"目录号: HY-13761
Cell Cycle/DNA Damage-
Teniposide(VM-26)是半合成的鬼臼毒素衍生物,能通过与拓扑异构酶II的相互作用促使DNA断裂。
Topoisomerase
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生物活性
Description
Teniposide(VM-26) is a semisynthetic derivative of podophyllotoxin and are increasingly used in cancer medicine; causing breaks in DNA via an interaction with DNA topoisomerase II.IC50 value:Target: Topo IITeniposide is a phase-specific cytotoxic drug acting in the late S and early G2 phases of the cell cycle. It appears to act by causing breaks in DNA via an interaction with DNA topoisomerase II or by the formation of free radicals. The number of DNA-topoisomerase-II covalent complexes stabilized by VM-26 in WEHI-3B D+ cells was greatly increased when cells were exposed simultaneously to VM-26 and novobiocin for 1 hr, but not when cells were treated with m-AMSA and novobiocin for the same period of time.
Clinical Trial
NCT00004916
Northwestern University-National Cancer Institute (NCI)
Lymphoma
February 1999
Phase 1-Phase 2
NCT00186875
St. Jude Children's Research Hospital
Acute Lymphoblastic Leukemia-Lymphoma, Lymphoblastic
November 2003
Phase 2
NCT01700946
St. Jude Children's Research Hospital-Cookies for Kids' Cancer-Assisi Foundation
Recurrent B-Cell Childhood Acute Lymphoblastic Leukemia-Recurrent Childhood B-Lymphoblastic Lymphoma
April 15, 2013
Phase 2
NCT00853008
PETHEMA Foundation
Acute Lymphoblastic Leukemia
January 2003
Phase 4
NCT00187083
St. Jude Children's Research Hospital
Acute Lymphoblastic Leukemia
February 1997
Phase 3
NCT00343369
Universitätsklinikum Hamburg-Eppendorf-National Cancer Institute (NCI)
Leukemia
January 2003
NCT00004231
Northwestern University-National Cancer Institute (NCI)
Lymphoma
October 1999
Phase 2
NCT00002531
Johann Wolfgang Goethe University Hospital-National Cancer Institute (NCI)
Leukemia
January 1993
Phase 2
NCT00184041
University of Southern California
Acute Lymphoblastic Leukemia
July 2004
Phase 2
NCT00199095
Johann Wolfgang Goethe University Hospital
Adult Acute Lymphocytic Leukemia
February 1997
Phase 4
NCT00199069
Johann Wolfgang Goethe University Hospital-Deutsche Krebshilfe e.V., Bonn (Germany)
Adult Acute Lymphocytic Leukemia
April 1993
Phase 4
NCT00199056
Johann Wolfgang Goethe University Hospital
Adult Acute Lymphocytic Leukemia
October 1999
Phase 4
NCT00199004
Johann Wolfgang Goethe University Hospital
Adult Acute Lymphocytic Leukemia
April 2004
Phase 4
NCT00198991
Johann Wolfgang Goethe University Hospital-Deutsche Krebshilfe e.V., Bonn (Germany)-German Federal Ministry of Education and Research
Adult Acute Lymphocytic Leukemia
April 2003
Phase 4
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References
[1].Clark PI, Slevin ML. The clinical pharmacology of etoposide and teniposide. Clin Pharmacokinet. 1987 Apr;12(4):223-52.
[2].Rappa G, Lorico A, Sartorelli AC. Potentiation by novobiocin of the cytotoxic activity of etoposide (VP-16) and teniposide (VM-26). Int J Cancer. 1992 Jul 9;51(5):780-7.
[3].Lee T, Roberts D. Flux of teniposide (VM-26) across the plasma membrane of teniposide-resistant sublines of L1210 cells.Cancer Res. 1984 Jul;44(7):2986-90.
[4].Postmus PE, Smit EF, Berendsen HH, Treatment of brain metastases of small cell lung cancer with teniposide. Semin Oncol. 1992 Apr;19(2 Suppl 6):89-94.