Peringatan Keamanan

Data regarding overdoses of setmelanotide are not readily available.L24569 In the event of an overdose, patients should be treated with symptomatic and supportive care.L24569

Setmelanotide

DB11700

small molecule approved investigational

Deskripsi

Setmelanotide is the first available treatment for patients with pro-opiomelanocortin, proprotein subilisin/kexin type 1, or leptin deficiencies.L24474 It is an agonist of the melanocortin 4 receptor.A224449 Earlier attempts at agonizing MC4R (such as LY2112688) lead to successful weight loss, but also an increase in blood pressure and heart rate.A224449 Other earlier treatments for these patients included gastric bypass surgery.A224449 Patients taking setmelanotide experienced an average weight loss of 0.6 kg/week.A224449

Imcivree was granted EMA orphan designation on November 19, 2018 L24559 and FDA approval on November 25, 2020.L24429 On May 4, 2023, it was approved by Health Canada.L46327

Struktur Molekul 2D

Berat 1117.32
Wujud liquid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The elimination had life of setmelanotide is approximately 11 hours.[L24569]
Volume Distribusi The apparent volume of distribution of setmelanotide is 48.7 L.[L24569]
Klirens (Clearance) A 3mg subcutaneous dose of setmelanotide has an estimated clearance of 4.86 L/h.[L24569]

Absorpsi

Setmelanotide has a Tmax of 8 hours.L24569

Metabolisme

Setmelanotide is expected to be metabolized to small peptides and amino acids.L24569

Rute Eliminasi

A 3mg subcutaneous dose of setmelanotide is 39% eliminated in the urine as the unchanged parent compound.L24569

Interaksi Obat

0 Data
Tidak ada data.

Target Protein

Melanocortin receptor 4 MC4R

Referensi & Sumber

Artikel (PubMed)
  • PMID: 29031731
    Collet TH, Dubern B, Mokrosinski J, Connors H, Keogh JM, Mendes de Oliveira E, Henning E, Poitou-Bernert C, Oppert JM, Tounian P, Marchelli F, Alili R, Le Beyec J, Pepin D, Lacorte JM, Gottesdiener A, Bounds R, Sharma S, Folster C, Henderson B, O'Rahilly S, Stoner E, Gottesdiener K, Panaro BL, Cone RD, Clement K, Farooqi IS, Van der Ploeg LHT: Evaluation of a melanocortin-4 receptor (MC4R) agonist (Setmelanotide) in MC4R deficiency. Mol Metab. 2017 Oct;6(10):1321-1329. doi: 10.1016/j.molmet.2017.06.015. Epub 2017 Jul 8.
  • PMID: 29736023
    Clement K, Biebermann H, Farooqi IS, Van der Ploeg L, Wolters B, Poitou C, Puder L, Fiedorek F, Gottesdiener K, Kleinau G, Heyder N, Scheerer P, Blume-Peytavi U, Jahnke I, Sharma S, Mokrosinski J, Wiegand S, Muller A, Weiss K, Mai K, Spranger J, Gruters A, Blankenstein O, Krude H, Kuhnen P: MC4R agonism promotes durable weight loss in patients with leptin receptor deficiency. Nat Med. 2018 May;24(5):551-555. doi: 10.1038/s41591-018-0015-9. Epub 2018 May 7.
  • PMID: 30048591
    Falls BA, Zhang Y: Insights into the Allosteric Mechanism of Setmelanotide (RM-493) as a Potent and First-in-Class Melanocortin-4 Receptor (MC4R) Agonist To Treat Rare Genetic Disorders of Obesity through an in Silico Approach. ACS Chem Neurosci. 2019 Mar 20;10(3):1055-1065. doi: 10.1021/acschemneuro.8b00346. Epub 2018 Aug 13.
  • PMID: 27288825
    Ramos-Molina B, Martin MG, Lindberg I: PCSK1 Variants and Human Obesity. Prog Mol Biol Transl Sci. 2016;140:47-74. doi: 10.1016/bs.pmbts.2015.12.001. Epub 2016 Jan 29.

Contoh Produk & Brand

Produk: 4 • International brands: 1
Produk
  • Imcivree
    Solution • 10 mg / mL • Subcutaneous • Canada • Approved
  • Imcivree
    Injection, solution • 10 mg/ml • Subcutaneous • EU • Approved
  • Imcivree
    Injection, solution • 10 mg/ml • Subcutaneous • EU • Approved
  • Imcivree
    Solution • 10 mg/1mL • Subcutaneous • US • Approved
International Brands
  • Imcivree

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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