Peringatan Keamanan

Patients that received 10,000 International Units/m2 of pegaspargase intravenously, had a slight increase in liver enzymes and a rash that developed 10 minutes after the start of the infusion, which was controlled with the administration of an antihistamine and by slowing down the infusion rate. There is no specific antidote for pegaspargase overdosage. The product label recommends to monitor patients closely for signs and symptoms of adverse reactions, and appropriately manage with symptomatic and supportive treatment in case of overdose. The carcinogenic, mutagenic and fertility effects of pegaspargase have not been evaluated.L44667

Pegaspargase

DB00059

biotech approved investigational

Deskripsi

Pegaspargase is a conjugate of monomethoxypolyethylene glycol (mPEG) and L-asparaginase (L-asparagine amidohydrolase), an asparagine-specific enzyme that converts L-asparagine into aspartic acid and ammonia.L44667 Asparagine is an amino acid that is vital for cell survival. In humans, most normal tissues can produce asparagine through the action of asparagine synthetase. However, leukemia cells have low levels of this enzyme and depend on exogenous sources. Therefore, the use of pegaspargase results in leukemic cell death.A103,A255912,L44667

Pegaspargase has the same mechanism of action as L-asparaginase derived from Escherichia coli, a previously developed enzyme used for the treatment of acute lymphoblastic leukemia (ALL). However, using L-asparaginase derived from Escherichia coli may cause hypersensitivity in some patients and require frequent administration. The pegylation of pegaspargase allows access to the enzyme's active sites while limiting reticuloendothelial system uptake and reducing immune detection, and it also increases the half-life of L-asparaginase.A255912,A255917 In February 1994, pegaspargase was approved by the FDA for the treatment of ALL in patients with hypersensitivity to native forms of L-asparaginase.A255927

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) The mean elimination half-life of pegaspargase was approximately 5.8 days after a single intramuscular dose, and 5.3 days after a single intravenous dose.[L44667]
Volume Distribusi Based on a non-compartmental analysis, pegaspargase has a steady-state volume of distribution of approximately 1.86 L/m2 after a single intramuscular injection and 2 L after a single intravenous infusion.[L44667]
Klirens (Clearance) For a single intramuscular and intravenous dose, the clearance of pegaspargase is 0.17 L/m2/day and 0.2 L/day, respectively.[L44667]

Absorpsi

In patients with acute lymphoblastic leukemia given 2,500 International Units (IU)/m2 of pegaspargase, the mean asparaginase Cmax was reached at approximately 1 IU/mL (n=45-52) five days after a single intramuscular injection. Pegaspargase had a relative bioavailability of 82% after the first intramuscular dose and 98% following repeat dosing. In patients given pegaspargase intravenously in a single infusion (n=47) during the induction phase, the mean Cmax and AUC0-inf were 1.6 IU/mL and 16.6 IU/mL?day, respectively.L44667 The Tmax for these patients was 1.25 hr.L44672 The impact of renal and hepatic impairment on pegaspargase pharmacokinetics is unknown.L44667

Metabolisme

As a pegylated form of L-asparaginase, pegaspargase is expected to be metabolized by proteolytic enzymes throughout the body. Since these enzymes are ubiquitously distributed, the exact role of the liver is unknown.L44672

Rute Eliminasi

Due to its high molecular weight, pegaspargase is not excreted renally.L44672

Interaksi Makanan

1 Data
  • 1. Avoid excessive or chronic alcohol consumption. Alcohol and pegaspargase can both cause hepatoxicity, therefore if they are used together they may have additive hepatoxic effects.

Interaksi Obat

446 Data
Denosumab The risk or severity of adverse effects can be increased when Denosumab is combined with Pegaspargase.
Etanercept The risk or severity of adverse effects can be increased when Etanercept is combined with Pegaspargase.
Peginterferon alfa-2a The risk or severity of adverse effects can be increased when Peginterferon alfa-2a is combined with Pegaspargase.
Interferon alfa-n1 The risk or severity of adverse effects can be increased when Interferon alfa-n1 is combined with Pegaspargase.
Interferon alfa-n3 The risk or severity of adverse effects can be increased when Interferon alfa-n3 is combined with Pegaspargase.
Peginterferon alfa-2b The risk or severity of adverse effects can be increased when Peginterferon alfa-2b is combined with Pegaspargase.
Anakinra The risk or severity of adverse effects can be increased when Anakinra is combined with Pegaspargase.
Interferon gamma-1b The risk or severity of adverse effects can be increased when Interferon gamma-1b is combined with Pegaspargase.
Interferon alfa-2a The risk or severity of adverse effects can be increased when Interferon alfa-2a is combined with Pegaspargase.
Aldesleukin The risk or severity of adverse effects can be increased when Aldesleukin is combined with Pegaspargase.
Adalimumab The risk or severity of adverse effects can be increased when Adalimumab is combined with Pegaspargase.
Gemtuzumab ozogamicin The risk or severity of adverse effects can be increased when Gemtuzumab ozogamicin is combined with Pegaspargase.
Infliximab The risk or severity of adverse effects can be increased when Pegaspargase is combined with Infliximab.
Interferon beta-1b The risk or severity of adverse effects can be increased when Pegaspargase is combined with Interferon beta-1b.
Interferon alfacon-1 The risk or severity of adverse effects can be increased when Pegaspargase is combined with Interferon alfacon-1.
Rituximab The risk or severity of adverse effects can be increased when Pegaspargase is combined with Rituximab.
Basiliximab The risk or severity of adverse effects can be increased when Pegaspargase is combined with Basiliximab.
Muromonab The risk or severity of adverse effects can be increased when Pegaspargase is combined with Muromonab.
Ibritumomab tiuxetan The risk or severity of adverse effects can be increased when Pegaspargase is combined with Ibritumomab tiuxetan.
Tositumomab The risk or severity of adverse effects can be increased when Pegaspargase is combined with Tositumomab.
Alemtuzumab The risk or severity of adverse effects can be increased when Pegaspargase is combined with Alemtuzumab.
Alefacept The risk or severity of adverse effects can be increased when Pegaspargase is combined with Alefacept.
Efalizumab The risk or severity of adverse effects can be increased when Pegaspargase is combined with Efalizumab.
Antithymocyte immunoglobulin (rabbit) The risk or severity of adverse effects can be increased when Pegaspargase is combined with Antithymocyte immunoglobulin (rabbit).
Interferon alfa-2b The risk or severity of adverse effects can be increased when Pegaspargase is combined with Interferon alfa-2b.
Daclizumab The risk or severity of adverse effects can be increased when Pegaspargase is combined with Daclizumab.
Phenylalanine The risk or severity of adverse effects can be increased when Pegaspargase is combined with Phenylalanine.
Flunisolide The risk or severity of adverse effects can be increased when Pegaspargase is combined with Flunisolide.
Bortezomib The risk or severity of adverse effects can be increased when Pegaspargase is combined with Bortezomib.
Cladribine Pegaspargase may increase the immunosuppressive activities of Cladribine.
Carmustine The risk or severity of adverse effects can be increased when Pegaspargase is combined with Carmustine.
Amsacrine The risk or severity of adverse effects can be increased when Pegaspargase is combined with Amsacrine.
Bleomycin The risk or severity of adverse effects can be increased when Pegaspargase is combined with Bleomycin.
Chlorambucil The risk or severity of adverse effects can be increased when Pegaspargase is combined with Chlorambucil.
Raltitrexed The risk or severity of adverse effects can be increased when Pegaspargase is combined with Raltitrexed.
Mitomycin The risk or severity of adverse effects can be increased when Pegaspargase is combined with Mitomycin.
Bexarotene The risk or severity of adverse effects can be increased when Pegaspargase is combined with Bexarotene.
Vindesine The risk or severity of adverse effects can be increased when Pegaspargase is combined with Vindesine.
Floxuridine The risk or severity of adverse effects can be increased when Pegaspargase is combined with Floxuridine.
Indomethacin The risk or severity of adverse effects can be increased when Pegaspargase is combined with Indomethacin.
Tioguanine The risk or severity of adverse effects can be increased when Pegaspargase is combined with Tioguanine.
Vinorelbine The risk or severity of adverse effects can be increased when Pegaspargase is combined with Vinorelbine.
Dexrazoxane The risk or severity of adverse effects can be increased when Pegaspargase is combined with Dexrazoxane.
Beclomethasone dipropionate The serum concentration of Beclomethasone dipropionate can be increased when it is combined with Pegaspargase.
Sorafenib The risk or severity of adverse effects can be increased when Pegaspargase is combined with Sorafenib.
Streptozocin The risk or severity of adverse effects can be increased when Pegaspargase is combined with Streptozocin.
Trifluridine The risk or severity of adverse effects can be increased when Pegaspargase is combined with Trifluridine.
Gemcitabine The risk or severity of adverse effects can be increased when Pegaspargase is combined with Gemcitabine.
Betamethasone The serum concentration of Betamethasone can be increased when it is combined with Pegaspargase.
Teniposide The risk or severity of adverse effects can be increased when Pegaspargase is combined with Teniposide.
Epirubicin The risk or severity of adverse effects can be increased when Pegaspargase is combined with Epirubicin.
Chloramphenicol The risk or severity of adverse effects can be increased when Pegaspargase is combined with Chloramphenicol.
Lenalidomide The risk or severity of adverse effects can be increased when Pegaspargase is combined with Lenalidomide.
Altretamine The risk or severity of adverse effects can be increased when Pegaspargase is combined with Altretamine.
Zidovudine The risk or severity of adverse effects can be increased when Pegaspargase is combined with Zidovudine.
Cisplatin The risk or severity of adverse effects can be increased when Pegaspargase is combined with Cisplatin.
Oxaliplatin The risk or severity of adverse effects can be increased when Pegaspargase is combined with Oxaliplatin.
Cyclophosphamide The risk or severity of adverse effects can be increased when Pegaspargase is combined with Cyclophosphamide.
Vincristine The risk or severity of adverse effects can be increased when Pegaspargase is combined with Vincristine.
Fluorouracil The risk or severity of adverse effects can be increased when Pegaspargase is combined with Fluorouracil.
Propylthiouracil The risk or severity of adverse effects can be increased when Pegaspargase is combined with Propylthiouracil.
Pentostatin The risk or severity of adverse effects can be increased when Pegaspargase is combined with Pentostatin.
Carbamazepine The risk or severity of adverse effects can be increased when Pegaspargase is combined with Carbamazepine.
Vinblastine The risk or severity of adverse effects can be increased when Pegaspargase is combined with Vinblastine.
Fluticasone propionate The serum concentration of Fluticasone propionate can be increased when it is combined with Pegaspargase.
Fluocinolone acetonide The risk or severity of adverse effects can be increased when Pegaspargase is combined with Fluocinolone acetonide.
Linezolid The risk or severity of adverse effects can be increased when Pegaspargase is combined with Linezolid.
Triamcinolone The serum concentration of Triamcinolone can be increased when it is combined with Pegaspargase.
Clofarabine The risk or severity of adverse effects can be increased when Pegaspargase is combined with Clofarabine.
Prednisone The serum concentration of Prednisone can be increased when it is combined with Pegaspargase.
Pemetrexed The risk or severity of adverse effects can be increased when Pegaspargase is combined with Pemetrexed.
Fludrocortisone The risk or severity of adverse effects can be increased when Pegaspargase is combined with Fludrocortisone.
Mycophenolate mofetil The risk or severity of adverse effects can be increased when Pegaspargase is combined with Mycophenolate mofetil.
Daunorubicin The risk or severity of adverse effects can be increased when Pegaspargase is combined with Daunorubicin.
Irinotecan The risk or severity of adverse effects can be increased when Pegaspargase is combined with Irinotecan.
Methimazole The risk or severity of adverse effects can be increased when Pegaspargase is combined with Methimazole.
Etoposide The risk or severity of adverse effects can be increased when Pegaspargase is combined with Etoposide.
Sulfasalazine The risk or severity of adverse effects can be increased when Pegaspargase is combined with Sulfasalazine.
Dacarbazine The risk or severity of adverse effects can be increased when Pegaspargase is combined with Dacarbazine.
Temozolomide The risk or severity of adverse effects can be increased when Pegaspargase is combined with Temozolomide.
Penicillamine The risk or severity of adverse effects can be increased when Pegaspargase is combined with Penicillamine.
Prednisolone The risk or severity of adverse effects can be increased when Pegaspargase is combined with Prednisolone.
Sirolimus The risk or severity of adverse effects can be increased when Pegaspargase is combined with Sirolimus.
Mechlorethamine The risk or severity of adverse effects can be increased when Pegaspargase is combined with Mechlorethamine.
Azacitidine The risk or severity of adverse effects can be increased when Pegaspargase is combined with Azacitidine.
Carboplatin The risk or severity of adverse effects can be increased when Pegaspargase is combined with Carboplatin.
Methylprednisolone The risk or severity of adverse effects can be increased when Pegaspargase is combined with Methylprednisolone.
Dactinomycin The risk or severity of adverse effects can be increased when Pegaspargase is combined with Dactinomycin.
Cytarabine The risk or severity of adverse effects can be increased when Pegaspargase is combined with Cytarabine.
Azathioprine The risk or severity of adverse effects can be increased when Pegaspargase is combined with Azathioprine.
Doxorubicin The risk or severity of adverse effects can be increased when Pegaspargase is combined with Doxorubicin.
Hydroxyurea The risk or severity of adverse effects can be increased when Pegaspargase is combined with Hydroxyurea.
Busulfan The risk or severity of adverse effects can be increased when Pegaspargase is combined with Busulfan.
Mycophenolic acid The risk or severity of adverse effects can be increased when Pegaspargase is combined with Mycophenolic acid.
Topotecan The risk or severity of adverse effects can be increased when Pegaspargase is combined with Topotecan.
Mercaptopurine The risk or severity of adverse effects can be increased when Pegaspargase is combined with Mercaptopurine.
Thalidomide The risk or severity of adverse effects can be increased when Pegaspargase is combined with Thalidomide.
Melphalan The risk or severity of adverse effects can be increased when Pegaspargase is combined with Melphalan.
Fludarabine The risk or severity of adverse effects can be increased when Pegaspargase is combined with Fludarabine.
Flucytosine The risk or severity of adverse effects can be increased when Pegaspargase is combined with Flucytosine.

Target Protein

L-asparagine

Referensi & Sumber

Artikel (PubMed)
  • PMID: 14499708
    Graham ML: Pegaspargase: a review of clinical studies. Adv Drug Deliv Rev. 2003 Sep 26;55(10):1293-302.
  • PMID: 19063697
    Zeidan A, Wang ES, Wetzler M: Pegasparaginase: where do we stand? Expert Opin Biol Ther. 2009 Jan;9(1):111-9. doi: 10.1517/14712590802586058.
  • PMID: 31030380
    Heo YA, Syed YY, Keam SJ: Pegaspargase: A Review in Acute Lymphoblastic Leukaemia. Drugs. 2019 May;79(7):767-777. doi: 10.1007/s40265-019-01120-1.
  • PMID: 17696798
    Fu CH, Sakamoto KM: PEG-asparaginase. Expert Opin Pharmacother. 2007 Aug;8(12):1977-84. doi: 10.1517/14656566.8.12.1977.

Contoh Produk & Brand

Produk: 9 • International brands: 1
Produk
  • Lyophilized Pegaspargase
    Injection, powder, lyophilized, for solution • 750 U/1mL • Intramuscular • US
  • Lyophilized Pegaspargase
    Injection, powder, lyophilized, for solution • 750 [iU]/1mL • Intravenous • US
  • Oncaspar
    Injection, solution • 750 [iU]/1mL • Intramuscular; Intravenous • US • Approved
  • Oncaspar
    Injection, solution • 750 [iU]/1mL • Intramuscular; Intravenous • US • Approved
  • Oncaspar
    Injection, solution • 750 [iU]/1mL • Intramuscular; Intravenous • US • Approved
  • Oncaspar
    Solution • 750 unit / mL • Intramuscular; Intravenous • Canada • Approved
  • Oncaspar
    Liquid • 750 unit / mL • Intramuscular; Intravenous • Canada • Approved
  • Oncaspar
    Injection, solution • 750 U/ml • Intramuscular; Intravenous • EU • Approved
Menampilkan 8 dari 9 produk.
International Brands
  • Oncaspar — Servier Pharmaceuticals

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