About: VNP 40101M     Goto   Sponge   NotDistinct   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
  • VNP40101M is a novel alkylating agent that is being evaluated for the treatment of acute myelogenous leukemia (AML. It is undergoing phase III development for the treatment of acute myeloid leukemia (AML) and earlier clinical trials for a range of other cancers. (en)
http://linked.open...generalReferences
  • # Giles F, Rizzieri D, Karp J, Vey N, Ravandi F, Faderl S, Khan KD, Verhoef G, Wijermans P, Advani A, Roboz G, Kantarjian H, Bilgrami SF, Ferrant A, Daenen SM, Karsten V, Cahill A, Albitar M, Mufti G, O'Brien S: Cloretazine (VNP40101M), a novel sulfonylhydrazine alkylating agent, in patients age 60 years or older with previously untreated acute myeloid leukemia. J Clin Oncol. 2007 Jan 1;25(1):25-31. Epub 2006 Dec 4. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/17146105 (en)
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  • investigational (en)
http://linked.open...ugbank/indication
  • Investigated for use/treatment in brain cancer, cancer/tumors (unspecified), colorectal cancer, leukemia (lymphoid), leukemia (myeloid), lung cancer, myelodysplastic syndrome, pediatric indications, and solid tumors. (en)
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Title
  • VNP 40101M (en)
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http://linked.open...mechanismOfAction
  • VNP40101M is a small molecule that works by damaging DNA. It releases the DNA chloroethylating agent 90CE after entering the blood stream. 90CE chloroethylates the O6 position of guanine residues, ultimately resulting in an interstrand DNA cross-link. Interstrand DNA cross-links are difficult to repair and are toxic to cells. VNP40101M demonstrates a broad spectrum of anticancer activity in preclinical studies, including activity in selected cell lines resistant to other alkylating agents such as BCNU, cyclophosphamide and melphalan. In preclinical studies, Cloretazine (VNP40101M) has been combined with other anticancer agents such as cytarabine (Ara-C). In addition, Cloretazine (VNP40101M) or its metabolite, has been shown to be capable of crossing the blood brain barrier in preclinical models. (en)
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