"目錄號: HY-13624A
Epirubicin hydrochloride 是阿霉素的半合成的 L-阿拉伯糖衍生物茴恰，能夠抑制Topoisomerase，起到抗腫瘤的作用。
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Doxorubicin hydrochloride-Etoposide-INNO-206-Irinotecan hydrochloride-Campathecin-Daunorubicin Hydrochloride-Topotecan Hydrochloride-Exatecan Mesylate-SN-38-Idarubicin hydrochloride-Daun02-Tirapazamine-Amsacrine-TAS-103 dihydrochloride-PNU-159682-
生物活性
Description
Epirubicin (hydrochloride) is a semisynthetic L-arabino derivative of doxorubicin, and an antineoplastic agent by inhibitingTopoisomerase.
In Vitro
Epirubicin, like doxorubicin, exerts its antitumor effects by complex with DNA, resulting in damage to DNA and interference with the synthesis of DNA, RNA, and proteins. Epirubicin may also affect the integrity and activity of cellular membranes. Maximal cell kill caused by Epirubicin occurs during the S phase of the cell cycle. With higher concentrations effects are also seen in early G2 as well as G1 and M phases[1].?Epirubicin display antineoplastic activity against most cancer cells. Epirubicin is cytotoxic to Hepatoma G2 cells with IC50of 1.6 μg/mL at 24 hr. 1.6 μg/mL Epirubicin induces apoptosis of Hep G2 cells, and higher activity of catalase by 50%, Se-dependent glutathione peroxidase by 110%, Cu, Zn-superoxide dismutase by 172% and Mn-superoxide dismutase by 135%. Epirbicin increases the cellular expression of NADPH-CYP 450 reductase, and reduces GST-π expression[2].
In Vivo
Epirubicin are clinically active against a broad range of tumor types, including breast cancer, malignant lymphomas, soft tissue sarcomas, lung cancer, pleural mesothelioma, gastrointestinal cancer, head and neck cancer, ovarian cancer, prostatic carcinoma, transitional bladder carcinoma and so on[3].?Epirubicin at a dose of 3.5 mg/kg suppresses tumor mass of human breast tumor xenograft R-27 by 74.4 %[4].?
Clinical Trial
University of Medicine and Dentistry of New Jersey-National Cancer Institute (NCI)-Rutgers, The State University of New Jersey
Breast Cancer
June 2003
Phase 2
University of Bergen-Haukeland University Hospital
Stage III Breast Cancer AJCC V7
September 2007
Phase 2
National Cancer Institute (NCI)
Estrogen Receptor Negative-HER2/Neu Negative-Male Breast Carcinoma-Progesterone Receptor Negative-Recurrent Breast Carcinoma-Stage IV Breast Cancer-Triple-Negative Breast Carcinoma
August 21, 2012
Phase 1
Xijing Hospital
Breast Cancer
October 2011
Phase 3
Yonsei University
Stomach Neoplasms
September 2006
Phase 2
AHS Cancer Control Alberta
Breast Neoplasms
December 2012
Phase 2
Mansoura University
Carcinoma of Urinary Bladder, Superficial
July 2014
Phase 4
Pfizer
Adenocarcinoma
November 2000
Phase 3
SCRI Development Innovations, LLC-Aventis Pharmaceuticals-Pharmacia and Upjohn
Breast Cancer
September 2001
Phase 2
Danish Breast Cancer Cooperative Group-Fonden Til Fremme af Klinisk- Eksperimentel Cancerforskning-Sanofi-Dako
Breast Neoplasms
June 2008
Phase 3
German Breast Group-Pharmacia-Amgen-Bristol-Myers Squibb
Breast Cancer
August 2002
Phase 3
Indiana University School of Medicine-Indiana University
Germ Cell Tumor
October 2000
Phase 2
Hebei Medical University Fourth Hospital
Diffuse Large B-cell Lymphoma
November 2016
Cancer Trials Ireland
Breast Cancer
October 2007
Phase 1
Memorial Sloan Kettering Cancer Center-Amgen-Pfizer
Breast Cancer-Adenocarcinoma of the Breast
November 2004
Pfizer
Breast Neoplasm
January 1999
Department of Veterans Affairs, New Jersey-Pfizer
Prostate Cancer
July 2002
Phase 2
Alliance for Clinical Trials in Oncology-National Cancer Institute (NCI)
Malignant Mesothelioma
July 2001
Phase 2
Tianjin Medical University Cancer Institute and Hospital
Metastatic Breast Cancer
December 2013
Phase 4
National Taiwan University Hospital
Non-Small Cell Lung Cancer
October 1998
Phase 2
German Breast Group-AGO Study Group
Breast Cancer
January 2002
Phase 2
Hellenic Oncology Research Group
Breast Cancer
May 2008
Phase 1-Phase 2
Fudan University
Breast Cancer
April 2015
Phase 3
Cancer Trials Ireland
Gastro Oesophageal Cancer
May 2007
Phase 2
H. Lee Moffitt Cancer Center and Research Institute-National Cancer Institute (NCI)-Pfizer
Neoplasms, Advanced
March 2004
Phase 1
Craig A. Bunnell, MD, MPH-Dana-Farber Cancer Institute-Massachusetts General Hospital-Brigham and Women's Hospital-Beth Israel Deaconess Medical Center-Pharmacia
Breast Cancer-Stage I Breast Cancer-Stage II Breast Cancer-Stage IIIA Breast Cancer
April 2002
SCRI Development Innovations, LLC-Eli Lilly and Company-Celgene Corporation
Breast Cancer
September 2005
Phase 2
Hellenic Oncology Research Group-University Hospital of Crete
Breast Cancer
June 2003
Phase 2
SCRI Development Innovations, LLC-Pharmacia and Upjohn-Eli Lilly and Company-Aventis Pharmaceuticals
Breast Cancer
November 2001
Phase 2
Hospices Civils de Lyon
Metastatic Breast Cancer
June 2005
Phase 1
Thomas Hatschek-Karolinska University Hospital
Metastatic Breast Cancer
December 2002
Phase 3
Guangdong General Hospital
HER2-Positive Breast Cancer
September 1, 2016
Phase 2
Case Comprehensive Cancer Center-National Cancer Institute (NCI)
Breast Cancer
June 2002
Phase 2
Xijing Hospital
Breast Cancer
February 2008
Phase 2
Disphar International B.V.
Patients With Advanced or Metastatic Solid Tumors
January 2012
Phase 1
Chinese Academy of Medical Sciences
Triple Negative Breast Cancer
January 2008
Phase 2
R-Pharm
Metastatic Breast Cancer
August 2006
Phase 1
Klinikum Weissenfels
Primary Breast Cancer
May 2006
Phase 2
Chinese Academy of Medical Sciences
Breast Cancer
May 2011
Phase 3
GlaxoSmithKline
Neoplasms, Breast
July 2008
Phase 1
Massachusetts General Hospital
Esophageal Adenocarcinoma-Gastric Adenocarcinoma
April 2008
Phase 1-Phase 2
Cancer Trials Ireland
Melanoma (Skin)
August 2007
Phase 2
Jules Bordet Institute-Gustave Roussy, Cancer Campus, Grand Paris-Centre Paul Strauss-Centre Hospitalier du Luxembourg-Clinique Louis Cathy - Baudour - Belgium-HIS - Site Etterbeek - Ixelles - Belgium-Clinique Saint Pierre - Ottignies -Belgium-Clinique Ste Elisabeth - Namur - Belgium-University Hospital of Crete-Feculdade de Medicina da Universidade de Sao Paulo - Brasil
Breast Cancer
January 2003
Phase 2
Ruijin Hospital
Breast Neoplasms
October 2015
Phase 4
Northwestern University-National Cancer Institute (NCI)
Liver Cancer
October 2002
Phase 1-Phase 2
NCIC Clinical Trials Group-Canadian Cancer Trials Group
Breast Cancer
February 2003
Phase 1-Phase 2
