General Information of Drug (ID: DMZC1HS)

Drug Name
Ivacaftor
Synonyms Kalydeco (TN)
Indication
Disease Entry ICD 11 Status REF
Cystic fibrosis CA25 Approved [1], [2], [3]
Drug Type
Small molecular drug
Structure
3D MOL 2D MOL
#Ro5 Violations (Lipinski): 1 Molecular Weight (mw) 392.5
Topological Polar Surface Area (xlogp) 5.6
Rotatable Bond Count (rotbonds) 4
Hydrogen Bond Donor Count (hbonddonor) 3
Hydrogen Bond Acceptor Count (hbondacc) 4
ADMET Property
Absorption AUC
The area under the plot of plasma concentration (AUC) of drug is 10600 mcgh/L [4]
Absorption Cmax
The maximum plasma concentration (Cmax) of drug is 768 mcg/L [4]
Absorption Tmax
The time to maximum plasma concentration (Tmax) is 4 h [4]
BDDCS Class
Biopharmaceutics Drug Disposition Classification System (BDDCS) Class 2: low solubility and high permeability [5]
Clearance
The clearance of drug is 17.3 L/h in healthy subjects [6]
Elimination
After oral administration, ivacaftor is mainly eliminated in the feces after metabolic conversion and this elimination represents 87.8% of the dose [4]
Half-life
The concentration or amount of drug in body reduced by one-half in 12 hours [6]
Metabolism
The drug is metabolized via the CYP3A [4]
Vd
The volume of distribution (Vd) of drug is 353 L [6]
Chemical Identifiers
Formula
C24H28N2O3
IUPAC Name
N-(2,4-ditert-butyl-5-hydroxyphenyl)-4-oxo-1H-quinoline-3-carboxamide
Canonical SMILES
CC(C)(C)C1=CC(=C(C=C1NC(=O)C2=CNC3=CC=CC=C3C2=O)O)C(C)(C)C
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)
InChIKey
PURKAOJPTOLRMP-UHFFFAOYSA-N
Cross-matching ID
PubChem CID
16220172
ChEBI ID
CHEBI:66901
CAS Number
873054-44-5
DrugBank ID
DB08820
TTD ID
D0W7WC
VARIDT ID
DR00466
INTEDE ID
DR0898
ACDINA ID
D00339

Molecular Interaction Atlas of This Drug


Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
cAMP-dependent chloride channel (CFTR) TTRLZHP CFTR_HUMAN Modulator [7]

Drug Transporter (DTP)
DTP Name DTP ID UniProt ID MOA REF
P-glycoprotein 1 (ABCB1) DTUGYRD MDR1_HUMAN Substrate [8]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID MOA REF
Cytochrome P450 3A4 (CYP3A4)
Main DME
DE4LYSA CP3A4_HUMAN Substrate [9]
Cytochrome P450 3A5 (CYP3A5) DEIBDNY CP3A5_HUMAN Substrate [9]
Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This Drug

Drug-Drug Interaction (DDI) Information of This Drug

Coadministration of a Drug Treating the Disease Different from Ivacaftor (Comorbidity)
DDI Drug Name DDI Drug ID Severity Mechanism Comorbidity REF
Remdesivir DMBFZ6L Moderate Increased risk of hepatotoxicity by the combination of Ivacaftor and Remdesivir. 1D6YCoronavirus Disease 2019 [1D6YCoronavirus Disease 2019] [39]
Metreleptin DM1NOEK Moderate Increased metabolism of Ivacaftor caused by Metreleptin mediated induction of CYP450 enzyme. Acute diabete complication [5A2Y] [40]
Ivosidenib DM8S6T7 Moderate Increased metabolism of Ivacaftor caused by Ivosidenib mediated induction of CYP450 enzyme. Acute myeloid leukaemia [2A60] [40]
Arn-509 DMT81LZ Major Increased metabolism of Ivacaftor caused by Arn-509 mediated induction of CYP450 enzyme. Acute myeloid leukaemia [2A60] [39]
Gilteritinib DMWQ4MZ Moderate Decreased metabolism of Ivacaftor caused by Gilteritinib mediated inhibition of CYP450 enzyme. Acute myeloid leukaemia [2A60] [41]
Ivabradine DM0L594 Moderate Decreased metabolism of Ivacaftor caused by Ivabradine mediated inhibition of CYP450 enzyme. Angina pectoris [BA40] [41]
Bedaquiline DM3906J Moderate Increased risk of hepatotoxicity by the combination of Ivacaftor and Bedaquiline. Antimicrobial drug resistance [MG50-MG52] [42]
Troleandomycin DMUZNIG Major Decreased metabolism of Ivacaftor caused by Troleandomycin mediated inhibition of CYP450 enzyme. Bacterial infection [1A00-1C4Z] [39]
Erdafitinib DMI782S Moderate Increased metabolism of Ivacaftor caused by Erdafitinib mediated induction of CYP450 enzyme. Bladder cancer [2C94] [43]
Pexidartinib DMS2J0Z Major Increased risk of hepatotoxicity by the combination of Ivacaftor and Pexidartinib. Bone/articular cartilage neoplasm [2F7B] [44]
Talazoparib DM1KS78 Moderate Decreased clearance of Ivacaftor due to the transporter inhibition by Talazoparib. Breast cancer [2C60-2C6Y] [45]
Tucatinib DMBESUA Major Decreased metabolism of Ivacaftor caused by Tucatinib mediated inhibition of CYP450 enzyme. Breast cancer [2C60-2C6Y] [39]
Palbociclib DMD7L94 Moderate Decreased metabolism of Ivacaftor caused by Palbociclib mediated inhibition of CYP450 enzyme. Breast cancer [2C60-2C6Y] [40]
Macitentan DMP79A1 Moderate Decreased metabolism of Ivacaftor caused by Macitentan mediated inhibition of CYP450 enzyme. Cardiovascular disease [BA00-BE2Z] [46]
PF-04449913 DMSB068 Moderate Decreased metabolism of Ivacaftor caused by PF-04449913 mediated inhibition of CYP450 enzyme. Chronic myelomonocytic leukaemia [2A40] [47]
Fidaxomicin DMFP6MV Minor Decreased clearance of Ivacaftor due to the transporter inhibition by Fidaxomicin. Clostridium difficile enterocolitis [1A04] [39]
Intedanib DMSTA36 Moderate Decreased clearance of Ivacaftor due to the transporter inhibition by Intedanib. Colorectal cancer [2B91] [48]
Osilodrostat DMIJC9X Moderate Decreased metabolism of Ivacaftor caused by Osilodrostat mediated inhibition of CYP450 enzyme. Cushing syndrome [5A70] [40]
MK-8228 DMOB58Q Major Decreased metabolism of Ivacaftor caused by MK-8228 mediated inhibition of CYP450 enzyme. Cytomegaloviral disease [1D82] [41]
Polatuzumab vedotin DMF6Y0L Moderate Decreased metabolism of Ivacaftor caused by Polatuzumab vedotin mediated inhibition of CYP450 enzyme. Diffuse large B-cell lymphoma [2A81] [49]
Stiripentol DMMSDOY Moderate Decreased metabolism of Ivacaftor caused by Stiripentol mediated inhibition of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [41]
Eslicarbazepine DMZREFQ Moderate Increased metabolism of Ivacaftor caused by Eslicarbazepine mediated induction of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [40]
Cannabidiol DM0659E Moderate Increased risk of hepatotoxicity by the combination of Ivacaftor and Cannabidiol. Epileptic encephalopathy [8A62] [41]
Tazemetostat DMWP1BH Moderate Decreased metabolism of Ivacaftor caused by Tazemetostat mediated inhibition of CYP450 enzyme. Follicular lymphoma [2A80] [50]
Mirabegron DMS1GYT Minor Decreased metabolism of Ivacaftor caused by Mirabegron mediated inhibition of CYP450 enzyme. Functional bladder disorder [GC50] [51]
Ripretinib DM958QB Moderate Decreased metabolism of Ivacaftor caused by Ripretinib mediated inhibition of CYP450 enzyme. Gastrointestinal stromal tumour [2B5B] [39]
Avapritinib DMK2GZX Moderate Decreased metabolism of Ivacaftor caused by Avapritinib mediated inhibition of CYP450 enzyme. Gastrointestinal stromal tumour [2B5B] [41]
Boceprevir DMBSHMF Major Decreased metabolism of Ivacaftor caused by Boceprevir mediated inhibition of CYP450 enzyme. Hepatitis virus infection [1E50-1E51] [39]
Brentuximab vedotin DMWLC57 Moderate Decreased metabolism of Ivacaftor caused by Brentuximab vedotin mediated inhibition of CYP450 enzyme. Hodgkin lymphoma [2B30] [52]
MK-1439 DM215WE Minor Decreased metabolism of Ivacaftor caused by MK-1439 mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [53]
Cobicistat DM6L4H2 Major Decreased metabolism of Ivacaftor caused by Cobicistat mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [39]
Dolutegravir DMCZGRE Minor Decreased metabolism of Ivacaftor caused by Dolutegravir mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [54]
Rilpivirine DMJ0QOW Moderate Decreased metabolism of Ivacaftor caused by Rilpivirine mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [39]
Teriflunomide DMQ2FKJ Major Increased risk of hepatotoxicity by the combination of Ivacaftor and Teriflunomide. Hyper-lipoproteinaemia [5C80] [55]
BMS-201038 DMQTAGO Major Increased risk of hepatotoxicity by the combination of Ivacaftor and BMS-201038. Hyper-lipoproteinaemia [5C80] [56]
Aliskiren DM1BV7W Moderate Decreased metabolism of Ivacaftor caused by Aliskiren mediated inhibition of CYP450 enzyme. Hypertension [BA00-BA04] [55]
Levamlodipine DM92S6N Moderate Decreased metabolism of Ivacaftor caused by Levamlodipine mediated inhibition of CYP450 enzyme. Hypertension [BA00-BA04] [40]
Lesinurad DMUR64T Moderate Decreased metabolism of Ivacaftor caused by Lesinurad mediated inhibition of CYP450 enzyme. Inborn purine/pyrimidine/nucleotide metabolism error [5C55] [57]
Berotralstat DMWA2DZ Major Decreased clearance of Ivacaftor due to the transporter inhibition by Berotralstat. Innate/adaptive immunodeficiency [4A00] [58]
Tasimelteon DMLOQ1V Moderate Decreased metabolism of Ivacaftor caused by Tasimelteon mediated inhibition of CYP450 enzyme. Insomnia [7A00-7A0Z] [59]
Naloxegol DML0B41 Minor Decreased clearance of Ivacaftor due to the transporter inhibition by Naloxegol. Large intestine motility disorder [DB32] [60]
Pemigatinib DM819JF Moderate Decreased metabolism of Ivacaftor caused by Pemigatinib mediated inhibition of CYP450 enzyme. Liver cancer [2C12] [41]
Crizotinib DM4F29C Major Decreased metabolism of Ivacaftor caused by Crizotinib mediated inhibition of CYP450 enzyme. Lung cancer [2C25] [41]
Brigatinib DM7W94S Moderate Decreased metabolism of Ivacaftor caused by Brigatinib mediated inhibition of CYP450 enzyme. Lung cancer [2C25] [39]
Ceritinib DMB920Z Major Decreased metabolism of Ivacaftor caused by Ceritinib mediated inhibition of CYP450 enzyme. Lung cancer [2C25] [39]
Lurbinectedin DMEFRTZ Moderate Decreased metabolism of Ivacaftor caused by Lurbinectedin mediated inhibition of CYP450 enzyme. Lung cancer [2C25] [61]
Osimertinib DMRJLAT Moderate Increased metabolism of Ivacaftor caused by Osimertinib mediated induction of CYP450 enzyme. Lung cancer [2C25] [41]
Pralsetinib DMWU0I2 Moderate Decreased metabolism of Ivacaftor caused by Pralsetinib mediated inhibition of CYP450 enzyme. Lung cancer [2C25] [62]
Selpercatinib DMZR15V Moderate Decreased metabolism of Ivacaftor caused by Selpercatinib mediated inhibition of CYP450 enzyme. Lung cancer [2C25] [40]
Artesunate DMR27C8 Moderate Decreased clearance of Ivacaftor due to the transporter inhibition by Artesunate. Malaria [1F40-1F45] [40]
Calaspargase pegol DMQZBXI Moderate Increased risk of hepatotoxicity by the combination of Ivacaftor and Calaspargase pegol. Malignant haematopoietic neoplasm [2B33] [63]
Idelalisib DM602WT Major Decreased metabolism of Ivacaftor caused by Idelalisib mediated inhibition of CYP450 enzyme. Mature B-cell leukaemia [2A82] [39]
GDC-0199 DMH0QKA Major Decreased clearance of Ivacaftor due to the transporter inhibition by GDC-0199. Mature B-cell leukaemia [2A82] [39]
IPI-145 DMWA24P Major Decreased metabolism of Ivacaftor caused by IPI-145 mediated inhibition of CYP450 enzyme. Mature B-cell leukaemia [2A82] [41]
Acalabrutinib DM7GCVW Moderate Decreased metabolism of Ivacaftor caused by Acalabrutinib mediated inhibition of CYP450 enzyme. Mature B-cell lymphoma [2A85] [64]
Ibrutinib DMHZCPO Moderate Decreased metabolism of Ivacaftor caused by Ibrutinib mediated inhibition of CYP450 enzyme. Mature B-cell lymphoma [2A85] [65]
Arry-162 DM1P6FR Moderate Decreased clearance of Ivacaftor due to the transporter inhibition by Arry-162. Melanoma [2C30] [39]
Vemurafenib DM62UG5 Moderate Increased metabolism of Ivacaftor caused by Vemurafenib mediated induction of CYP450 enzyme. Melanoma [2C30] [40]
Selumetinib DMC7W6R Moderate Decreased metabolism of Ivacaftor caused by Selumetinib mediated inhibition of CYP450 enzyme. Melanoma [2C30] [66]
LGX818 DMNQXV8 Moderate Increased metabolism of Ivacaftor caused by LGX818 mediated induction of CYP450 enzyme. Melanoma [2C30] [67]
Dabrafenib DMX6OE3 Moderate Increased metabolism of Ivacaftor caused by Dabrafenib mediated induction of CYP450 enzyme. Melanoma [2C30] [41]
Ubrogepant DM749I3 Moderate Decreased metabolism of Ivacaftor caused by Ubrogepant mediated inhibition of CYP450 enzyme. Migraine [8A80] [68]
Rimegepant DMHOAUG Moderate Decreased clearance of Ivacaftor due to the transporter inhibition by Rimegepant. Migraine [8A80] [69]
Siponimod DM2R86O Moderate Decreased metabolism of Ivacaftor caused by Siponimod mediated inhibition of CYP450 enzyme. Multiple sclerosis [8A40] [40]
Fedratinib DM4ZBK6 Major Decreased metabolism of Ivacaftor caused by Fedratinib mediated inhibition of CYP450 enzyme. Myeloproliferative neoplasm [2A20] [41]
Netupitant DMEKAYI Major Decreased metabolism of Ivacaftor caused by Netupitant mediated inhibition of CYP450 enzyme. Nausea/vomiting [MD90] [41]
Entrectinib DMMPTLH Moderate Decreased metabolism of Ivacaftor caused by Entrectinib mediated inhibition of CYP450 enzyme. Non-small cell lung cancer [2C25] [40]
S-297995 DM26IH8 Moderate Decreased clearance of Ivacaftor due to the transporter inhibition by S-297995. Opioid use disorder [6C43] [41]
Olaparib DM8QB1D Moderate Decreased clearance of Ivacaftor due to the transporter inhibition by Olaparib. Ovarian cancer [2C73] [39]
Rucaparib DM9PVX8 Moderate Decreased metabolism of Ivacaftor caused by Rucaparib mediated inhibition of CYP450 enzyme. Ovarian cancer [2C73] [40]
Abametapir DM2RX0I Moderate Decreased metabolism of Ivacaftor caused by Abametapir mediated inhibition of CYP450 enzyme. Pediculosis [1G00] [70]
Lefamulin DME6G97 Moderate Decreased metabolism of Ivacaftor caused by Lefamulin mediated inhibition of CYP450 enzyme. Pneumonia [CA40] [71]
Enzalutamide DMGL19D Major Increased metabolism of Ivacaftor caused by Enzalutamide mediated induction of CYP450 enzyme. Prostate cancer [2C82] [39]
Relugolix DMK7IWL Major Decreased clearance of Ivacaftor due to the transporter inhibition by Relugolix. Prostate cancer [2C82] [72]
Riociguat DMXBLMP Moderate Decreased metabolism of Ivacaftor caused by Riociguat mediated inhibition of CYP450 enzyme. Pulmonary hypertension [BB01] [39]
Voxelotor DMCS6M5 Major Decreased metabolism of Ivacaftor caused by Voxelotor mediated inhibition of CYP450 enzyme. Sickle-cell disorder [3A51] [41]
LDE225 DMM9F25 Moderate Decreased metabolism of Ivacaftor caused by LDE225 mediated inhibition of CYP450 enzyme. Skin cancer [2C30-2C37] [73]
Telotristat ethyl DMDIYFZ Moderate Increased metabolism of Ivacaftor caused by Telotristat ethyl mediated induction of CYP450 enzyme. Small intestine developmental anomaly [DA90] [41]
Larotrectinib DM26CQR Moderate Decreased metabolism of Ivacaftor caused by Larotrectinib mediated inhibition of CYP450 enzyme. Solid tumour/cancer [2A00-2F9Z] [40]
LEE011 DMMX75K Major Decreased metabolism of Ivacaftor caused by LEE011 mediated inhibition of CYP450 enzyme. Solid tumour/cancer [2A00-2F9Z] [41]
Fostamatinib DM6AUHV Moderate Decreased metabolism of Ivacaftor caused by Fostamatinib mediated inhibition of CYP450 enzyme. Thrombocytopenia [3B64] [74]
Lusutrombopag DMH6IKO Moderate Decreased clearance of Ivacaftor due to the transporter inhibition by Lusutrombopag. Thrombocytopenia [3B64] [40]
Elagolix DMB2C0E Moderate Increased metabolism of Ivacaftor caused by Elagolix mediated induction of CYP450 enzyme. Uterine fibroid [2E86] [40]
Betrixaban DM2C4RF Moderate Decreased clearance of Ivacaftor due to the transporter inhibition by Betrixaban. Venous thromboembolism [BD72] [75]
⏷ Show the Full List of 84 DDI Information of This Drug

Drug Inactive Ingredient(s) (DIG) and Formulation(s) of This Drug

DIG
DIG Name DIG ID PubChem CID Functional Classification
FD&C blue no. 2 E00446 2723854 Colorant
Sodium lauryl sulfate E00464 3423265 Emulsifying agent; Modified-release agent; Penetration agent; Solubilizing agent; Surfactant; lubricant
Ammonia E00007 222 Alkalizing agent
Carmellose sodium E00625 Not Available Disintegrant
Ferrosoferric oxide E00231 14789 Colorant
Lactose monohydrate E00393 104938 Binding agent; Diluent; Dry powder inhaler carrier; Lyophilization aid
Magnesium stearate E00208 11177 lubricant
Polyethylene glycol 3350 E00652 Not Available Coating agent; Diluent; Ointment base; Plasticizing agent; Solvent; Suppository base; lubricant
Propylene glycol E00040 1030 Antimicrobial preservative; Humectant; Plasticizing agent; Solvent
Silicon dioxide E00670 Not Available Anticaking agent; Opacifying agent; Viscosity-controlling agent
Talc E00520 16211421 Anticaking agent; Diluent; Glidant; lubricant
Titanium dioxide E00322 26042 Coating agent; Colorant; Opacifying agent
⏷ Show the Full List of 12 Pharmaceutical Excipients of This Drug
Pharmaceutical Formulation
Formulation Name Drug Dosage Dosage Form Route
Ivacaftor 150 mg tablet 150 mg Oral Tablet Oral
Jump to Detail Pharmaceutical Formulation Page of This Drug

References

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45 Product Information. Talzenna (talazoparib). Pfizer U.S. Pharmaceuticals Group, New York, NY.
46 Product Information. Opsumit (macitentan). Actelion Pharmaceuticals US Inc, South San Francisco, CA.
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48 Product Information. Ofev (nintedanib). Boehringer Ingelheim, Ridgefield, CT.
49 Product Information. Polivy (polatuzumab vedotin). Genentech, South San Francisco, CA.
50 Product Information. Tazverik (tazemetostat). Epizyme, Inc, Cambridge, MA.
51 Product Information. Myrbetriq (mirabegron). Astellas Pharma US, Inc, Deerfield, IL.
52 Product Information. VFEND (voriconazole). Pfizer U.S. Pharmaceuticals, New York, NY.
53 Product Information. Pifeltro (doravirine). Merck & Company Inc, Whitehouse Station, NJ.
54 Product Information. Tivicay (dolutegravir). ViiV Healthcare, Research Triangle Park, NC.
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56 Product Information. Juxtapid (lomitapide). Aegerion Pharmaceuticals Inc, Cambridge, MA.
57 Product Information. Zurampic (lesinurad). Astra-Zeneca Pharmaceuticals, Wilmington, DE.
58 Product Information. Orladeyo (berotralstat). BioCryst Pharmaceuticals Inc, Durham, NC.
59 Product Information. Hetlioz (tasimelteon). Vanda Pharmaceuticals Inc, Rockville, MD.
60 Product Information. Movantik (naloxegol). Astra-Zeneca Pharmaceuticals, Wilmington, DE.
61 Product Information. Zepzelca (lurbinectedin). Jazz Pharmaceuticals, Palo Alto, CA.
62 Product Information. Gavreto (pralsetinib). Blueprint Medicines Corporation, Cambridge, MA.
63 Al-Nawakil C, Willems L, Mauprivez C, et.al "Successful treatment of l-asparaginase-induced severe acute hepatotoxicity using mitochondrial cofactors." Leuk Lymphoma 55 (2014): 1670-4. [PMID: 24090500]
64 Product Information. Calquence (acalabrutinib). Astra-Zeneca Pharmaceuticals, Wilmington, DE.
65 Product Information. Imbruvica (ibrutinib). Pharmacyclics Inc, Sunnyvale, CA.
66 Product Information. Koselugo (selumetinib). Astra-Zeneca Pharmaceuticals, Wilmington, DE.
67 Product Information. Braftovi (encorafenib). Array BioPharma Inc., Boulder, CO.
68 Product Information. Ubrelvy (ubrogepant). Allergan Inc, Irvine, CA.
69 Product Information. Nurtec ODT (rimegepant). Biohaven Pharmaceuticals, New Haven, CT.
70 Product Information. Xeglyze (abametapir topical). Dr. Reddy's Laboratories Inc, Upper Saddle River, NJ.
71 Product Information. Xenleta (lefamulin). Nabriva Therapeutics US, Inc., King of Prussia, PA.
72 Product Information. Orgovyx (relugolix). Myovant Sciences, Inc., Brisbane, CA.
73 Product Information. Odomzo (sonidegib). Novartis Pharmaceuticals, East Hanover, NJ.
74 Product Information. Tavalisse (fostamatinib). Rigel Pharmaceuticals, South San Francisco, CA.
75 Product Information. Bevyxxa (betrixaban). Portola Pharmaceuticals, South San Francisco, CA.