Peringatan Keamanan

Oral and intravenous LD50 in rats are 1915 mg/kg and 631 mg/kg, respectively.L43962 There is limited information on the acute toxicity of edaravone.

Edaravone

DB12243

small molecule approved investigational

Deskripsi

Edaravone is a free radical scavenger and neuroprotective agent with antioxidant properties.A254257 It has three tautomers.A19140 Edaravone works to scavenge reactive oxygen species, which have been implicated in neurological disorders, such as amyotrophic lateral sclerosis (ALS) and cerebral ischemia.A19140,L44007,A254257

The intravenous formulation of edaravone was first approved in Japan in 2001 for the treatment of acute ischemic stroke.L44007 It was later approved for the treatment of amyotrophic lateral sclerosis (ALS) in Japan and South Korea in 2015, followed by the FDA approval in May 2017 L41810 and Health Canada approval in October 2018.L44007 The oral suspension formulation of edaravone was approved by the FDA in May 2022 and by Health Canada in November 2022.L44017

Edaravone was initially granted orphan designation by the European Medicines Agency on June 19, 2015 L44007 and was under regulatory review in Europe. However, the drug manufacturer, Mitsubishi Tanabe Pharma, withdrew the Marketing Authorization Application (MAA) for edaravone from the European market on May 24, 2019, in response to the request made by the Committee for Medicinal Products for Human Use (CHMP) for a long-term study demonstrating the long-term efficacy and safety of edaravone.L44002,L44012 Edaravone was also investigated in other disorders, such as Alzheimer's disease,A19138 neuropathic pain, and ischemia-induced nerve injury.A19139

Struktur Molekul 2D

Berat 174.203
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 elimination half-life of edaravone is approximately 4.5 to nine hours. The half-lives of its metabolites range from three to six hours.[L41810]
Volume Distribusi After intravenous administration, edaravone has a mean volume of distribution of 63.1 L, suggesting substantial tissue distribution. Edaravone has an apparent volume of distribution of 164 L following oral administration.[L43952] Edaravone readily crosses the blood-brain barrier.[A19141]
Klirens (Clearance) Following intravenous administration, the total clearance of edaravone is estimated to be 35.9 L/h.[L41810] The apparent total clearance of edaravone is estimated to be 67.9L/h following oral administration.[L43952]

Absorpsi

One study investigated the absorption of edaravone in healthy adults, who either received a single oral (105 mg/mL) or intravenous (60 mg/60 min) dose. The mean Cmax (CV%) and Tmax were 1656 (44.3) ng/mL and 0.5 hours, respectively, following oral administration.L43952 The absolute oral bioavailability is about 57% because of first-pass metabolism.L41810 The mean Cmax (CV%) and Tmax were 1253 (18.3) ng/mL and one hour, respectively, following intravenous administration.L43952 When intravenously administered, the maximum plasma concentration (Cmax) of edaravone was reached by the end of infusion.L41810 The Cmax and area under the concentration-time curve (AUC) of edaravone increases more than dose-proportional over the dose range of 30 to 300 mg. Edaravone does not accumulate in plasma with once-daily or multiple-dose administration. The Cmax and AUC decreased when the oral suspension formulation of edaravone was administered with a high-fat meal.L43952

Metabolisme

The metabolites of edaravone have not been fully characterized. Edaravone is metabolized to a sulfate conjugate and a glucuronide conjugate, which are not pharmacologically active. The glucuronide conjugation of edaravone involves multiple uridine diphosphate glucuronosyltransferase (UGT) isoforms (UGT1A1, UGT1A6, UGT1A7, UGT1A8, UGT1A9, UGT1A10, UGT2B7, and UGT2B17). In human plasma, edaravone is mainly detected as the sulfate conjugate, which is presumed to be formed by sulfotransferases. Oral edaravone results in 1.3- and 1.7-fold higher exposures for both sulfate and glucuronide metabolites, respectively, when compared to intravenously-administered edaravone because of first-pass metabolism.L41810

Rute Eliminasi

In Japanese and Caucasian healthy volunteer studies, edaravone was excreted mainly in the urine as its glucuronide conjugate (60-80% of the dose up to 48 hours). Approximately 6-8% of the dose was recovered in the urine as the sulfate conjugate, and <1% of the dose was recovered in the urine as the unchanged drug. In vitro studies suggest that the sulfate conjugate of edaravone is hydrolyzed back to edaravone, which is then converted to the glucuronide conjugate in the kidney before excretion into the urine.L41810

Interaksi Makanan

1 Data
  • 1. Take on an empty stomach. RADICAVA ORS should be taken in the morning on an empty stomach after overnight fasting. Food should not be consumed for 1 hour after administration except water. The higher the fat content of the previous meal, the longer the fasting time before taking RADICAVA ORS will be.

Interaksi Obat

0 Data
Tidak ada data.

Target Protein

Apoptosis regulator Bcl-2 BCL2

Referensi & Sumber

Artikel (PubMed)
  • PMID: 25847999
    Jiao SS, Yao XQ, Liu YH, Wang QH, Zeng F, Lu JJ, Liu J, Zhu C, Shen LL, Liu CH, Wang YR, Zeng GH, Parikh A, Chen J, Liang CR, Xiang Y, Bu XL, Deng J, Li J, Xu J, Zeng YQ, Xu X, Xu HW, Zhong JH, Zhou HD, Zhou XF, Wang YJ: Edaravone alleviates Alzheimer's disease-type pathologies and cognitive deficits. Proc Natl Acad Sci U S A. 2015 Apr 21;112(16):5225-30. doi: 10.1073/pnas.1422998112. Epub 2015 Apr 6.
  • PMID: 22762844
    Li H, Xu K, Wang Y, Zhang H, Li T, Meng L, Gong X, Zhang H, Ou N, Ruan J: Phase I clinical study of edaravone in healthy Chinese volunteers: safety and pharmacokinetics of single or multiple intravenous infusions. Drugs R D. 2012 Jun 1;12(2):65-70. doi: 10.2165/11634290-000000000-00000.
  • PMID: 18485133
    Watanabe T, Tahara M, Todo S: The novel antioxidant edaravone: from bench to bedside. Cardiovasc Ther. 2008 Summer;26(2):101-14. doi: 10.1111/j.1527-3466.2008.00041.x.
  • PMID: 21922128
    Kikuchi K, Uchikado H, Miyagi N, Morimoto Y, Ito T, Tancharoen S, Miura N, Miyata K, Sakamoto R, Kikuchi C, Iida N, Shiomi N, Kuramoto T, Kawahara K: Beyond neurological disease: new targets for edaravone (Review). Int J Mol Med. 2011 Dec;28(6):899-906. doi: 10.3892/ijmm.2011.795. Epub 2011 Sep 15.
  • PMID: 29290672
    Cruz MP: Edaravone (Radicava): A Novel Neuroprotective Agent for the Treatment of Amyotrophic Lateral Sclerosis. P T. 2018 Jan;43(1):25-28.

Contoh Produk & Brand

Produk: 12 • International brands: 2
Produk
  • Edaravone
    Injection, solution • 30 mg/100mL • Intravenous • US • Generic • Approved
  • Edaravone
    Injection, solution • 60 mg/100mL • Intravenous • US • Generic • Approved
  • Edaravone
    Injection, solution • 30 mg/100mL • Intravenous • US • Generic • Approved
  • Edaravone
    Injection, solution • 30 mg/100mL • Intravenous • US • Generic • Approved
  • Edaravone
    Injection, solution • 60 mg/100mL • Intravenous • US • Generic • Approved
  • Edaravone
    Solution • 30 mg/100mL • Intravenous • US • Generic • Approved
  • Radicava
    Injection • 30 mg/100mL • Intravenous • US • Approved
  • Radicava
    Solution • 30 mg / 100 mL • Intravenous • Canada • Approved
Menampilkan 8 dari 12 produk.
International Brands
  • Arone — Edinburgh Pharmaceuticals (India)
  • Radicut — Mitsubishi Tanabe Pharma Corporation

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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