Peringatan Keamanan

Data regarding overdoses of lumasiran are not readily available.L23519 In the event of an overdose, patients should be monitored for signs of adverse reactions and be treated symptomatically.L23519

Lumasiran

DB15935

biotech approved investigational

Deskripsi

Lumasiran is a small interfering RNA used in the treatment of primary hyperoxaluria type 1 (PH1).L23554 This condition, caused by a deficiency in the enzyme alanine-glyoxylate aminotransferase, leads to an accumulation of oxalate, causing calcium crystal formation.L23554 These patients experience frequent kidney stones, nephrocalcinosis, and renal failure.L23554

Oxlumo, producted by Alnylam Pharmaceuticals, represents the first approved treatment for PH1.L23394 Prior to this approval, therapy consisted of symptomatic treatment such as hyperhydration, inhibitors of crystallization, pyridoxine, and renal transplant.L23554

Lumasiran was granted FDA approval on 23 November 2020.L23394

Struktur Molekul 2D

Struktur tidak tersedia

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 lumasiran is 5.2 hours.[L23519]
Volume Distribusi The apparent central volume of distribution based on population estimate is 4.9 L.[L23519]
Klirens (Clearance) The apparent plasma clearance of lumasiran based on population estimate is 26.5 L/h for an average 70 kg adult.[L23519] The mean renal clearance is 2.0-3.4 L/h.[L23519]

Absorpsi

In patients ?20 kg; a 3 mg/kg subcutaneous dose of lumasiran reacheas a Cmax of 529 ng/mL, with a Tmax of 4.0 hours, and an AUC of 7400 ng\*h/mL.L23519 In patients <20 kg; a 6 mg/kg subcutaneous dose of lumasiran reaches a Cmax of 912 ng/mL and an AUC of 7960 ng\*h/mL.L23519

Metabolisme

Lumasiran is metabolized to smaller oligonucleotides by endo- and exonucleases.L23519 The sense strand is less prone to metabolism due to protection by the GalNac group at the 3' end.L23554 Lumasiran weakly inhibits CYP2C8 with an IC50 of 461 µM, 14000 times pharmacologically relevant concentrations.L23554 It is not a substrate or inducer of any CYP450 enzymes.L23554

Rute Eliminasi

7-26% of a dose of lumasiran is recovered in the urine as the unmetabolized parent compound.L23519 A radiolabelled dose administered to rats was 19.5% recovered in urine and 33.9% recovered in feces.L23554

Interaksi Obat

0 Data
Tidak ada data.

Target Protein

2-Hydroxyacid oxidase 1 HAO1

Referensi & Sumber

Artikel (PubMed)
  • PMID: 32207686
    McGregor TL, Hunt KA, Yee E, Mason D, Nioi P, Ticau S, Pelosi M, Loken PR, Finer S, Lawlor DA, Fauman EB, Huang QQ, Griffiths CJ, MacArthur DG, Trembath RC, Oglesbee D, Lieske JC, Erbe DV, Wright J, van Heel DA: Characterising a healthy adult with a rare HAO1 knockout to support a therapeutic strategy for primary hyperoxaluria. Elife. 2020 Mar 24;9. pii: 54363. doi: 10.7554/eLife.54363.
  • PMID: 30430197
    Dindo M, Conter C, Oppici E, Ceccarelli V, Marinucci L, Cellini B: Molecular basis of primary hyperoxaluria: clues to innovative treatments. Urolithiasis. 2019 Feb;47(1):67-78. doi: 10.1007/s00240-018-1089-z. Epub 2018 Nov 14.

Contoh Produk & Brand

Produk: 3 • International brands: 1
Produk
  • Oxlumo
    Injection, solution • 94.5 mg/0.5mL • Subcutaneous • EU • Approved
  • Oxlumo
    Solution • 94.5 mg / 0.5 mL • Subcutaneous • Canada • Approved
  • Oxlumo
    Injection, solution • 94.5 mg/0.5mL • Subcutaneous • US • Approved
International Brands
  • Oxlumo

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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