"目录号: HY-13727
Pixantrone (BBR 2778)具有抗肿瘤活性。
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生物活性
Description
Pixantrone (BBR 2778) is an experimental antineoplastic drug.Target: OthersPixantrone is an experimental antineoplastic (anti-cancer) drug, an analogue of mitoxantrone with fewer toxic effects on cardiac tissue, It acts as a topoisomerase II poison and intercalating agent. Pixantrone may be useful in patients pretreated with anthracyclines [1]. An in vitro crosslinking assay demonstrated that Pixantrone is efficiently activated by formaldehyde to generate covalent drug-DNA adducts capable of stabilizing double-stranded DNA in denaturing conditions. Pixantrone-DNA adduct formation is both concentration and time dependent and the reaction exhibits an absolute requirement for formaldehyde. Pixantrone exhibited a 10- to 100-fold greater propensity to generate adducts at equimolar formaldehyde and drug concentrations. Pixantrone-DNA adducts are thermally and temporally labile, yet they exhibit a greater thermal midpoint temperature and an extended half-life at 37 degrees C when compared to mitoxantrone-DNA adducts [2].
Clinical Trial
CTI BioPharma
Lymphoma, Follicular-Lymphoma, Mixed-Cell, Follicular-Lymphoma, Small Cleaved-Cell, Follicular-Lymphoma, Low-Grade
January 2005
Phase 3
CTI BioPharma
Lymphoma, Low-Grade-Lymphoma, Small Lymphocytic-Lymphoma, Mixed-Cell, Follicular-Lymphoma, Small Cleaved-Cell, Follicular
December 2001
Phase 1
CTI BioPharma
Lymphoma, Follicular-Lymphoma, Mixed-Cell, Follicular-Lymphoma, Small Cleaved-Cell, Follicular-Lymphoma, Low-Grade
January 2005
Phase 3
CTI BioPharma
Lymphoma, Low-Grade-Lymphoma, Small Lymphocytic-Lymphoma, Mixed-Cell, Follicular-Lymphoma, Small Cleaved-Cell, Follicular
December 2001
Phase 1
Johannes Gutenberg University Mainz-Roche Pharma AG-CTI BioPharma
Lymphoma, Non-Hodgkin
August 2015
Phase 2
CTI BioPharma
Lymphoma-Solid Tumor (Excluding CNS)
October 2016
Phase 1
Anne Beaven, MD-CTI BioPharma-Duke University
Non-Hodgkin's Lymphoma
November 2011
Phase 1-Phase 2
CTI BioPharma
Lymphoma, Non-Hodgkin
July 2004
Phase 3
CTI BioPharma
Acute Myelogenous Leukemia
March 2005
Phase 1-Phase 2
Alliance for Clinical Trials in Oncology-National Cancer Institute (NCI)
Breast Cancer
May 2010
Phase 2
CTI BioPharma
Metastatic Cancer
May 2012
Phase 1
CTI BioPharma
Diffuse Large B-cell Lymphoma-de Novo DLBCL-DLBCL Transformed From Indolent Lymphoma-Follicular Grade 3 Lymphoma
April 2011
Phase 3
CTI BioPharma
Non-Hodgkin's Lymphoma
September 2007
Phase 3
CTI BioPharma-National Cancer Institute (NCI)
Leukemia-Lymphoma
August 2007
Phase 3
Theradex-National Cancer Institute (NCI)
Lymphoma
April 2003
Phase 2
Theradex-National Cancer Institute (NCI)
Lymphoma
February 2002
Phase 1
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