"目录号: HY-13777
Zoledronic acid(CGP 42446; ZOL 446)是PKC活化剂，能诱导多发性骨髓瘤细胞系凋亡和抑制hFOB细胞增殖。
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生物活性
Description
Zoledronic acid(CGP 42446; ZOL 446) is an activator of protein kinase C with apoptotic effects on multiple myeloma cell lines. It inhibited proliferation of human foetal osteoblastic cell line (hFOB) with an IC50 of 40 uM.Target: PKCZoledronic acid at doses of 2.0 and 4.0 mg and pamidronate at a dose of 90 mg each significantly reduced the need for radiation therapy to bone (P < 0.05) in contrast with 0.4 mg zoledronic acid, which did not. Skeletal-related events of any kind, pathologic fractures, and hypercalcemia also occurred less frequently in patients treated with 2.0 or 4.0 mg zoledronic acid or pamidronate than with 0.4 mg zoledronic acid [1]. Zoledronic acid administration may be a potentially valuable adjunct to distraction osteogenesis treatment, to enhance bone strength, thus reducing refracture complications [2]. Zoledronic acid, a more recent drug, was compared with pamidronic acid in two clinical trials, but the results are unconvincing because of the unusually poor performance of pamidronic acid. Safety of zoledronic acid is uncertain, owing to a lack of long-term data [3].Clinical indications: Bone metastases; Breast tumor; Complex regional pain syndrome; Hypercalcemia; Lower back pain; Male osteoporosis; Mesothelioma; Metastasis; Metastatic breast cancer; Multiple myeloma; Osteoarthritis; Osteogenesis imperfectaFDA Approved Date: 2007Toxicity: Overdosage may cause clinically significant hypocalcemia, hypophosphatemia, and hypomagnesemia.
Clinical Trial
Mario Negri Institute for Pharmacological Research-Associazione Italiana per la Ricerca sul Cancro
Breast Cancer
January 2015
Phase 2
Barbara Ann Karmanos Cancer Institute-United States Department of Defense
Prostate Cancer
September 2010
University of Wisconsin, Madison
Breast Cancer
January 2000
Phase 2
University of Wisconsin, Madison
Acute Myeloid Leukemia-Acute Lymphoblastic Leukemia-Hodgkin Lymphoma-Non-Hodgkin Lymphoma-Myelodysplastic Syndrome-Myeloproliferative Syndrome-Rhabdomyosarcoma-Ewing Sarcoma-Primitive Neuroectodermal Tumor-Osteosarcoma-Neuroblastoma
January 2016
Phase 1
First Affiliated Hospital, Sun Yat-Sen University
Breast Neoplasms-Bone Loss
July 2011
M.D. Anderson Cancer Center-Novartis Pharmaceuticals
Kidney Cancer-Renal Cell Carcinoma
October 2006
Phase 2
Hoffmann-La Roche-Roche Pharma AG
Multiple Myeloma
February 2006
Phase 3
Southwest Oncology Group-National Cancer Institute (NCI)
Breast Cancer-Hypercalcemia of Malignancy-Metastatic Cancer-Pain
May 2006
Phase 3
National Institute of Allergy and Infectious Diseases (NIAID)
HIV Infections-Osteopenia-Osteoporosis
May 2005
Phase 2
Axsome Therapeutics, Inc.
Complex Regional Pain Syndrome-Reflex Sympathetic Dystrophy
July 2015
Phase 3
Per Aspenberg-University Hospital, Linkoeping
Pre-integration Failure of Dental Implant
January 2014
Phase 2
Medical University of Vienna
Osteoporosis-Liver Transplantation
April 2002
HaEmek Medical Center, Israel
Chemotherapy-Breast Cancer, Metastatic
March 2010
Phase 2
Medical University Innsbruck
Bone Density-Pain-Fracture
February 2013
Ottawa Hospital Research Institute
Breast Cancer-Prostate Cancer-Metastasis
August 2016
Phase 4
Washington University School of Medicine
Adenocarcinoma
December 2009
Phase 1
German Breast Group-Austrian Breast & Colorectal Cancer Study Group-Novartis Pharmaceuticals
Breast Cancer
December 2004
Phase 3
Shriners Hospitals for Children-Novartis
Osteogenesis Imperfecta
October 2007
Phase 3
M.D. Anderson Cancer Center-Bristol-Myers Squibb
Breast Cancer-Bone Metastases
November 2007
Phase 1-Phase 2
University of Sao Paulo General Hospital-Novartis
Complex Regional Pain Syndromes
December 2013
Phase 2
James J. Peters Veterans Affairs Medical Center-Kessler Institute for Rehabilitation
Disuse Osteoporosis
May 2006
Phase 4
Novartis Pharmaceuticals-Novartis
Prostate Cancer
November 2003
Phase 4
Novartis Pharmaceuticals-Novartis
Osteoporosis
October 25, 2010
Phase 3
Leiden University Medical Center
Giant Cell Tumor of Bone-Osteoclastoma
December 2008
Phase 2
Carmen Gómez-Vaquero-Hospital Universitari de Bellvitge
Arthritis, Rheumatoid
May 2014
Phase 3
Novartis
Osteoporosis
May 2005
Phase 3
Novartis Pharmaceuticals-Novartis
Non-Small-Cell Lung Cancer
March 2005
Phase 3
Thomas Jefferson University-Department of Health and Human Services
Spinal Cord Injury
May 2012
Phase 3
The Cleveland Clinic-Novartis Pharmaceuticals
Osteoporosis
August 2006
Soroka University Medical Center-Tel-Aviv Sourasky Medical Center
Breast Cancer
September 2005
Phase 3
Peter Bushunow MD-Novartis Pharmaceuticals-Rochester General Hospital
Malignant Pleural Effusion-Non Small Cell Lung Cancer
November 2009
Phase 2
Hoosier Cancer Research Network-Novartis Pharmaceuticals-Walther Cancer Institute
Multiple Myeloma
June 2005
Phase 2
Tehran University of Medical Sciences-Novartis
Beta-Thalassemia-Bone Marrow Transplantation
November 2009
Phase 2-Phase 3
Daping Hospital and the Research Institute of Surgery of the Third Military Medical University
Non-small Cell Lung Cancer-Bone Metastasis
June 2016
Phase 4
Novartis Pharmaceuticals-Novartis
Multiple Myeloma-Breast Cancer
November 2006
Phase 1
Novartis Pharmaceuticals-Novartis
Breast Cancer With Bone Metastasis
February 2006
Phase 3
Massachusetts General Hospital-Dana-Farber Cancer Institute
Bone Loss-Prostate Cancer
September 2003
Phase 2
Novartis Pharmaceuticals-Novartis
Breast Cancer
February 2006
Phase 3
Novartis Pharmaceuticals-Novartis
Bone Neoplasms
December 2006
Phase 4
Thomas J. Schnitzer-Novartis-Northwestern University
Bone Loss
March 2010
Phase 2
Virginia Commonwealth University-Novartis
Sickle Cell Disease
June 2007
Phase 1-Phase 2
City of Hope Medical Center-National Cancer Institute (NCI)
Estrogen Receptor-positive Breast Cancer-Invasive Ductal Breast Carcinoma-Progesterone Receptor-positive Breast Cancer-Stage IA Breast Cancer-Stage IB Breast Cancer-Stage IIA Breast Cancer-Stage IIB Breast Cancer
September 14, 2012
Children's Hospital of Eastern Ontario
Osteoporosis-Osteonecrosis-Acute Lymphoblastic Leukemia
October 2016
Phase 2
Novartis Pharmaceuticals-Novartis
Breast Cancer
March 2004
Phase 3
Instituto Mexicano del Seguro Social
Multiple Myeloma
June 2002
University of Wisconsin, Madison-Novartis
Kidney Cancer
August 2003
Phase 2
Seoul National Universi
