Drug intelligence / Profile preview

[Ru(5-FU)(PPh3)2(bipy)]PF6

Development stage
Preclinical
Modality
DNA Intercalators/Alkylators → Nucleic Acid-Directed Small Molecules → Small Molecules, Light/Condition-Responsive Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules
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Overview

[Ru(5-FU)(PPh3)2(bipy)]PF6 is a novel ruthenium-based metal complex that incorporates the chemotherapeutic agent 5-fluorouracil (5-FU). This small molecule complex is designed to enhance the cytotoxicity of 5-FU and target cancer stemness, particularly in colorectal cancer (CRC). Its mechanism of action involves the inhibition of the Akt/mTOR signaling pathway, which leads to the suppression of AKT1 gene transcripts and the reduction of downstream proteins such as mTOR, S6, and 4EBP1. Preclinical studies have demonstrated that the complex induces apoptosis and cytoprotective autophagy, inhibits epithelial-mesenchymal transition (EMT), and reduces the formation of colonospheres. In vivo research using mouse xenograft models has shown its efficacy in inhibiting HCT116 cell development and experimental lung metastases.

Other names
ruthenium-based 5-fluorouracil complexruthenium-based5-fluorouracil complexruthenium-based-5-fluorouracil complexruthenium + 5-fluorouracil
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Targets

AKT1 (Proto-oncogene serine/threonine-protein kinase Akt1)mTOR (Mammalian target of rapamycin kinase)

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