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Identification
NameIvacaftor
Accession NumberDB08820  (DB05989)
TypeSmall Molecule
GroupsApproved
Description

Ivacaftor (also known as Kalydeco or VX-770) is a drug for the treatment of cystic fibrosis, developed by Vertex Pharmaceuticals and the Cystic Fibrosis Foundation. FDA approved on January 31, 2012.

Structure
Thumb
Synonyms
Ivacaftorum
Kalydeco
External Identifiers
  • VX-770
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Kalydecotablet, film coated150 mg/1oralVertex Pharmaceuticals Incorporated2012-01-31Not applicableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Kalydecogranules75 mgoralVertex Pharmaceuticals (Canada) Incorporated2015-09-14Not applicableCanada 5f16b84899037e23705f146ff57e3794121879cb055f0954756d94bc690476b4
Kalydecogranules50 mgoralVertex Pharmaceuticals (Canada) Incorporated2015-09-14Not applicableCanada 5f16b84899037e23705f146ff57e3794121879cb055f0954756d94bc690476b4
Kalydecotablet150 mgoralVertex Pharmaceuticals (Canada) Incorporated2012-11-27Not applicableCanada 5f16b84899037e23705f146ff57e3794121879cb055f0954756d94bc690476b4
Kalydecogranule75 mg/1oralVertex Pharmaceuticals Incorporated2015-03-23Not applicableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Kalydecogranule50 mg/1oralVertex Pharmaceuticals Incorporated2015-03-23Not applicableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Generic Prescription ProductsNot Available
Over the Counter ProductsNot Available
International BrandsNot Available
Brand mixtures
NameLabellerIngredients
OrkambiVertex Pharmaceuticals Incorporated
SaltsNot Available
CategoriesNot Available
CAS number873054-44-5
WeightAverage: 392.4907
Monoisotopic: 392.209992772
Chemical FormulaC24H28N2O3
InChI KeyInChIKey=PURKAOJPTOLRMP-UHFFFAOYSA-N
InChI
InChI=1S/C24H28N2O3/c1-23(2,3)16-11-17(24(4,5)6)20(27)12-19(16)26-22(29)15-13-25-18-10-8-7-9-14(18)21(15)28/h7-13,27H,1-6H3,(H,25,28)(H,26,29)
IUPAC Name
N-(2,4-di-tert-butyl-5-hydroxyphenyl)-4-oxo-1,4-dihydroquinoline-3-carboxamide
SMILES
CC(C)(C)C1=CC(=C(O)C=C1NC(=O)C1=CNC2=CC=CC=C2C1=O)C(C)(C)C
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as quinoline-3-carboxamides. These are quinolines in which the quinoline ring system is substituted by one carboxamide group at the 3-position.
KingdomOrganic compounds
Super ClassOrganoheterocyclic compounds
ClassQuinolines and derivatives
Sub ClassQuinoline carboxamides
Direct ParentQuinoline-3-carboxamides
Alternative Parents
Substituents
  • Quinoline-3-carboxamide
  • Dihydroquinolone
  • N-arylamide
  • Dihydroquinoline
  • Pyridine carboxylic acid or derivatives
  • Phenylpropane
  • Phenol
  • Benzenoid
  • Pyridine
  • Monocyclic benzene moiety
  • Heteroaromatic compound
  • Vinylogous amide
  • Secondary carboxylic acid amide
  • Carboxamide group
  • Azacycle
  • Carboxylic acid derivative
  • Hydrocarbon derivative
  • Organooxygen compound
  • Organonitrogen compound
  • Carbonyl group
  • Aromatic heteropolycyclic compound
Molecular FrameworkAromatic heteropolycyclic compounds
External Descriptors
Pharmacology
IndicationFor the treatment of cystic fibrosis (CF) in patients age 6 years and older who have a G551D mutation in the CFTR gene.
PharmacodynamicsIvacaftor is a cystic fibrosis transmembrane conductance regulator (CFTR). In patients with the G551D mutation, Kalydeco, a pill taken two times a day with fat-containing food, helps the protein made by the CFTR gene function better and as a result, improves lung function and other aspects of CF such as increasing weight gain.
Mechanism of actionCystic fibrosis is caused by any one of several defects in a protein, cystic fibrosis transmembrane conductance regulator, which regulates fluid flow within cells and affects the components of sweat, digestive fluids, and mucus. The defect, which is caused by a mutation in the individual's DNA, can be in any of several locations along the protein, each of which interferes with a different function of the protein. One mutation, G551D, lets the CFTR protein reach the epithelial cell surface, but doesn't let it transport chloride through the ion channel. Ivacaftor is a potentiator of the CFTR protein. The CFTR protein is a chloride channel present at the surface of epithelial cells in multiple organs. Ivacaftor facilitates increased chloride transport by potentiating the channel-open probability (or gating) of the G551D-CFTR protein.
AbsorptionThe pharmacokinetics of ivacaftor is similar between healthy adult volunteers and patients with CF. When given a single oral dose of 150 mg to healthy subjects, the parameters were as follows: Tmax = 4 hours; Cmax = 768 ng/mL; AUC = 10600 ng*hr/mL; Time to steady state, 12 hour dosing = 3-5 days Following repeated doses for ivacaftor, accumulation occurs. When given with a fatty meal, exposure increases 2-4 fold.
Volume of distribution

The mean apparent volume of distribution (Vz/F) of ivacaftor after a single dose of 275 mg of Ivacaftor in the fed state was similar for healthy subjects and patients with CF. After oral administration of 150 mg every 12 hours for 7 days to healthy volunteers in a fed state, the mean (±SD) for apparent volume of distribution was 353 (122) L.

Protein bindingIvacaftor is approximately 99% bound to plasma proteins, primarily to alpha 1-acid glycoprotein and albumin. Ivacaftor does not bind to human red blood cells.
Metabolism

Ivacaftor is extensively metabolized in humans. In vitro and clinical studies indicate that ivacaftor is primarily metabolized by CYP3A. M1 and M6 are the two major metabolites of ivacaftor in humans. M1 has approximately one-sixth the potency of ivacaftor and is considered pharmacologically active. M6 has less than one-fiftieth the potency of ivacaftor and is not considered pharmacologically active.

Route of eliminationFollowing oral administration, the majority of ivacaftor (87.8%) is eliminated in the feces after metabolic conversion. The major metabolites M1 and M6 accounted for approximately 65% of the total dose eliminated with 22% as M1 and 43% as M6. There was negligible urinary excretion of ivacaftor as unchanged parent.
Half life12 hours following a single dose
Clearance

The CL/F (SD) for the 150 mg dose was 17.3 (8.4) L/hr in healthy subjects.

ToxicityThere have been no reports of overdose with Ivacaftor. The highest single dose used in a clinical study was 800 mg in a solution formulation without any treatment-related adverse events.
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated Effects
Interacting Gene/EnzymeSNP RS IDAllele nameDefining changeEffectReference(s)
Cystic fibrosis transmembrane conductance regulator
Gene symbol: CFTR
UniProt: P13569
rs75527207 Not AvailableA allele (G > A)Cystic Fibrosis patients with the A allele will response to ivacaftor23757359
Cystic fibrosis transmembrane conductance regulator
Gene symbol: CFTR
UniProt: P13569
rs75527207 Not AvailableA allele (G > A)Cystic Fibrosis patients with the A allele will response to ivacaftor23891399
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9577
Blood Brain Barrier+0.6561
Caco-2 permeable-0.5608
P-glycoprotein substrateNon-substrate0.5474
P-glycoprotein inhibitor INon-inhibitor0.7677
P-glycoprotein inhibitor IINon-inhibitor0.7609
Renal organic cation transporterNon-inhibitor0.945
CYP450 2C9 substrateNon-substrate0.7374
CYP450 2D6 substrateNon-substrate0.8362
CYP450 3A4 substrateSubstrate0.5686
CYP450 1A2 substrateInhibitor0.5438
CYP450 2C9 inhibitorInhibitor0.6456
CYP450 2D6 inhibitorNon-inhibitor0.9469
CYP450 2C19 inhibitorNon-inhibitor0.6422
CYP450 3A4 inhibitorNon-inhibitor0.8404
CYP450 inhibitory promiscuityHigh CYP Inhibitory Promiscuity0.5791
Ames testNon AMES toxic0.8394
CarcinogenicityNon-carcinogens0.8149
BiodegradationNot ready biodegradable1.0
Rat acute toxicity2.2868 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9961
hERG inhibition (predictor II)Non-inhibitor0.819
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
ManufacturersNot Available
PackagersNot Available
Dosage forms
FormRouteStrength
Granuleoral50 mg/1
Granuleoral75 mg/1
Granulesoral50 mg
Granulesoral75 mg
Tabletoral150 mg
Tablet, film coatedoral150 mg/1
Tablet, film coatedoral
PricesNot Available
Patents
CountryPatent NumberApprovedExpires (estimated)
United States74951032012-01-312027-05-20
United States83242422012-01-312027-04-18
United States84102742012-01-312026-12-28
Properties
StateSolid
Experimental Properties
PropertyValueSource
water solubilityInsoluble (<0.05 µg/mL)FDA label
Predicted Properties
PropertyValueSource
Water Solubility0.002 mg/mLALOGPS
logP5ALOGPS
logP5.76ChemAxon
logS-5.3ALOGPS
pKa (Strongest Acidic)6.57ChemAxon
pKa (Strongest Basic)-0.95ChemAxon
Physiological Charge-1ChemAxon
Hydrogen Acceptor Count4ChemAxon
Hydrogen Donor Count3ChemAxon
Polar Surface Area78.43 Å2ChemAxon
Rotatable Bond Count4ChemAxon
Refractivity118.68 m3·mol-1ChemAxon
Polarizability43.04 Å3ChemAxon
Number of Rings3ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
SpectraNot Available
References
Synthesis ReferenceNot Available
General References
  1. Accurso FJ, Rowe SM, Clancy JP, Boyle MP, Dunitz JM, Durie PR, Sagel SD, Hornick DB, Konstan MW, Donaldson SH, Moss RB, Pilewski JM, Rubenstein RC, Uluer AZ, Aitken ML, Freedman SD, Rose LM, Mayer-Hamblett N, Dong Q, Zha J, Stone AJ, Olson ER, Ordonez CL, Campbell PW, Ashlock MA, Ramsey BW: Effect of VX-770 in persons with cystic fibrosis and the G551D-CFTR mutation. N Engl J Med. 2010 Nov 18;363(21):1991-2003. Pubmed
  2. Ramsey BW, Davies J, McElvaney NG, Tullis E, Bell SC, Drevinek P, Griese M, McKone EF, Wainwright CE, Konstan MW, Moss R, Ratjen F, Sermet-Gaudelus I, Rowe SM, Dong Q, Rodriguez S, Yen K, Ordonez C, Elborn JS: A CFTR potentiator in patients with cystic fibrosis and the G551D mutation. N Engl J Med. 2011 Nov 3;365(18):1663-72. Pubmed
External Links
ATC CodesR07AX02
AHFS Codes
  • 48:92
PDB EntriesNot Available
FDA labelDownload (239 KB)
MSDSDownload (353 KB)
Interactions
Drug Interactions
Drug
ado-trastuzumab emtansineThe serum concentration of ado-trastuzumab emtansine can be increased when it is combined with Ivacaftor.
AfatinibThe serum concentration of Afatinib can be increased when it is combined with Ivacaftor.
AlfentanilThe serum concentration of Alfentanil can be increased when it is combined with Ivacaftor.
AlfuzosinThe serum concentration of Alfuzosin can be increased when it is combined with Ivacaftor.
AlitretinoinThe serum concentration of Alitretinoin can be increased when it is combined with Ivacaftor.
AlprazolamThe serum concentration of Alprazolam can be increased when it is combined with Ivacaftor.
AminophyllineThe serum concentration of Aminophylline can be increased when it is combined with Ivacaftor.
AmiodaroneThe serum concentration of Amiodarone can be increased when it is combined with Ivacaftor.
AmlodipineThe serum concentration of Amlodipine can be increased when it is combined with Ivacaftor.
AmodiaquineThe serum concentration of Amodiaquine can be increased when it is combined with Ivacaftor.
AprepitantThe serum concentration of Ivacaftor can be increased when it is combined with Aprepitant.
AripiprazoleThe serum concentration of Aripiprazole can be increased when it is combined with Ivacaftor.
ArmodafinilThe serum concentration of Armodafinil can be increased when it is combined with Ivacaftor.
AtazanavirThe serum concentration of Ivacaftor can be increased when it is combined with Atazanavir.
AtorvastatinThe serum concentration of Atorvastatin can be increased when it is combined with Ivacaftor.
AvanafilThe serum concentration of Avanafil can be increased when it is combined with Ivacaftor.
AxitinibThe serum concentration of Axitinib can be increased when it is combined with Ivacaftor.
BenzphetamineThe serum concentration of Benzphetamine can be increased when it is combined with Ivacaftor.
BexaroteneThe serum concentration of Ivacaftor can be decreased when it is combined with Bexarotene.
BisoprololThe serum concentration of Bisoprolol can be increased when it is combined with Ivacaftor.
BoceprevirThe serum concentration of Ivacaftor can be increased when it is combined with Boceprevir.
BosentanThe serum concentration of Ivacaftor can be decreased when it is combined with Bosentan.
BosutinibThe serum concentration of Bosutinib can be increased when it is combined with Ivacaftor.
Brentuximab vedotinThe serum concentration of Brentuximab vedotin can be increased when it is combined with Ivacaftor.
BrexpiprazoleThe serum concentration of Brexpiprazole can be increased when it is combined with Ivacaftor.
BromocriptineThe serum concentration of Bromocriptine can be increased when it is combined with Ivacaftor.
BudesonideThe serum concentration of Budesonide can be increased when it is combined with Ivacaftor.
BuprenorphineThe serum concentration of Buprenorphine can be increased when it is combined with Ivacaftor.
BuspironeThe serum concentration of Buspirone can be increased when it is combined with Ivacaftor.
CabazitaxelThe serum concentration of Cabazitaxel can be increased when it is combined with Ivacaftor.
CabozantinibThe serum concentration of Cabozantinib can be increased when it is combined with Ivacaftor.
CalcitriolThe serum concentration of Calcitriol can be increased when it is combined with Ivacaftor.
CarbamazepineThe serum concentration of Ivacaftor can be decreased when it is combined with Carbamazepine.
CeritinibThe serum concentration of Ivacaftor can be increased when it is combined with Ceritinib.
ChlordiazepoxideThe serum concentration of Chlordiazepoxide can be increased when it is combined with Ivacaftor.
ChloroquineThe serum concentration of Chloroquine can be increased when it is combined with Ivacaftor.
CilostazolThe serum concentration of Cilostazol can be increased when it is combined with Ivacaftor.
CinacalcetThe serum concentration of Cinacalcet can be increased when it is combined with Ivacaftor.
CisaprideThe serum concentration of Cisapride can be increased when it is combined with Ivacaftor.
CitalopramThe serum concentration of Citalopram can be increased when it is combined with Ivacaftor.
ClarithromycinThe serum concentration of Ivacaftor can be increased when it is combined with Clarithromycin.
ClonazepamThe serum concentration of Clonazepam can be increased when it is combined with Ivacaftor.
ClorazepateThe serum concentration of Clorazepate can be increased when it is combined with Ivacaftor.
CobicistatThe serum concentration of Ivacaftor can be increased when it is combined with Cobicistat.
CobimetinibThe serum concentration of Cobimetinib can be increased when it is combined with Ivacaftor.
CocaineThe serum concentration of Cocaine can be increased when it is combined with Ivacaftor.
ColchicineThe serum concentration of Colchicine can be increased when it is combined with Ivacaftor.
ConivaptanThe serum concentration of Ivacaftor can be increased when it is combined with Conivaptan.
CrizotinibThe serum concentration of Ivacaftor can be increased when it is combined with Crizotinib.
CyclosporineThe serum concentration of Cyclosporine can be increased when it is combined with Ivacaftor.
Cyproterone acetateThe serum concentration of Cyproterone acetate can be increased when it is combined with Ivacaftor.
Dabigatran etexilateThe serum concentration of the active metabolites of Dabigatran etexilate can be increased when Dabigatran etexilate is used in combination with Ivacaftor.
DabrafenibThe serum concentration of Ivacaftor can be decreased when it is combined with Dabrafenib.
DaclatasvirThe serum concentration of Daclatasvir can be increased when it is combined with Ivacaftor.
DantroleneThe serum concentration of Dantrolene can be increased when it is combined with Ivacaftor.
DapsoneThe serum concentration of Dapsone can be increased when it is combined with Ivacaftor.
DarifenacinThe serum concentration of Darifenacin can be increased when it is combined with Ivacaftor.
DarunavirThe serum concentration of Ivacaftor can be increased when it is combined with Darunavir.
DasatinibThe serum concentration of Dasatinib can be increased when it is combined with Ivacaftor.
DeferasiroxThe serum concentration of Ivacaftor can be decreased when it is combined with Deferasirox.
DelavirdineThe serum concentration of Ivacaftor can be increased when it is combined with Delavirdine.
DexamethasoneThe serum concentration of Dexamethasone can be increased when it is combined with Ivacaftor.
DiazepamThe serum concentration of Diazepam can be increased when it is combined with Ivacaftor.
DihydroergotamineThe serum concentration of Dihydroergotamine can be increased when it is combined with Ivacaftor.
DiltiazemThe serum concentration of Ivacaftor can be increased when it is combined with Diltiazem.
DisopyramideThe serum concentration of Disopyramide can be increased when it is combined with Ivacaftor.
DocetaxelThe serum concentration of Docetaxel can be increased when it is combined with Ivacaftor.
DofetilideThe serum concentration of Dofetilide can be increased when it is combined with Ivacaftor.
DomperidoneThe serum concentration of Domperidone can be increased when it is combined with Ivacaftor.
DoxazosinThe serum concentration of Doxazosin can be increased when it is combined with Ivacaftor.
DoxorubicinThe serum concentration of Doxorubicin can be increased when it is combined with Ivacaftor.
DronedaroneThe serum concentration of Ivacaftor can be increased when it is combined with Dronedarone.
EdoxabanThe serum concentration of Edoxaban can be increased when it is combined with Ivacaftor.
EletriptanThe serum concentration of Eletriptan can be increased when it is combined with Ivacaftor.
EliglustatThe serum concentration of Eliglustat can be increased when it is combined with Ivacaftor.
EnzalutamideThe serum concentration of Ivacaftor can be decreased when it is combined with Enzalutamide.
EplerenoneThe serum concentration of Eplerenone can be increased when it is combined with Ivacaftor.
Ergoloid mesylateThe serum concentration of Ergoloid mesylate can be increased when it is combined with Ivacaftor.
ErgonovineThe serum concentration of Ergonovine can be increased when it is combined with Ivacaftor.
ErgotamineThe serum concentration of Ergotamine can be increased when it is combined with Ivacaftor.
ErlotinibThe serum concentration of Erlotinib can be increased when it is combined with Ivacaftor.
ErythromycinThe serum concentration of Ivacaftor can be increased when it is combined with Erythromycin.
EscitalopramThe serum concentration of Escitalopram can be increased when it is combined with Ivacaftor.
EszopicloneThe serum concentration of Eszopiclone can be increased when it is combined with Ivacaftor.
EthosuximideThe serum concentration of Ethosuximide can be increased when it is combined with Ivacaftor.
EtoposideThe serum concentration of Etoposide can be increased when it is combined with Ivacaftor.
EverolimusThe serum concentration of Everolimus can be increased when it is combined with Ivacaftor.
FelbamateThe serum concentration of Felbamate can be increased when it is combined with Ivacaftor.
FelodipineThe serum concentration of Felodipine can be increased when it is combined with Ivacaftor.
FentanylThe serum concentration of Fentanyl can be increased when it is combined with Ivacaftor.
FesoterodineThe serum concentration of Fesoterodine can be increased when it is combined with Ivacaftor.
FlibanserinThe serum concentration of Flibanserin can be increased when it is combined with Ivacaftor.
FluconazoleThe serum concentration of Ivacaftor can be increased when it is combined with Fluconazole.
FlunisolideThe serum concentration of Flunisolide can be increased when it is combined with Ivacaftor.
FlurazepamThe serum concentration of Flurazepam can be increased when it is combined with Ivacaftor.
FlutamideThe serum concentration of Flutamide can be increased when it is combined with Ivacaftor.
FosamprenavirThe serum concentration of Ivacaftor can be increased when it is combined with Fosamprenavir.
FosaprepitantThe serum concentration of Fosaprepitant can be increased when it is combined with Ivacaftor.
FosphenytoinThe serum concentration of Ivacaftor can be decreased when it is combined with Fosphenytoin.
Fusidic AcidThe serum concentration of Ivacaftor can be increased when it is combined with Fusidic Acid.
GefitinibThe serum concentration of Gefitinib can be increased when it is combined with Ivacaftor.
GuanfacineThe serum concentration of Guanfacine can be increased when it is combined with Ivacaftor.
HaloperidolThe serum concentration of Haloperidol can be increased when it is combined with Ivacaftor.
HydrocodoneThe serum concentration of Hydrocodone can be increased when it is combined with Ivacaftor.
Hydroxyprogesterone caproateThe serum concentration of Hydroxyprogesterone caproate can be increased when it is combined with Ivacaftor.
IbrutinibThe serum concentration of Ibrutinib can be increased when it is combined with Ivacaftor.
IdelalisibThe serum concentration of Ivacaftor can be increased when it is combined with Idelalisib.
ImatinibThe serum concentration of Ivacaftor can be increased when it is combined with Imatinib.
IndinavirThe serum concentration of Ivacaftor can be increased when it is combined with Indinavir.
IrinotecanThe serum concentration of Irinotecan can be increased when it is combined with Ivacaftor.
IsavuconazoniumThe serum concentration of Ivacaftor can be increased when it is combined with Isavuconazonium.
IsosorbideThe serum concentration of Isosorbide can be increased when it is combined with Ivacaftor.
Isosorbide DinitrateThe serum concentration of Isosorbide Dinitrate can be increased when it is combined with Ivacaftor.
Isosorbide MononitrateThe serum concentration of Isosorbide Mononitrate can be increased when it is combined with Ivacaftor.
IsradipineThe serum concentration of Isradipine can be increased when it is combined with Ivacaftor.
ItraconazoleThe serum concentration of Ivacaftor can be increased when it is combined with Itraconazole.
IvabradineThe serum concentration of Ivabradine can be increased when it is combined with Ivacaftor.
IxabepiloneThe serum concentration of Ixabepilone can be increased when it is combined with Ivacaftor.
KetamineThe serum concentration of Ketamine can be increased when it is combined with Ivacaftor.
KetoconazoleThe serum concentration of Ivacaftor can be increased when it is combined with Ketoconazole.
LapatinibThe serum concentration of Lapatinib can be increased when it is combined with Ivacaftor.
LedipasvirThe serum concentration of Ledipasvir can be increased when it is combined with Ivacaftor.
LevomilnacipranThe serum concentration of Levomilnacipran can be increased when it is combined with Ivacaftor.
LidocaineThe serum concentration of Lidocaine can be increased when it is combined with Ivacaftor.
LomitapideThe serum concentration of Lomitapide can be increased when it is combined with Ivacaftor.
LovastatinThe serum concentration of Lovastatin can be increased when it is combined with Ivacaftor.
LuliconazoleThe serum concentration of Ivacaftor can be increased when it is combined with Luliconazole.
LurasidoneThe serum concentration of Lurasidone can be increased when it is combined with Ivacaftor.
MACITENTANThe serum concentration of MACITENTAN can be increased when it is combined with Ivacaftor.
MaravirocThe serum concentration of Maraviroc can be increased when it is combined with Ivacaftor.
MefloquineThe serum concentration of Mefloquine can be increased when it is combined with Ivacaftor.
MethadoneThe serum concentration of Methadone can be increased when it is combined with Ivacaftor.
MidazolamThe serum concentration of Midazolam can be increased when it is combined with Ivacaftor.
MifepristoneThe serum concentration of Ivacaftor can be increased when it is combined with Mifepristone.
MirtazapineThe serum concentration of Mirtazapine can be increased when it is combined with Ivacaftor.
MitotaneThe serum concentration of Ivacaftor can be decreased when it is combined with Mitotane.
ModafinilThe serum concentration of Modafinil can be increased when it is combined with Ivacaftor.
NaloxegolThe serum concentration of Naloxegol can be increased when it is combined with Ivacaftor.
NateglinideThe serum concentration of Nateglinide can be increased when it is combined with Ivacaftor.
NefazodoneThe serum concentration of Ivacaftor can be increased when it is combined with Nefazodone.
NelfinavirThe serum concentration of Ivacaftor can be increased when it is combined with Nelfinavir.
NicardipineThe serum concentration of Nicardipine can be increased when it is combined with Ivacaftor.
NifedipineThe serum concentration of Nifedipine can be increased when it is combined with Ivacaftor.
NilotinibThe serum concentration of Ivacaftor can be increased when it is combined with Nilotinib.
NimodipineThe serum concentration of Nimodipine can be increased when it is combined with Ivacaftor.
NisoldipineThe serum concentration of Nisoldipine can be increased when it is combined with Ivacaftor.
OlaparibThe serum concentration of Olaparib can be increased when it is combined with Ivacaftor.
OxycodoneThe serum concentration of Oxycodone can be increased when it is combined with Ivacaftor.
PaclitaxelThe serum concentration of Paclitaxel can be increased when it is combined with Ivacaftor.
PalbociclibThe serum concentration of Ivacaftor can be increased when it is combined with Palbociclib.
PanobinostatThe serum concentration of Panobinostat can be increased when it is combined with Ivacaftor.
PazopanibThe serum concentration of Pazopanib can be increased when it is combined with Ivacaftor.
PhenobarbitalThe serum concentration of Ivacaftor can be decreased when it is combined with Phenobarbital.
PhenytoinThe serum concentration of Ivacaftor can be decreased when it is combined with Phenytoin.
PimozideThe serum concentration of Pimozide can be increased when it is combined with Ivacaftor.
PipotiazineThe serum concentration of Pipotiazine can be increased when it is combined with Ivacaftor.
PosaconazoleThe serum concentration of Ivacaftor can be increased when it is combined with Posaconazole.
PraziquantelThe serum concentration of Praziquantel can be increased when it is combined with Ivacaftor.
PrimidoneThe serum concentration of Ivacaftor can be decreased when it is combined with Primidone.
PrucaloprideThe serum concentration of Prucalopride can be increased when it is combined with Ivacaftor.
QuetiapineThe serum concentration of Quetiapine can be increased when it is combined with Ivacaftor.
QuinidineThe serum concentration of Quinidine can be increased when it is combined with Ivacaftor.
QuinineThe serum concentration of Quinine can be increased when it is combined with Ivacaftor.
RanolazineThe serum concentration of Ranolazine can be increased when it is combined with Ivacaftor.
RegorafenibThe serum concentration of Regorafenib can be increased when it is combined with Ivacaftor.
RifabutinThe serum concentration of Ivacaftor can be decreased when it is combined with Rifabutin.
RifampicinThe serum concentration of Ivacaftor can be decreased when it is combined with Rifampicin.
RifapentineThe serum concentration of Ivacaftor can be decreased when it is combined with Rifapentine.
RifaximinThe serum concentration of Rifaximin can be increased when it is combined with Ivacaftor.
RitonavirThe serum concentration of Ivacaftor can be increased when it is combined with Ritonavir.
RuxolitinibThe serum concentration of Ruxolitinib can be increased when it is combined with Ivacaftor.
SalmeterolThe serum concentration of Salmeterol can be increased when it is combined with Ivacaftor.
SaquinavirThe serum concentration of Ivacaftor can be increased when it is combined with Saquinavir.
SaxagliptinThe serum concentration of Saxagliptin can be increased when it is combined with Ivacaftor.
SildenafilThe serum concentration of Sildenafil can be increased when it is combined with Ivacaftor.
SilodosinThe serum concentration of Silodosin can be increased when it is combined with Ivacaftor.
SiltuximabThe serum concentration of Ivacaftor can be decreased when it is combined with Siltuximab.
SimeprevirThe serum concentration of Simeprevir can be increased when it is combined with Ivacaftor.
SimvastatinThe serum concentration of Simvastatin can be increased when it is combined with Ivacaftor.
SirolimusThe serum concentration of Sirolimus can be increased when it is combined with Ivacaftor.
SolifenacinThe serum concentration of Solifenacin can be increased when it is combined with Ivacaftor.
SonidegibThe serum concentration of Sonidegib can be increased when it is combined with Ivacaftor.
SpiramycinThe serum concentration of Spiramycin can be increased when it is combined with Ivacaftor.
St. John's WortThe serum concentration of Ivacaftor can be decreased when it is combined with St. John&#39;s Wort.
StiripentolThe serum concentration of Ivacaftor can be increased when it is combined with Stiripentol.
SufentanilThe serum concentration of Sufentanil can be increased when it is combined with Ivacaftor.
SunitinibThe serum concentration of Sunitinib can be increased when it is combined with Ivacaftor.
SuvorexantThe serum concentration of Suvorexant can be increased when it is combined with Ivacaftor.
TacrolimusThe serum concentration of Tacrolimus can be increased when it is combined with Ivacaftor.
TadalafilThe serum concentration of Tadalafil can be increased when it is combined with Ivacaftor.
TamoxifenThe serum concentration of Tamoxifen can be increased when it is combined with Ivacaftor.
TamsulosinThe serum concentration of Tamsulosin can be increased when it is combined with Ivacaftor.
TelaprevirThe serum concentration of Ivacaftor can be increased when it is combined with Telaprevir.
TelithromycinThe serum concentration of Ivacaftor can be increased when it is combined with Telithromycin.
TemsirolimusThe serum concentration of Temsirolimus can be increased when it is combined with Ivacaftor.
TeniposideThe serum concentration of Teniposide can be increased when it is combined with Ivacaftor.
TheophyllineThe serum concentration of Theophylline can be increased when it is combined with Ivacaftor.
TiagabineThe serum concentration of Tiagabine can be increased when it is combined with Ivacaftor.
TocilizumabThe serum concentration of Ivacaftor can be decreased when it is combined with Tocilizumab.
TofacitinibThe serum concentration of Tofacitinib can be increased when it is combined with Ivacaftor.
TolterodineThe serum concentration of Tolterodine can be increased when it is combined with Ivacaftor.
TolvaptanThe serum concentration of Tolvaptan can be increased when it is combined with Ivacaftor.
TopotecanThe serum concentration of Topotecan can be increased when it is combined with Ivacaftor.
TrabectedinThe serum concentration of Trabectedin can be increased when it is combined with Ivacaftor.
TrazodoneThe serum concentration of Trazodone can be increased when it is combined with Ivacaftor.
TriazolamThe serum concentration of Triazolam can be increased when it is combined with Ivacaftor.
TrimipramineThe serum concentration of Trimipramine can be increased when it is combined with Ivacaftor.
VardenafilThe serum concentration of Vardenafil can be increased when it is combined with Ivacaftor.
VemurafenibThe serum concentration of Vemurafenib can be increased when it is combined with Ivacaftor.
VenlafaxineThe serum concentration of Venlafaxine can be increased when it is combined with Ivacaftor.
VerapamilThe serum concentration of Ivacaftor can be increased when it is combined with Verapamil.
VinblastineThe serum concentration of Vinblastine can be increased when it is combined with Ivacaftor.
VincristineThe serum concentration of Vincristine can be increased when it is combined with Ivacaftor.
VinorelbineThe serum concentration of Vinorelbine can be increased when it is combined with Ivacaftor.
VoriconazoleThe serum concentration of Ivacaftor can be increased when it is combined with Voriconazole.
ZolpidemThe serum concentration of Zolpidem can be increased when it is combined with Ivacaftor.
ZonisamideThe serum concentration of Zonisamide can be increased when it is combined with Ivacaftor.
ZopicloneThe serum concentration of Zopiclone can be increased when it is combined with Ivacaftor.
Food Interactions
  • Exposure increases 2- to 4- fold when given with a high fat meal. It is recommended that ivacaftor be given this way.

Targets

1. Cystic fibrosis transmembrane conductance regulator

Kind: Protein

Organism: Human

Pharmacological action: yes

Actions: potentiator

Components

Name UniProt ID Details
Cystic fibrosis transmembrane conductance regulator P13569 Details

References:

  1. 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 Jan 30. Pubmed

Enzymes

1. Cytochrome P450 3A4

Kind: Protein

Organism: Human

Pharmacological action: unknown

Actions: substrate inhibitor

Components

Name UniProt ID Details
Cytochrome P450 3A4 P08684 Details

References:

  1. FDA Label

Carriers

1. Serum albumin

Kind: Protein

Organism: Human

Pharmacological action: unknown

Actions: substrate

Components

Name UniProt ID Details
Serum albumin P02768 Details

References:

  1. FDA label

2. Alpha-1-acid glycoprotein 1

Kind: Protein

Organism: Human

Pharmacological action: unknown

Actions: substrate

Components

Name UniProt ID Details
Alpha-1-acid glycoprotein 1 P02763 Details

References:

  1. FDA label

Transporters

1. Multidrug resistance protein 1

Kind: Protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
Multidrug resistance protein 1 P08183 Details

References:

  1. FDA Label

Comments
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Drug created on February 24, 2012 11:15 / Updated on October 29, 2015 09:41