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teniposide
- Development stage
- Phase 4
- Lead developer
- Bristol Myers Squibb
- Modality
- Classical Binding Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules, Nucleic Acid-Directed Small Molecules → Small Molecules
- Administration
- Intravenous
01
Overview
Teniposide is a semisynthetic derivative of podophyllotoxin and belongs to the class of topoisomerase II inhibitors. It is primarily used in combination with other chemotherapy agents for the treatment of refractory or relapsed acute lymphoblastic leukemia (ALL) in children. Teniposide acts as a phase-specific cytotoxic agent, targeting cells in the late S or early G2 phase of the cell cycle and preventing them from entering mitosis. Its mechanism involves inhibition of DNA topoisomerase II, leading to single and double-stranded DNA breaks and DNA-protein cross-links, ultimately resulting in cell death. Teniposide does not intercalate into or bind strongly to DNA but stabilizes the topoisomerase II-DNA complex, increasing cytotoxicity through accumulation of double-stranded breaks[1][3][4][5][7].
- Brand names
- Vumon
- Other names
- teniposide4-demethylepipodophyllotoxin 9-[4,6-O-(R)-2-thenylidene-beta-D-glucopyranoside]
02
Targets
TOP2A (DNA topoisomerase II)
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