"目录号: HY-13669
AutophagyCell Cycle/DNA Damage-
Lomustine (CCNU)是用于化疗的烷基化亚硝基脲。
AutophagyDNA Alkylator/Crosslinker
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生物活性
Description
Lomustine (CCNU) is an alkylating nitrosourea compound used in chemotherapy. IC50 Value:in vitro: vincristine and lomustine trigger apoptosis in all these cells through the mitochondrial pathway via decrease in the level of the anti-apoptosis proteins Bcl-2 and Bcl-xl, respectively [1]. There was significant correlation between the level of cadherin-associated protein beta 1 (CTNNB1) and Aurora kinase A (STK15) proteins and neurotrophic tyrosine kinase receptor type 3 (TRKC) mRNA and the proportion of apoptosis induced by vincristine, the combination of both drugs, and lomustine, respectively [4].in vivo: IC50 values for CCNU admixed and encapsulated with lipid vesicles were 18+/-4.9 and 14.0+/-2.2 microM, respectively, compared to 83+/-11.0 microM for free CCNU in rats [2]. Eight of the 19 dogs (42%) had a measurable response to CCNU. One dog had a durable complete response for 440 days. Seven dogs (37%) had a partial response for a median and mean duration of 77 days and 109 days, respectively (range, 21-254 days) [3]. Clinical trial:
Clinical Trial
Bart Neyns-Pfizer-Universitair Ziekenhuis Brussel
Glioblastoma Multiforme
April 2014
Phase 2
AstraZeneca
Recurrent Glioblastoma-Brain Tumor
September 2007
Phase 1
Incheon St.Mary's Hospital-National Cancer Center, Korea
Recurrent Glioblastoma Multiforme
October 2012
Phase 2
Darell D. Bigner, MD, PhD-Duke University
Malignant Glioma
June 1, 2017
Phase 2
Orbus Therapeutics, Inc.
Anaplastic Astrocytoma-Recurrent Anaplastic Astrocytoma
July 2016
Phase 3
Annick Desjardins-Tactical Therapeutics, Inc.-Duke University
Malignant Glioma (WHO Grade III or IV)
May 2014
Phase 1
University Hospital, Bordeaux
Acute Myeloid Leukemia
February 2008
Phase 3
French Innovative Leukemia Organisation
Acute Myeloid Leukemia
July 1995
Phase 3
M.D. Anderson Cancer Center-Celgene Corporation
Brain Neoplasms-Melanoma
February 2006
Phase 1
M.D. Anderson Cancer Center-Celgene Corporation
Brain Neoplasms-Melanoma
February 2006
Phase 2
Eli Lilly and Company
Glioblastoma
January 2006
Phase 3
M.D. Anderson Cancer Center
Brain Cancer-Glioblastoma
January 2010
Phase 2
University Hospital, Bonn
Glioblastoma
October 2010
Phase 3
Bristol-Myers Squibb-European Organisation for Research and Treatment of Cancer - EORTC
Glioblastoma
October 2009
Phase 1-Phase 2
Sidney Kimmel Comprehensive Cancer Center-National Cancer Institute (NCI)
Lung Cancer
July 2005
Phase 2
University Hospital, Bonn-Mundipharma Research GmbH & Co KG
Leptomeningeal Metastasis From Malignant Melanoma
March 2012
Phase 1
Novartis Pharmaceuticals-Novartis
Recurrent Glioblastoma Multiforme
February 28, 2014
Phase 1-Phase 2
AstraZeneca
Recurrent Glioblastoma
October 2008
Phase 3
Proximagen, LLC
Solid Tumors (Phase 1)-Relapsed/Recurrent GBM (Phase 2)
April 2016
Phase 1-Phase 2
Children's Oncology Group-National Cancer Institute (NCI)
Brain Tumors-Central Nervous System Tumors
July 2005
Phase 2
AbbVie-European Organisation for Research and Treatment of Cancer - EORTC
Glioblastoma Multiforme
February 11, 2015
Phase 2
VU University Medical Center
Glioblastoma Multiforme-Glioblastoma, Adult-Glioblastoma-Recurrent Brain Tumor-GBM
June 2017
Phase 2-Phase 3
European Organisation for Research and Treatment of Cancer - EORTC-Hoffmann-La Roche
Glioblastoma Multiforme-Cognition Disorders-Disability Evaluation
October 2011
Phase 3
Hoffmann-La Roche
Glioblastoma
August 2013
Phase 2
Eli Lilly and Company
Glioma
December 2005
Phase 1
Memorial Sloan Kettering Cancer Center-National Cancer Institute (NCI)
Intraocular Melanoma-Melanoma (Skin)
July 2003
Phase 2
Children's Oncology Group-National Cancer Institute (NCI)
Brain Tumor-Central Nervous System Tumor
November 2000
Phase 1
Eli Lilly and Company
Glioblastoma
April 2012
Phase 2
M.D. Anderson Cancer Center-Monteris Medical
Malignant Neoplasms of Eye Brain and Other Parts of Central Nervous System-Glioblastoma-Anaplastic Astrocytoma
August 2017
Phase 2
M.D. Anderson Cancer Center
Anaplastic Glioma of Brain-Glioblastoma Multiforme-Brain Cancer
September 2003
Phase 2
Pfizer
Glioblastoma
August 2003
Phase 3
Istituto Oncologico Veneto IRCCS-BAYER S.p.A. - Italia
Glioblastoma Multiforme
November 2015
Phase 2
OHSU Knight Cancer Institute-National Cancer Institute (NCI)
Lymphoma
January 2000
Phase 2
Institute of Cancer Research, United Kingdom-National Cancer Institute (NCI)
Brain and Central Nervous System Tumors
October 2002
Phase 3
Case Comprehensive Cancer Center-National Cancer Institute (NCI)
Lymphoma
June 1998
Phase 2
Tocagen Inc.
Glioblastoma Multiforme-Anaplastic Astrocytoma
November 2015
Phase 2-Phase 3
Alliance for Clinical Trials in Oncology-National Cancer Institute (NCI)
Brain and Central Nervous System Tumors
July 1996
Phase 2
Children's Cancer and Leukaemia Group-National Cancer Institute (NCI)
Brain and Central Nervous System Tumors
November 2001
Phase 2
Children's Cancer and Leukaemia Group-National Cancer Institute (NCI)
Brain and Central Nervous System Tumors
February 2004
Phase 2
Case Comprehensive Cancer Center-National Cancer Institute (NCI)
Lymphoma
July 1997
Phase 2
DelMar Pharmaceuticals, Inc.
Glioblastoma Multiforme-Glioblastoma-Glioma-GBM-Brain Cancer
June 2017
Phase 3
Children's Oncology Group-National Cancer Institute (NCI)-Pediatric Oncology Group
Brain Tumors-Central Nervous System Tumors
December 1996
Phase 3
Isarna Therapeutics GmbH
Anaplastic Astrocytoma-Glioblastoma
December 2008
Phase 3
European Organisation for Research and Treatment of Cancer - EORTC-Medical Research Council
Brain and Central Nervous System Tumors
August 1996
Phase 3
University Hospital Freiburg-Universitätsklinikum Köln-Ludwig-Maximilians - University of Munich-University Hospital Heidelberg-University Hospital Ulm
Primary Non Hodgkin Lymphoma of the Central Nervous System
September 2009
Phase 2
Children's Oncology Group-National Cancer Institute (NCI)
Untreated Childhood Medulloblastoma
October 2016
Phase 2
Hebei Yanda Hospital-Beijing Tiantan Hospital
Recurrent High-grade Glioma
February 2015
