Elexacaftor
Identification
- Summary
Elexacaftor is a small molecule CFTR corrector used in combination with tezacaftor and ivacaftor for the treatment of cystic fibrosis patients with one F508del-CFTR mutation.
- Brand Names
- Trikafta (100 Mg / 50 Mg / 75 Mg; 150 Mg)
- Generic Name
- Elexacaftor
- DrugBank Accession Number
- DB15444
- Background
Elexacaftor (previously VX-445) is a small molecule, next-generation corrector of the cystic fibrosis transmembrane conductance regulator (CFTR) protein.3 It received FDA approval in October 2019 in combination with tezacaftor and ivacaftor as the combination product TrikaftaTM.6 Elexacaftor is considered a next-generation CFTR corrector as it possesses both a different structure and mechanism as compared to first generation correctors like tezacaftor.3 While dual corrector/potentiator combination therapy has proven useful in the treatment of a subset of CF patients,2 their use is typically limited to patients who are homozygous for the F508del-CFTR gene.3 Elexacaftor, along with VX-659, was designed to fill the need for an efficacious CF therapy for patients who are heterozygous for F508del-CFTR and a gene that does not produce protein or produces proteins unresponsive to ivacaftor or tezacaftor.3 The triple combination product TrikaftaTM, manufactured by Vertex Pharmaceuticals, is the first product approved for the treatment of CF in individuals who are either homo- or heterozygous for the F508del-CFTR gene - this represents approximately 704-90%3,1 of all CF patients.
- Type
- Small Molecule
- Groups
- Approved, Investigational
- Structure
- Weight
- Average: 597.66
Monoisotopic: 597.234508266 - Chemical Formula
- C26H34F3N7O4S
- Synonyms
- Elexacaftor
- External IDs
- VX-445
- WHO 11180
Pharmacology
- Indication
Elexacaftor, in combination with ivacaftor and tezacaftor as the combination product TrikaftaTM, is indicated for the treatment of cystic fibrosis (CF) in patients 12 years of age and older who have at least one F508del mutation in the CTFR gene.6
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 Used in combination to manage Cystic fibrosis Combination Product in combination with: Ivacaftor (DB08820), Tezacaftor (DB11712) •••••••••••• ••••••• Used in combination to manage Cystic fibrosis Combination Product in combination with: Tezacaftor (DB11712), Ivacaftor (DB08820) •••••••••••• •••••• - Contraindications & Blackbox Warnings
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- Pharmacodynamics
As a CFTR corrector, elexacaftor works to increase the amount of mature CFTR proteins present on the surface of cells.6 When used in combination with CFTR potentiators, which enhance the function of cell-surface CFTR proteins, drugs like elexacaftor help to improve a variety of multi-organ cystic fibrosis symptoms, including lung function, nutritional status, and overall quality of life.3 TrikaftaTM, the triple combination product containing elexacaftor, may cause elevations in liver transaminases. Liver function testing should be conducted prior to beginning Trikafta, every 3 months for the first year of treatment, and annually thereafter.6
- Mechanism of action
Cystic fibrosis (CF) is the result of a mutation in the cystic fibrosis transmembrane conductance regulator (CFTR) gene.4 The CFTR proteins produced by this gene are transmembrane ion channels that move sodium and chloride across cell membranes - water follows the flow of chloride ions to the cell surface, which consequently helps to hydrate the surface of the cell and thin the secretions (i.e. mucous) around the cell.4 Mutations in the CFTR gene produce CFTR proteins of insufficient quantity and/or function, leading to defective ion transport and a build-up of thick mucous throughout the body that causes multi-organ disease involving the pulmonary, gastrointestinal, and pancreatic systems (amongst others). The most common CFTR mutation, the F508del mutation, is estimated to account for 704 to 90%3,1 of all CFTR mutations and results in severe processing and trafficking defects of the CFTR protein.2
Elexacaftor is a CFTR corrector that modulates CFTR proteins to facilitate trafficking to the cell surface for incorporation into the cell membrane.6 The end result is an increase in the number of mature CFTR proteins present at the cell surface and, therefore, improved ion transport and CF symptomatology. Elexacaftor is used in combination with tezacaftor, another CFTR corrector with a different mechanism of action, and ivacaftor, a CFTR potentiator that improves the function of CFTR proteins on the cell surface - this multi-faceted, triple-drug approach confers a synergistic effect beyond that seen in typical corrector/potentiator dual therapy regimens.6,3
Target Actions Organism ACystic fibrosis transmembrane conductance regulator positive allosteric modulatorHumans - Absorption
The absolute oral bioavailability of elexacaftor is approximately 80%. The steady-state AUC0-24h and Cmax following once daily dosing with elexacaftor 200mg are 162 mcg∙h/mL and 8.7 mcg/mL, respectively, and the median Tmax is 6 hours.6 The AUC of elexacaftor is increased 1.9-2.5-fold following a moderate-fat meal - for this reason, it is recommended to give TrikaftaTM with fat-containing food.6
- Volume of distribution
The apparent volume of distribution of elexacaftor is 53.7 L.6
- Protein binding
Elexacaftor is >99% protein bound in plasma, primarily to albumin.6
- Metabolism
The metabolism of elexacaftor is extensive and primarily catalyzed via CYP3A4/5.6 Its main active metabolite, M23-ELX, carries a similar potency as the parent drug.6 The precise metabolic pathway of elexacaftor has not yet been elucidated in published research.
- Route of elimination
Approximately 87.3% of an administered radio-labeled dose of elexacaftor was found in the feces, mostly as metabolites, while only 0.23% of that same dose was found excreted in the urine.6
- Half-life
The mean terminal half-life of elexacaftor is approximately 24.7 hours.6
- Clearance
The mean apparent clearance of elexacaftor is 1.18 L/h.6
- Adverse Effects
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- Toxicity
As elexacaftor is currently only available in the combination product TrikaftaTM (ivacaftor/tezacaftor/elexacaftor), data regarding overdose of elexacaftor on its own is unavailable.6 Treatment of TrikaftaTM overdose should consist of general supportive and symptomatic treatment, including monitoring of vital signs and close observation of the affected patient.
- 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 softwareAbametapir The serum concentration of Elexacaftor can be increased when it is combined with Abametapir. Abatacept The metabolism of Elexacaftor can be increased when combined with Abatacept. Abemaciclib The metabolism of Abemaciclib can be decreased when combined with Elexacaftor. Acalabrutinib The metabolism of Acalabrutinib can be decreased when combined with Elexacaftor. Acenocoumarol The metabolism of Acenocoumarol can be decreased when combined with Elexacaftor. - Food Interactions
- Avoid grapefruit products. Co-administration of grapefruit can inhibit elexacaftor metabolism and increase serum concentrations.
- Avoid St. John's Wort. This herb induces CYP3A metabolism and may reduce serum levels of elexacaftor.
- Take with a high fat meal. Examples include food prepared with eggs, cheeses, nuts, oils, and butter.
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 Kaftrio Elexacaftor (100 mg) + Ivacaftor (75 mg) + Tezacaftor (50 mg) Tablet, film coated Oral Vertex Pharmaceuticals (Ireland) Limited 2020-12-15 Not applicable EU KAFTRIO Elexacaftor (100 MG) + Ivacaftor (75 MG) + Tezacaftor (50 MG) Tablet, film coated Oral Vertex Pharmaceuticals (Ireland) Limited 2020-11-14 Not applicable Italy Kaftrio Elexacaftor (50 mg) + Ivacaftor (37.5 mg) + Tezacaftor (25 mg) Tablet, film coated Oral Vertex Pharmaceuticals (Ireland) Limited 2022-05-04 Not applicable EU Trikafta Elexacaftor (100 mg) + Ivacaftor (75 mg) + Ivacaftor (75 mg) + Tezacaftor (50 mg) Granule Oral Vertex Pharmaceuticals Incorporated 2023-10-27 Not applicable Canada Trikafta Elexacaftor (50 mg) + Ivacaftor (37.5 mg) + Ivacaftor (75 mg) + Tezacaftor (25 mg) Tablet Oral Vertex Pharmaceuticals Incorporated 2022-04-22 Not applicable Canada
Categories
- ATC Codes
- R07AX32 — Ivacaftor, tezacaftor and elexacaftor
- Drug Categories
- Cystic Fibrosis Transmembrane Conductance Regulator Correctors
- Cytochrome P-450 CYP1A2 Inhibitors
- Cytochrome P-450 CYP1A2 Inhibitors (strength unknown)
- Cytochrome P-450 CYP2B6 Inhibitors
- Cytochrome P-450 CYP2B6 Inhibitors (strength unknown)
- Cytochrome P-450 CYP2C19 Inhibitors
- Cytochrome P-450 CYP2C19 inhibitors (strength unknown)
- Cytochrome P-450 CYP2C8 Inhibitors
- Cytochrome P-450 CYP2C8 Inhibitors (strength unknown)
- Cytochrome P-450 CYP2C9 Inhibitors
- Cytochrome P-450 CYP2C9 Inhibitors (strength unknown)
- Cytochrome P-450 CYP2D6 Inhibitors
- Cytochrome P-450 CYP2D6 Inhibitors (strength unknown)
- Cytochrome P-450 CYP3A Inhibitors
- Cytochrome P-450 CYP3A Substrates
- Cytochrome P-450 CYP3A4 Inhibitors
- Cytochrome P-450 CYP3A4 Inhibitors (strength unknown)
- Cytochrome P-450 CYP3A4 Substrates
- Cytochrome P-450 CYP3A4 Substrates (strength unknown)
- Cytochrome P-450 CYP3A5 Substrates
- Cytochrome P-450 Enzyme Inhibitors
- Cytochrome P-450 Substrates
- Membrane Transport Modulators
- OATP1B1/SLCO1B1 Inhibitors
- OATP1B3 inhibitors
- P-glycoprotein inhibitors
- P-glycoprotein substrates
- Classification
- Not classified
- Affected organisms
- Not Available
Chemical Identifiers
- UNII
- RRN67GMB0V
- CAS number
- 2216712-66-0
- InChI Key
- MVRHVFSOIWFBTE-INIZCTEOSA-N
- InChI
- InChI=1S/C26H34F3N7O4S/c1-16-12-25(5,6)35(13-16)22-18(23(37)33-41(38,39)19-14-34(7)31-17(19)2)8-9-20(30-22)36-11-10-21(32-36)40-15-24(3,4)26(27,28)29/h8-11,14,16H,12-13,15H2,1-7H3,(H,33,37)/t16-/m0/s1
- IUPAC Name
- N-[(1,3-dimethyl-1H-pyrazol-4-yl)sulfonyl]-6-[3-(3,3,3-trifluoro-2,2-dimethylpropoxy)-1H-pyrazol-1-yl]-2-[(4S)-2,2,4-trimethylpyrrolidin-1-yl]pyridine-3-carboxamide
- SMILES
- C[C@@H]1CN(C2=NC(=CC=C2C(=O)NS(=O)(=O)C2=CN(C)N=C2C)N2C=CC(OCC(C)(C)C(F)(F)F)=N2)C(C)(C)C1
References
- General References
- Keating D, Marigowda G, Burr L, Daines C, Mall MA, McKone EF, Ramsey BW, Rowe SM, Sass LA, Tullis E, McKee CM, Moskowitz SM, Robertson S, Savage J, Simard C, Van Goor F, Waltz D, Xuan F, Young T, Taylor-Cousar JL: VX-445-Tezacaftor-Ivacaftor in Patients with Cystic Fibrosis and One or Two Phe508del Alleles. N Engl J Med. 2018 Oct 25;379(17):1612-1620. doi: 10.1056/NEJMoa1807120. Epub 2018 Oct 18. [Article]
- Davies JC, Moskowitz SM, Brown C, Horsley A, Mall MA, McKone EF, Plant BJ, Prais D, Ramsey BW, Taylor-Cousar JL, Tullis E, Uluer A, McKee CM, Robertson S, Shilling RA, Simard C, Van Goor F, Waltz D, Xuan F, Young T, Rowe SM: VX-659-Tezacaftor-Ivacaftor in Patients with Cystic Fibrosis and One or Two Phe508del Alleles. N Engl J Med. 2018 Oct 25;379(17):1599-1611. doi: 10.1056/NEJMoa1807119. Epub 2018 Oct 18. [Article]
- Taylor-Cousar JL, Mall MA, Ramsey BW, McKone EF, Tullis E, Marigowda G, McKee CM, Waltz D, Moskowitz SM, Savage J, Xuan F, Rowe SM: Clinical development of triple-combination CFTR modulators for cystic fibrosis patients with one or two F508del alleles. ERJ Open Res. 2019 Jun 17;5(2). pii: 00082-2019. doi: 10.1183/23120541.00082-2019. eCollection 2019 Apr. [Article]
- Brown SD, White R, Tobin P: Keep them breathing: Cystic fibrosis pathophysiology, diagnosis, and treatment. JAAPA. 2017 May;30(5):23-27. doi: 10.1097/01.JAA.0000515540.36581.92. [Article]
- FDA News Release: Trikafta Approval [Link]
- FDA Approved Drug Products: Trikafta (elexacaftor, tezacaftor and ivacaftor tablets; ivacaftor tablets) [Link]
- FDA Approved Drug Products: TRIKAFTA® (elexacaftor, tezacaftor, and ivacaftor tablets; ivacaftor tablets), co-packaged for oral use May 2023 [Link]
- External Links
- Human Metabolome Database
- HMDB0304881
- ChemSpider
- 75531299
- 2256951
- ChEMBL
- CHEMBL4298128
- PDBe Ligand
- WJX
- Wikipedia
- Elexacaftor
- PDB Entries
- 8eig / 8eio / 8eiq
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 Other Adherence, Medication / Cystic Fibrosis (CF) / Cystic Fibrosis Gastrointestinal Disease / Cystic Fibrosis in Children / Cystic Fibrosis Liver Disease 1 4 Recruiting Other Drug Drug Interaction (DDI) 1 4 Recruiting Treatment Cystic Fibrosis (CF) 1 4 Recruiting Treatment Noncystic Fibrosis Bronchiectasis (NCFB) 1 3 Active Not Recruiting Treatment Cystic Fibrosis (CF) 2
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Tablet, film coated Oral Granule Oral Granule; kit Oral Kit; tablet, film coated Oral Tablet Oral - Prices
- Not Available
- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region US8324242 No 2012-12-04 2027-04-18 US US8354427 No 2013-01-15 2026-07-06 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 US8883206 No 2014-11-11 2033-02-27 US US9670163 No 2017-06-06 2026-12-28 US US8415387 No 2013-04-09 2027-11-12 US US9012496 No 2015-04-21 2033-07-15 US US8598181 No 2013-12-03 2027-05-01 US US8629162 No 2014-01-14 2025-06-24 US US8623905 No 2014-01-07 2027-05-01 US US7645789 No 2010-01-12 2027-05-01 US US7776905 No 2010-08-17 2027-06-03 US US9931334 No 2018-04-03 2026-12-28 US US9974781 No 2018-05-22 2027-04-09 US US10022352 No 2018-07-17 2027-04-09 US US10081621 No 2018-09-25 2031-03-25 US US10239867 No 2019-03-26 2027-04-09 US US10272046 No 2019-04-30 2033-02-27 US US10646481 No 2020-05-12 2029-08-13 US US10758534 No 2020-09-01 2035-10-06 US US10793547 No 2020-10-06 2037-12-08 US US11179367 No 2021-11-23 2037-12-08 US US11147770 No 2021-10-19 2033-02-27 US US11426407 No 2015-10-06 2035-10-06 US US11453655 No 2017-12-08 2037-12-08 US US11517564 No 2017-12-08 2037-12-08 US US11564916 No 2009-08-13 2029-08-13 US US11578062 No 2011-03-25 2031-03-25 US US11639347 No 2007-04-09 2027-04-09 US US11752106 No 2013-02-27 2033-02-27 US
Properties
- State
- Solid
- Experimental Properties
Property Value Source water solubility <1mg/mL Trikafta FDA Label - Predicted Properties
Property Value Source Water Solubility 0.0192 mg/mL ALOGPS logP 4.46 ALOGPS logP 5.04 Chemaxon logS -4.5 ALOGPS pKa (Strongest Acidic) 4.1 Chemaxon pKa (Strongest Basic) 2.09 Chemaxon Physiological Charge -1 Chemaxon Hydrogen Acceptor Count 8 Chemaxon Hydrogen Donor Count 1 Chemaxon Polar Surface Area 124.24 Å2 Chemaxon Rotatable Bond Count 8 Chemaxon Refractivity 160.13 m3·mol-1 Chemaxon Polarizability 60.59 Å3 Chemaxon Number of Rings 4 Chemaxon Bioavailability 0 Chemaxon Rule of Five No Chemaxon Ghose Filter No Chemaxon Veber's Rule No Chemaxon MDDR-like Rule Yes Chemaxon - Predicted ADMET Features
- Not Available
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
- Chromatographic Properties
Collision Cross Sections (CCS)
Not Available
Targets
![](https://go.drugbank.com/assets/locked/DrugTargets2-682eb846d210ae4bf33ca03febccfb57bb1c61318e699b729e5df4dfab2c5b67.png)
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Positive allosteric 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
- FDA Approved Drug Products: Trikafta (elexacaftor, tezacaftor and ivacaftor tablets; ivacaftor tablets) [Link]
Enzymes
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- SubstrateInhibitor
- 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
- FDA Approved Drug Products: Trikafta (elexacaftor, tezacaftor and ivacaftor tablets; ivacaftor tablets) [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Substrate
- General Function
- Oxygen binding
- 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
- CYP3A5
- Uniprot ID
- P20815
- Uniprot Name
- Cytochrome P450 3A5
- Molecular Weight
- 57108.065 Da
References
- FDA Approved Drug Products: Trikafta (elexacaftor, tezacaftor and ivacaftor tablets; ivacaftor tablets) [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Inhibitor
- 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
- FDA Approved Drug Products: Trikafta (elexacaftor, tezacaftor and ivacaftor tablets; ivacaftor tablets) [Link]
- 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
- CYP2B6
- Uniprot ID
- P20813
- Uniprot Name
- Cytochrome P450 2B6
- Molecular Weight
- 56277.81 Da
References
- FDA Approved Drug Products: Trikafta (elexacaftor, tezacaftor and ivacaftor tablets; ivacaftor tablets) [Link]
- 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
- FDA Approved Drug Products: Trikafta (elexacaftor, tezacaftor and ivacaftor tablets; ivacaftor tablets) [Link]
- 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
- CYP2C9
- Uniprot ID
- P11712
- Uniprot Name
- Cytochrome P450 2C9
- Molecular Weight
- 55627.365 Da
References
- FDA Approved Drug Products: Trikafta (elexacaftor, tezacaftor and ivacaftor tablets; ivacaftor tablets) [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Inhibitor
- 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
- FDA Approved Drug Products: Trikafta (elexacaftor, tezacaftor and ivacaftor tablets; ivacaftor tablets) [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Inhibitor
- General Function
- Steroid hydroxylase activity
- Specific Function
- Responsible for the metabolism of many drugs and environmental chemicals that it oxidizes. It is involved in the metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic...
- Gene Name
- CYP2D6
- Uniprot ID
- P10635
- Uniprot Name
- Cytochrome P450 2D6
- Molecular Weight
- 55768.94 Da
References
- FDA Approved Drug Products: Trikafta (elexacaftor, tezacaftor and ivacaftor tablets; ivacaftor tablets) [Link]
Carriers
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- 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
- FDA Approved Drug Products: Trikafta (elexacaftor, tezacaftor and ivacaftor tablets; ivacaftor tablets) [Link]
Transporters
- 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
- FDA Approved Drug Products: Trikafta (elexacaftor, tezacaftor and ivacaftor tablets; ivacaftor tablets) [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 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: Trikafta (elexacaftor, tezacaftor and ivacaftor tablets; ivacaftor tablets) [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- SubstrateInhibitor
- 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: Trikafta (elexacaftor, tezacaftor and ivacaftor tablets; ivacaftor tablets) [Link]
Drug created at May 20, 2019 15:32 / Updated at May 13, 2023 04:08