Peringatan Keamanan

The LD50 of an oral dose in rats is >2000 mg/kg.L6826

Overdose symptoms may include dizziness and diarrhea. There have been no reports to this date of tezacaftor overdose, but the highest dose of 450 mg every 12 hours commonly resulted in reports of dizziness and diarrhea. No antidote exists for treating an overdose with this drug. General supportive measures should be undertaken along with monitoring of vital signs and close monitoring of clinical status.L6814

Tezacaftor

DB11712

small molecule approved investigational

Deskripsi

Tezacaftor is a drug of the cystic fibrosis transmembrane conductance regulator (CFTR) potentiator class.L1595 It was developed by Vertex Pharmaceuticals and FDA approved in combination with ivacaftor to manage cystic fibrosis.L6814 This drug was approved by the FDA on February 12, 2018.L4894

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

Struktur Molekul 2D

Berat 520.505
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The apparent half-life of tezacaftor is approximately 57.2 hours.[A179665,L6829]
Volume Distribusi The apparent volume of distribution of tezacaftor was 271 L in a study of patients in the fed state who received 100 mg of tezacaftor every 12 hours.[L6814]
Klirens (Clearance) The apparent clearance of tezacaftor has been measured at 1.31 L/h for patients in the fed state during a clinical trial.[A32094]

Absorpsi

The Cmax, Tmax and AUC of tezacaftor, when administered with ivacaftor, are 5.95 mcg/ml, 2-6 h, and 84.5 mcg.h/ml respectively.L6814 Exposure of tezacaftor/ivacaftor increases 3-fold when it is administered with a high-fat meal.L6814

Metabolisme

Tezacaftor is metabolized extensively in humans by the action of CYP3A4 and CYP3A5. There are three main circulating metabolites; M1, M2, and M5. The M1 is an active metabolite with similar activity to the parent drug, tezacaftor. The M2 metabolite is significantly less active and M5 is considered an inactive metabolite.A179665,L6814 An additional circulating metabolite, M3, corresponding to the glucuronide form of tezacaftor.L6814

Rute Eliminasi

After oral administration, the majority of tezacaftor dose (72%) is found excreted in the feces either unchanged or as its metabolite, M2. About 14% of the administered dose is found excreted in the urine as the metabolite, M2. It was noted that less than 1% of the administered dose is excreted unchanged in the urine and thus, renal excretion is not the major elimination pathway.L6814

Interaksi Makanan

3 Data
  • 1. Avoid grapefruit products. Grapefruit inhibits CYP3A metabolism, which may increase the serum concentration of tezacaftor.
  • 2. Avoid St. John's Wort. This herb induces CYP3A metabolism and may reduce serum levels of tezacaftor.
  • 3. Take with food. Tezacaftor should be taken with fat-containing food to increase exposure.

Interaksi Obat

522 Data
Ranolazine The serum concentration of Tezacaftor can be increased when it is combined with Ranolazine.
Vemurafenib The serum concentration of Tezacaftor can be increased when it is combined with Vemurafenib.
Apalutamide The serum concentration of Tezacaftor can be decreased when it is combined with Apalutamide.
Pitolisant The serum concentration of Tezacaftor can be decreased when it is combined with Pitolisant.
Loxapine The serum concentration of Tezacaftor can be increased when it is combined with Loxapine.
Quinine The serum concentration of Tezacaftor can be increased when it is combined with Quinine.
Toremifene The serum concentration of Tezacaftor can be increased when it is combined with Toremifene.
Mifepristone The serum concentration of Tezacaftor can be increased when it is combined with Mifepristone.
Zonisamide The serum concentration of Tezacaftor can be increased when it is combined with Zonisamide.
Carvedilol The serum concentration of Tezacaftor can be increased when it is combined with Carvedilol.
Propafenone The serum concentration of Tezacaftor can be increased when it is combined with Propafenone.
Lapatinib The serum concentration of Tezacaftor can be increased when it is combined with Lapatinib.
Paliperidone The serum concentration of Tezacaftor can be increased when it is combined with Paliperidone.
Mibefradil The serum concentration of Tezacaftor can be increased when it is combined with Mibefradil.
Biricodar The serum concentration of Tezacaftor can be increased when it is combined with Biricodar.
Elacridar The serum concentration of Tezacaftor can be increased when it is combined with Elacridar.
Flibanserin The serum concentration of Tezacaftor can be increased when it is combined with Flibanserin.
Vandetanib The serum concentration of Tezacaftor can be increased when it is combined with Vandetanib.
Zosuquidar The serum concentration of Tezacaftor can be increased when it is combined with Zosuquidar.
Tariquidar The serum concentration of Tezacaftor can be increased when it is combined with Tariquidar.
Brefeldin A The serum concentration of Tezacaftor can be increased when it is combined with Brefeldin A.
Mirabegron The serum concentration of Tezacaftor can be increased when it is combined with Mirabegron.
Regorafenib The serum concentration of Tezacaftor can be increased when it is combined with Regorafenib.
Canagliflozin The serum concentration of Tezacaftor can be increased when it is combined with Canagliflozin.
Vorapaxar The serum concentration of Tezacaftor can be increased when it is combined with Vorapaxar.
Suvorexant The serum concentration of Tezacaftor can be increased when it is combined with Suvorexant.
Palbociclib The serum concentration of Tezacaftor can be increased when it is combined with Palbociclib.
Daclatasvir The serum concentration of Tezacaftor can be increased when it is combined with Daclatasvir.
Niguldipine The serum concentration of Tezacaftor can be increased when it is combined with Niguldipine.
Rolapitant The serum concentration of Tezacaftor can be increased when it is combined with Rolapitant.
Asunaprevir The serum concentration of Tezacaftor can be increased when it is combined with Asunaprevir.
Velpatasvir The serum concentration of Tezacaftor can be increased when it is combined with Velpatasvir.
Carfilzomib The serum concentration of Tezacaftor can be increased when it is combined with Carfilzomib.
Valspodar The serum concentration of Tezacaftor can be increased when it is combined with Valspodar.
Dacomitinib The serum concentration of Tezacaftor can be increased when it is combined with Dacomitinib.
Glasdegib The serum concentration of Tezacaftor can be increased when it is combined with Glasdegib.
Elagolix The serum concentration of Tezacaftor can be increased when it is combined with Elagolix.
Voxilaprevir The serum concentration of Tezacaftor can be increased when it is combined with Voxilaprevir.
Rucaparib The metabolism of Tezacaftor can be decreased when combined with Rucaparib.
Pibrentasvir The serum concentration of Tezacaftor can be increased when it is combined with Pibrentasvir.
Glecaprevir The serum concentration of Tezacaftor can be increased when it is combined with Glecaprevir.
Ivosidenib The metabolism of Tezacaftor can be increased when combined with Ivosidenib.
Neratinib The serum concentration of Tezacaftor can be increased when it is combined with Neratinib.
Sarecycline The serum concentration of Tezacaftor can be increased when it is combined with Sarecycline.
Laniquidar The serum concentration of Tezacaftor can be increased when it is combined with Laniquidar.
Enasidenib The serum concentration of Tezacaftor can be increased when it is combined with Enasidenib.
Dexniguldipine The serum concentration of Tezacaftor can be increased when it is combined with Dexniguldipine.
ONT-093 The serum concentration of Tezacaftor can be increased when it is combined with ONT-093.
Lomitapide The serum concentration of Tezacaftor can be increased when it is combined with Lomitapide.
Entrectinib The serum concentration of Tezacaftor can be increased when it is combined with Entrectinib.
Fedratinib The serum concentration of Tezacaftor can be increased when it is combined with Fedratinib.
Istradefylline The serum concentration of Tezacaftor can be increased when it is combined with Istradefylline.
Cethromycin The serum concentration of Tezacaftor can be increased when it is combined with Cethromycin.
Norgestimate The serum concentration of Tezacaftor can be increased when it is combined with Norgestimate.
Afatinib The serum concentration of Tezacaftor can be increased when it is combined with Afatinib.
Ledipasvir The serum concentration of Tezacaftor can be increased when it is combined with Ledipasvir.
Quinidine The serum concentration of Tezacaftor can be increased when it is combined with Quinidine.
Favipiravir The serum concentration of Tezacaftor can be increased when it is combined with Favipiravir.
Methylene blue The serum concentration of Tezacaftor can be increased when it is combined with Methylene blue.
Ripretinib The serum concentration of Tezacaftor can be increased when it is combined with Ripretinib.
Pralsetinib The serum concentration of Tezacaftor can be increased when it is combined with Pralsetinib.
Arsenic trioxide The serum concentration of Tezacaftor can be increased when it is combined with Arsenic trioxide.
Mefloquine The serum concentration of Tezacaftor can be increased when it is combined with Mefloquine.
Ixabepilone The serum concentration of Tezacaftor can be increased when it is combined with Ixabepilone.
Voclosporin The serum concentration of Tezacaftor can be increased when it is combined with Voclosporin.
Eliglustat The serum concentration of Tezacaftor can be increased when it is combined with Eliglustat.
Umbralisib The serum concentration of Tezacaftor can be increased when it is combined with Umbralisib.
Diosmin The serum concentration of Tezacaftor can be increased when it is combined with Diosmin.
Sapropterin The serum concentration of Tezacaftor can be increased when it is combined with Sapropterin.
Capmatinib The serum concentration of Capmatinib can be increased when it is combined with Tezacaftor.
Belumosudil The serum concentration of Tezacaftor can be increased when it is combined with Belumosudil.
Metreleptin The metabolism of Tezacaftor can be increased when combined with Metreleptin.
Cyclosporine The metabolism of Tezacaftor can be decreased when combined with Cyclosporine.
Diltiazem The metabolism of Tezacaftor can be decreased when combined with Diltiazem.
Verapamil The metabolism of Tezacaftor can be decreased when combined with Verapamil.
Isavuconazole The metabolism of Tezacaftor can be decreased when combined with Isavuconazole.
Fluconazole The metabolism of Tezacaftor can be decreased when combined with Fluconazole.
Erythromycin The metabolism of Tezacaftor can be decreased when combined with Erythromycin.
Isradipine The metabolism of Tezacaftor can be decreased when combined with Isradipine.
Haloperidol The metabolism of Tezacaftor can be decreased when combined with Haloperidol.
Nicardipine The metabolism of Tezacaftor can be decreased when combined with Nicardipine.
Primaquine The metabolism of Tezacaftor can be decreased when combined with Primaquine.
Miconazole The metabolism of Tezacaftor can be decreased when combined with Miconazole.
Zimelidine The metabolism of Tezacaftor can be decreased when combined with Zimelidine.
Simeprevir The metabolism of Tezacaftor can be decreased when combined with Simeprevir.
Isavuconazonium The metabolism of Tezacaftor can be decreased when combined with Isavuconazonium.
Crizotinib The metabolism of Crizotinib can be decreased when combined with Tezacaftor.
Linagliptin The metabolism of Tezacaftor can be decreased when combined with Linagliptin.
Netupitant The metabolism of Tezacaftor can be decreased when combined with Netupitant.
Venetoclax The metabolism of Tezacaftor can be decreased when combined with Venetoclax.
Clozapine The metabolism of Tezacaftor can be decreased when combined with Clozapine.
Ciprofloxacin The metabolism of Tezacaftor can be decreased when combined with Ciprofloxacin.
Fluvoxamine The metabolism of Tezacaftor can be decreased when combined with Fluvoxamine.
Voriconazole The metabolism of Tezacaftor can be decreased when combined with Voriconazole.
Ziprasidone The metabolism of Tezacaftor can be decreased when combined with Ziprasidone.
Isoniazid The metabolism of Tezacaftor can be decreased when combined with Isoniazid.
Danazol The metabolism of Tezacaftor can be decreased when combined with Danazol.
Fusidic acid The metabolism of Tezacaftor can be decreased when combined with Fusidic acid.
Milnacipran The metabolism of Tezacaftor can be decreased when combined with Milnacipran.
Desvenlafaxine The metabolism of Tezacaftor can be decreased when combined with Desvenlafaxine.

Target Protein

Cystic fibrosis transmembrane conductance regulator CFTR

Referensi & Sumber

Artikel (PubMed)
  • PMID: 28930490
    Donaldson SH, Pilewski JM, Griese M, Cooke J, Viswanathan L, Tullis E, Davies JC, Lekstrom-Himes JA, Wang LT: Tezacaftor/Ivacaftor in Subjects with Cystic Fibrosis and F508del/F508del-CFTR or F508del/G551D-CFTR. Am J Respir Crit Care Med. 2018 Jan 15;197(2):214-224. doi: 10.1164/rccm.201704-0717OC.
  • PMID: 29099344
    Taylor-Cousar JL, Munck A, McKone EF, van der Ent CK, Moeller A, Simard C, Wang LT, Ingenito EP, McKee C, Lu Y, Lekstrom-Himes J, Elborn JS: Tezacaftor-Ivacaftor in Patients with Cystic Fibrosis Homozygous for Phe508del. N Engl J Med. 2017 Nov 23;377(21):2013-2023. doi: 10.1056/NEJMoa1709846. Epub 2017 Nov 3.
  • PMID: 29099333
    Rowe SM, Daines C, Ringshausen FC, Kerem E, Wilson J, Tullis E, Nair N, Simard C, Han L, Ingenito EP, McKee C, Lekstrom-Himes J, Davies JC: Tezacaftor-Ivacaftor in Residual-Function Heterozygotes with Cystic Fibrosis. N Engl J Med. 2017 Nov 23;377(21):2024-2035. doi: 10.1056/NEJMoa1709847. Epub 2017 Nov 3.
  • PMID: 30694595
    Garg V, Shen J, Li C, Agarwal S, Gebre A, Robertson S, Huang J, Han L, Jiang L, Stephan K, Wang LT, Lekstrom-Himes J: Pharmacokinetic and Drug-Drug Interaction Profiles of the Combination of Tezacaftor/Ivacaftor. Clin Transl Sci. 2019 May;12(3):267-275. doi: 10.1111/cts.12610. Epub 2019 Jan 29.
  • 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: 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.
  • PMID: 27636560
    Fohner AE, McDonagh EM, Clancy JP, Whirl Carrillo M, Altman RB, Klein TE: PharmGKB summary: ivacaftor pathway, pharmacokinetics/pharmacodynamics. Pharmacogenet Genomics. 2017 Jan;27(1):39-42. doi: 10.1097/FPC.0000000000000246.
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