Peringatan Keamanan

The administration of Emicizumab has reported cases of microangiopathy and thrombotic events with concomitant use of activated prothrombin complex concentrate at doses higher of 100 U/kg/24 hours. There are also reports of injection site reaction, headaches and arthralgia.L1018

Genotoxicity and carcinogenicity studies have not been performed as it is not expected that emicizumab can have any interaction with DNA, or chromosomal material.F1947

Emicizumab

DB13923

biotech approved investigational

Deskripsi

Emicizumab is a humanized recombinant monoclonal antibody that mimics the function of the coagulation Factor VIII and it has the capacity to bind simultaneously to activated Factor IX and Factor X. The ability of Emicizumab to bind to all these three different factors allows it to overcome immunogenicity and unstable hemostatic efficacy produced by previous Factor VII agents. Emicizumab was originated as an improved form of hBS23 and it was approved on November 16, 2017.A31279, L1016 It was created by Chugai Pharmaceuticals Co. Ltd. and co-developed with Roche and Genentech.L1015

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) Emcicizumab presents a long half-life ranging from 27.8 to 34.4 days.[FDA label, A31279]
Volume Distribusi The apparent volume of distribution is 11.4 L when administered subcutaneously and there are reports indicating that this value can increase with increasing body weight.[A39524] When emicizumab is administered intravenously, the volume of distribution at steady state is 106 ml/kg.[F1947]
Klirens (Clearance) The apparent clearance is 0.24 L/day when administered in multiple subcutaneous injections and there are reports indicating that this value can increase with increasing body weight.[A39524]

Absorpsi

Subcutaneous administration of Emicizumab presents a very high bioavailability ranging from 80.4% to 93.1% when administered subcutaneously in a dose of 1 mg/kg.A39524 In clinical trials, at the same dose, Emicizumab presented a linear exposure which concentration peaked 1-2 weeks after administration and presented a profile framed by a Cmax of 5.92 mcg/ml and an AUC of 304 mcg day/ml.A31279 After subcutaneous administration, the absorption half-life was 1.7 days and the pharmacokinetic profile seemed to be shared when the medication was administered in the abdomen, upper arm, and thigh.F1947

Metabolisme

Emicizumab is a monoclonal antibody and thus, it is thought to be internalized in endothelial cells bound to Fc receptor and rescued from metabolism by recycling. Later, they are degraded in the reticuloendothelial system to small peptides and amino acids which can be used for de-novo protein synthesis.A31470

Rute Eliminasi

The elimination of Emicizumab was monophasic in clinical trials.A31279

Interaksi Obat

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

Target Protein

Coagulation factor IX F9
Coagulation factor X F10

Referensi & Sumber

Artikel (PubMed)
  • PMID: 26626991
    Uchida N, Sambe T, Yoneyama K, Fukazawa N, Kawanishi T, Kobayashi S, Shima M: A first-in-human phase 1 study of ACE910, a novel factor VIII-mimetic bispecific antibody, in healthy subjects. Blood. 2016 Mar 31;127(13):1633-41. doi: 10.1182/blood-2015-06-650226. Epub 2015 Dec 1.
  • PMID: 27223146
    Shima M, Hanabusa H, Taki M, Matsushita T, Sato T, Fukutake K, Fukazawa N, Yoneyama K, Yoshida H, Nogami K: Factor VIII-Mimetic Function of Humanized Bispecific Antibody in Hemophilia A. N Engl J Med. 2016 May 26;374(21):2044-53. doi: 10.1056/NEJMoa1511769.
  • PMID: 6424437
    Chavin SI: Factor VIII: structure and function in blood clotting. Am J Hematol. 1984 Apr;16(3):297-306.
  • PMID: 27207420
    Nogami K: Bispecific antibody mimicking factor VIII. Thromb Res. 2016 May;141 Suppl 2:S34-5. doi: 10.1016/S0049-3848(16)30361-9.
  • PMID: 16478695
    Tabrizi MA, Tseng CM, Roskos LK: Elimination mechanisms of therapeutic monoclonal antibodies. Drug Discov Today. 2006 Jan;11(1-2):81-8. doi: 10.1016/S1359-6446(05)03638-X.
  • PMID: 29214439
    Yoneyama K, Schmitt C, Kotani N, Levy GG, Kasai R, Iida S, Shima M, Kawanishi T: A Pharmacometric Approach to Substitute for a Conventional Dose-Finding Study in Rare Diseases: Example of Phase III Dose Selection for Emicizumab in Hemophilia A. Clin Pharmacokinet. 2018 Sep;57(9):1123-1134. doi: 10.1007/s40262-017-0616-3.

Contoh Produk & Brand

Produk: 16 • International brands: 0
Produk
  • Hemlibra
    Injection, solution • 30 mg/1mL • Subcutaneous • US • Approved
  • Hemlibra
    Injection, solution • 150 mg/1mL • Subcutaneous • US • Approved
  • Hemlibra
    Solution • 30 mg / 1 mL • Subcutaneous • Canada • Approved
  • Hemlibra
    Solution • 60 mg / 0.4 mL • Subcutaneous • Canada • Approved
  • Hemlibra
    Solution • 105 mg / 0.7 mL • Subcutaneous • Canada • Approved
  • Hemlibra
    Solution • 150 mg / mL • Subcutaneous • Canada • Approved
  • Hemlibra
    Injection, solution • 60 mg/0.4mL • Subcutaneous • US • Approved
  • Hemlibra
    Injection, solution • 105 mg/0.7mL • Subcutaneous • US • Approved
Menampilkan 8 dari 16 produk.

Sekuens Gen/Protein (FASTA)

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