Peringatan Keamanan

There are no data regarding overdosage with evinacumab. Symptoms of overdose are likely to be consistent with evinacumab's adverse effect profile and may therefore include significant infusion reactions or dizziness.L31833 Patients experiencing an overdose should be treated with symptomatic and supportive measures.

Evinacumab

DB15354

biotech approved investigational

Deskripsi

Evinacumab is a recombinant human IgG4 monoclonal antibody targeted against angiopoietin-like protein 3 (ANGPTL3) and the first drug of its kind. The ANGPTL family of proteins serve a number of physiologic functions - including involvement in the regulation of lipid metabolism - which have made them desirable therapeutic targets in recent years.A229273 Loss-of-function mutations in ANGPTL3 have been noted to result in hypolipidemia and subsequent reductions in cardiovascular risk, whereas increases in function appear to be associated with cardiovascular risk, and it was these observations that provided a rationale for the development of a therapy targeted against ANGPTL3.A229278

In February 2021, evinacumab became the first-and-only inhibitor of ANGPTL3 to receive FDA approval after it was granted approval for the adjunctive treatment of homozygous familial hypercholesterolemia (HoFH) under the brand name "Evkeeza". Evinacumab is novel in its mechanism of action compared with other lipid-lowering therapies and therefore provides a unique and synergistic therapeutic option in the treatment of HoFH.L31838 In September and December 2023, evinacumab was also approved by Health Canada and EMA, respectively, for the same indication.L49956,L49966

Struktur Molekul 2D

Struktur tidak tersedia

Peta Jejaring Molekuler
Legenda: ObatTargetGenEnzim(Panah → menunjukkan arah efek / relasi)TransporterCarrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) The elimination half-life of evinacumab is a function of its serum concentration and is therefore variable.[L31833] This is because evinacumab is eliminated by two parallel pathways: at higher concentrations it is eliminated primarily through a non-saturable proteolytic pathway, while at lower concentrations its elimination occurs primarily via a saturable target-mediated pathway.[L31833]
Volume Distribusi The volume of distribution of evinacumab was estimated to be 4.8 L via population pharmacokinetic analysis.[L31833]
Klirens (Clearance) -

Absorpsi

Following the recommended dosing regimen (15 mg/kg intravenously every 4 weeks), steady-state concentrations are reached after four doses. According to population pharmacokinetic modeling, the mean steady-state trough concentration is approximately 241 mg/L and the Cmax at the end of infusion is approximately 689 mg/L.L31833

Metabolisme

The biotransformation of evinacumab has not been characterized.L31833 Monoclonal antibodies as a class are typically degraded via catabolic pathways into smaller peptides and amino acids.A216712

Rute Eliminasi

Monoclonal antibodies are typically eliminated via uptake into cells and subsequent catabolism via lysosomal degradation. Due to their large size, they are only eliminated renally under pathologic conditions.A216712

Interaksi Obat

0 Data
Tidak ada data.

Target Protein

Angiopoietin-related protein 3 ANGPTL3

Referensi & Sumber

Artikel (PubMed)
  • PMID: 31847708
    Kaplon H, Muralidharan M, Schneider Z, Reichert JM: Antibodies to watch in 2020. MAbs. 2020 Jan-Dec;12(1):1703531. doi: 10.1080/19420862.2019.1703531.
  • PMID: 28538136
    Dewey FE, Gusarova V, Dunbar RL, O'Dushlaine C, Schurmann C, Gottesman O, McCarthy S, Van Hout CV, Bruse S, Dansky HM, Leader JB, Murray MF, Ritchie MD, Kirchner HL, Habegger L, Lopez A, Penn J, Zhao A, Shao W, Stahl N, Murphy AJ, Hamon S, Bouzelmat A, Zhang R, Shumel B, Pordy R, Gipe D, Herman GA, Sheu WHH, Lee IT, Liang KW, Guo X, Rotter JI, Chen YI, Kraus WE, Shah SH, Damrauer S, Small A, Rader DJ, Wulff AB, Nordestgaard BG, Tybjaerg-Hansen A, van den Hoek AM, Princen HMG, Ledbetter DH, Carey DJ, Overton JD, Reid JG, Sasiela WJ, Banerjee P, Shuldiner AR, Borecki IB, Teslovich TM, Yancopoulos GD, Mellis SJ, Gromada J, Baras A: Genetic and Pharmacologic Inactivation of ANGPTL3 and Cardiovascular Disease. N Engl J Med. 2017 Jul 20;377(3):211-221. doi: 10.1056/NEJMoa1612790. Epub 2017 May 24.
  • PMID: 31242752
    Ahmad Z, Banerjee P, Hamon S, Chan KC, Bouzelmat A, Sasiela WJ, Pordy R, Mellis S, Dansky H, Gipe DA, Dunbar RL: Inhibition of Angiopoietin-Like Protein 3 With a Monoclonal Antibody Reduces Triglycerides in Hypertriglyceridemia. Circulation. 2019 Aug 6;140(6):470-486. doi: 10.1161/CIRCULATIONAHA.118.039107. Epub 2019 Jun 27.
  • PMID: 33130482
    Harada-Shiba M, Ali S, Gipe DA, Gasparino E, Son V, Zhang Y, Pordy R, Catapano AL: A randomized study investigating the safety, tolerability, and pharmacokinetics of evinacumab, an ANGPTL3 inhibitor, in healthy Japanese and Caucasian subjects. Atherosclerosis. 2020 Dec;314:33-40. doi: 10.1016/j.atherosclerosis.2020.10.013. Epub 2020 Oct 10.
  • PMID: 33470417
    Surma S, Romanczyk M, Filipiak KJ: Angiopoietin-like proteins inhibitors: New horizons in the treatment of atherogenic dyslipidemia and familial hypercholesterolemia. Cardiol J. 2021 Jan 20. pii: VM/OJS/J/69566. doi: 10.5603/CJ.a2021.0006.
  • PMID: 32052309
    Temrikar ZH, Suryawanshi S, Meibohm B: Pharmacokinetics and Clinical Pharmacology of Monoclonal Antibodies in Pediatric Patients. Paediatr Drugs. 2020 Apr;22(2):199-216. doi: 10.1007/s40272-020-00382-7.

Contoh Produk & Brand

Produk: 5 • International brands: 1
Produk
  • Evkeeza
    Injection, solution, concentrate • 150 mg/ml • Intravenous • EU • Approved
  • Evkeeza
    Solution • 150 mg / mL • Intravenous • Canada • Approved
  • Evkeeza
    Injection, solution, concentrate • 150 mg/ml • Intravenous • EU • Approved
  • Evkeeza
    Injection, solution, concentrate • 150 mg/1mL • Intravenous • US • Approved
  • Evkeeza
    Injection, solution, concentrate • 150 mg/1mL • Intravenous • US • Approved
International Brands
  • Evkeeza — Regeneron Pharmaceuticals, Inc.

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
© 2025 Digital Pharmacy Research - Universitas Esa Unggul