Ataluren

DB05016

small molecule approved investigational

Deskripsi

Ataluren is a novel, orally administered drug that targets nonsense mutations. Ataluren is approved for use by the European Medicines Agency to treat Duchenne Muscular Dystrophy in patients aged 5 years and older who are able to walk. More specifically, ataluren is used in the small group of patients whose disease is caused by a specific genetic defect (called a ‘nonsense mutation’) in the dystrophin gene.

This drug does not yet have approval by the US Food and Drug Administration or by Health Canada for any indications.

Struktur Molekul 2D

Berat 284.242
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) Ataluren plasma half-life ranges from 2-6 hours and is unaffected either by dose or repeated administration [L925].
Volume Distribusi -
Klirens (Clearance) -

Absorpsi

Peak plasma levels of ataluren are attained approximately 1.5 hours after dosing in subjects who received medicinal product within 30 minutes of a meal L925.

Metabolisme

Ataluren is metabolized by conjugation via uridine diphosphate glucuronosyltransferase (UGT) enzymes, predominantly UGT1A9 in liver and intestine. In vivo, the only metabolite detected in plasma after oral administration of radio-labelled ataluren was the ataluren-O-1?-acyl glucuronide; exposure to this metabolite in humans was approximately 8% of the plasma AUC of ataluren L925.

Rute Eliminasi

After a single oral dose of radiolabeled ataluren, approximately half of the administered radioactive dose is recovered in the faeces and the remainder was recovered in the urine. In the urine, unchanged ataluren and the acyl glucuronide metabolite account for less than 1% and 49%, respectively, of the administered dose L925.

Interaksi Obat

115 Data
Succinic acid The excretion of Succinic acid can be decreased when combined with Ataluren.
Citrulline The excretion of Citrulline can be decreased when combined with Ataluren.
Pravastatin The excretion of Pravastatin can be decreased when combined with Ataluren.
Oseltamivir The excretion of Oseltamivir can be decreased when combined with Ataluren.
Cefotiam The excretion of Cefotiam can be decreased when combined with Ataluren.
Conjugated estrogens The excretion of Conjugated estrogens can be decreased when combined with Ataluren.
Tenofovir disoproxil The excretion of Tenofovir disoproxil can be decreased when combined with Ataluren.
Piperacillin The excretion of Piperacillin can be decreased when combined with Ataluren.
Indomethacin The excretion of Indomethacin can be decreased when combined with Ataluren.
Aminohippuric acid The excretion of Aminohippuric acid can be decreased when combined with Ataluren.
Trifluridine The excretion of Trifluridine can be decreased when combined with Ataluren.
Allopurinol The excretion of Allopurinol can be decreased when combined with Ataluren.
Zidovudine The excretion of Zidovudine can be decreased when combined with Ataluren.
Cimetidine The excretion of Cimetidine can be decreased when combined with Ataluren.
Cefdinir The excretion of Cefdinir can be decreased when combined with Ataluren.
Methotrexate The excretion of Methotrexate can be decreased when combined with Ataluren.
Cephalexin The excretion of Cephalexin can be decreased when combined with Ataluren.
Valaciclovir The excretion of Valaciclovir can be decreased when combined with Ataluren.
Levocarnitine The excretion of Levocarnitine can be decreased when combined with Ataluren.
Leucovorin The excretion of Leucovorin can be decreased when combined with Ataluren.
Fluorescein The excretion of Fluorescein can be decreased when combined with Ataluren.
Hydrocortisone The excretion of Hydrocortisone can be decreased when combined with Ataluren.
Tetracycline The excretion of Tetracycline can be decreased when combined with Ataluren.
Estradiol The excretion of Estradiol can be decreased when combined with Ataluren.
Acyclovir The excretion of Acyclovir can be decreased when combined with Ataluren.
Cefaclor The excretion of Cefaclor can be decreased when combined with Ataluren.
Ranitidine The excretion of Ranitidine can be decreased when combined with Ataluren.
Quinapril The excretion of Quinapril can be decreased when combined with Ataluren.
Bumetanide The excretion of Bumetanide can be decreased when combined with Ataluren.
Dinoprostone The excretion of Dinoprostone can be decreased when combined with Ataluren.
Famotidine The excretion of Famotidine can be decreased when combined with Ataluren.
Fexofenadine The excretion of Fexofenadine can be decreased when combined with Ataluren.
Benzylpenicillin The excretion of Benzylpenicillin can be decreased when combined with Ataluren.
Rosuvastatin The excretion of Rosuvastatin can be decreased when combined with Ataluren.
Captopril The excretion of Captopril can be decreased when combined with Ataluren.
Sitagliptin The excretion of Sitagliptin can be decreased when combined with Ataluren.
Cefazolin The excretion of Cefazolin can be decreased when combined with Ataluren.
Ceftizoxime The excretion of Ceftizoxime can be decreased when combined with Ataluren.
Cefacetrile The excretion of Cefacetrile can be decreased when combined with Ataluren.
Ceftibuten The excretion of Ceftibuten can be decreased when combined with Ataluren.
Tazobactam The excretion of Tazobactam can be decreased when combined with Ataluren.
Cyclic adenosine monophosphate The excretion of Cyclic adenosine monophosphate can be decreased when combined with Ataluren.
Cholic Acid The excretion of Cholic Acid can be decreased when combined with Ataluren.
Glutaric Acid The excretion of Glutaric Acid can be decreased when combined with Ataluren.
Oxalic Acid The excretion of Oxalic Acid can be decreased when combined with Ataluren.
Taurocholic acid The excretion of Taurocholic acid can be decreased when combined with Ataluren.
Doripenem The excretion of Doripenem can be decreased when combined with Ataluren.
Saxagliptin The excretion of Saxagliptin can be decreased when combined with Ataluren.
Ellagic acid The excretion of Ellagic acid can be decreased when combined with Ataluren.
Cefaloridine The excretion of Cefaloridine can be decreased when combined with Ataluren.
Avibactam The excretion of Avibactam can be decreased when combined with Ataluren.
Eluxadoline The excretion of Eluxadoline can be decreased when combined with Ataluren.
Silibinin The excretion of Silibinin can be decreased when combined with Ataluren.
Tenofovir alafenamide The excretion of Tenofovir alafenamide can be decreased when combined with Ataluren.
Baricitinib The serum concentration of Baricitinib can be increased when it is combined with Ataluren.
Relebactam The excretion of Relebactam can be decreased when combined with Ataluren.
Tenofovir The excretion of Tenofovir can be decreased when combined with Ataluren.
Hydrochlorothiazide The excretion of Hydrochlorothiazide can be decreased when combined with Ataluren.
Dexamethasone The excretion of Dexamethasone can be decreased when combined with Ataluren.
Oxytetracycline The excretion of Oxytetracycline can be decreased when combined with Ataluren.
Polythiazide The excretion of Polythiazide can be decreased when combined with Ataluren.
Prednisolone phosphate The excretion of Prednisolone phosphate can be decreased when combined with Ataluren.
Dexamethasone acetate The excretion of Dexamethasone acetate can be decreased when combined with Ataluren.
Acamprosate The excretion of Acamprosate can be decreased when combined with Ataluren.
Pemetrexed Ataluren 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 Ataluren.
Valproic acid The excretion of Valproic acid can be decreased when combined with Ataluren.
Clofarabine The excretion of Clofarabine can be decreased when combined with Ataluren.
Grepafloxacin The excretion of Grepafloxacin can be decreased when combined with Ataluren.
Cidofovir The excretion of Cidofovir can be decreased when combined with Ataluren.
Stavudine The excretion of Stavudine can be decreased when combined with Ataluren.
Lamivudine The excretion of Lamivudine can be decreased when combined with Ataluren.
Adefovir dipivoxil The excretion of Adefovir dipivoxil can be decreased when combined with Ataluren.
Didanosine The excretion of Didanosine can be decreased when combined with Ataluren.
Zalcitabine The excretion of Zalcitabine can be decreased when combined with Ataluren.
Levofloxacin The excretion of Levofloxacin can be decreased when combined with Ataluren.
Valsartan The excretion of Valsartan can be decreased when combined with Ataluren.
Erythromycin The excretion of Erythromycin can be decreased when combined with Ataluren.
Liothyronine The excretion of Liothyronine can be decreased when combined with Ataluren.
Raloxifene The excretion of Raloxifene can be decreased when combined with Ataluren.
Caspofungin The excretion of Caspofungin can be decreased when combined with Ataluren.
Mycophenolate mofetil The excretion of Mycophenolate mofetil can be decreased when combined with Ataluren.
Atorvastatin The excretion of Atorvastatin can be decreased when combined with Ataluren.
Ouabain The excretion of Ouabain can be decreased when combined with Ataluren.
Fluvastatin The excretion of Fluvastatin can be decreased when combined with Ataluren.
Paclitaxel The excretion of Paclitaxel can be decreased when combined with Ataluren.
Docetaxel The excretion of Docetaxel can be decreased when combined with Ataluren.
Liotrix The excretion of Liotrix can be decreased when combined with Ataluren.
Simeprevir The excretion of Simeprevir can be decreased when combined with Ataluren.
Ambrisentan The excretion of Ambrisentan can be decreased when combined with Ataluren.
Cholecystokinin The excretion of Cholecystokinin can be decreased when combined with Ataluren.
Gadoxetic acid The excretion of Gadoxetic acid can be decreased when combined with Ataluren.
Technetium Tc-99m mebrofenin The excretion of Technetium Tc-99m mebrofenin can be decreased when combined with Ataluren.
Sincalide The excretion of Sincalide can be decreased when combined with Ataluren.
Paritaprevir The excretion of Paritaprevir can be decreased when combined with Ataluren.
Selexipag The excretion of Selexipag can be decreased when combined with Ataluren.
Grazoprevir The excretion of Grazoprevir can be decreased when combined with Ataluren.
Voxilaprevir The excretion of Voxilaprevir can be decreased when combined with Ataluren.
Letermovir The excretion of Letermovir can be decreased when combined with Ataluren.
Levosalbutamol The excretion of Levosalbutamol can be decreased when combined with Ataluren.

Target Protein

Dystrophin DMD

Referensi & Sumber

Artikel (PubMed)
  • PMID: 17450125
    Welch EM, Barton ER, Zhuo J, Tomizawa Y, Friesen WJ, Trifillis P, Paushkin S, Patel M, Trotta CR, Hwang S, Wilde RG, Karp G, Takasugi J, Chen G, Jones S, Ren H, Moon YC, Corson D, Turpoff AA, Campbell JA, Conn MM, Khan A, Almstead NG, Hedrick J, Mollin A, Risher N, Weetall M, Yeh S, Branstrom AA, Colacino JM, Babiak J, Ju WD, Hirawat S, Northcutt VJ, Miller LL, Spatrick P, He F, Kawana M, Feng H, Jacobson A, Peltz SW, Sweeney HL: PTC124 targets genetic disorders caused by nonsense mutations. Nature. 2007 May 3;447(7140):87-91. Epub 2007 Apr 22.
  • PMID: 17389552
    Hirawat S, Welch EM, Elfring GL, Northcutt VJ, Paushkin S, Hwang S, Leonard EM, Almstead NG, Ju W, Peltz SW, Miller LL: Safety, tolerability, and pharmacokinetics of PTC124, a nonaminoglycoside nonsense mutation suppressor, following single- and multiple-dose administration to healthy male and female adult volunteers. J Clin Pharmacol. 2007 Apr;47(4):430-44.
  • PMID: 17096300
    Hamed SA: Drug evaluation: PTC-124--a potential treatment of cystic fibrosis and Duchenne muscular dystrophy. IDrugs. 2006 Nov;9(11):783-9.
  • PMID: 27702906
    Roy B, Friesen WJ, Tomizawa Y, Leszyk JD, Zhuo J, Johnson B, Dakka J, Trotta CR, Xue X, Mutyam V, Keeling KM, Mobley JA, Rowe SM, Bedwell DM, Welch EM, Jacobson A: Ataluren stimulates ribosomal selection of near-cognate tRNAs to promote nonsense suppression. Proc Natl Acad Sci U S A. 2016 Nov 1;113(44):12508-12513. Epub 2016 Oct 4.
  • PMID: 27791186
    Siddiqui N, Sonenberg N: Proposing a mechanism of action for ataluren. Proc Natl Acad Sci U S A. 2016 Nov 1;113(44):12353-12355. Epub 2016 Oct 19.

Contoh Produk & Brand

Produk: 3 • International brands: 0
Produk
  • Translarna
    Granule • 125 mg • Oral • EU • Approved
  • Translarna
    Granule • 250 mg • Oral • EU • Approved
  • Translarna
    Granule • 1000 mg • Oral • EU • Approved

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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