Nelarabine

Gefahreninformationscode (GHS)

• Bildanzeige (GHS)

  

• Alarmwort

  Warnung

• Gefahrenhinweise

  H302：Gesundheitsschädlich bei Verschlucken.

  H315：Verursacht Hautreizungen.

  H319：Verursacht schwere Augenreizung.

  H335：Kann die Atemwege reizen.

• Sicherheit

  P261：Einatmen von Staub vermeiden.

  P305+P351+P338：BEI KONTAKT MIT DEN AUGEN: Einige Minuten lang behutsam mit Wasser spülen. Eventuell vorhandene Kontaktlinsen nach Möglichkeit entfernen. Weiter spülen.

Nelarabine Chemische Eigenschaften,Einsatz,Produktion Methoden

• Beschreibung

  Nelarabine is a new member of the purine nucleoside antimetabolite class of drugs. It was launched as an intravenous infusion for treating relapsed or refractory T-cell acute lymphoblastic leukemia (T-ALL) and T-cell lymphoblastic lymphoma (T-LBL) after at least two prior chemotherapy regimens. Nelarabine is a pro-drug of 9-b-D-arabinofuranosylguanine (ara-G), a deoxyguanosine derivative with a high level of T-cell selective cytotoxicity. Although Ara-G has been known since the 1960s, it has not been used in clinical studies due to its poor solubility. Nelarabine is the O-methyl derivative of ara-G with approximately 10 times greater aqueous solubility. It is demethylated in vivo by adenosine deaminase to produce ara-G, which is subsequently converted to the active 5’-triphosphate, ara-GTP. Accumulation of ara-GTP in leukemic blasts allows for incorporation into DNA, leading to inhibition of DNA synthesis and cell death.

• Originator

  Glaxo Wellcome (US)

• Verwenden

  A chemotherapy drug used in the treatment of relapsed/refractory T-cell acute lymphoblastic leukemia (T-ALL) and T-cell lymphoblastic lymphoma (T-LBL).

• Definition

  ChEBI: Nelarabine is a purine nucleoside in which O-methylguanine is attached to arabinofuranose via a beta-N(9)-glycosidic bond. Inhibits DNA synthesis and causes cell death; a prodrug of 9-beta-D-arabinofuranosylguanine (ara-G). It has a role as an antineoplastic agent, a DNA synthesis inhibitor and a prodrug. It is a purine nucleoside, a beta-D-arabinoside and a monosaccharide derivative. It is functionally related to a guanine and a 9-beta-D-arabinofuranosylguanine.

• Trademarks

  Arranon (SmithKline Beecham).

• Clinical Use

  Antineoplastic agent:
  T-cell acute lymphoblastic leukaemia (T-ALL)
  T-cell lymphoblastic lymphoma (T-LBL)

• Synthese

  The drug was synthesized by enzymatic coupling of arabinosyluracil 87, prepared according to literature and 2-amino- 6-methoxy purine 88 using purine nucleoside phosphorylase (PNP) and uridine phosphorylase (UP) in phosphate buffer for 30 days to give the nelarabine (XIII) in 48% yield.

  

• Stoffwechsel

  Nelarabine is a pro-drug of the deoxyguanosine analogue ara-G. Extensive metabolism by O-demethylation by adenosine deaminase to form ara-G, which undergoes hydrolysis to form guanine. In addition, some nelarabine is hydrolysed to form methylguanine, which is O-demethylated to form guanine. Guanine is N-deaminated to form xanthine, which is further oxidised to yield uric acid. Nelarabine and ara-G are partially eliminated by the kidneys.

• Lager

  Store at +4°C

• Einzelnachweise

  [1] cohen mh, johnson jr, massie t, et al. approval summary: nelarabine for the treatment of t-cell lymphoblastic leukemia/lymphoma. clin cancer res. september 2006. 18:5329–35.
  [2] yesid alvarado, mary alma welch, ronan swords, john bruzzi, ellen schlette, francis j. giles. nelarabine activity in acute biphenotypic leukemia. leukemia research. november 2007. 31(11): 1600-1603.

Nelarabine Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

Global(273)Suppliers

121032-29-9, Nelarabine Verwandte Suche: