Evolocumab

DB09303

biotech approved

Deskripsi

Evolocumab is a monoclonal antibody designed for the treatment of hyperlipidemia by Amgen. It is a subcutaneous injection approved by the FDA for individuals on maximum statin therapy who still require additional LDL-cholesterol lowering. It is approved for both homozygous and heterozygous familial cholesterolemia as an adjunct to other first-line therapies. Evolocumab is a human IgG2 monoclonal antibody that targets the proprotein convertase subtilisin/kexin type 9 (PCSK9). PCSK9 is a protein that targets LDL receptors for degradation, therefore reducing the liver's ability to remove LDL-cholesterol (LDL-C), or "bad" cholesterol, from the blood. Evolocumab is designed to bind to PCSK9 and inhibit PCSK9 from binding to LDL receptors on the liver surface, resulting in more LDL receptors on the surface of the liver to remove LDL-C from the blood. Evolocumab is the second PCSK9 inhibitor on the market, first being alirocumab.

Struktur Molekul 2D

Struktur tidak tersedia

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) -
Volume Distribusi -
Klirens (Clearance) Evolocumab showed non-linear, dose-dependent clearance in healthy volunteers; clearance decreased with increasing dose.

Absorpsi

Total bioavailability from subcutaneous injection was 82% in cynomolgus monkeys.

Metabolisme

Data metabolisme tidak tersedia.

Rute Eliminasi

Data eliminasi belum tersedia.

Interaksi Obat

373 Data
Diethylstilbestrol Diethylstilbestrol may increase the thrombogenic activities of Evolocumab.
Chlorotrianisene Chlorotrianisene may increase the thrombogenic activities of Evolocumab.
Conjugated estrogens Conjugated estrogens may increase the thrombogenic activities of Evolocumab.
Estrone Estrone may increase the thrombogenic activities of Evolocumab.
Estradiol Estradiol may increase the thrombogenic activities of Evolocumab.
Dienestrol Dienestrol may increase the thrombogenic activities of Evolocumab.
Ethinylestradiol Ethinylestradiol may increase the thrombogenic activities of Evolocumab.
Mestranol Mestranol may increase the thrombogenic activities of Evolocumab.
Estriol Estriol may increase the thrombogenic activities of Evolocumab.
Estrone sulfate Estrone sulfate may increase the thrombogenic activities of Evolocumab.
Quinestrol Quinestrol may increase the thrombogenic activities of Evolocumab.
Hexestrol Hexestrol may increase the thrombogenic activities of Evolocumab.
Tibolone Tibolone may increase the thrombogenic activities of Evolocumab.
Synthetic Conjugated Estrogens, A Synthetic Conjugated Estrogens, A may increase the thrombogenic activities of Evolocumab.
Synthetic Conjugated Estrogens, B Synthetic Conjugated Estrogens, B may increase the thrombogenic activities of Evolocumab.
Polyestradiol phosphate Polyestradiol phosphate may increase the thrombogenic activities of Evolocumab.
Esterified estrogens Esterified estrogens may increase the thrombogenic activities of Evolocumab.
Zeranol Zeranol may increase the thrombogenic activities of Evolocumab.
Equol Equol may increase the thrombogenic activities of Evolocumab.
Promestriene Promestriene may increase the thrombogenic activities of Evolocumab.
Methallenestril Methallenestril may increase the thrombogenic activities of Evolocumab.
Epimestrol Epimestrol may increase the thrombogenic activities of Evolocumab.
Moxestrol Moxestrol may increase the thrombogenic activities of Evolocumab.
Estradiol acetate Estradiol acetate may increase the thrombogenic activities of Evolocumab.
Estradiol benzoate Estradiol benzoate may increase the thrombogenic activities of Evolocumab.
Estradiol cypionate Estradiol cypionate may increase the thrombogenic activities of Evolocumab.
Estradiol valerate Estradiol valerate may increase the thrombogenic activities of Evolocumab.
Biochanin A Biochanin A may increase the thrombogenic activities of Evolocumab.
Formononetin Formononetin may increase the thrombogenic activities of Evolocumab.
Estetrol Estetrol may increase the thrombogenic activities of Evolocumab.
Cetuximab The risk or severity of adverse effects can be increased when Cetuximab is combined with Evolocumab.
Human immunoglobulin G The risk or severity of adverse effects can be increased when Human immunoglobulin G is combined with Evolocumab.
Omalizumab The risk or severity of adverse effects can be increased when Omalizumab is combined with Evolocumab.
Adalimumab The risk or severity of adverse effects can be increased when Adalimumab is combined with Evolocumab.
Abciximab The risk or severity of adverse effects can be increased when Abciximab is combined with Evolocumab.
Gemtuzumab ozogamicin The risk or severity of adverse effects can be increased when Gemtuzumab ozogamicin is combined with Evolocumab.
Indium In-111 satumomab pendetide The risk or severity of adverse effects can be increased when Indium In-111 satumomab pendetide is combined with Evolocumab.
Infliximab The risk or severity of adverse effects can be increased when Infliximab is combined with Evolocumab.
Trastuzumab The risk or severity of adverse effects can be increased when Trastuzumab is combined with Evolocumab.
Rituximab The risk or severity of adverse effects can be increased when Rituximab is combined with Evolocumab.
Basiliximab The risk or severity of adverse effects can be increased when Basiliximab is combined with Evolocumab.
Muromonab The risk or severity of adverse effects can be increased when Muromonab is combined with Evolocumab.
Digoxin Immune Fab (Ovine) The risk or severity of adverse effects can be increased when Digoxin Immune Fab (Ovine) is combined with Evolocumab.
Ibritumomab tiuxetan The risk or severity of adverse effects can be increased when Ibritumomab tiuxetan is combined with Evolocumab.
Tositumomab The risk or severity of adverse effects can be increased when Tositumomab is combined with Evolocumab.
Alemtuzumab The risk or severity of adverse effects can be increased when Alemtuzumab is combined with Evolocumab.
Capromab pendetide The risk or severity of adverse effects can be increased when Capromab pendetide is combined with Evolocumab.
Efalizumab The risk or severity of adverse effects can be increased when Efalizumab is combined with Evolocumab.
Antithymocyte immunoglobulin (rabbit) The risk or severity of adverse effects can be increased when Antithymocyte immunoglobulin (rabbit) is combined with Evolocumab.
Natalizumab The risk or severity of adverse effects can be increased when Natalizumab is combined with Evolocumab.
Palivizumab The risk or severity of adverse effects can be increased when Palivizumab is combined with Evolocumab.
Daclizumab The risk or severity of adverse effects can be increased when Daclizumab is combined with Evolocumab.
Bevacizumab The risk or severity of adverse effects can be increased when Bevacizumab is combined with Evolocumab.
Technetium Tc-99m arcitumomab The risk or severity of adverse effects can be increased when Technetium Tc-99m arcitumomab is combined with Evolocumab.
Eculizumab The risk or severity of adverse effects can be increased when Eculizumab is combined with Evolocumab.
Panitumumab The risk or severity of adverse effects can be increased when Panitumumab is combined with Evolocumab.
Ranibizumab The risk or severity of adverse effects can be increased when Ranibizumab is combined with Evolocumab.
Galiximab The risk or severity of adverse effects can be increased when Galiximab is combined with Evolocumab.
Pexelizumab The risk or severity of adverse effects can be increased when Pexelizumab is combined with Evolocumab.
Afelimomab The risk or severity of adverse effects can be increased when Afelimomab is combined with Evolocumab.
Epratuzumab The risk or severity of adverse effects can be increased when Epratuzumab is combined with Evolocumab.
Bectumomab The risk or severity of adverse effects can be increased when Bectumomab is combined with Evolocumab.
Oregovomab The risk or severity of adverse effects can be increased when Oregovomab is combined with Evolocumab.
IGN311 The risk or severity of adverse effects can be increased when IGN311 is combined with Evolocumab.
Adecatumumab The risk or severity of adverse effects can be increased when Adecatumumab is combined with Evolocumab.
Labetuzumab The risk or severity of adverse effects can be increased when Labetuzumab is combined with Evolocumab.
Matuzumab The risk or severity of adverse effects can be increased when Matuzumab is combined with Evolocumab.
Fontolizumab The risk or severity of adverse effects can be increased when Fontolizumab is combined with Evolocumab.
Bavituximab The risk or severity of adverse effects can be increased when Bavituximab is combined with Evolocumab.
CR002 The risk or severity of adverse effects can be increased when CR002 is combined with Evolocumab.
Rozrolimupab The risk or severity of adverse effects can be increased when Rozrolimupab is combined with Evolocumab.
Girentuximab The risk or severity of adverse effects can be increased when Girentuximab is combined with Evolocumab.
Obiltoxaximab The risk or severity of adverse effects can be increased when Obiltoxaximab is combined with Evolocumab.
XTL-001 The risk or severity of adverse effects can be increased when XTL-001 is combined with Evolocumab.
NAV 1800 The risk or severity of adverse effects can be increased when NAV 1800 is combined with Evolocumab.
Briakinumab The risk or severity of adverse effects can be increased when Briakinumab is combined with Evolocumab.
Otelixizumab The risk or severity of adverse effects can be increased when Otelixizumab is combined with Evolocumab.
AMG 108 The risk or severity of adverse effects can be increased when AMG 108 is combined with Evolocumab.
Iratumumab The risk or severity of adverse effects can be increased when Iratumumab is combined with Evolocumab.
Enokizumab The risk or severity of adverse effects can be increased when Enokizumab is combined with Evolocumab.
Ramucirumab The risk or severity of adverse effects can be increased when Ramucirumab is combined with Evolocumab.
Farletuzumab The risk or severity of adverse effects can be increased when Farletuzumab is combined with Evolocumab.
Veltuzumab The risk or severity of adverse effects can be increased when Veltuzumab is combined with Evolocumab.
Ustekinumab The risk or severity of adverse effects can be increased when Ustekinumab is combined with Evolocumab.
Trastuzumab emtansine The risk or severity of adverse effects can be increased when Trastuzumab emtansine is combined with Evolocumab.
PRO-542 The risk or severity of adverse effects can be increased when PRO-542 is combined with Evolocumab.
TNX-901 The risk or severity of adverse effects can be increased when TNX-901 is combined with Evolocumab.
Inotuzumab ozogamicin The risk or severity of adverse effects can be increased when Inotuzumab ozogamicin is combined with Evolocumab.
RI 624 The risk or severity of adverse effects can be increased when RI 624 is combined with Evolocumab.
Stamulumab The risk or severity of adverse effects can be increased when MYO-029 is combined with Evolocumab.
CT-011 The risk or severity of adverse effects can be increased when CT-011 is combined with Evolocumab.
Leronlimab The risk or severity of adverse effects can be increased when Leronlimab is combined with Evolocumab.
Glembatumumab vedotin The risk or severity of adverse effects can be increased when Glembatumumab vedotin is combined with Evolocumab.
Olaratumab The risk or severity of adverse effects can be increased when Olaratumab is combined with Evolocumab.
IPH 2101 The risk or severity of adverse effects can be increased when IPH 2101 is combined with Evolocumab.
TB-402 The risk or severity of adverse effects can be increased when TB-402 is combined with Evolocumab.
Caplacizumab The risk or severity of adverse effects can be increased when Caplacizumab is combined with Evolocumab.
IMC-1C11 The risk or severity of adverse effects can be increased when IMC-1C11 is combined with Evolocumab.
Eldelumab The risk or severity of adverse effects can be increased when Eldelumab is combined with Evolocumab.
Lumiliximab The risk or severity of adverse effects can be increased when Lumiliximab is combined with Evolocumab.

Target Protein

Proprotein convertase subtilisin/kexin type 9 PCSK9

Referensi & Sumber

Artikel (PubMed)
  • PMID: 26445204
    Authors unspecified: Evolocumab (Repatha)--a second PCSK9 inhibitor to lower LDL-Cholesterol. Med Lett Drugs Ther. 2015 Oct 12;57(1479):140-1.
  • PMID: 26293511
    Page MM, Watts GF: Evolocumab in the treatment of dyslipidemia: pre-clinical and clinical pharmacology. Expert Opin Drug Metab Toxicol. 2015;11(9):1505-15. doi: 10.1517/17425255.2015.1073712.

Contoh Produk & Brand

Produk: 17 • International brands: 0
Produk
  • Repatha
    Injection, solution • 140 mg/1mL • Subcutaneous • US • Approved
  • Repatha
    Injection, solution • 140 mg/1mL • Subcutaneous • US • Approved
  • Repatha
    Injection, solution; Kit • 420 mg/3.5mL • Subcutaneous • US • Approved
  • Repatha
    Injection, solution • 140 mg/1mL • Subcutaneous • US • Approved
  • Repatha
    Injection, solution • 140 mg/1mL • Subcutaneous • US • Approved
  • Repatha
    Injection, solution; Kit • 420 mg/3.5mL • Subcutaneous • US • Approved
  • Repatha
    Solution • 140 mg / mL • Subcutaneous • Canada • Approved
  • Repatha
    Solution • 120 mg / mL • Subcutaneous • Canada • Approved
Menampilkan 8 dari 17 produk.

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