Drug intelligence / Profile preview

topotecan liposome

Development stage
Phase 1
Lead developer
Fujifilm Pharmaceuticals
Modality
Small Molecules, Liposomes → Lipid-based Nanoparticles → Nanoparticles → Drug Delivery Systems
Administration
Intravenous
01

Overview

Topotecan liposome is a formulation of the chemotherapeutic agent topotecan encapsulated within a liposomal carrier. This delivery system is designed to enhance the pharmacokinetic profile and tumor targeting of topotecan by increasing its plasma half-life and reducing systemic toxicity compared to free drug administration[1][5]. Topotecan acts as an inhibitor of DNA topoisomerase I, stabilizing the enzyme-DNA complex and preventing religation of single-strand breaks during DNA replication. This leads to replication arrest and cell death in rapidly dividing cancer cells[6]. Liposomal encapsulation improves drug retention and allows for more efficient delivery into tumor cells via endocytosis or receptor-mediated uptake[2][3]. The formulation has been investigated for use in various cancers including neuroblastoma, ovarian cancer, small-cell lung cancer, cervical cancer, and lung tumors[1][2][5].

Brand names
BrakivaOptisomal topotecan
Other names
liposomal topotecanSphingosome-encapsulated topotecanliposomal topotecan hydrochloride
02

Targets

TOP1 (DNA Topoisomerase I)

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