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VP-16

PETHEMA Foundation · FDA-approved active Small molecule

VP-16 (etoposide) is a topoisomerase II inhibitor that prevents DNA religation, leading to DNA strand breaks and cell death.

VP-16 (etoposide) is a topoisomerase II inhibitor that prevents DNA religation, leading to DNA strand breaks and cell death. Used for Small cell lung cancer, Testicular cancer, Lymphomas.

At a glance

Generic nameVP-16
Also known asetoposide, Etoposide, Etoposide (VP-16; Vepesid(R) brand only), NSC-67574, Vepesid
SponsorPETHEMA Foundation
Drug classTopoisomerase II inhibitor
TargetTopoisomerase II
ModalitySmall molecule
Therapeutic areaOncology
PhaseFDA-approved

Mechanism of action

VP-16 binds to the topoisomerase II–DNA complex and stabilizes the cleavage complex, preventing the religation of DNA strands. This results in accumulation of DNA double-strand breaks, particularly during S phase of the cell cycle, triggering apoptosis in rapidly dividing cells. It is used primarily in cancer chemotherapy due to its ability to kill malignant cells.

Approved indications

Common side effects

Key clinical trials

Primary sources

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SourceUsed for
ClinicalTrials.govTrial enrolment, design, endpoints, results

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