Peringatan Keamanan

Although available data on efbemalenograstim alfa use in pregnant women are insufficient to establish whether there is a drug-associated risk of major birth defects, miscarriage, or adverse maternal or fetal outcomes, there are available data from published studies in pregnant women exposed to other human G-CSF products. These studies have not established an association of G-CSF product use during pregnancy with major birth defects, miscarriage, or adverse maternal or fetal outcomes.L48852

In animal studies, no evidence of reproductive/developmental toxicity occurred in the offspring of pregnant rats and
rabbits that received cumulative doses of efbemalenograstim alfa-vuxw approximately 2.6 and 0.7 times, respectively, the
recommended human dose (based on body surface area).L48852

Overdosage of efbemalenograstim alfa may result in leukocytosis and bone pain. In the event of an overdose, general supportive measures should be instituted, as necessary. Monitor the patient for adverse reactions.L48852

No carcinogenicity or mutagenesis studies have been conducted with efbemalenograstim alfa-vuxw.L48852

Efbemalenograstim alfa did not affect reproductive performance or fertility in male or female rats at cumulative weekly doses approximately 2.2 times higher than the recommended human dose (based on body surface area).L48852

Efbemalenograstim alfa

DB18704

biotech approved

Deskripsi

Efbemalenograstim alfa is a long-acting recombinant fusion protein of granulocyte-colony stimulating factor (G-CSF) due to the addition of the Fc portion of human IgG2, allowing for once-per-cycle administration.L48852,A262167 As endogenous G-CSF mediates the differentiation of hematopoietic stem cells into granulocytes and eventually neutrophils, the administration of recombinant G-CSF like efbemalenograstim alfa can stimulate the production of neutrophils and thus reducing the severity and duration of neutropenia.A33650,A262172

On November 22, 2023, efbemalenograstim alfa was approved by the FDA under the brand name Ryzneuta for the treatment of chemotherapy-induced neutropenia in adult patients with non-myeloid malignancies receiving myelosuppressive anti-cancer drugs associated with a clinically significant incidence of febrile neutropenia. This approval was contingent on positive results observed in two pivotal Phase 3 Studies GC-627-04 and GC-627-05 in the US and Europe respectively.L48887

Struktur Molekul 2D

Struktur tidak tersedia

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The geometric mean (CV%) elimination half-life of efbemalenograstim alfa-vuxw was 35.6 h (108%) in Cycle 1 and 36.9 h (120%) in Cycle 3.[L48852]
Volume Distribusi The geometric mean (CV%) apparent volume of distribution of efbemalenograstim alfa-vuxw was 18.8 L (257%) in Cycle 1 and 40.7 L (387%) in Cycle 3 in female patients with breast cancer.[L48852]
Klirens (Clearance) The geometric mean (CV%) apparent clearance of efbemalenograstim alfa-vuxw was 0.36 L/h (110%) in Cycle 1 and 0.76 L/h (167%) in Cycle 3.[L48852]

Absorpsi

The median tmax of efbemalenograstim alfa-vuxw administered as 80 to 320 ?g/kg in female patients with breast cancer receiving EC chemotherapy ranged from 24 hours to 48 hours in Cycle 1 and 9 to 30 hours in Cycle 3. The median tmax of efbemalenograstim alfa-vuxw administered as 240 to 320 ?g/kg in female participants with breast cancer receiving TAC chemotherapy was 36 hours in Cycle 1 and ranged from 24 to 30 hours in Cycle 3.L48852

Metabolisme

Efbemalenograstim alfa-vuxw is expected to be metabolized into small peptides by catabolic pathways.L48852

Rute Eliminasi

Neutrophil receptor binding is an important component of the clearance of efbemalenograstim alfa-vuxw, and serum clearance is directly related to the number of neutrophils.L48852

Interaksi Obat

9 Data
Cyclophosphamide The risk or severity of pulmonary toxicity can be increased when Efbemalenograstim alfa is combined with Cyclophosphamide.
Topotecan The risk or severity of neutropenia can be increased when Efbemalenograstim alfa is combined with Topotecan.
Vindesine The risk or severity of peripheral neuropathy can be increased when Efbemalenograstim alfa is combined with Vindesine.
Vinorelbine The risk or severity of peripheral neuropathy can be increased when Efbemalenograstim alfa is combined with Vinorelbine.
Vincristine The risk or severity of peripheral neuropathy can be increased when Efbemalenograstim alfa is combined with Vincristine.
Vinblastine The risk or severity of peripheral neuropathy can be increased when Efbemalenograstim alfa is combined with Vinblastine.
Vintafolide The risk or severity of peripheral neuropathy can be increased when Efbemalenograstim alfa is combined with Vintafolide.
Vinflunine The risk or severity of peripheral neuropathy can be increased when Efbemalenograstim alfa is combined with Vinflunine.
Vincamine The risk or severity of peripheral neuropathy can be increased when Efbemalenograstim alfa is combined with Vincamine.

Target Protein

Granulocyte colony-stimulating factor receptor CSF3R

Referensi & Sumber

Artikel (PubMed)
  • PMID: 34114525
    Shayne M, Harvey RD, Lyman GH: Prophylaxis and treatment strategies for optimizing chemotherapy relative dose intensity. Expert Rev Anticancer Ther. 2021 Oct;21(10):1145-1159. doi: 10.1080/14737140.2021.1941891. Epub 2021 Jun 21.
  • PMID: 26254266
    Mehta HM, Malandra M, Corey SJ: G-CSF and GM-CSF in Neutropenia. J Immunol. 2015 Aug 15;195(4):1341-9. doi: 10.4049/jimmunol.1500861.
  • PMID: 17402806
    Cosler LE, Eldar-Lissai A, Culakova E, Kuderer NM, Dale D, Crawford J, Lyman GH: Therapeutic use of granulocyte colony-stimulating factors for established febrile neutropenia: effect on costs from a hospital perspective. Pharmacoeconomics. 2007;25(4):343-51. doi: 10.2165/00019053-200725040-00006.

Contoh Produk & Brand

Produk: 3 • International brands: 0
Produk
  • Ryzneuta
    Injection, solution • 20 mg • Subcutaneous • EU • Approved
  • Ryzneuta
    Injection • 20 mg/1mL • Subcutaneous • US • Approved
  • Ryzneuta
    Injection • 20 mg/1mL • Subcutaneous • US • Approved

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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