Identification
- Summary
Lumacaftor is a protein chaperone used in combination with ivacaftor for the treatment of cystic fibrosis in patients who are homozygous for the F508del mutation in the CFTR gene.
- Brand Names
- Orkambi
- Generic Name
- Lumacaftor
- DrugBank Accession Number
- DB09280
- Background
Lumacaftor is a drug used in combination with Ivacaftor as the fixed dose combination product Orkambi for the management of Cystic Fibrosis (CF) in patients aged 6 years and older. Cystic Fibrosis is an autosomal recessive disorder caused by one of several different mutations in the gene for the Cystic Fibrosis Transmembrane Conductance Regulator (CFTR) protein, a transmembrane ion channel involved in the transport of chloride and sodium ions across cell membranes of the lungs, pancreas, and other organs. Mutations in the CFTR gene result in altered production, misfolding, or function of the CFTR protein and consequently abnormal fluid and ion transport across cell membranes.3,4 As a result, CF patients produce thick, sticky mucus that clogs the ducts of organs where it is produced making patients more susceptible to infections, lung damage, pancreatic insufficiency, and malnutrition.5 Lumacaftor improves CF symptoms and underlying disease pathology by aiding the conformational stability of F508del-mutated CFTR proteins, preventing misfolding and resulting in increased processing and trafficking of mature protein to the cell surface.
Results from clinical trials indicated that treatment with Orkambi (lumacaftor/ivacaftor) results in improved lung function, reduced chance of experiencing a pulmonary exacerbation, increased weight gain, and improvements in CF symptoms.Label This data has been heavily scrutinized, however, with clinical trials showing only modest improvements despite a hefty yearly cost of $259,000 for Orkambi.8 Improvements in lung function (ppFEV1) were found to be statistically significant, but minimal, with only a 2.6-3.0% change from baseline with more than 70% of patients failing to achieve an absolute improvement of at least 5%.8,9
A wide variety of CFTR mutations correlate to the Cystic Fibrosis phenotype and are associated with differing levels of disease severity. The most common mutation, affecting approximately 70% of patients with CF worldwide, is known as F508del-CFTR, or delta-F508 (ΔF508), in which a deletion in the amino acid phenylalanine at position 508 results in impaired production of the CFTR protein, thereby causing a significant reduction in the amount of ion transporter present on cell membranes.6 When used in combination with Ivacaftor as the fixed dose combination product Orkambi, lumacaftor is specific for the management of CF in patients with delta-F508 mutations as it acts as a protein-folding chaperone, aiding the conformational stability of the mutated CFTR protein. Consequently, lumacaftor increases successful production of CFTR ion channels and the total number of receptors available for use at the cell membrane for fluid and ion transport.2 The next most common mutation, G551D, affecting 4-5% of CF patients worldwide, is characterized as a missense mutation, whereby there is sufficient amount of protein at the cell surface, but opening and closing mechanisms of the channel are altered.7 Treatment of patients with G551D and other rarer missense mutations is usually managed with Ivacaftor (Kalydeco), as it aids with altered gating mechanisms by potentiating channel opening probability of CFTR protein.
Prior to the development of lumacaftor and Ivacaftor (Kalydeco), management of CF primarily involved therapies for the control of infections, nutritional support, clearance of mucus, and management of symptoms rather than improvements in the underlying disease process. Approved for use by the Food and Drug Administration in July 2015 and by Health Canada in January 2016, Orkambi was the first combination product approved for the management of Cystic Fibrosis with delta-F508 mutations.
Ivacaftor is manufactured and distributed by Vertex Pharmaceuticals.
- Type
- Small Molecule
- Groups
- Approved
- Structure
- Weight
- Average: 452.414
Monoisotopic: 452.118378014 - Chemical Formula
- C24H18F2N2O5
- Synonyms
- 3-(6-{[1-(2,2-difluoro-2H-1,3-benzodioxol-5-yl)cyclopropane-1-carbonyl]amino}-3-methylpyridin-2-yl)benzoic acid
- Lumacaftor
- External IDs
- VRT 826809
- VRT-826809
- VX 809
- VX-809
Pharmacology
- Indication
When used in combination with the drug lumacaftor as the product Orkambi, ivacaftor is indicated for the management of CF in patients age 2 years and older who are homozygous for the F508del mutation in the CFTR gene. If the patient’s genotype is unknown, an FDA-cleared CF mutation test should be used to detect the presence of the F508del mutation on both alleles of the CFTR gene.10
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
- Contraindications & Blackbox Warnings
- Avoid life-threatening adverse drug eventsImprove clinical decision support with information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.Avoid life-threatening adverse drug events & improve clinical decision support.
- Pharmacodynamics
Results from clinical trials indicated that treatment with Orkambi (lumacaftor/ Ivacaftor) results in improved lung function, reduced chance of experiencing a pulmonary exacerbation, reduced sweat chloride, increased weight gain, and improvements in CF symptoms and quality of life.Label
Orkambi was not found to increase the QTc interval to any clinically relevant extent.Label
- Mechanism of action
Lumacaftor improves CF symptoms and underlying disease pathology by aiding the conformational stability of F508del-mutated CFTR, resulting in increased processing and trafficking of mature protein to the cell surface.Label More specifically, lumacaftor acts as a protein-folding chaperone, preventing misfolding of CFTR ion channels and consequent destruction during processing in the endoplasmic reticulum.
Target Actions Organism ACystic fibrosis transmembrane conductance regulator modulatorHumans - Absorption
Following administration of Orkambi (lumacaftor/Ivacaftor) with fat containing foods, peak plasma concentrations were reached at 4 hours (Tmax). It's recommended that Orkambi should be taken with fat-containing foods as they increase absorption of lumacaftor by approximately 2-fold, and[DB08820 by 3-fold.Label
- Volume of distribution
Following oral administration of 200 mg of lumacaftor every 24 hours to cystic fibrosis patients in a fed state for 28 days, the mean (+/-SD) for apparent volumes of distribution was 86.0 (69.8) L.Label
- Protein binding
Lumacaftor is extensively protein bound in the plasma (99%), and binds primarily to albumin.Label
- Metabolism
Lumacaftor is mostly excreted unchanged in the feces and is not extensively metabolized. When metabolism does occur, oxidation and glucuronidation are the main processes involved.Label
- Route of elimination
Lumacaftor is primarily excreted unchanged in the feces (51%). A minimal amount of the parent compound and its metabolites are excreted in the urine.Label
- Half-life
The half-life of lumacaftor is approximately 26 hours.Label
- Clearance
The typical apparent clearance, CL/F (CV), of lumacaftor was estimated to be 2.38 L/hr.Label
- Adverse Effects
- Improve decision support & research outcomesWith structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates.Improve decision support & research outcomes with our structured adverse effects data.
- Toxicity
The most common side effects (occuring in >5% of patients during clinical trials) associated with the use of Orkambi include dyspnea, nasopharyngitis, nausea, diarrhea, upper respiratory tract infection, fatigue, respiration abnormal, blood creatine phosphokinase increased, rash, flatulence, rhinorrhea, and influenza.Label
- 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.
Drug Interaction Integrate drug-drug
interactions in your software1,2-Benzodiazepine The metabolism of 1,2-Benzodiazepine can be increased when combined with Lumacaftor. Abemaciclib The serum concentration of Abemaciclib can be decreased when it is combined with Lumacaftor. Abiraterone The metabolism of Abiraterone can be increased when combined with Lumacaftor. Abrocitinib The serum concentration of Abrocitinib can be decreased when it is combined with Lumacaftor. Acalabrutinib The metabolism of Acalabrutinib can be increased when combined with Lumacaftor. Acenocoumarol The serum concentration of Acenocoumarol can be decreased when it is combined with Lumacaftor. Acetaminophen The metabolism of Acetaminophen can be increased when combined with Lumacaftor. Acetohexamide The metabolism of Acetohexamide can be decreased when combined with Lumacaftor. Acetylsalicylic acid The metabolism of Acetylsalicylic acid can be decreased when combined with Lumacaftor. Afatinib The serum concentration of Afatinib can be increased when it is combined with Lumacaftor. Identify potential medication risksEasily compare up to 40 drugs with our drug interaction checker.Get severity rating, description, and management advice.Learn more - Food Interactions
- No interactions found.
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.
- Mixture Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image Orkambi Lumacaftor (200 mg) + Ivacaftor (125 mg) Tablet, film coated Oral Vertex Pharmaceuticals (Ireland) Limited 2016-09-08 Not applicable EU Orkambi Lumacaftor (100 mg) + Ivacaftor (125 mg) Tablet Oral Vertex Pharmaceuticals Incorporated 2017-05-03 Not applicable Canada Orkambi Lumacaftor (100 mg/1) + Ivacaftor (125 mg/1) Granule Oral Vertex Pharmaceuticals Incorporated 2018-08-07 Not applicable US Orkambi Lumacaftor (200 mg) + Ivacaftor (125 mg) Tablet, film coated Oral Vertex Pharmaceuticals (Ireland) Limited 2016-09-08 2021-11-12 EU Orkambi Lumacaftor (150 mg / sachet) + Ivacaftor (188 mg / sachet) Granule Oral Vertex Pharmaceuticals Incorporated 2018-12-14 Not applicable Canada Orkambi Lumacaftor (200 mg) + Ivacaftor (125 mg) Tablet Oral Vertex Pharmaceuticals Incorporated 2016-01-27 Not applicable Canada Orkambi Lumacaftor (150 mg) + Ivacaftor (188 mg) Granule Oral Vertex Pharmaceuticals (Ireland) Limited 2020-12-22 Not applicable EU Orkambi Lumacaftor (100 mg/1) + Ivacaftor (125 mg/1) Tablet, film coated Oral Vertex Pharmaceuticals Incorporated 2016-09-28 Not applicable US Orkambi Lumacaftor (200 mg) + Ivacaftor (125 mg) Tablet, film coated Oral Vertex Pharmaceuticals (Ireland) Limited 2016-09-08 2020-12-14 EU Orkambi Lumacaftor (100 mg / sachet) + Ivacaftor (125 mg / sachet) Granule Oral Vertex Pharmaceuticals Incorporated 2018-12-14 Not applicable Canada
Categories
- ATC Codes
- R07AX30 — Ivacaftor and lumacaftor
- Drug Categories
- Amines
- Cytochrome P-450 CYP2B6 Inducers
- Cytochrome P-450 CYP2B6 Inducers (strength unknown)
- Cytochrome P-450 CYP2C19 Inducers
- Cytochrome P-450 CYP2C19 Inducers (strength unknown)
- Cytochrome P-450 CYP2C8 Inducers
- Cytochrome P-450 CYP2C8 Inducers (strength unknown)
- Cytochrome P-450 CYP2C8 Inhibitors
- Cytochrome P-450 CYP2C8 Inhibitors (strength unknown)
- Cytochrome P-450 CYP2C9 Inducers
- Cytochrome P-450 CYP2C9 Inducers (strength unknown)
- Cytochrome P-450 CYP2C9 Inhibitors
- Cytochrome P-450 CYP2C9 Inhibitors (strength unknown)
- Cytochrome P-450 CYP3A Inducers
- Cytochrome P-450 CYP3A Inducers (strong)
- Cytochrome P-450 CYP3A4 Inducers
- Cytochrome P-450 CYP3A4 Inducers (strong)
- Cytochrome P-450 Enzyme Inducers
- Cytochrome P-450 Enzyme Inhibitors
- Dioxoles
- Heterocyclic Compounds, Fused-Ring
- P-glycoprotein inducers
- P-glycoprotein inhibitors
- Pyridines
- Chemical TaxonomyProvided by Classyfire
- Description
- This compound belongs to the class of organic compounds known as phenylpyridines. These are polycyclic aromatic compounds containing a benzene ring linked to a pyridine ring through a CC or CN bond.
- Kingdom
- Organic compounds
- Super Class
- Organoheterocyclic compounds
- Class
- Pyridines and derivatives
- Sub Class
- Phenylpyridines
- Direct Parent
- Phenylpyridines
- Alternative Parents
- Benzodioxoles / Benzoic acids / Benzoyl derivatives / N-arylamides / Methylpyridines / Imidolactams / Cyclopropanecarboxylic acids and derivatives / Heteroaromatic compounds / Secondary carboxylic acid amides / Azacyclic compounds show 9 more
- Substituents
- 2-phenylpyridine / Alkyl fluoride / Alkyl halide / Aromatic heteropolycyclic compound / Azacycle / Benzenoid / Benzodioxole / Benzoic acid / Benzoic acid or derivatives / Benzoyl show 22 more
- Molecular Framework
- Aromatic heteropolycyclic compounds
- External Descriptors
- Not Available
- Affected organisms
- Not Available
Chemical Identifiers
- UNII
- EGP8L81APK
- CAS number
- 936727-05-8
- InChI Key
- UFSKUSARDNFIRC-UHFFFAOYSA-N
- InChI
- InChI=1S/C24H18F2N2O5/c1-13-5-8-19(27-20(13)14-3-2-4-15(11-14)21(29)30)28-22(31)23(9-10-23)16-6-7-17-18(12-16)33-24(25,26)32-17/h2-8,11-12H,9-10H2,1H3,(H,29,30)(H,27,28,31)
- IUPAC Name
- 3-{6-[1-(2,2-difluoro-2H-1,3-benzodioxol-5-yl)cyclopropaneamido]-3-methylpyridin-2-yl}benzoic acid
- SMILES
- CC1=CC=C(NC(=O)C2(CC2)C2=CC=C3OC(F)(F)OC3=C2)N=C1C1=CC(=CC=C1)C(O)=O
References
- General References
- Boyle MP, Bell SC, Konstan MW, McColley SA, Rowe SM, Rietschel E, Huang X, Waltz D, Patel NR, Rodman D: A CFTR corrector (lumacaftor) and a CFTR potentiator (ivacaftor) for treatment of patients with cystic fibrosis who have a phe508del CFTR mutation: a phase 2 randomised controlled trial. Lancet Respir Med. 2014 Jul;2(7):527-38. doi: 10.1016/S2213-2600(14)70132-8. Epub 2014 Jun 24. [Article]
- Kuk K, Taylor-Cousar JL: Lumacaftor and ivacaftor in the management of patients with cystic fibrosis: current evidence and future prospects. Ther Adv Respir Dis. 2015 Dec;9(6):313-26. doi: 10.1177/1753465815601934. Epub 2015 Sep 28. [Article]
- Saint-Criq V, Gray MA: Role of CFTR in epithelial physiology. Cell Mol Life Sci. 2017 Jan;74(1):93-115. doi: 10.1007/s00018-016-2391-y. Epub 2016 Oct 6. [Article]
- Kunzelmann K, Mall M: Pharmacotherapy of the ion transport defect in cystic fibrosis: role of purinergic receptor agonists and other potential therapeutics. Am J Respir Med. 2003;2(4):299-309. [Article]
- Fraser-Pitt D, O'Neil D: Cystic fibrosis - a multiorgan protein misfolding disease. Future Sci OA. 2015 Sep 1;1(2):FSO57. doi: 10.4155/fso.15.57. eCollection 2015 Sep. [Article]
- MacDonald KD, McKenzie KR, Zeitlin PL: Cystic fibrosis transmembrane regulator protein mutations: 'class' opportunity for novel drug innovation. Paediatr Drugs. 2007;9(1):1-10. [Article]
- Yu H, Burton B, Huang CJ, Worley J, Cao D, Johnson JP Jr, Urrutia A, Joubran J, Seepersaud S, Sussky K, Hoffman BJ, Van Goor F: Ivacaftor potentiation of multiple CFTR channels with gating mutations. J Cyst Fibros. 2012 May;11(3):237-45. doi: 10.1016/j.jcf.2011.12.005. Epub 2012 Jan 30. [Article]
- Mayer M: Lumacaftor-ivacaftor (Orkambi) for cystic fibrosis: behind the 'breakthrough'. Evid Based Med. 2016 Jun;21(3):83-6. doi: 10.1136/ebmed-2015-110325. Epub 2015 Dec 30. [Article]
- The Canadian Drug Expert Committee (CDEC): Lumacaftor/Ivacaftor Recommendation [Link]
- FDA Approved Drug Products: ORKAMBI (lumacaftor/ivacaftor) granules or tablets, for oral use [Link]
- External Links
- KEGG Drug
- D10134
- PubChem Compound
- 16678941
- PubChem Substance
- 310265173
- ChemSpider
- 17611836
- BindingDB
- 50289703
- 1655922
- ChEBI
- 90951
- ChEMBL
- CHEMBL2103870
- ZINC
- ZINC000064033452
- PharmGKB
- PA166114483
- PDBe Ligand
- VX8
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- Wikipedia
- Lumacaftor
- PDB Entries
- 7svd / 7svr
- FDA label
- Download (335 KB)
Clinical Trials
- Clinical Trials
Phase Status Purpose Conditions Count 4 Completed Other Cystic Fibrosis (CF) 1 4 Terminated Treatment Cystic Fibrosis (CF) 2 3 Active Not Recruiting Treatment Cystic Fibrosis (CF) 1 3 Completed Treatment Advanced Lung Disease / Cystic Fibrosis (CF) 1 3 Completed Treatment Cystic Fibrosis (CF) 6 3 Completed Treatment Cystic Fibrosis, Homozygous for the F508del CFTR Mutation 2 3 Completed Treatment Cystic Fibrosis, Homozygous or Heterozygous for the F508del-CFTR Mutation 1 2 Completed Treatment Cystic Fibrosis (CF) 5 2 Recruiting Treatment Long QT Syndrome (LQTS) 1 1 Completed Not Available Cystic Fibrosis (CF) 1
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Granule Oral Tablet Oral Tablet, film coated Oral - Prices
- Not Available
- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region US8324242 No 2012-12-04 2027-04-18 US US8754224 No 2014-06-17 2026-12-28 US US8410274 No 2013-04-02 2026-12-28 US US7495103 No 2009-02-24 2027-05-20 US US8741933 No 2014-06-03 2026-11-08 US US8716338 No 2014-05-06 2026-11-08 US US8846718 No 2014-09-30 2028-12-04 US US8653103 No 2014-02-18 2028-12-04 US US9216969 No 2015-12-22 2026-11-08 US US8507534 No 2013-08-13 2030-09-20 US US8993600 No 2015-03-31 2030-12-11 US US9670163 No 2017-06-06 2026-12-28 US US9192606 No 2015-11-24 2029-09-29 US US7973038 No 2011-07-05 2026-11-08 US US9150552 No 2015-10-06 2028-12-04 US US9931334 No 2018-04-03 2026-12-28 US US10076513 No 2018-09-18 2028-12-04 US US10597384 No 2020-03-24 2028-12-04 US US10646481 No 2020-05-12 2029-08-13 US US11052075 No 2021-07-06 2028-12-04 US
Properties
- State
- Solid
- Experimental Properties
- Not Available
- Predicted Properties
Property Value Source Water Solubility 0.00376 mg/mL ALOGPS logP 4.37 ALOGPS logP 5.77 ChemAxon logS -5.1 ALOGPS pKa (Strongest Acidic) 4.17 ChemAxon pKa (Strongest Basic) 3.5 ChemAxon Physiological Charge -1 ChemAxon Hydrogen Acceptor Count 6 ChemAxon Hydrogen Donor Count 2 ChemAxon Polar Surface Area 97.75 Å2 ChemAxon Rotatable Bond Count 5 ChemAxon Refractivity 111.97 m3·mol-1 ChemAxon Polarizability 44.12 Å3 ChemAxon Number of Rings 5 ChemAxon Bioavailability 1 ChemAxon Rule of Five No ChemAxon Ghose Filter No 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 MS/MS Spectrum - 10V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 20V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 40V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 10V, Negative (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 20V, Negative (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 40V, Negative (Annotated) Predicted LC-MS/MS Not Available
Targets

- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Modulator
- General Function
- Pdz domain binding
- Specific Function
- Involved in the transport of chloride ions. May regulate bicarbonate secretion and salvage in epithelial cells by regulating the SLC4A7 transporter. Can inhibit the chloride channel activity of ANO...
- Gene Name
- CFTR
- Uniprot ID
- P13569
- Uniprot Name
- Cystic fibrosis transmembrane conductance regulator
- Molecular Weight
- 168139.895 Da
References
- Kuk K, Taylor-Cousar JL: Lumacaftor and ivacaftor in the management of patients with cystic fibrosis: current evidence and future prospects. Ther Adv Respir Dis. 2015 Dec;9(6):313-26. doi: 10.1177/1753465815601934. Epub 2015 Sep 28. [Article]
Enzymes
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Inducer
- General Function
- Vitamin d3 25-hydroxylase activity
- Specific Function
- Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
- Gene Name
- CYP3A4
- Uniprot ID
- P08684
- Uniprot Name
- Cytochrome P450 3A4
- Molecular Weight
- 57342.67 Da
References
- Jordan CL, Noah TL, Henry MM: Therapeutic challenges posed by critical drug-drug interactions in cystic fibrosis. Pediatr Pulmonol. 2016 Oct;51(S44):S61-S70. doi: 10.1002/ppul.23505. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Inducer
- 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
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- InhibitorInducer
- 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
- InhibitorInducer
- Curator comments
- Enzyme action is based on in vitro data.
- 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
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Inducer
- Curator comments
- Data supporting CYP2C19 induction by this drug 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
Carriers
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Carrier
- 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
Transporters
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- InhibitorInducer
- 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
Drug created at October 29, 2015 15:12 / Updated at April 01, 2022 19:23