Peringatan Keamanan

The LD50 for the oral dose is 5200 mg/kg (mouse); Oral TDLO (woman): 0.12 mg/kgMSDS

A note on altered endocrine function and immunosuppression

Deflazacort, as a steroid prodrug used over a long-term period, can cause hormone imbalance leading to diseases such as Cushing's Syndrome and hypothalamic-pituitary-adrenal axis suppression. It can also predispose to infection, as it promotes immunosuppression.A179464 It is important to monitor for hormonal imbalance and infection and provide necessary treatment if they occur.FDA label

Mutagenicity/carcinogenicity

Mutagenicity assays were negative in various laboratory and in vivo assays performed on rats.FDA label,L6703 Chronic use in mice for 2 years in one study resulted in a higher rate of osteoma and osteosarcomas in mice receiving 0.06, 0.12, 0.25, 0.50, or 1.0 mg/kg of deflazacort daily.FDA label

Use in pregnancy

There are no sufficient data to support the administration of deflazacort during pregnancy. Corticosteroid drugs such as deflazacort should only be used during pregnancy only if the benefits of therapy outweigh the potential risks.FDA label,L6703

Use in lactation

Corticosteroids, when administered systemically, are excreted in the breastmilk. Exposure may lead to disturbances in bone development and growth and endocrine disturbances in the exposed infant.FDA label,L6703

Deflazacort

DB11921

small molecule approved investigational

Deskripsi

Deflazacort, also known as Emflaza, is a corticosteroid prodrug used as an agent to manage Duchenne Muscular Dystrophy (DMD). It is marketed by Marathon Pharmaceuticals and was approved in February 2017 by the FDA.L6694,FDA label

Duchenne Muscular Dystrophy is an inherited disorder resulting from mutations of the dystrophin gene, which is important for muscle function. This disease can cause serious muscle weakness and progressive breathing and cardiovascular disability, severely impacting patient quality of life and survival.A179446,A179449,L6697 This disease usually manifests by muscle weakness in early childhood followed by loss of the ability to walk (ambulation) as early as age 7.A179449

Deflazacort delays the onset of muscle related complications resulting from DMDA179455, prolonging the lives of children diagnosed with this disease and exerting less harmful effects on the bone health and weight than other steroid medications.A179452,A25340

Struktur Molekul 2D

Berat 441.524
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 deflazacort ranges from 1.1 to 1.9 h [A18725,L6703]
Volume Distribusi One study determined the volume of distribution to be 204 ± 84 L.[A18725]
Klirens (Clearance) 114 ±27 L/h, according to one noncompartmental pharmacokinetic study.[A18725] The clearance of corticosteroids is enhanced in hypothyroid patients and increased in patients with hyperthyroidism. Dosing adjustments may be considered according to thyroid status.[FDA label] A study of corticosteroid clearance was performed in patients with a creatinine clearance of 15 mL/min or less, and determined that the active metabolite of deflazacort, 21-deflazacort was similar to that in patients with normal renal clearance.[FDA label]

Absorpsi

Deflazacort is rapidly absorbed after oral administration with peak concentration occurring within 1-2 hours.A179464,FDA label One pharmacokinetic study determined an AUC (area under the curve) of 280 ng/ml · h.A18725 The bioavailability of both the oral suspension and tablet are similar.FDA label In clinical studies, coadministration of deflazacort crushed with food or applesauce did not affect absorption or bioavailability.FDA label

Metabolisme

After oral ingestion, deflazacort is deacetylated at position 21 by plasma esterases, producing the active metabolite 21-deflazacort.A18725,A179464,FDA label,L6703 21-deflazacort is then further metabolized by CYP3A4 to inactive metabolite products.FDA label,A179473 Deflazacort 21-OH metabolism is extensive. The metabolite of deflazacort-21-OH is deflazacort 6-beta-OH.A179473,L6703

Rute Eliminasi

Urinary excretion is the major route of deflazacort elimination, accounting for about about 70% of the excreted dose.A18725 The remainder of the dose (about 30%) is excreted in the fecesA18725. Elimination is almost completed by 24 hours post-dose.A179467 21-deflazacort makes up about 18% of the eliminated drug in the urine.FDA label

Interaksi Makanan

3 Data
  • 1. Avoid grapefruit products. Grapefruit inhibits CYP3A metabolism, which may increase the serum concentration of deflazacort.
  • 2. Avoid St. John's Wort. This herb induces CYP3A metabolism and may reduce serum levels of deflazacort.
  • 3. Take with or without food. The tablets may be crushed and mixed with applesauce and consumed immediately.

Interaksi Obat

1131 Data
Denosumab The risk or severity of adverse effects can be increased when Denosumab is combined with Deflazacort.
Peginterferon alfa-2a The risk or severity of adverse effects can be increased when Peginterferon alfa-2a is combined with Deflazacort.
Interferon alfa-n1 The risk or severity of adverse effects can be increased when Interferon alfa-n1 is combined with Deflazacort.
Interferon alfa-n3 The risk or severity of adverse effects can be increased when Interferon alfa-n3 is combined with Deflazacort.
Peginterferon alfa-2b The risk or severity of adverse effects can be increased when Peginterferon alfa-2b is combined with Deflazacort.
Interferon gamma-1b The risk or severity of adverse effects can be increased when Interferon gamma-1b is combined with Deflazacort.
Interferon alfa-2a The risk or severity of adverse effects can be increased when Interferon alfa-2a is combined with Deflazacort.
Gemtuzumab ozogamicin The risk or severity of adverse effects can be increased when Gemtuzumab ozogamicin is combined with Deflazacort.
Pegaspargase The serum concentration of Deflazacort can be increased when it is combined with Pegaspargase.
Interferon beta-1b The risk or severity of adverse effects can be increased when Interferon beta-1b is combined with Deflazacort.
Interferon alfacon-1 The risk or severity of adverse effects can be increased when Interferon alfacon-1 is combined with Deflazacort.
Rituximab The risk or severity of adverse effects can be increased when Rituximab is combined with Deflazacort.
Basiliximab The risk or severity of adverse effects can be increased when Basiliximab is combined with Deflazacort.
Muromonab The risk or severity of adverse effects can be increased when Muromonab is combined with Deflazacort.
Ibritumomab tiuxetan The risk or severity of adverse effects can be increased when Ibritumomab tiuxetan is combined with Deflazacort.
Tositumomab The risk or severity of adverse effects can be increased when Tositumomab is combined with Deflazacort.
Alemtuzumab The risk or severity of adverse effects can be increased when Alemtuzumab is combined with Deflazacort.
Alefacept The risk or severity of adverse effects can be increased when Alefacept is combined with Deflazacort.
Efalizumab The risk or severity of adverse effects can be increased when Efalizumab is combined with Deflazacort.
Antithymocyte immunoglobulin (rabbit) The risk or severity of adverse effects can be increased when Antithymocyte immunoglobulin (rabbit) is combined with Deflazacort.
Interferon alfa-2b The risk or severity of adverse effects can be increased when Interferon alfa-2b is combined with Deflazacort.
Daclizumab The risk or severity of adverse effects can be increased when Daclizumab is combined with Deflazacort.
Phenylalanine The risk or severity of adverse effects can be increased when Phenylalanine is combined with Deflazacort.
Cladribine Deflazacort may increase the immunosuppressive activities of Cladribine.
Carmustine The risk or severity of adverse effects can be increased when Carmustine is combined with Deflazacort.
Amsacrine The risk or severity of adverse effects can be increased when Amsacrine is combined with Deflazacort.
Bleomycin The risk or severity of adverse effects can be increased when Bleomycin is combined with Deflazacort.
Chlorambucil The risk or severity of adverse effects can be increased when Chlorambucil is combined with Deflazacort.
Raltitrexed The risk or severity of adverse effects can be increased when Raltitrexed is combined with Deflazacort.
Mitomycin The risk or severity of adverse effects can be increased when Mitomycin is combined with Deflazacort.
Floxuridine The risk or severity of adverse effects can be increased when Floxuridine is combined with Deflazacort.
Tioguanine The risk or severity of adverse effects can be increased when Tioguanine is combined with Deflazacort.
Dexrazoxane The risk or severity of adverse effects can be increased when Dexrazoxane is combined with Deflazacort.
Streptozocin The risk or severity of adverse effects can be increased when Streptozocin is combined with Deflazacort.
Trifluridine The risk or severity of adverse effects can be increased when Trifluridine is combined with Deflazacort.
Gemcitabine The risk or severity of adverse effects can be increased when Gemcitabine is combined with Deflazacort.
Epirubicin The risk or severity of adverse effects can be increased when Epirubicin is combined with Deflazacort.
Chloramphenicol The risk or severity of adverse effects can be increased when Chloramphenicol is combined with Deflazacort.
Lenalidomide The risk or severity of adverse effects can be increased when Lenalidomide is combined with Deflazacort.
Altretamine The risk or severity of adverse effects can be increased when Altretamine is combined with Deflazacort.
Zidovudine The risk or severity of adverse effects can be increased when Zidovudine is combined with Deflazacort.
Oxaliplatin The risk or severity of adverse effects can be increased when Oxaliplatin is combined with Deflazacort.
Fluorouracil The risk or severity of adverse effects can be increased when Fluorouracil is combined with Deflazacort.
Propylthiouracil The risk or severity of adverse effects can be increased when Propylthiouracil is combined with Deflazacort.
Pentostatin The risk or severity of adverse effects can be increased when Pentostatin is combined with Deflazacort.
Linezolid The risk or severity of adverse effects can be increased when Linezolid is combined with Deflazacort.
Clofarabine The risk or severity of adverse effects can be increased when Clofarabine is combined with Deflazacort.
Pemetrexed The risk or severity of adverse effects can be increased when Pemetrexed is combined with Deflazacort.
Mycophenolate mofetil The risk or severity of adverse effects can be increased when Mycophenolate mofetil is combined with Deflazacort.
Dacarbazine The risk or severity of adverse effects can be increased when Dacarbazine is combined with Deflazacort.
Temozolomide The risk or severity of adverse effects can be increased when Temozolomide is combined with Deflazacort.
Penicillamine The risk or severity of adverse effects can be increased when Penicillamine is combined with Deflazacort.
Azacitidine The risk or severity of adverse effects can be increased when Azacitidine is combined with Deflazacort.
Carboplatin The risk or severity of adverse effects can be increased when Carboplatin is combined with Deflazacort.
Dactinomycin The risk or severity of adverse effects can be increased when Dactinomycin is combined with Deflazacort.
Azathioprine The risk or severity of adverse effects can be increased when Azathioprine is combined with Deflazacort.
Hydroxyurea The risk or severity of adverse effects can be increased when Hydroxyurea is combined with Deflazacort.
Mycophenolic acid The risk or severity of adverse effects can be increased when Mycophenolic acid is combined with Deflazacort.
Topotecan The risk or severity of adverse effects can be increased when Topotecan is combined with Deflazacort.
Mercaptopurine The risk or severity of adverse effects can be increased when Mercaptopurine is combined with Deflazacort.
Thalidomide The risk or severity of adverse effects can be increased when Thalidomide is combined with Deflazacort.
Melphalan The risk or severity of adverse effects can be increased when Melphalan is combined with Deflazacort.
Fludarabine The risk or severity of adverse effects can be increased when Fludarabine is combined with Deflazacort.
Flucytosine The risk or severity of adverse effects can be increased when Flucytosine is combined with Deflazacort.
Capecitabine The risk or severity of adverse effects can be increased when Capecitabine is combined with Deflazacort.
Procarbazine The risk or severity of adverse effects can be increased when Procarbazine is combined with Deflazacort.
Arsenic trioxide The risk or severity of adverse effects can be increased when Arsenic trioxide is combined with Deflazacort.
Idarubicin The risk or severity of adverse effects can be increased when Idarubicin is combined with Deflazacort.
Estramustine The risk or severity of adverse effects can be increased when Estramustine is combined with Deflazacort.
Mitoxantrone The risk or severity of adverse effects can be increased when Mitoxantrone is combined with Deflazacort.
Lomustine The risk or severity of adverse effects can be increased when Lomustine is combined with Deflazacort.
Eculizumab The risk or severity of adverse effects can be increased when Eculizumab is combined with Deflazacort.
Decitabine The risk or severity of adverse effects can be increased when Decitabine is combined with Deflazacort.
Nelarabine The risk or severity of adverse effects can be increased when Nelarabine is combined with Deflazacort.
Stepronin The risk or severity of adverse effects can be increased when Stepronin is combined with Deflazacort.
Hydroxychloroquine The risk or severity of adverse effects can be increased when Hydroxychloroquine is combined with Deflazacort.
Castanospermine The risk or severity of adverse effects can be increased when Castanospermine is combined with Deflazacort.
Vorinostat The risk or severity of adverse effects can be increased when Vorinostat is combined with Deflazacort.
2-Methoxyethanol The risk or severity of adverse effects can be increased when 2-Methoxyethanol is combined with Deflazacort.
Brequinar The risk or severity of adverse effects can be increased when Brequinar is combined with Deflazacort.
Pirfenidone The risk or severity of adverse effects can be increased when Pirfenidone is combined with Deflazacort.
Interferon alfa The risk or severity of adverse effects can be increased when Interferon alfa is combined with Deflazacort.
Glatiramer The risk or severity of adverse effects can be increased when Glatiramer is combined with Deflazacort.
Briakinumab The risk or severity of adverse effects can be increased when Briakinumab is combined with Deflazacort.
Human interferon omega-1 The risk or severity of adverse effects can be increased when Human interferon omega-1 is combined with Deflazacort.
Mepolizumab The risk or severity of adverse effects can be increased when Mepolizumab is combined with Deflazacort.
Abetimus The risk or severity of adverse effects can be increased when Abetimus is combined with Deflazacort.
Belatacept The risk or severity of adverse effects can be increased when Belatacept is combined with Deflazacort.
Bendamustine The risk or severity of adverse effects can be increased when Bendamustine is combined with Deflazacort.
Pralatrexate The risk or severity of adverse effects can be increased when Pralatrexate is combined with Deflazacort.
Wortmannin The risk or severity of adverse effects can be increased when Wortmannin is combined with Deflazacort.
Eribulin The risk or severity of adverse effects can be increased when Eribulin is combined with Deflazacort.
Belimumab The risk or severity of adverse effects can be increased when Belimumab is combined with Deflazacort.
Teriflunomide The risk or severity of adverse effects can be increased when Teriflunomide is combined with Deflazacort.
Carfilzomib The risk or severity of adverse effects can be increased when Carfilzomib is combined with Deflazacort.
Dimethyl fumarate The risk or severity of adverse effects can be increased when Dimethyl fumarate is combined with Deflazacort.
Obinutuzumab The risk or severity of adverse effects can be increased when Obinutuzumab is combined with Deflazacort.
Vedolizumab The risk or severity of adverse effects can be increased when Vedolizumab is combined with Deflazacort.
Blinatumomab The risk or severity of adverse effects can be increased when Blinatumomab is combined with Deflazacort.
Dinutuximab The risk or severity of adverse effects can be increased when Dinutuximab is combined with Deflazacort.

Target Protein

Glucocorticoid receptor NR3C1

Referensi & Sumber

Artikel (PubMed)
  • PMID: 7494809
    Mollmann H, Hochhaus G, Rohatagi S, Barth J, Derendorf H: Pharmacokinetic/pharmacodynamic evaluation of deflazacort in comparison to methylprednisolone and prednisolone. Pharm Res. 1995 Jul;12(7):1096-100.
  • PMID: 25212041
    Ding W, Ding L, Li WB, Pan H, Lin HD: Pharmacokinetics of deflazacort tablets in healthy Chinese volunteers. Yao Xue Xue Bao. 2014 Jun;49(6):921-6.
  • PMID: 26457695
    Falzarano MS, Scotton C, Passarelli C, Ferlini A: Duchenne Muscular Dystrophy: From Diagnosis to Therapy. Molecules. 2015 Oct 7;20(10):18168-84. doi: 10.3390/molecules201018168.
  • PMID: 26140716
    Gao QQ, McNally EM: The Dystrophin Complex: Structure, Function, and Implications for Therapy. Compr Physiol. 2015 Jul 1;5(3):1223-39. doi: 10.1002/cphy.c140048.
  • PMID: 20083885
    Joshi N, Rajeshwari K: Deflazacort. J Postgrad Med. 2009 Oct-Dec;55(4):296-300. doi: 10.4103/0022-3859.58942.
  • PMID: 22655512
    McAdam LC, Mayo AL, Alman BA, Biggar WD: The Canadian experience with long-term deflazacort treatment in Duchenne muscular dystrophy. Acta Myol. 2012 May;31(1):16-20.
  • PMID: 10912543
    Ferraris JR, Pasqualini T, Legal S, Sorroche P, Galich AM, Pennisi P, Domene H, Jasper H: Effect of deflazacort versus methylprednisone on growth, body composition, lipid profile, and bone mass after renal transplantation. The Deflazacort Study Group. Pediatr Nephrol. 2000 Jul;14(7):682-8.
  • PMID: 18279756
    Houde S, Filiatrault M, Fournier A, Dube J, D'Arcy S, Berube D, Brousseau Y, Lapierre G, Vanasse M: Deflazacort use in Duchenne muscular dystrophy: an 8-year follow-up. Pediatr Neurol. 2008 Mar;38(3):200-6. doi: 10.1016/j.pediatrneurol.2007.11.001.
Menampilkan 8 dari 13 artikel.

Contoh Produk & Brand

Produk: 15 • International brands: 7
Produk
  • Deflazacort
    Tablet • 6 mg/1 • Oral • US • Generic • Approved
  • Deflazacort
    Tablet • 18 mg/1 • Oral • US • Generic • Approved
  • Deflazacort
    Tablet • 30 mg/1 • Oral • US • Generic • Approved
  • Deflazacort
    Tablet • 36 mg/1 • Oral • US • Generic • Approved
  • Deflazacort Oral Suspension
    Suspension • 22.75 mg/1mL • Oral • US • Generic • Approved
  • Emflaza
    Tablet • 6 mg/1 • Oral • US • Approved
  • Emflaza
    Tablet • 18 mg/1 • Oral • US • Approved
  • Emflaza
    Tablet • 30 mg/1 • Oral • US • Approved
Menampilkan 8 dari 15 produk.
International Brands
  • Calcort — Shire
  • Cortax
  • Decortil
  • Deflanil
  • MOAID
  • Xalcort — Beacon Pharmaceuticals Limited
  • Zamen

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