapone for the treatment of Parkinson's disease [Link]
- EMA assessment report [Link]
- Opicapone: a short lived and very long acting novel catechol-O-methyltransferase inhibitor following multiple dose administration in healthy subjects [Link]
- Summary of Product Characteristics: Ongentys (opicapone) oral capsules [Link]
- Pharmacological Profile of Opicapone, a Third Generation Nitrocatechol COMT Inhibitor, in the Rat [Link]
- Wikigenes [Link]
- FDA Approved Drug Products: ONGENTYS (opicapone) capsules, for oral use [Link]
- External Links
- ChemSpider
- 24667564
- BindingDB
- 50019329
- 2362167
- ChEBI
- 134699
- ChEMBL
- CHEMBL1089318
- ZINC
- ZINC000034602275
- PDBe Ligand
- DNI
- Wikipedia
- Opicapone
- PDB Entries
- 7xgi / 7xjb
Clinical Trials
- Clinical Trials Learn More" title="About Clinical Trials" id="clinical-trials-info" class="drug-info-popup" href="javascript:void(0);">
Phase Status Purpose Conditions Count 4 Active Not Recruiting Treatment Parkinson's Disease (PD) 2 4 Completed Treatment Parkinson's Disease (PD) 1 4 Completed Treatment Parkinson's Disease With Wearing-off Motor Fluctuations 1 4 Recruiting Treatment Parkinson's Disease (PD) 1 3 Active Not Recruiting Treatment Parkinson's Disease (PD) 1
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Capsule Oral 25 mg/1 Capsule Oral 25 MG Capsule Oral 50 MG Capsule Oral 50 mg/1 - Prices
- Not Available
- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region US9550759 No 2017-01-24 2026-07-26 US US9745290 No 2017-08-29 2027-10-10 US US9630955 No 2017-04-25 2032-12-12 US US10583130 No 2020-03-10 2030-03-31 US US8524746 No 2013-09-03 2029-07-14 US US8168793 No 2012-05-01 2029-04-02 US US10357468 No 2019-07-23 2035-05-27 US US10071085 No 2018-09-11 2030-03-31 US US8907099 No 2014-12-09 2027-05-12 US
Properties
- State
- Solid
- Experimental Properties
Property Value Source water solubility minimal http://www.ema.europa.eu/docs/en_GB/document_library/EPAR_-_Public_assessment_report/human/002790/WC500209538.pdf - Predicted Properties
Property Value Source logP 3.05 Chemaxon pKa (Strongest Acidic) 6.12 Chemaxon pKa (Strongest Basic) -0.47 Chemaxon Physiological Charge -1 Chemaxon Hydrogen Acceptor Count 7 Chemaxon Hydrogen Donor Count 2 Chemaxon Polar Surface Area 149.46 Å2 Chemaxon Rotatable Bond Count 3 Chemaxon Refractivity 118.12 m3·mol-1 Chemaxon Polarizability 37.42 Å3 Chemaxon Number of Rings 3 Chemaxon Bioavailability 1 Chemaxon Rule of Five Yes Chemaxon Ghose Filter Yes Chemaxon Veber's Rule No Chemaxon MDDR-like Rule No Chemaxon - Predicted ADMET Features
- Not Available
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
Spectrum Spectrum Type Splash Key Predicted GC-MS Spectrum - GC-MS Predicted GC-MS splash10-0059-0539000000-7474afd576b5551b7ce4 Predicted 1H NMR Spectrum 1D NMR Not Applicable Predicted 13C NMR Spectrum 1D NMR Not Applicable - Chromatographic Properties
Collision Cross Sections (CCS)
Adduct CCS Value (Å2) Source type Source [M-H]- 189.81471 predictedDeepCCS 1.0 (2019) [M+H]+ 191.95326 predictedDeepCCS 1.0 (2019) [M+Na]+ 197.8658 predictedDeepCCS 1.0 (2019)
Targets
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Inhibitor
- General Function
- O-methyltransferase activity
- Specific Function
- Catalyzes the O-methylation, and thereby the inactivation, of catecholamine neurotransmitters and catechol hormones. Also shortens the biological half-lives of certain neuroactive drugs, like L-DOP...
- Gene Name
- COMT
- Uniprot ID
- P21964
- Uniprot Name
- Catechol O-methyltransferase
- Molecular Weight
- 30036.77 Da
References
- Scott LJ: Opicapone: A Review in Parkinson's Disease. Drugs. 2016 Sep;76(13):1293-1300. doi: 10.1007/s40265-016-0623-y. [Article]
- Tardy B, Lecompte T, Boelhen F, Tardy-Poncet B, Elalamy I, Morange P, Gruel Y, Wolf M, Francois D, Racadot E, Camarasa P, Blouch MT, Nguyen F, Doubine S, Dutrillaux F, Alhenc-Gelas M, Martin-Toutain I, Bauters A, Ffrench P, de Maistre E, Grunebaum L, Mouton C, Huisse MG, Gouault-Heilmann M, Lucke V: Predictive factors for thrombosis and major bleeding in an observational study in 181 patients with heparin-induced thrombocytopenia treated with lepirudin. Blood. 2006 Sep 1;108(5):1492-6. Epub 2006 May 11. [Article]
- EMA assessment report [Link]
- Opicapone: a short lived and very long acting novel catechol-O-methyltransferase inhibitor following multiple dose administration in healthy subjects [Link]
- Summary of Product Characteristics: Ongentys (opicapone) oral capsules [Link]
Enzymes
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Inducer
- Curator comments
- Data supporting this enzyme induction is limited to in vitro studies.
- 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
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Inhibitor
- 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
- CYP2C8
- Uniprot ID
- P10632
- Uniprot Name
- Cytochrome P450 2C8
- Molecular Weight
- 55824.275 Da
References
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Inhibitor
- Curator comments
- According to the EU prescribing information, opicapone reduces CYP2C9 activity through competitive or mixed type mode of inhibition.
- 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
- Summary of Product Characteristics: Ongentys (opicapone) oral capsules [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Inhibitor
- Curator comments
- In vitro, the reduction in enzyme activity was observed at the highest concentration of opicapone (10 mcg/mL).
- General Function
- Oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen
- 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
- CYP1A2
- Uniprot ID
- P05177
- Uniprot Name
- Cytochrome P450 1A2
- Molecular Weight
- 58293.76 Da
References
- Summary of Product Characteristics: Ongentys (opicapone) oral capsules [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Inhibitor
- Curator comments
- In vitro, the reduction in enzyme activity was observed at the highest concentration of opicapone (10 mcg/mL).
- 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
- CYP2B6
- Uniprot ID
- P20813
- Uniprot Name
- Cytochrome P450 2B6
- Molecular Weight
- 56277.81 Da
References
- Summary of Product Characteristics: Ongentys (opicapone) oral capsules [Link]
Transporters
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Substrate
- General Function
- Xenobiotic-transporting atpase activity
- Specific Function
- Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
- Gene Name
- ABCB1
- Uniprot ID
- P08183
- Uniprot Name
- Multidrug resistance protein 1
- Molecular Weight
- 141477.255 Da
References
- FDA Approved Drug Products: ONGENTYS (opicapone) capsules, for oral use [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Substrate
- General Function
- Xenobiotic-transporting atpase activity
- Specific Function
- High-capacity urate exporter functioning in both renal and extrarenal urate excretion. Plays a role in porphyrin homeostasis as it is able to mediates the export of protoporhyrin IX (PPIX) both fro...
- Gene Name
- ABCG2
- Uniprot ID
- Q9UNQ0
- Uniprot Name
- ATP-binding cassette sub-family G member 2
- Molecular Weight
- 72313.47 Da
References
- FDA Approved Drug Products: ONGENTYS (opicapone) capsules, for oral use [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Substrate
- General Function
- Sodium-independent organic anion transmembrane transporter activity
- Specific Function
- Mediates the Na(+)-independent uptake of organic anions such as 17-beta-glucuronosyl estradiol, taurocholate, triiodothyronine (T3), leukotriene C4, dehydroepiandrosterone sulfate (DHEAS), methotre...
- Gene Name
- SLCO1B3
- Uniprot ID
- Q9NPD5
- Uniprot Name
- Solute carrier organic anion transporter family member 1B3
- Molecular Weight
- 77402.175 Da
References
- FDA Approved Drug Products: ONGENTYS (opicapone) capsules, for oral use [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Substrate
- General Function
- Sodium-independent organic anion transmembrane transporter activity
- Specific Function
- Mediates the Na(+)-independent transport of organic anions such as taurocholate, the prostaglandins PGD2, PGE1, PGE2, leukotriene C4, thromboxane B2 and iloprost.
- Gene Name
- SLCO2B1
- Uniprot ID
- O94956
- Uniprot Name
- Solute carrier organic anion transporter family member 2B1
- Molecular Weight
- 76709.98 Da
References
- FDA Approved Drug Products: ONGENTYS (opicapone) capsules, for oral use [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- 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
- Summary of Product Characteristics: Ongentys (opicapone) oral capsules [Link]
Drug created at October 17, 2016 21:26 / Updated at February 21, 2021 18:53