Peringatan Keamanan

Simoctocog alfa is not expected to cause any adverse effects on the human reproductive functions or the human fetus. As genotoxicity studies and carcinogenicity studies are not applicable for recombinant products, such studies were not performed.

According to the single-dose toxicity study in rats, there were no deaths or notable life-threatening changes to the treatment and the highest non-lethal intravenous dose was determined to be < 10,000 IU/kg L1115. In a repeated-dose toxicity study in monkeys, there was no evidence of systemic toxicity. There were no observable local reactions at the injection sites based on the findings of a rabbit local tolerance study L1115.

Although the formation of neutralizing antibodies (inhibitors) to FVIII is a specified warning/precaution of simoctocog alfa treatment, there have been no cases of inhibitior development throughout clinical studies L1115.

No cases of overdose have been reported with simoctocog alfa L1115.

Simoctocog alfa

DB09108

biotech approved

Deskripsi

Simoctocog alfa is a recombinant B-domain deleted (BDD) rFVIII produced in genetically modified human embryonic kidney (HEK) 293F cells. The harvested product is concentrated and purified by a series of chromatography steps. It is an antihemorrhagic agent used as a replacement therapy in individuals with Haemophilia A who lack the factor VIII in the intrinsic pathway of blood coagulation system. As patients with haemophilia A are predisposed to episodes of recurrent bleeding L1115, simoctocog alfa can be administered for the treatment or prevention of bleeding such as prior to surgical procedures.

Simoctocog alfa is a glycoprotein consisting of 1440 amino acids with an approximate molecular mass of 170 kDa, comprising the FVIII domains A1-A2 + A3-C1-C2 whereas the B-domain, present in the full-length plasma-derived FVIII, has been deleted and replaced by a 16 amino acid linker. Simoctocog alfa is a fourth-generation BDD FVIII product made in the human embryonic kidney (HEK) cell line. Full human post-translational modifications via elimination of potentially immunogenic glycosylation patterns found in non-human cell lines led to decreased immunogenicity and longer half-life A31525.

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) At initial assessment following administration of 50 IU/kg simoctocog alfa in adolescent or adult patients with severe haemophilia A, the mean terminal half-life (T1/2) was 17.05 ± 11.23 h [L1115]. The mean T1/2 in pediatric patients was 12.50 ± 4.17 h [L1115]. At 6-month assessment in adolescent or adult patients with the same dose, the value was 14.05 ± 4.70 h [L1115].
Volume Distribusi It is observed that simoctocog alfa is mainly distributed in the intravascular compartment. At initial assessment following administration of 50 IU/kg simoctocog alfa in adolescent or adult patients with severe haemophilia A, the mean ± SD volume of distribution at steady state is 59.75 ± 19.76 mL/kg [L1115]. The value in pediatric patients was 67.18 ± 13.27 mL/kg [L1115]. At 6-month assessment in adolescent or adult patients with the same dose, the value was 56.90 ± 9.07 mL/kg [L1115].
Klirens (Clearance) At initial assessment following administration of 50 IU/kg simoctocog alfa in adolescent or adult patients with severe haemophilia A, the mean clearance rate (CL) was 2.96 ± 0.97 mL/h/kg [L1115]. The mean CL in pediatric patients was 4.73 ± 1.87 mL/h/kg [L1115]. At 6-month assessment in adolescent or adult patients with the same dose, the value was 3.39 ± 1.42 mL/h/kg [L1115].

Absorpsi

At initial assessment following administration of 50 IU/kg simoctocog alfa in adolescent or adult patients with severe haemophilia A, the mean ± SD AUC (FVIII:C) was 17.95 ± 5.57 h·IU/mL/(IU/kg) L1115. The mean ± SD maximum plasma concentration divided by the dose (Cmaxnorm) was 0.022 ± 0.003 IU/mL/(IU/kg) L1115. The values of mean ± SD AUC (FVIII:C) and Cmaxnorm in pediatric patients were 10.92 ± 3.80 h·IU/mL/(IU/kg) and 0.017 ± 0.003 IU/mL/(IU/kg), respectively L1115. At 6-month assessment in adolescent or adult patients with the same dose, the mean ± SD AUC (FVIII:C) and Cmaxnorm were 16.86 ± 6.12 h·IU/mL/(IU/kg) and 0.021 ± 0.003 IU/mL/(IU/kg), respectively L1115.

Metabolisme

Data metabolisme tidak tersedia.

Rute Eliminasi

In a non-bleeding state, simoctocog alfa is assumed to be cleared by low-density lipoprotein receptor-related protein (LRP) and low-density lipoprotein receptor (LDLR) as expected of endogenous factor VIII. In cases of bleeding or surgery, simoctocog alfa is believed to be consumed at the bleeding site as expected of factor VIII L1115.

Interaksi Obat

0 Data
Tidak ada data.

Target Protein

von Willebrand factor VWF

Referensi & Sumber

Artikel (PubMed)
  • PMID: 28670147
    Lieuw K: Many factor VIII products available in the treatment of hemophilia A: an embarrassment of riches? J Blood Med. 2017 Jun 15;8:67-73. doi: 10.2147/JBM.S103796. eCollection 2017.

Contoh Produk & Brand

Produk: 31 • International brands: 0
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Menampilkan 8 dari 31 produk.

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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