Peringatan Keamanan

Based on findings from a rabbit thrombogenicity test and rat or monkey repeated-dose toxicity studies, eftrenonacog alfa displays no special hazards for humans. Studies to investigate the genotoxicity, carcinogenicity, toxicity to reproduction or embryo-foetal development have not been conducted. Eftrenonacog alfa has shown to cross the placenta in small amounts according to a mouse placental transfer study FDA Label.

Eftrenonacog alfa

DB11608

biotech approved investigational

Deskripsi

Eftrenonacog alfa is a long-acting recombinant fusion protein used in the treatment of hemophilia B. It is comprised of a single molecule of human factor IX (FIX) covalently linked to the constant region (Fc) domain of human IgG1 via recombinant DNA technology in a human embryonic kidney cell line (HEK293H) A31556. The presence of the Fc domain extends the terminal half-life which confers clinical benefits of prolonged therapeutic efficacy, less frequent intravenous injections for patient convenience and improved adherence to prophylaxis.

Hemophilia B is a blood disorder with an incidence of approximately once every 30,000 male births in all populations and ethnic groups A31557. It is an X-linked genetic disease caused by mutation of the gene for coagulation protein factor IX (FIX), leading to decreased levels of endogenous factor IX and increased susceptibility to recurrent bleeding episodes caused spontaneously or as a result of accidental or surgical trauma FDA Label. When untreated, most patients die from bleeding complications before 25 years of age A31557. Eftrenonacog alfa acts as a replacement therapy to restore the levels of factor IX and allow normal hemostasis.

Eftrenonacog alfa was developed and marketed as Alprolix for intravenous injection by Biogen. It was first approved by the FDA in March 2014 and later approved by the EMA in May 2016. Eftrenonacog alfa treatment demonstrated good tolerability with no reports of inhibitor development in clinical studies A31556.

Struktur Molekul 2D

Struktur tidak tersedia

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) Following administration of a single intravenous dose of 50 IU/kg of eftrenonacog alfa in patients ?19 years of age with hemophilia B, the mean terminal half life (t1/2) was 77.6 hours [FDA Label]. In pediatric and adolescent patients (< 18 years of age) receiving the same dose, the mean t1/2 ranged from 66.49 to 82.22 hours [FDA Label].
Volume Distribusi Following administration of a single intravenous dose of 50 IU/kg of eftrenonacog alfa in patients ?19 years of age with hemophilia B, the mean volume of distribution at steady-state (Vss) was 303.4 mL/kg [FDA Label]. In pediatric and adolescent patients (< 18 years of age) receiving the same dose, the mean Vss ranged from 289 to 365.1 mL/kg [FDA Label].
Klirens (Clearance) Following administration of a single intravenous dose of 50 IU/kg of eftrenonacog alfa in patients ?19 years of age with hemophilia B, the mean clearance (CL) was 3.17 mL/h/kg [FDA Label]. In pediatric and adolescent patients (< 18 years of age) receiving the same dose, mean CL ranged from 3.390 to 4.365 mL/h/kg [FDA Label].

Absorpsi

Following administration of a single intravenous dose of 50 IU/kg of eftrenonacog alfa in patients ?19 years of age with hemophilia B, the mean peak plasma concentration (Cmax) was 46.10 IU/dL FDA Label. The mean area under the FIX activity time curve (AUC) was 31.58 Uxh/dL per IU/kg FDA Label. In pediatric and adolescent patients (< 18 years of age) receiving the same dose, the mean AUC ranged from 22.71 to 29.50 Uxh/dL per IU/kg FDA Label.

Metabolisme

The Fc domain of eftrenonacog alfa is expected to undergo lysosomal degradation while the remaining recombinant FIX (rFIX) portion is expected to be metabolized by the same pathway as endogenous factor IX.

Rute Eliminasi

Eftrenonacog alfa is expected to undergo renal clearance A31557.

Interaksi Obat

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

Target Protein

IgG receptor FcRn large subunit p51 FCGRT

Referensi & Sumber

Artikel (PubMed)
  • PMID: 28646426
    Hoy SM: Eftrenonacog Alfa: A Review in Haemophilia B. Drugs. 2017 Jul;77(11):1235-1246. doi: 10.1007/s40265-017-0778-1.
  • PMID: 25143713
    Miguelino MG, Powell JS: Clinical utility and patient perspectives on the use of extended half-life rFIXFc in the management of hemophilia B. Patient Prefer Adherence. 2014 Aug 8;8:1073-83. doi: 10.2147/PPA.S54951. eCollection 2014.

Contoh Produk & Brand

Produk: 23 • International brands: 0
Produk
  • Alprolix
    Kit; Powder, for solution • 500 [iU]/5mL • Intravenous • US • Approved
  • Alprolix
    Kit; Powder, for solution • 1000 [iU]/5mL • Intravenous • US • Approved
  • Alprolix
    Kit; Powder, for solution • 2000 [iU]/5mL • Intravenous • US • Approved
  • Alprolix
    Kit; Powder, for solution • 3000 [iU]/5mL • Intravenous • US • Approved
  • Alprolix
    Kit; Powder, for solution • 250 [iU]/5mL • Intravenous • US • Approved
  • Alprolix
    Kit; Powder, for solution • 4000 [iU]/5mL • Intravenous • US • Approved
  • Alprolix
    Kit • 500 [iU]/5mL • Intravenous • US • Approved
  • Alprolix
    Kit • 1000 [iU]/5mL • Intravenous • US • Approved
Menampilkan 8 dari 23 produk.

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