About: Nelarabine     Goto   Sponge   Distinct   Permalink

An Entity of Type : http://linked.opendata.cz/ontology/drugbank/Drug, within Data Space : linked.opendata.cz associated with source document(s)

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http://linked.open...gbank/description
  • Nelarabine is a chemotherapy drug used in T-cell acute lymphoblastic leukemia. Nelarabine is a purine nucleoside analog converted to its corresponding arabinosylguanine nucleotide triphosphate (araGTP), resulting in inhibition of DNA synthesis and cytotoxicity. (en)
http://linked.open...y/drugbank/dosage
http://linked.open...generalReferences
  • # Buie LW, Epstein SS, Lindley CM: Nelarabine: a novel purine antimetabolite antineoplastic agent. Clin Ther. 2007 Sep;29(9):1887-99. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/18035189 # DeAngelo DJ: Nelarabine for the treatment of patients with relapsed or refractory T-cell acute lymphoblastic leukemia or lymphoblastic lymphoma. Hematol Oncol Clin North Am. 2009 Oct;23(5):1121-35, vii-viii. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/19825456 # Roecker AM, Allison JC, Kisor DF: Nelarabine: efficacy in the treatment of clinical malignancies. Future Oncol. 2006 Aug;2(4):441-8. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/16922610 # Sanford M, Lyseng-Williamson KA: Nelarabine. Drugs. 2008;68(4):439-47. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/18318562 # Reilly KM, Kisor DF: Profile of nelarabine: use in the treatment of T-cell acute lymphoblastic leukemia. Onco Targets Ther. 2009 Feb 18;2:219-28. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/20616909 # Cooper TM: Role of nelarabine in the treatment of T-cell acute lymphoblastic leukemia and T-cell lymphoblastic lymphoma. Ther Clin Risk Manag. 2007 Dec;3(6):1135-41. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/18516261 # Curbo S, Karlsson A: Nelarabine: a new purine analog in the treatment of hematologic malignancies. Rev Recent Clin Trials. 2006 Sep;1(3):185-92. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/18473971 # Sigalas P, Tourvas AD, Moulakakis A, Pangalis G, Kontopidou F: Nelarabine induced complete remission in an adult with refractory T-lineage acute lymphoblastic leukemia: A case report and review of the literature. Leuk Res. 2009 Jul;33(7):e61-3. Epub 2009 Jan 21. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/19157550 # Gandhi V, Keating MJ, Bate G, Kirkpatrick P: Nelarabine. Nat Rev Drug Discov. 2006 Jan;5(1):17-8. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/16485343 (en)
http://linked.open...gy/drugbank/group
  • approved (en)
  • investigational (en)
http://linked.open...drugbank/halfLife
  • Nelarabine and ara-G are rapidly eliminated from plasma with a half-life of approximately 30 minutes and 3 hours. (en)
http://linked.open...ugbank/indication
  • For the treatment of pediatric and adult patients with acute T-cell lymphoblastic leukemia and T-cell lymphoblastic lymphoma whose disease has not responded to or has relapsed following treatment with at least two chemotherapy regimens. (en)
sameAs
Title
  • Nelarabine (en)
adms:identifier
http://linked.open...mechanismOfAction
  • Once nelarabine is metabolized into ara-GTP, the metabolite accumulates in leukemic blasts and incorporates into DNA to exert its S phase-specific cytotoxic effects, leading to the induction of fragmentation and apoptosis. Ara-GTP competes with endogenous deoxyGTP (dGTP) for incorporation into DNA. Once ara-GTP is incorporated at the 3' end of DNA, further DNA elongation is inhibited, which signals apoptosis and leads to cellular destruction. Additional cytotoxic activities may exist, but these are not fully understood. (en)
http://linked.open...drugbank/packager
http://linked.open...y/drugbank/patent
http://linked.open...outeOfElimination
  • Excretion: Nelarabine and ara-G are partially eliminated by the kidneys. (en)
http://linked.open.../drugbank/synonym
  • Arranon (en)
  • GW-506U78 (en)
  • Nelzarabine (en)
  • 2-Amino-9-beta-D-arabinofuranosyl-6-methoxy-9H-purine (en)
http://linked.open...drugbank/toxicity
  • A single IV dose of 4,800 mg/m^2 was lethal in monkeys, and was associated with CNS signs including reduced/shallow respiration, reduced reflexes, and flaccid muscle tone. It is anticipated that overdosage would result in severe neurotoxicity (possibly including paralysis, coma), myelosuppression, and potentially death. (en)
http://linked.open...nk/proteinBinding
  • Nelarabine and ara-G are not substantially bound to human plasma proteins (<25%) in vitro, and binding is independent of nelarabine or ara-G concentrations up to 600 mM. (en)
foaf:page
http://linked.open...ugbank/IUPAC-Name
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http://linked.open...Molecular-Formula
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http://linked.open...noisotopic-Weight
http://linked.open...y/drugbank/SMILES
http://linked.open.../Water-Solubility
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http://linked.open...ogy/drugbank/logS
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http://linked.open...nd-Acceptor-Count
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http://linked.open...urface-Area--PSA-
http://linked.open...nk/Polarizability
http://linked.open...bank/Refractivity
http://linked.open...atable-Bond-Count
http://linked.open.../affectedOrganism
  • Humans and other mammals (en)
http://linked.open...casRegistryNumber
  • 121032-29-9 (en)
http://linked.open...rugbank/clearance
  • * 197  +/-  189 L/h/m2 [Adult patients with refractory leukemia or lymphoma receiving doses of 199 to 2,900 mg/m2] * 259  +/-  409 L/h/m2 [Pediatric patients with refractory leukemia or lymphoma receiving doses of 104 to 2,900 mg/m2] (en)
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http://linked.open...bank/Rule-of-Five
http://linked.open...tional-IUPAC-Name
http://linked.open...strongest-acidic-
http://linked.open...-strongest-basic-
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