Peringatan Keamanan

Data regarding overdoses of tafamidis are not readily available.L11280 In a clinical trial, some patients were given up to 6 times the normal dose with one reported case of mild hordeolum.L11280

Tafamidis

DB11644

small molecule approved investigational

Deskripsi

Tafamidis and tafamidis meglumine (FX-1006A) are benzoxazole derivativesA27206 developed by FoldRX.A189717 Tafamidis is structurally similar to diflusinal.A189717

Tafamidis was granted an EMA market authorisation on 16 November 2011L6247 and FDA approval on 3 May 2019.L11280

Struktur Molekul 2D

Berat 308.116
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The half life of tafamidis is 49h.[L11280]
Volume Distribusi The apparent volume of distribution at steady state is 18.5L.[L11280]
Klirens (Clearance) The oral clearance of tafamidis is 0.263L/h.[L11280] The apparent total clearance is 0.44L/h.[A27206]

Absorpsi

Tafamidis reaches a Cmax of 1430.93ng/mL with a Tmax of 1.75h fasted and 4h fed.A27206 The AUC of tafamidis is 47,864.31ng\*h/mL.A27206

Metabolisme

Tafamidis is largely not subject to first pass or oxidative metabolism, being 90% unchanged after in in vitro experiments.A189744 Preclinical data suggest tafamidis is mainly metabolized through glucuronidation and excreted in bile.L11280

Rute Eliminasi

A 20mg oral dose of tafamidis is approximately 59% recovered in the feces, largely as unchanged drug.L11280 Approximately 22% of a 20mg oral dose is recovered in the urine, mostly as the glucuronide metabolite.L11280

Interaksi Makanan

1 Data
  • 1. Take with or without food.

Interaksi Obat

170 Data
Succinic acid The excretion of Succinic acid can be decreased when combined with Tafamidis.
Citrulline The excretion of Citrulline can be decreased when combined with Tafamidis.
Oseltamivir The excretion of Oseltamivir can be decreased when combined with Tafamidis.
Cefotiam The excretion of Cefotiam can be decreased when combined with Tafamidis.
Tenofovir disoproxil The excretion of Tenofovir disoproxil can be decreased when combined with Tafamidis.
Piperacillin The excretion of Piperacillin can be decreased when combined with Tafamidis.
Indomethacin The excretion of Indomethacin can be decreased when combined with Tafamidis.
Aminohippuric acid The excretion of Aminohippuric acid can be decreased when combined with Tafamidis.
Trifluridine The excretion of Trifluridine can be decreased when combined with Tafamidis.
Cimetidine The excretion of Cimetidine can be decreased when combined with Tafamidis.
Cefdinir The excretion of Cefdinir can be decreased when combined with Tafamidis.
Cephalexin The excretion of Cephalexin can be decreased when combined with Tafamidis.
Valaciclovir The excretion of Valaciclovir can be decreased when combined with Tafamidis.
Levocarnitine The excretion of Levocarnitine can be decreased when combined with Tafamidis.
Oxytetracycline The excretion of Oxytetracycline can be decreased when combined with Tafamidis.
Leucovorin The excretion of Leucovorin can be decreased when combined with Tafamidis.
Fluorescein The excretion of Fluorescein can be decreased when combined with Tafamidis.
Hydrocortisone The excretion of Hydrocortisone can be decreased when combined with Tafamidis.
Tetracycline The excretion of Tetracycline can be decreased when combined with Tafamidis.
Estradiol The excretion of Estradiol can be decreased when combined with Tafamidis.
Acyclovir The excretion of Acyclovir can be decreased when combined with Tafamidis.
Cefaclor The excretion of Cefaclor can be decreased when combined with Tafamidis.
Ranitidine The excretion of Ranitidine can be decreased when combined with Tafamidis.
Quinapril The excretion of Quinapril can be decreased when combined with Tafamidis.
Bumetanide The excretion of Bumetanide can be decreased when combined with Tafamidis.
Dinoprostone The excretion of Dinoprostone can be decreased when combined with Tafamidis.
Famotidine The excretion of Famotidine can be decreased when combined with Tafamidis.
Fexofenadine The excretion of Fexofenadine can be decreased when combined with Tafamidis.
Hydrochlorothiazide The excretion of Hydrochlorothiazide can be decreased when combined with Tafamidis.
Benzylpenicillin The excretion of Benzylpenicillin can be decreased when combined with Tafamidis.
Captopril The excretion of Captopril can be decreased when combined with Tafamidis.
Dexamethasone The excretion of Dexamethasone can be decreased when combined with Tafamidis.
Sitagliptin The excretion of Sitagliptin can be decreased when combined with Tafamidis.
Polythiazide The excretion of Polythiazide can be decreased when combined with Tafamidis.
Cefazolin The excretion of Cefazolin can be decreased when combined with Tafamidis.
Ceftizoxime The excretion of Ceftizoxime can be decreased when combined with Tafamidis.
Cefacetrile The excretion of Cefacetrile can be decreased when combined with Tafamidis.
Ceftibuten The excretion of Ceftibuten can be decreased when combined with Tafamidis.
Tazobactam The excretion of Tazobactam can be decreased when combined with Tafamidis.
Cyclic adenosine monophosphate The excretion of Cyclic adenosine monophosphate can be decreased when combined with Tafamidis.
Cholic Acid The excretion of Cholic Acid can be decreased when combined with Tafamidis.
Glutaric Acid The excretion of Glutaric Acid can be decreased when combined with Tafamidis.
Oxalic Acid The excretion of Oxalic Acid can be decreased when combined with Tafamidis.
Taurocholic acid The excretion of Taurocholic acid can be decreased when combined with Tafamidis.
Doripenem The excretion of Doripenem can be decreased when combined with Tafamidis.
Saxagliptin The excretion of Saxagliptin can be decreased when combined with Tafamidis.
Ellagic acid The excretion of Ellagic acid can be decreased when combined with Tafamidis.
Cefaloridine The excretion of Cefaloridine can be decreased when combined with Tafamidis.
Avibactam The excretion of Avibactam can be decreased when combined with Tafamidis.
Eluxadoline The excretion of Eluxadoline can be decreased when combined with Tafamidis.
Silibinin The excretion of Silibinin can be decreased when combined with Tafamidis.
Baricitinib The serum concentration of Baricitinib can be increased when it is combined with Tafamidis.
Relebactam The excretion of Relebactam can be decreased when combined with Tafamidis.
Tenofovir The excretion of Tenofovir can be decreased when combined with Tafamidis.
Prednisolone phosphate The excretion of Prednisolone phosphate can be decreased when combined with Tafamidis.
Dexamethasone acetate The excretion of Dexamethasone acetate can be decreased when combined with Tafamidis.
Acamprosate The excretion of Acamprosate can be decreased when combined with Tafamidis.
Valproic acid The excretion of Valproic acid can be decreased when combined with Tafamidis.
Pemetrexed Tafamidis may decrease the excretion rate of Pemetrexed which could result in a higher serum level.
Mercaptopurine The excretion of Mercaptopurine can be decreased when combined with Tafamidis.
Grepafloxacin The excretion of Grepafloxacin can be decreased when combined with Tafamidis.
Cidofovir The excretion of Cidofovir can be decreased when combined with Tafamidis.
Stavudine The excretion of Stavudine can be decreased when combined with Tafamidis.
Adefovir dipivoxil The excretion of Adefovir dipivoxil can be decreased when combined with Tafamidis.
Didanosine The excretion of Didanosine can be decreased when combined with Tafamidis.
Zalcitabine The excretion of Zalcitabine can be decreased when combined with Tafamidis.
Levofloxacin The excretion of Levofloxacin can be decreased when combined with Tafamidis.
Folic acid The serum concentration of Folic acid can be increased when it is combined with Tafamidis.
Pravastatin The serum concentration of Pravastatin can be increased when it is combined with Tafamidis.
Conjugated estrogens The serum concentration of Conjugated estrogens can be increased when it is combined with Tafamidis.
Gefitinib The serum concentration of Gefitinib can be increased when it is combined with Tafamidis.
Allopurinol The serum concentration of Allopurinol can be increased when it is combined with Tafamidis.
Cerivastatin The serum concentration of Cerivastatin can be increased when it is combined with Tafamidis.
Teniposide The serum concentration of Teniposide can be increased when it is combined with Tafamidis.
Prazosin The serum concentration of Prazosin can be increased when it is combined with Tafamidis.
Raloxifene The serum concentration of Raloxifene can be increased when it is combined with Tafamidis.
Celecoxib The serum concentration of Celecoxib can be increased when it is combined with Tafamidis.
Zidovudine The serum concentration of Zidovudine can be increased when it is combined with Tafamidis.
Ritonavir The serum concentration of Ritonavir can be increased when it is combined with Tafamidis.
Oxaliplatin The serum concentration of Oxaliplatin can be increased when it is combined with Tafamidis.
Vincristine The serum concentration of Vincristine can be increased when it is combined with Tafamidis.
Fluorouracil The serum concentration of Fluorouracil can be increased when it is combined with Tafamidis.
Methotrexate The serum concentration of Methotrexate can be increased when it is combined with Tafamidis.
Ivermectin The serum concentration of Ivermectin can be increased when it is combined with Tafamidis.
Imatinib The serum concentration of Imatinib can be increased when it is combined with Tafamidis.
Testosterone The serum concentration of Testosterone can be increased when it is combined with Tafamidis.
Clofarabine The serum concentration of Clofarabine can be increased when it is combined with Tafamidis.
Sumatriptan The serum concentration of Sumatriptan can be increased when it is combined with Tafamidis.
Tamoxifen The serum concentration of Tamoxifen can be increased when it is combined with Tafamidis.
Mycophenolate mofetil The serum concentration of Mycophenolate mofetil can be increased when it is combined with Tafamidis.
Daunorubicin The serum concentration of Daunorubicin can be increased when it is combined with Tafamidis.
Nitrofurantoin The serum concentration of Nitrofurantoin can be increased when it is combined with Tafamidis.
Lamivudine The serum concentration of Lamivudine can be increased when it is combined with Tafamidis.
Riluzole The serum concentration of Riluzole can be increased when it is combined with Tafamidis.
Irinotecan The serum concentration of Irinotecan can be increased when it is combined with Tafamidis.
Etoposide The serum concentration of Etoposide can be increased when it is combined with Tafamidis.
Sulfasalazine The serum concentration of Sulfasalazine can be increased when it is combined with Tafamidis.
Donepezil The serum concentration of Donepezil can be increased when it is combined with Tafamidis.
Dactinomycin The serum concentration of Dactinomycin can be increased when it is combined with Tafamidis.
Ezetimibe The serum concentration of Ezetimibe can be increased when it is combined with Tafamidis.

Target Protein

Transthyretin TTR

Referensi & Sumber

Artikel (PubMed)
  • PMID: 26894299
    Coelho T, Merlini G, Bulawa CE, Fleming JA, Judge DP, Kelly JW, Maurer MS, Plante-Bordeneuve V, Labaudiniere R, Mundayat R, Riley S, Lombardo I, Huertas P: Mechanism of Action and Clinical Application of Tafamidis in Hereditary Transthyretin Amyloidosis. Neurol Ther. 2016 Jun;5(1):1-25. doi: 10.1007/s40120-016-0040-x. Epub 2016 Feb 19.
  • PMID: 31913401
    Gurwitz JH, Maurer MS: Tafamidis-A Pricey Therapy for a Not-So-Rare Condition. JAMA Cardiol. 2020 Jan 8. pii: 2758314. doi: 10.1001/jamacardio.2019.5233.
  • PMID: 31735731
    Endo J, Sano M, Izumiya Y, Tsujita K, Nakamura K, Tahara N, Kuwahara K, Inomata T, Ueda M, Sekijima Y, Ando Y, Tsutsui H, Isobe M, Fukuda K: A Statement on the Appropriate Administration of Tafamidis in Patients With Transthyretin Cardiac Amyloidosis. Circ J. 2019 Dec 25;84(1):15-17. doi: 10.1253/circj.CJ-19-0811. Epub 2019 Nov 16.
  • PMID: 19816426
    Ratner M: Spotlight focuses on protein-misfolding therapies. Nat Biotechnol. 2009 Oct;27(10):874. doi: 10.1038/nbt1009-874c.
  • PMID: 28803538
    Lee KR, Jeong JW, Hyun HC, Jang E, Ahn S, Choi S, Joo SH, Kim S, Koo TS: Pharmacokinetics of tafamidis, a transthyretin amyloidosis drug, in rats. Xenobiotica. 2018 Aug;48(8):831-838. doi: 10.1080/00498254.2017.1366575. Epub 2017 Nov 16.

Contoh Produk & Brand

Produk: 9 • International brands: 0
Produk
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    Capsule, liquid filled • 61 mg/1 • Oral • US • Approved
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  • Vyndaqel
    Capsule • 20 mg • Oral • EU • Approved
  • Vyndaqel
    Capsule • 20 mg • Oral • EU • Approved
  • Vyndaqel
    Capsule • 20 mg • Oral • Canada • Approved
  • Vyndaqel
    Capsule, liquid filled • 20 mg/1 • Oral • US • Approved
  • Vyndaqel
    Capsule • 61 mg • Oral • EU • Approved
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Menampilkan 8 dari 9 produk.

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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