Drug intelligence / Profile preview

Ti-DFX-TPP

Development stage
Preclinical
Lead developer
Sun Yat-sen University
Modality
Light/Condition-Responsive Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules, DNA Intercalators/Alkylators → Nucleic Acid-Directed Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules
Administration
Unknown
01

Overview

Ti-DFX-TPP is a novel mitochondria-targeted titanium complex that incorporates a triphenylphosphine (TPP) moiety and a deferasirox (DFX) ligand, designed for anticancer therapy—particularly for triple-negative breast cancer (TNBC). Its mechanism involves disruption of iron homeostasis via transmetalation, depleting the labile iron pool inside cancer cells. This iron depletion upregulates transferrin receptor 1 (TfR1) as a compensatory mechanism, increases reactive oxygen species (ROS) production, induces mitochondrial dysfunction, and causes DNA damage leading to the inhibition of cancer cell proliferation. In vivo studies in mice have demonstrated antitumor efficacy without significant toxicity to major organs[1][2][3].

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