Peringatan Keamanan

Pancreatitis, hepatotoxicity, hemorrhage, and thrombosis have been observed with calaspargase pegol use FDA label.

Pancreatitis:
Discontinue this drug in patients with pancreatitis, and monitor blood glucose.

Hepatotoxicity:
Hepatic function should be tested regularly, and trough levels of this drug should be measured during the recovery phase of the drug cycle FDA label.

Hemorrhage or Thrombosis: Discontinue this drug in serious or life-threatening hemorrhage or thrombosis. In cases of hemorrhage, identify the cause of hemorrhage and treat appropriately. Administer anticoagulant therapy as indicated in thrombotic events FDA label.

A note on hypersensitivity:

Observe the patient for 1 hour after administration of calaspargase pegol for possible hypersensitivity FDA label. In cases of previous hypersensitivity to this drug, discontinue this drug immediately.

Lactation: Advise women not to breastfeed while taking this drug FDA label.

Pregnancy: There are no available data on the use of calaspargase pegol in pregnant women to confirm a risk of drug-associated major birth defects and miscarriage. Published literature studies in pregnant animals suggest asparagine depletion can cause harm to the animal offspring. It is therefore advisable to inform women of childbearing age of this risk. The background risk of major birth defects and miscarriage for humans is unknown at this time FDA label.

Pregnancy testing should occur before initiating treatment. Advise females of reproductive potential to avoid becoming pregnant while taking this drug. Females should use effective contraceptive methods, including a barrier methods, during treatment and for at least 3 months after the last dose. There is a risk for an interaction between calaspargase pegol and oral contraceptives. The concurrent use of this drug with oral contraceptives should be avoided. Other non-oral contraceptive methods should be used in women of childbearing potential FDA label.

Calaspargase pegol

DB14730

biotech approved

Deskripsi

Asparaginase is an important agent used to treat acute lymphoblastic leukemia (ALL) A40270. Asparagine is incorporated into most proteins, and the synthesis of proteins is stopped when asparagine is absent, which inhibits RNA and DNA synthesis, resulting in a halt in cellular proliferation. This forms the basis of asparaginase treatment in ALL A40270, A40273, F2432.

Calaspargase pegol, also known as asparlas, is an asparagine specific enzyme which is indicated as a part of a multi-agent chemotherapy regimen for the treatment of ALL L4890. The asparagine specific enzyme is derived from Escherichia coli, as a conjugate of L-asparaginase (L-asparagine amidohydrolase) and monomethoxypolyethylene glycol (mPEG) with a succinimidyl carbonate (SC) linker to create a stable molecule which increases the half-life and decreases the dosing frequency FDA label, A40270.

Calaspargase pegol, by Shire pharmaceuticals, was approved by the FDA on December 20, 2018 for acute lymphoblastic anemia (ALL) L4890.

Struktur Molekul 2D

Struktur tidak tersedia

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) 16.1 days [FDA label]
Volume Distribusi Vss (L): 2.96 [FDA label]
Klirens (Clearance) 0.147 L/day [FDA label]

Absorpsi

Mean Tmax (1 h): 1.7 FDA label.

Metabolisme

Data metabolisme tidak tersedia.

Rute Eliminasi

Data eliminasi belum tersedia.

Interaksi Obat

26 Data
Desogestrel The therapeutic efficacy of Desogestrel can be decreased when used in combination with Calaspargase pegol.
Megestrol acetate The therapeutic efficacy of Megestrol acetate can be decreased when used in combination with Calaspargase pegol.
Levonorgestrel The therapeutic efficacy of Levonorgestrel can be decreased when used in combination with Calaspargase pegol.
Medroxyprogesterone acetate The therapeutic efficacy of Medroxyprogesterone acetate can be decreased when used in combination with Calaspargase pegol.
Norethisterone The therapeutic efficacy of Norethisterone can be decreased when used in combination with Calaspargase pegol.
Estradiol The therapeutic efficacy of Estradiol can be decreased when used in combination with Calaspargase pegol.
Ethynodiol diacetate The therapeutic efficacy of Ethynodiol diacetate can be decreased when used in combination with Calaspargase pegol.
Mifepristone The therapeutic efficacy of Mifepristone can be decreased when used in combination with Calaspargase pegol.
Norgestimate The therapeutic efficacy of Norgestimate can be decreased when used in combination with Calaspargase pegol.
Ethinylestradiol The therapeutic efficacy of Ethinylestradiol can be decreased when used in combination with Calaspargase pegol.
Drospirenone The therapeutic efficacy of Drospirenone can be decreased when used in combination with Calaspargase pegol.
Cyproterone acetate The therapeutic efficacy of Cyproterone acetate can be decreased when used in combination with Calaspargase pegol.
Gestodene The therapeutic efficacy of Gestodene can be decreased when used in combination with Calaspargase pegol.
Dienogest The therapeutic efficacy of Dienogest can be decreased when used in combination with Calaspargase pegol.
Norethynodrel The therapeutic efficacy of Norethynodrel can be decreased when used in combination with Calaspargase pegol.
Norgestrel The therapeutic efficacy of Norgestrel can be decreased when used in combination with Calaspargase pegol.
Gestrinone The therapeutic efficacy of Gestrinone can be decreased when used in combination with Calaspargase pegol.
Lynestrenol The therapeutic efficacy of Lynestrenol can be decreased when used in combination with Calaspargase pegol.
Ormeloxifene The therapeutic efficacy of Ormeloxifene can be decreased when used in combination with Calaspargase pegol.
Chlormadinone The therapeutic efficacy of Chlormadinone can be decreased when used in combination with Calaspargase pegol.
Norgestrienone The therapeutic efficacy of Norgestrienone can be decreased when used in combination with Calaspargase pegol.
Quingestanol The therapeutic efficacy of Quingestanol can be decreased when used in combination with Calaspargase pegol.
Demegestone The therapeutic efficacy of Demegestone can be decreased when used in combination with Calaspargase pegol.
Nomegestrol acetate The therapeutic efficacy of Nomegestrol acetate can be decreased when used in combination with Calaspargase pegol.
Estetrol The therapeutic efficacy of Estetrol can be decreased when used in combination with Calaspargase pegol.
Mestranol The therapeutic efficacy of Mestranol can be decreased when used in combination with Calaspargase pegol.

Target Protein

L-asparagine

Referensi & Sumber

Artikel (PubMed)
  • PMID: 25348002
    Angiolillo AL, Schore RJ, Devidas M, Borowitz MJ, Carroll AJ, Gastier-Foster JM, Heerema NA, Keilani T, Lane AR, Loh ML, Reaman GH, Adamson PC, Wood B, Wood C, Zheng HW, Raetz EA, Winick NJ, Carroll WL, Hunger SP: Pharmacokinetic and pharmacodynamic properties of calaspargase pegol Escherichia coli L-asparaginase in the treatment of patients with acute lymphoblastic leukemia: results from Children's Oncology Group Study AALL07P4. J Clin Oncol. 2014 Dec 1;32(34):3874-82. doi: 10.1200/JCO.2014.55.5763. Epub 2014 Oct 27.
  • PMID: 18580955
    Appel IM, Kazemier KM, Boos J, Lanvers C, Huijmans J, Veerman AJ, van Wering E, den Boer ML, Pieters R: Pharmacokinetic, pharmacodynamic and intracellular effects of PEG-asparaginase in newly diagnosed childhood acute lymphoblastic leukemia: results from a single agent window study. Leukemia. 2008 Sep;22(9):1665-79. doi: 10.1038/leu.2008.165. Epub 2008 Jun 26.

Contoh Produk & Brand

Produk: 2 • International brands: 0
Produk
  • Asparlas
    Injection, solution • 750 U/1mL • Intravenous • US • Approved
  • Asparlas
    Solution • 3750 unit / 5 mL • Intravenous • Canada • Approved

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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