Peringatan Keamanan

The most common side effects of erenumab include pain, redness, or swelling at the injection site, and constipation. Information regarding overdosage is not available FDA Label.

Erenumab

DB14039

biotech approved investigational

Deskripsi

Erenumab (AMG-334) (INN; trade name Aimovig) is a human monoclonal antibody designed specifically to bind and antagonize the calcitonin gene-related peptide receptor (CGRPR) as a means to prevent migraines. Aimovig, as released and marketed by Novartis and Amgen, is in fact a novel therapeutic approach as the first and only FDA approved treatment specifically developed to prevent migraine by blocking the CGRP receptor, which is believed to play a critical role in migraine L2823.

In particular, erenumab-aooe is a human immunoglobulin G2 monoclonal antibody that has high affinity binding to the CGRP receptor FDA Label. The antibody is produced utlilizing recombinant DNA technology in Chinese hamster ovary cells FDA Label. It is composed of 2 heavy chains, each containing 456 amino acids, and 2 light chains of the lambda subclass, each containing 216 amino acids, with an approximate molecular weight of 150 kDa FDA Label.

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) Erenumab exhibits non-linear kinetics as a result of binding to the CGRP receptor [FDA Label]. Lower than 2-fold accumulation was recorded in trough serum concentrations (Cmin) for episodic and chronic migraine patients following subcutaneous administration of 70 mg once-monthly and 140 mg once-monthly doses [FDA Label]. Serum trough concentrations approached steady state by 3 months of dosing [FDA Label]. The effective half-life of erenumab was observed to be 28 days [FDA Label].
Volume Distribusi After a single 140 mg intravenous dose, the mean (SD) volume of distribution during the terminal phase (Vz) was estimated to be approximately 3.86 (0.77) L [FDA Label].
Klirens (Clearance) Certain studies show that the population estimate of linear clearance is independent of erenumab concentrations and stays approximately constant at 0.214 L/day (95% CI: 0.191–0.243) [A33091]. In contrast, the nonlinear clearance is dependent on the target receptor density and the amount of erenumab bound to the receptors [A33091]. Nevertheless, the maximal nonlinear clearance was observed to be about 1.84L/day [A33091].

Absorpsi

Following a single subcutaneous dose of 70 mg or 140 mg erenumab administered to healthy adults, the median peak serum concentrations were attained in about 6 days, and the estimated absolute bioavailability was approximately 82% FDA Label.

Metabolisme

Erenumab CGRP antibodies demonstrate a low risk for drug-drug interactions and hepatotoxicity since they are predominantly metabolized by degradation into peptides and single amino acids A33090.

Rute Eliminasi

Two elimination phases are observed for erenumab. At low concentrations, the elimination is mainly through saturable binding to target (CGRP receptor), while at higher concentrations the elimination of erenumab is primarily through a non-specific, non-saturable proteolytic pathway FDA Label. These phases correspond to studies that demonstrated two parallel elimination pathways: (a) a slow non-specific elimination pathway through the hepatic reticuloendothelial system, and (b) a rapid saturable elimination pathway mediated by degradation or internalization of the erenumab-receptor complex A33091.

Interaksi Obat

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

Target Protein

Calcitonin gene-related peptide type 1 receptor CALCRL

Referensi & Sumber

Artikel (PubMed)
  • PMID: 28948500
    Deen M, Correnti E, Kamm K, Kelderman T, Papetti L, Rubio-Beltran E, Vigneri S, Edvinsson L, Maassen Van Den Brink A: Blocking CGRP in migraine patients - a review of pros and cons. J Headache Pain. 2017 Sep 25;18(1):96. doi: 10.1186/s10194-017-0807-1.
  • PMID: 28593473
    Vu T, Ma P, Chen JS, de Hoon J, Van Hecken A, Yan L, Wu LS, Hamilton L, Vargas G: Pharmacokinetic-Pharmacodynamic Relationship of Erenumab (AMG 334) and Capsaicin-Induced Dermal Blood Flow in Healthy and Migraine Subjects. Pharm Res. 2017 Sep;34(9):1784-1795. doi: 10.1007/s11095-017-2183-6. Epub 2017 Jun 7.

Contoh Produk & Brand

Produk: 14 • International brands: 0
Produk
  • Aimovig
    Injection, solution • 70 mg • Subcutaneous • EU • Approved
  • Aimovig
    Injection, solution • 70 mg • Subcutaneous • EU • Approved
  • Aimovig
    Injection, solution • 70 mg • Subcutaneous • EU • Approved
  • Aimovig
    Injection, solution • 140 mg • Subcutaneous • EU • Approved
  • Aimovig
    Injection, solution • 140 mg • Subcutaneous • EU • Approved
  • Aimovig
    Solution • 70 mg / mL • Subcutaneous • Canada • Approved
  • Aimovig
    Injection, solution • 140 mg • Subcutaneous • EU • Approved
  • Aimovig
    Injection • 70 mg/1mL • Subcutaneous • US • Approved
Menampilkan 8 dari 14 produk.

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