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Topotecan + pegylated doxorubicin

Development stage
Unknown
Lead developer
GSK
Modality
Small Molecules, Biodegradable Polymers → Polymer-based Nanoparticles → Nanoparticles → Drug Delivery Systems
Administration
Intravenous
01

Overview

Topotecan + pegylated doxorubicin is a combination chemotherapy regimen used primarily for the treatment of recurrent or advanced ovarian cancer, especially after failure of first-line platinum-based chemotherapy. Topotecan is a small molecule inhibitor of DNA topoisomerase I, an enzyme essential for DNA replication and transcription; it stabilizes the cleavable complex between DNA and topoisomerase I, leading to double-stranded DNA breaks and apoptosis in rapidly dividing cells. Pegylated liposomal doxorubicin (PLDH) is an anthracycline antibiotic encapsulated in a polyethylene glycol-coated liposome, which enhances its circulation time and reduces cardiotoxicity compared to conventional doxorubicin. Doxorubicin intercalates into DNA and inhibits topoisomerase II, preventing replication and leading to cell death. The combination exploits complementary mechanisms targeting different aspects of tumor cell proliferation[1][2][4][5][6][8].

Brand names
Caelyx
Other names
PLDHDoxorubicin liposomal
02

Targets

DNATOP1 (DNA Topoisomerase I)TOP2A (DNA topoisomerase II)

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