"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.