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tasisulam + liposomal doxorubicin

Development stage
Discontinued
Lead developer
Eli Lilly
Modality
Small Molecules, Liposomes → Lipid-based Nanoparticles → Nanoparticles → Drug Delivery Systems
Administration
Intravenous
01

Overview

Tasisulam + liposomal doxorubicin is an investigational combination of **tasisulam**, a highly albumin-bound small molecule with pro-apoptotic and antiangiogenic effects, and **liposomal doxorubicin** (Doxil), an anthracycline chemotherapy agent in a pegylated liposomal formulation designed for improved tumor targeting and reduced systemic toxicity. Tasisulam induces tumor cell apoptosis and inhibits angiogenesis. Liposomal doxorubicin acts by intercalating into DNA and inhibiting topoisomerase II, leading to impaired DNA synthesis and increased cell death. The liposomal encapsulation of doxorubicin allows for prolonged circulation and better tumor uptake due to the enhanced permeability and retention effect, and significantly reduces risk of dose-limiting cardiotoxicity compared to free doxorubicin. This combination has been evaluated in phase 1b studies, notably for platinum-resistant, doxorubicin-naïve ovarian cancer; however, development was discontinued early for business reasons, with partial data suggesting feasibility and preliminary antitumor activity[3][2][4][6][8].

Other names
pegylated liposomal doxorubicin
02

Targets

TOP2A (DNA topoisomerase II)DNA

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