Peringatan Keamanan

As elexacaftor is currently only available in the combination product TrikaftaTM (ivacaftor/tezacaftor/elexacaftor), data regarding overdose of elexacaftor on its own is unavailable.L9395 Treatment of TrikaftaTM overdose should consist of general supportive and symptomatic treatment, including monitoring of vital signs and close observation of the affected patient.

Elexacaftor

DB15444

small molecule approved investigational

Deskripsi

Elexacaftor (previously VX-445) is a small molecule, next-generation corrector of the cystic fibrosis transmembrane conductance regulator (CFTR) protein.A187361 It received FDA approval in October 2019 in combination with tezacaftor and ivacaftor as the combination product TrikaftaTM.L9395 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.A187361 While dual corrector/potentiator combination therapy has proven useful in the treatment of a subset of CF patients,A187358 their use is typically limited to patients who are homozygous for the F508del-CFTR gene.A187361 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.A187361 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 70A187373-90%A187361,A187355 of all CF patients.

Struktur Molekul 2D

Berat 597.66
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The mean terminal half-life of elexacaftor is approximately 24.7 hours.[L9395]
Volume Distribusi The apparent volume of distribution of elexacaftor is 53.7 L.[L9395]
Klirens (Clearance) The mean apparent clearance of elexacaftor is 1.18 L/h.[L9395]

Absorpsi

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.L9395 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.L9395

Metabolisme

The metabolism of elexacaftor is extensive and primarily catalyzed via CYP3A4/5.L9395 Its main active metabolite, M23-ELX, carries a similar potency as the parent drug.L9395 The precise metabolic pathway of elexacaftor has not yet been elucidated in published research.

Rute Eliminasi

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.L9395

Interaksi Makanan

3 Data
  • 1. Avoid grapefruit products. Co-administration of grapefruit can inhibit elexacaftor metabolism and increase serum concentrations.
  • 2. Avoid St. John's Wort. This herb induces CYP3A metabolism and may reduce serum levels of elexacaftor.
  • 3. Take with a high fat meal. Examples include food prepared with eggs, cheeses, nuts, oils, and butter.

Interaksi Obat

626 Data
Eluxadoline The serum concentration of Eluxadoline can be increased when it is combined with Elexacaftor.
Bexarotene The metabolism of Elexacaftor can be increased when combined with Bexarotene.
Bosentan The serum concentration of Bosentan can be increased when it is combined with Elexacaftor.
Nafcillin The metabolism of Elexacaftor can be increased when combined with Nafcillin.
Modafinil The metabolism of Elexacaftor can be increased when combined with Modafinil.
Etravirine The metabolism of Elexacaftor can be increased when combined with Etravirine.
Avasimibe The metabolism of Elexacaftor can be increased when combined with Avasimibe.
Echinacea The metabolism of Elexacaftor can be increased when combined with Echinacea.
Dexamethasone acetate The metabolism of Elexacaftor can be increased when combined with Dexamethasone acetate.
Pitolisant The serum concentration of Elexacaftor can be decreased when it is combined with Pitolisant.
Pravastatin The serum concentration of Pravastatin can be increased when it is combined with Elexacaftor.
Valsartan The serum concentration of Valsartan can be increased when it is combined with Elexacaftor.
Torasemide The serum concentration of Torasemide can be increased when it is combined with Elexacaftor.
Liothyronine The serum concentration of Liothyronine can be increased when it is combined with Elexacaftor.
Conjugated estrogens The serum concentration of Conjugated estrogens can be increased when it is combined with Elexacaftor.
Digoxin The serum concentration of Digoxin can be increased when it is combined with Elexacaftor.
Caspofungin The serum concentration of Caspofungin can be increased when it is combined with Elexacaftor.
Enalapril The serum concentration of Enalapril can be increased when it is combined with Elexacaftor.
Sumatriptan The serum concentration of Sumatriptan can be increased when it is combined with Elexacaftor.
Mycophenolate mofetil The serum concentration of Mycophenolate mofetil can be increased when it is combined with Elexacaftor.
Penicillamine The serum concentration of Penicillamine can be increased when it is combined with Elexacaftor.
Repaglinide The serum concentration of Repaglinide can be increased when it is combined with Elexacaftor.
Dinoprostone The serum concentration of Dinoprostone can be increased when it is combined with Elexacaftor.
Fexofenadine The serum concentration of Fexofenadine can be increased when it is combined with Elexacaftor.
Ezetimibe The serum concentration of Ezetimibe can be increased when it is combined with Elexacaftor.
Benzylpenicillin The serum concentration of Benzylpenicillin can be increased when it is combined with Elexacaftor.
Atorvastatin The serum concentration of Atorvastatin can be increased when it is combined with Elexacaftor.
Ouabain The serum concentration of Ouabain can be increased when it is combined with Elexacaftor.
Liotrix The serum concentration of Liotrix can be increased when it is combined with Elexacaftor.
Cholic Acid The serum concentration of Cholic Acid can be increased when it is combined with Elexacaftor.
Taurocholic acid The serum concentration of Taurocholic acid can be increased when it is combined with Elexacaftor.
Atrasentan The serum concentration of Atrasentan can be increased when it is combined with Elexacaftor.
Ambrisentan The serum concentration of Ambrisentan can be increased when it is combined with Elexacaftor.
Gimatecan The serum concentration of Gimatecan can be increased when it is combined with Elexacaftor.
Temocapril The serum concentration of Temocapril can be increased when it is combined with Elexacaftor.
Cholecystokinin The serum concentration of Cholecystokinin can be increased when it is combined with Elexacaftor.
Gadoxetic acid The serum concentration of Gadoxetic acid can be increased when it is combined with Elexacaftor.
Technetium Tc-99m mebrofenin The serum concentration of Technetium Tc-99m mebrofenin can be increased when it is combined with Elexacaftor.
Fimasartan The serum concentration of Fimasartan can be increased when it is combined with Elexacaftor.
Paritaprevir The serum concentration of Paritaprevir can be increased when it is combined with Elexacaftor.
Selexipag The serum concentration of Selexipag can be increased when it is combined with Elexacaftor.
Grazoprevir The serum concentration of Grazoprevir can be increased when it is combined with Elexacaftor.
Elagolix The serum concentration of Elagolix can be increased when it is combined with Elexacaftor.
Voxilaprevir The serum concentration of Voxilaprevir can be increased when it is combined with Elexacaftor.
Levosalbutamol The serum concentration of Levosalbutamol can be increased when it is combined with Elexacaftor.
Glecaprevir The serum concentration of Glecaprevir can be increased when it is combined with Elexacaftor.
Remdesivir The serum concentration of Remdesivir can be increased when it is combined with Elexacaftor.
Belantamab mafodotin The serum concentration of Belantamab mafodotin can be increased when it is combined with Elexacaftor.
Fluvastatin The serum concentration of Fluvastatin can be increased when it is combined with Elexacaftor.
Metreleptin The metabolism of Elexacaftor can be increased when combined with Metreleptin.
Asunaprevir The serum concentration of Asunaprevir can be increased when it is combined with Elexacaftor.
Rifabutin The metabolism of Elexacaftor can be increased when combined with Rifabutin.
Felbamate The metabolism of Elexacaftor can be increased when combined with Felbamate.
Genistein The metabolism of Elexacaftor can be increased when combined with Genistein.
Oritavancin The metabolism of Elexacaftor can be increased when combined with Oritavancin.
Rufinamide The metabolism of Elexacaftor can be increased when combined with Rufinamide.
Armodafinil The metabolism of Elexacaftor can be increased when combined with Armodafinil.
Glycerol phenylbutyrate The metabolism of Elexacaftor can be increased when combined with Glycerol phenylbutyrate.
Eslicarbazepine acetate The metabolism of Elexacaftor can be increased when combined with Eslicarbazepine acetate.
Sarilumab The metabolism of Elexacaftor can be increased when combined with Sarilumab.
Lesinurad The metabolism of Elexacaftor can be increased when combined with Lesinurad.
Esketamine The metabolism of Elexacaftor can be increased when combined with Esketamine.
Cerivastatin The serum concentration of Cerivastatin can be increased when it is combined with Elexacaftor.
Calcitriol The metabolism of Elexacaftor can be increased when combined with Calcitriol.
Vitamin E The metabolism of Elexacaftor can be increased when combined with Vitamin E.
Flunisolide The metabolism of Elexacaftor can be increased when combined with Flunisolide.
Troglitazone The metabolism of Elexacaftor can be increased when combined with Troglitazone.
Butalbital The metabolism of Elexacaftor can be increased when combined with Butalbital.
Flucloxacillin The metabolism of Elexacaftor can be increased when combined with Flucloxacillin.
Acetaminophen The metabolism of Elexacaftor can be increased when combined with Acetaminophen.
Clobazam The metabolism of Elexacaftor can be increased when combined with Clobazam.
Aminoglutethimide The metabolism of Elexacaftor can be increased when combined with Aminoglutethimide.
Beclomethasone dipropionate The metabolism of Elexacaftor can be increased when combined with Beclomethasone dipropionate.
Griseofulvin The metabolism of Elexacaftor can be increased when combined with Griseofulvin.
Secobarbital The metabolism of Elexacaftor can be increased when combined with Secobarbital.
Betamethasone The metabolism of Elexacaftor can be increased when combined with Betamethasone.
Quinine The metabolism of Elexacaftor can be increased when combined with Quinine.
Chlorpromazine The metabolism of Elexacaftor can be increased when combined with Chlorpromazine.
Dicloxacillin The metabolism of Elexacaftor can be increased when combined with Dicloxacillin.
Rofecoxib The metabolism of Elexacaftor can be increased when combined with Rofecoxib.
Fluocinolone acetonide The metabolism of Elexacaftor can be increased when combined with Fluocinolone acetonide.
Medroxyprogesterone acetate The metabolism of Elexacaftor can be increased when combined with Medroxyprogesterone acetate.
Triamcinolone The metabolism of Elexacaftor can be increased when combined with Triamcinolone.
Testosterone The serum concentration of Testosterone can be increased when it is combined with Elexacaftor.
Clofibrate The metabolism of Elexacaftor can be increased when combined with Clofibrate.
Hydrocortisone The metabolism of Elexacaftor can be increased when combined with Hydrocortisone.
Hydrocortamate The metabolism of Elexacaftor can be increased when combined with Hydrocortamate.
Oxcarbazepine The metabolism of Elexacaftor can be increased when combined with Oxcarbazepine.
Phenylbutazone The metabolism of Elexacaftor can be increased when combined with Phenylbutazone.
Mifepristone The metabolism of Elexacaftor can be increased when combined with Mifepristone.
Methylphenobarbital The metabolism of Elexacaftor can be increased when combined with Methylphenobarbital.
Terbinafine The metabolism of Elexacaftor can be increased when combined with Terbinafine.
Prednisolone The metabolism of Elexacaftor can be increased when combined with Prednisolone.
Ethanol The metabolism of Elexacaftor can be increased when combined with Ethanol.
Norgestimate The metabolism of Elexacaftor can be increased when combined with Norgestimate.
Methylprednisolone The metabolism of Elexacaftor can be increased when combined with Methylprednisolone.
Metyrapone The metabolism of Elexacaftor can be increased when combined with Metyrapone.
Probenecid The metabolism of Elexacaftor can be increased when combined with Probenecid.
Nifedipine The metabolism of Elexacaftor can be decreased when combined with Nifedipine.
Sulfinpyrazone The metabolism of Elexacaftor can be increased when combined with Sulfinpyrazone.

Target Protein

Cystic fibrosis transmembrane conductance regulator CFTR

Referensi & Sumber

Artikel (PubMed)
  • PMID: 30334692
    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.
  • PMID: 30334693
    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.
  • PMID: 31218221
    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.
  • PMID: 28441669
    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.

Contoh Produk & Brand

Produk: 12 • International brands: 0
Produk
  • Kaftrio
    Tablet, film coated • - • Oral • EU • Approved
  • Kaftrio
    Granule • - • Oral • EU • Approved
  • Kaftrio
    Granule • - • Oral • EU • Approved
  • Kaftrio
    Tablet, film coated • - • Oral • EU • Approved
  • Trikafta
    Kit; Tablet, film coated • - • Oral • US • Approved
  • Trikafta
    Tablet • - • Oral • Canada • Approved
  • Trikafta
    Granule • - • Oral • Canada • Approved
  • Trikafta
    Granule • - • Oral • Canada • Approved
Menampilkan 8 dari 12 produk.

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