Peringatan Keamanan

LD50 information is not readily available. There have been no reports of overdose with ivacaftor, but when given with tezacaftor, the highest clinical dose lead to diarrhea and dizziness. Provide supportive measures in cases of a suspected overdose. No antidote is available at this time.L6814

Ivacaftor

DB08820

small molecule approved

Deskripsi

Ivacaftor (also known as Kalydeco or VX-770) is a drug used for the management of Cystic Fibrosis (CF). It is manufactured and distributed by Vertex Pharmaceuticals. It was approved by the Food and Drug Administration on January 31, 2012L768, and by Health Canada in late 2012.L6841 Ivacaftor is administered as a monotherapy and also administered in combination with other drugs for the management of CF.L6814,L6979,L6847

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, an ion channel involved in the transport of chloride and sodium ions across cell membranes. CFTR is active in epithelial cells of organs such as of the lungs, pancreas, liver, digestive system, and reproductive tract. Alterations in the CFTR gene result in altered production, misfolding, or function of the protein and consequently abnormal fluid and ion transport across cell membranes.A20298, A20299 As a result, CF patients produce thick, sticky mucus that clogs the ducts of organs where it is produced making patients more susceptible to complications such as infections, lung damage, pancreatic insufficiency, and malnutrition.A20302

Prior to the development of ivacaftor, 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 or lung function (FEV1). Notably, ivacaftor was the first medication approved for the management of the underlying causes of CF (abnormalities in CFTR protein function) rather than control of symptoms.A20297

Struktur Molekul 2D

Berat 392.4907
Wujud solid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) In a clinical study, the apparent terminal half-life was approximately 12 hours following a single dose of ivacaftor.[L6979] One source mentions the half-life ranges from 12 to 14 hours.[A179674]
Volume Distribusi 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.[L6979]
Klirens (Clearance) The CL/F (SD) for the 150 mg dose was 17.3 (8.4) L/hr in healthy subjects.[L6979]

Absorpsi

Ivacaftor is well absorbed in the gastrointestinal tract.A179674 Following administration of ivacaftor with fat-containing foods, peak plasma concentrations were reached at 4 hours (Tmax) with a maximum concentration (Cmax) of 768 ng/mL and AUC of 10600 ng * hr/mL. It is recommended that ivacaftor is taken with fat-containing foods as they increase absorption by approximately 2.5- to 4-fold.L6979

Metabolisme

Ivacaftor is extensively metabolized in humans. In vitro and clinical studies indicate that ivacaftor is primarily metabolized by CYP3A. From this metabolism, the major formed metabolites are M1 and M6. M1 is considered pharmacologically active even though it just presents approximately one-sixth the effect of the parent compound ivacaftor. On the other hand, M6 is not considered pharmacologically active as it represents less than one-fiftieth of the effect of the parent compound.A179674,L6979

Rute Eliminasi

After oral administration, ivacaftor is mainly eliminated in the feces after metabolic conversion and this elimination represents 87.8% of the dose. From the total eliminated dose, the metabolites M1 and M6 account for the majority of the eliminated dose, being 22% for M1 and 43% for M6. Ivacaftor shows negligible urinary excretion as the unchanged drug.A179674,L6979

Farmakogenomik

1 Varian
CFTR (rs75527207)

Patients who carry this polymorphism in CFTR will respond to ivacaftor therapy.

Interaksi Makanan

1 Data
  • 1. Take with a high fat meal. Co-administration with a high fat meal increases exposure to ivacaftor.

Interaksi Obat

972 Data
Afatinib The serum concentration of Afatinib can be increased when it is combined with Ivacaftor.
Bosutinib The serum concentration of Bosutinib can be increased when it is combined with Ivacaftor.
Brentuximab vedotin The serum concentration of Brentuximab vedotin can be increased when it is combined with Ivacaftor.
Edoxaban The serum concentration of Edoxaban can be increased when it is combined with Ivacaftor.
Ledipasvir The serum concentration of Ledipasvir can be increased when it is combined with Ivacaftor.
Lomitapide The metabolism of Lomitapide can be decreased when combined with Ivacaftor.
Naloxegol The serum concentration of Naloxegol can be increased when it is combined with Ivacaftor.
Pazopanib The serum concentration of Pazopanib can be increased when it is combined with Ivacaftor.
Prucalopride The serum concentration of Prucalopride can be increased when it is combined with Ivacaftor.
Ranolazine The serum concentration of Ranolazine can be increased when it is combined with Ivacaftor.
Silodosin The excretion of Silodosin can be decreased when combined with Ivacaftor.
Topotecan The serum concentration of Topotecan can be increased when it is combined with Ivacaftor.
Eliglustat The metabolism of Eliglustat can be decreased when combined with Ivacaftor.
Ibrutinib The metabolism of Ibrutinib can be decreased when combined with Ivacaftor.
Cyclosporine The metabolism of Ivacaftor can be decreased when combined with Cyclosporine.
Diltiazem The metabolism of Ivacaftor can be decreased when combined with Diltiazem.
Verapamil The metabolism of Ivacaftor can be decreased when combined with Verapamil.
Erythromycin The metabolism of Ivacaftor can be decreased when combined with Erythromycin.
Clozapine The metabolism of Ivacaftor can be decreased when combined with Clozapine.
Haloperidol The metabolism of Ivacaftor can be decreased when combined with Haloperidol.
Ciprofloxacin The metabolism of Ivacaftor can be decreased when combined with Ciprofloxacin.
Nicardipine The metabolism of Ivacaftor can be decreased when combined with Nicardipine.
Simeprevir The metabolism of Ivacaftor can be decreased when combined with Simeprevir.
Crizotinib The serum concentration of Crizotinib can be increased when it is combined with Ivacaftor.
Linagliptin The metabolism of Ivacaftor can be decreased when combined with Linagliptin.
Venetoclax The metabolism of Ivacaftor can be decreased when combined with Venetoclax.
Fluvoxamine The metabolism of Ivacaftor can be decreased when combined with Fluvoxamine.
Voriconazole The serum concentration of Ivacaftor can be increased when it is combined with Voriconazole.
Fluconazole The metabolism of Ivacaftor can be decreased when combined with Fluconazole.
Ziprasidone The metabolism of Ivacaftor can be decreased when combined with Ziprasidone.
Isradipine The metabolism of Ivacaftor can be decreased when combined with Isradipine.
Isoniazid The metabolism of Ivacaftor can be decreased when combined with Isoniazid.
Primaquine The metabolism of Ivacaftor can be decreased when combined with Primaquine.
Miconazole The metabolism of Ivacaftor can be decreased when combined with Miconazole.
Danazol The metabolism of Ivacaftor can be decreased when combined with Danazol.
Fusidic acid The metabolism of Ivacaftor can be decreased when combined with Fusidic acid.
Zimelidine The metabolism of Ivacaftor can be decreased when combined with Zimelidine.
Milnacipran The metabolism of Ivacaftor can be decreased when combined with Milnacipran.
Desvenlafaxine The metabolism of Ivacaftor can be decreased when combined with Desvenlafaxine.
Nilvadipine The metabolism of Ivacaftor can be decreased when combined with Nilvadipine.
Seproxetine The metabolism of Ivacaftor can be decreased when combined with Seproxetine.
Indalpine The metabolism of Ivacaftor can be decreased when combined with Indalpine.
Netupitant The metabolism of Ivacaftor can be decreased when combined with Netupitant.
Barnidipine The metabolism of Ivacaftor can be decreased when combined with Barnidipine.
Benidipine The metabolism of Ivacaftor can be decreased when combined with Benidipine.
Fosnetupitant The metabolism of Ivacaftor can be decreased when combined with Fosnetupitant.
Isavuconazonium The metabolism of Ivacaftor can be decreased when combined with Isavuconazonium.
Aprepitant The metabolism of Ivacaftor can be decreased when combined with Aprepitant.
Dronedarone The metabolism of Ivacaftor can be decreased when combined with Dronedarone.
Isavuconazole The metabolism of Ivacaftor can be decreased when combined with Isavuconazole.
Berotralstat The metabolism of Ivacaftor can be decreased when combined with Berotralstat.
Everolimus The serum concentration of Everolimus can be increased when it is combined with Ivacaftor.
Rifaximin The serum concentration of Rifaximin can be increased when it is combined with Ivacaftor.
Cilostazol The metabolism of Cilostazol can be decreased when combined with Ivacaftor.
Colchicine The serum concentration of Colchicine can be increased when it is combined with Ivacaftor.
Iloperidone The metabolism of Iloperidone can be decreased when combined with Ivacaftor.
Retapamulin The metabolism of Retapamulin can be decreased when combined with Ivacaftor.
Tofacitinib The metabolism of Tofacitinib can be decreased when combined with Ivacaftor.
Vardenafil The metabolism of Vardenafil can be decreased when combined with Ivacaftor.
Eszopiclone The serum concentration of Eszopiclone can be increased when it is combined with Ivacaftor.
Zopiclone The serum concentration of Zopiclone can be increased when it is combined with Ivacaftor.
Lovastatin The metabolism of Lovastatin can be decreased when combined with Ivacaftor.
Alfuzosin The metabolism of Alfuzosin can be decreased when combined with Ivacaftor.
Alprazolam The metabolism of Alprazolam can be decreased when combined with Ivacaftor.
Warfarin The serum concentration of Warfarin can be increased when it is combined with Ivacaftor.
Acenocoumarol The serum concentration of Acenocoumarol can be increased when it is combined with Ivacaftor.
(R)-warfarin The serum concentration of (R)-warfarin can be increased when it is combined with Ivacaftor.
R,S-Warfarin alcohol The serum concentration of R,S-Warfarin alcohol can be increased when it is combined with Ivacaftor.
S,R-Warfarin alcohol The serum concentration of S,R-Warfarin alcohol can be increased when it is combined with Ivacaftor.
(S)-Warfarin The serum concentration of (S)-Warfarin can be increased when it is combined with Ivacaftor.
Midazolam The serum concentration of Midazolam can be increased when it is combined with Ivacaftor.
Tacrolimus The serum concentration of Tacrolimus can be increased when it is combined with Ivacaftor.
Atorvastatin The metabolism of Atorvastatin can be decreased when combined with Ivacaftor.
Vincristine The serum concentration of Vincristine can be increased when it is combined with Ivacaftor.
Doxorubicin The serum concentration of Doxorubicin can be increased when it is combined with Ivacaftor.
Betrixaban The serum concentration of Betrixaban can be increased when it is combined with Ivacaftor.
Pitolisant The serum concentration of Ivacaftor can be decreased when it is combined with Pitolisant.
Pravastatin The serum concentration of Pravastatin can be increased when it is combined with Ivacaftor.
Morphine The serum concentration of Morphine can be increased when it is combined with Ivacaftor.
Tenofovir disoproxil The serum concentration of Tenofovir disoproxil can be increased when it is combined with Ivacaftor.
Quinine The serum concentration of Quinine can be increased when it is combined with Ivacaftor.
Toremifene The serum concentration of Toremifene can be increased when it is combined with Ivacaftor.
Bisoprolol The serum concentration of Bisoprolol can be increased when it is combined with Ivacaftor.
Mannitol The serum concentration of Mannitol can be increased when it is combined with Ivacaftor.
Clomifene The serum concentration of Clomifene can be increased when it is combined with Ivacaftor.
Fexofenadine The serum concentration of Fexofenadine can be increased when it is combined with Ivacaftor.
Tegaserod The serum concentration of Tegaserod can be increased when it is combined with Ivacaftor.
Sitagliptin The serum concentration of Sitagliptin can be increased when it is combined with Ivacaftor.
Paliperidone The serum concentration of Paliperidone can be increased when it is combined with Ivacaftor.
Indacaterol The serum concentration of Indacaterol can be increased when it is combined with Ivacaftor.
Ambrisentan The serum concentration of Ambrisentan can be increased when it is combined with Ivacaftor.
Apixaban The serum concentration of Apixaban can be increased when it is combined with Ivacaftor.
Odanacatib The serum concentration of Odanacatib can be increased when it is combined with Ivacaftor.
Mirabegron The serum concentration of Mirabegron can be increased when it is combined with Ivacaftor.
Canagliflozin The serum concentration of Canagliflozin can be increased when it is combined with Ivacaftor.
Dolutegravir The serum concentration of Dolutegravir can be increased when it is combined with Ivacaftor.
Sofosbuvir The serum concentration of Sofosbuvir can be increased when it is combined with Ivacaftor.
Umeclidinium The serum concentration of Umeclidinium can be increased when it is combined with Ivacaftor.
Lenvatinib The serum concentration of Lenvatinib can be increased when it is combined with Ivacaftor.
Nintedanib The serum concentration of Nintedanib can be increased when it is combined with Ivacaftor.

Target Protein

Cystic fibrosis transmembrane conductance regulator CFTR

Referensi & Sumber

Artikel (PubMed)
  • PMID: 21083385
    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. doi: 10.1056/NEJMoa0909825.
  • PMID: 22047557
    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. doi: 10.1056/NEJMoa1105185.
  • PMID: 22942289
    Eckford PD, Li C, Ramjeesingh M, Bear CE: Cystic fibrosis transmembrane conductance regulator (CFTR) potentiator VX-770 (ivacaftor) opens the defective channel gate of mutant CFTR in a phosphorylation-dependent but ATP-independent manner. J Biol Chem. 2012 Oct 26;287(44):36639-49. doi: 10.1074/jbc.M112.393637. Epub 2012 Aug 31.
  • PMID: 19846789
    Van Goor F, Hadida S, Grootenhuis PD, Burton B, Cao D, Neuberger T, Turnbull A, Singh A, Joubran J, Hazlewood A, Zhou J, McCartney J, Arumugam V, Decker C, Yang J, Young C, Olson ER, Wine JJ, Frizzell RA, Ashlock M, Negulescu P: Rescue of CF airway epithelial cell function in vitro by a CFTR potentiator, VX-770. Proc Natl Acad Sci U S A. 2009 Nov 3;106(44):18825-30. doi: 10.1073/pnas.0904709106. Epub 2009 Oct 21.
  • PMID: 27714410
    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.
  • PMID: 14719996
    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.
  • PMID: 17291132
    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.
  • PMID: 28031875
    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.
Menampilkan 8 dari 12 artikel.

Contoh Produk & Brand

Produk: 67 • International brands: 0
Produk
  • Kaftrio
    Tablet, film coated • - • Oral • EU • Approved
  • Kaftrio
    Tablet, film coated • - • Oral • EU • Approved
  • Kaftrio
    Granule • - • Oral • EU • Approved
  • Kaftrio
    Granule • - • Oral • EU • Approved
  • Kalydeco
    Tablet, film coated • 150 mg/1 • Oral • US • Approved
  • Kalydeco
    Granule • 50 mg/1 • Oral • US • Approved
  • Kalydeco
    Granule • 75 mg/1 • Oral • US • Approved
  • Kalydeco
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