Peringatan Keamanan

No studies assessing the mutagenic or carcinogenic potential of E. coli L-asparagine have been conducted. In the Ames assay, no mutagenic effect was demonstrated when tested against Salmonella typhimurium strains FDA Label. No studies have been performed on impairment of fertility FDA Label. Following a single, intravenous injection of 12,500 to 50,000 International Units L-asparagine/kg in rabbits, edema and necrosis of pancreatic islets were observed. The clinical relevance of this finding is unclear as it does not indicate pancreatitis FDA Label.

Asparaginase Escherichia coli

DB00023

biotech approved investigational

Deskripsi

Asparaginase derived from Escherichia coli (L-asparagine amidohydrolase, EC 3.5.1.1) is an enzyme responsible for the metabolism of L-asparagine, by catalyzing L-asparagine into L-aspartic acid and ammonia. It also facilitates the production of oxaloacetate which is needed for general cellular metabolism. Asparaginase from E. coli has clinically shown to exhibit antitumor actions in models of leukaemias A31996, A31997. L-asparaginase of E. coli is marketed under several different trade names, including Elspar, for the treatment of acute lymphoblastic leukemia (ALL) as part of a multi-agent chemotherapeutic regimen. It is available as intramuscular or intravenous injections. Therapeutic L-asparaginase from E. coli works by depleting the levels of non-essential amino acid, asparagine, in lymphoblastic leukemic cells thus promoting apoptotic cell death A31999. For patients who develop hypersensitivity to E. coli-derived formulations of L-asparaginase, the use of PEGylated or non-PEGylated DB08886 is recommended A31999.

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) Plasma half life of L-asparagine derived from _E. coli_ following intravenous injection was 8-30 hrs [FDA Label]. Plasma half-life was 34 to 49 hours after intramuscular injection [FDA Label]. Half-life (mean ± SD) of native _E. coli_ asparaginase is approximately 1.28 ± 0.35 days [A31999].
Volume Distribusi Apparent volume of distribution was slightly greater than the plasma volume. Asparaginase levels in cerebrospinal fluid were less than 1% of concurrent plasma levels [A31999].
Klirens (Clearance) -

Absorpsi

In a study in patients with metastatic cancer and leukemia, daily intravenous administration of L-asparaginase derived from E. coli resulted in a cumulative increase in plasma levels. Following intramuscular injection in patients with metastatic cancer and leukemia, peak plasma levels of asparaginase was achieved 14 to 24 hours post-dosing FDA Label. Peak asparaginase activity of native E. coli asparaginase can be observed in 24 to 48 hours following administration A31999.

Metabolisme

Data metabolisme tidak tersedia.

Rute Eliminasi

Data eliminasi belum tersedia.

Interaksi Obat

59 Data
Dexamethasone The serum concentration of Dexamethasone can be increased when it is combined with Asparaginase Escherichia coli.
Methotrexate The therapeutic efficacy of Methotrexate can be decreased when used in combination with Asparaginase Escherichia coli.
Imatinib The risk or severity of liver damage can be increased when Asparaginase Escherichia coli is combined with Imatinib.
Phenytoin The therapeutic efficacy of Phenytoin can be increased when used in combination with Asparaginase Escherichia coli.
Liothyronine The therapeutic efficacy of Liothyronine can be increased when used in combination with Asparaginase Escherichia coli.
Levothyroxine The therapeutic efficacy of Levothyroxine can be increased when used in combination with Asparaginase Escherichia coli.
Mephenytoin The therapeutic efficacy of Mephenytoin can be increased when used in combination with Asparaginase Escherichia coli.
Carbamazepine The therapeutic efficacy of Carbamazepine can be increased when used in combination with Asparaginase Escherichia coli.
Furosemide The therapeutic efficacy of Furosemide can be increased when used in combination with Asparaginase Escherichia coli.
Nitrofurantoin The therapeutic efficacy of Nitrofurantoin can be increased when used in combination with Asparaginase Escherichia coli.
Ethotoin The therapeutic efficacy of Ethotoin can be increased when used in combination with Asparaginase Escherichia coli.
Meclofenamic acid The therapeutic efficacy of Meclofenamic acid can be increased when used in combination with Asparaginase Escherichia coli.
Heparin The therapeutic efficacy of Heparin can be increased when used in combination with Asparaginase Escherichia coli.
Dantrolene The therapeutic efficacy of Dantrolene can be increased when used in combination with Asparaginase Escherichia coli.
Fosphenytoin The therapeutic efficacy of Fosphenytoin can be increased when used in combination with Asparaginase Escherichia coli.
Liotrix The therapeutic efficacy of Liotrix can be increased when used in combination with Asparaginase Escherichia coli.
Etofenamate The therapeutic efficacy of Etofenamate can be increased when used in combination with Asparaginase Escherichia coli.
Liothyronine I-131 The therapeutic efficacy of Liothyronine I-131 can be increased when used in combination with Asparaginase Escherichia coli.
Neocitrullamon The therapeutic efficacy of Neocitrullamon can be increased when used in combination with Asparaginase Escherichia coli.
Allantoin The therapeutic efficacy of Allantoin can be increased when used in combination with Asparaginase Escherichia coli.
Darbepoetin alfa The risk or severity of Thrombosis can be increased when Darbepoetin alfa is combined with Asparaginase Escherichia coli.
Erythropoietin The risk or severity of Thrombosis can be increased when Erythropoietin is combined with Asparaginase Escherichia coli.
Peginesatide The risk or severity of Thrombosis can be increased when Peginesatide is combined with Asparaginase Escherichia coli.
Methoxy polyethylene glycol-epoetin beta The risk or severity of Thrombosis can be increased when Methoxy polyethylene glycol-epoetin beta is combined with Asparaginase Escherichia coli.
Lidocaine The risk or severity of methemoglobinemia can be increased when Asparaginase Escherichia coli is combined with Lidocaine.
Ropivacaine The risk or severity of methemoglobinemia can be increased when Asparaginase Escherichia coli is combined with Ropivacaine.
Bupivacaine The risk or severity of methemoglobinemia can be increased when Asparaginase Escherichia coli is combined with Bupivacaine.
Cinchocaine The risk or severity of methemoglobinemia can be increased when Asparaginase Escherichia coli is combined with Cinchocaine.
Dyclonine The risk or severity of methemoglobinemia can be increased when Asparaginase Escherichia coli is combined with Dyclonine.
Procaine The risk or severity of methemoglobinemia can be increased when Asparaginase Escherichia coli is combined with Procaine.
Prilocaine The risk or severity of methemoglobinemia can be increased when Asparaginase Escherichia coli is combined with Prilocaine.
Proparacaine The risk or severity of methemoglobinemia can be increased when Asparaginase Escherichia coli is combined with Proparacaine.
Meloxicam The risk or severity of methemoglobinemia can be increased when Asparaginase Escherichia coli is combined with Meloxicam.
Oxybuprocaine The risk or severity of methemoglobinemia can be increased when Asparaginase Escherichia coli is combined with Oxybuprocaine.
Cocaine The risk or severity of methemoglobinemia can be increased when Asparaginase Escherichia coli is combined with Cocaine.
Mepivacaine The risk or severity of methemoglobinemia can be increased when Asparaginase Escherichia coli is combined with Mepivacaine.
Levobupivacaine The risk or severity of methemoglobinemia can be increased when Asparaginase Escherichia coli is combined with Levobupivacaine.
Diphenhydramine The risk or severity of methemoglobinemia can be increased when Asparaginase Escherichia coli is combined with Diphenhydramine.
Benzocaine The risk or severity of methemoglobinemia can be increased when Asparaginase Escherichia coli is combined with Benzocaine.
Chloroprocaine The risk or severity of methemoglobinemia can be increased when Asparaginase Escherichia coli is combined with Chloroprocaine.
Phenol The risk or severity of methemoglobinemia can be increased when Asparaginase Escherichia coli is combined with Phenol.
Tetrodotoxin The risk or severity of methemoglobinemia can be increased when Asparaginase Escherichia coli is combined with Tetrodotoxin.
Benzyl alcohol The risk or severity of methemoglobinemia can be increased when Asparaginase Escherichia coli is combined with Benzyl alcohol.
Capsaicin The risk or severity of methemoglobinemia can be increased when Asparaginase Escherichia coli is combined with Capsaicin.
Etidocaine The risk or severity of methemoglobinemia can be increased when Asparaginase Escherichia coli is combined with Etidocaine.
Articaine The risk or severity of methemoglobinemia can be increased when Asparaginase Escherichia coli is combined with Articaine.
Tetracaine The risk or severity of methemoglobinemia can be increased when Asparaginase Escherichia coli is combined with Tetracaine.
Propoxycaine The risk or severity of methemoglobinemia can be increased when Asparaginase Escherichia coli is combined with Propoxycaine.
Pramocaine The risk or severity of methemoglobinemia can be increased when Asparaginase Escherichia coli is combined with Pramocaine.
Butamben The risk or severity of methemoglobinemia can be increased when Asparaginase Escherichia coli is combined with Butamben.
Butacaine The risk or severity of methemoglobinemia can be increased when Asparaginase Escherichia coli is combined with Butacaine.
Oxetacaine The risk or severity of methemoglobinemia can be increased when Asparaginase Escherichia coli is combined with Oxetacaine.
Ethyl chloride The risk or severity of methemoglobinemia can be increased when Asparaginase Escherichia coli is combined with Ethyl chloride.
Butanilicaine The risk or severity of methemoglobinemia can be increased when Asparaginase Escherichia coli is combined with Butanilicaine.
Metabutethamine The risk or severity of methemoglobinemia can be increased when Asparaginase Escherichia coli is combined with Metabutethamine.
Quinisocaine The risk or severity of methemoglobinemia can be increased when Asparaginase Escherichia coli is combined with Quinisocaine.
Nelarabine The risk or severity of adverse effects can be increased when Nelarabine is combined with Asparaginase Escherichia coli.
Ambroxol The risk or severity of methemoglobinemia can be increased when Asparaginase Escherichia coli is combined with Ambroxol.
Etrasimod The risk or severity of immunosuppression can be increased when Asparaginase Escherichia coli is combined with Etrasimod.

Target Protein

L-asparagine

Referensi & Sumber

Synthesis reference: Masao Nambu, "Process for producing immobilized L-asparaginase preparations for the therapy of leukemia." U.S. Patent US4617271, issued January, 1977.
Artikel (PubMed)
  • PMID: 5331901
    Roberts J, Prager MD, Bachynsky N: The antitumor activity of Escherichia coli L-asparaginase. Cancer Res. 1966 Oct;26(10):2213-7.
  • PMID: 5334543
    Boyse EA, Old LJ, Campbell HA, Mashburn LT: Suppression of murine leukemias by L-asparaginase. Incidence of sensitivity among leukemias of various types: comparative inhibitory activities of guinea pig serum L-asparaginase and Escherichia coli L-asparaginase. J Exp Med. 1967 Jan 1;125(1):17-31.
  • PMID: 25586605
    Asselin B, Rizzari C: Asparaginase pharmacokinetics and implications of therapeutic drug monitoring. Leuk Lymphoma. 2015;56(8):2273-80. doi: 10.3109/10428194.2014.1003056. Epub 2015 Mar 11.

Contoh Produk & Brand

Produk: 5 • International brands: 0
Produk
  • Elspar
    Injection, powder, lyophilized, for solution • 10000 [iU]/1 • Intramuscular; Intravenous • US • Approved
  • Kidrolase
    Powder, for solution • 10000 unit / vial • Intramuscular; Intravenous • Canada • Approved
  • Rylaze
    Injection • 20 mg/1mL • Intramuscular • US • Approved
  • Spectrila
    Injection, powder, for solution • 10000 U • Intravenous • EU • Approved
  • Spectrila
    Injection, powder, for solution • 10000 U • Intravenous • EU • Approved

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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