Korean researchers develop next-generation anticancer compound that tracks and treats tumors simultaneously

Korean researchers have developed a new anticancer candidate compound that can simultaneously attack cancer cells and track in real time where the drug travels inside the body and how long it remains there. The compound has also shown effectiveness against cancer cells resistant to existing anticancer drugs, drawing attention as a potential next-generation precision cancer treatment.

The Korea Research Institute of Bioscience and Biotechnology announced Friday that a research team led by Dr. Seong Nak-gyun of its Chemical Biology Research Center had developed BF-04, a novel anticancer candidate compound capable of combining cancer treatment with medical imaging diagnostics.

Conventional anticancer treatments have faced two persistent limitations: when cancer cells develop drug resistance, therapeutic effectiveness declines, and it is difficult to confirm how much of an administered drug actually reaches tumor tissue. There has been a growing demand for technology that can selectively target cancer cells while also tracking the drug's movement through the body.

BF-04 works by disrupting the formation of microtubules, which are essential for cancer cell division. It binds to tubulin protein — the building block of microtubules — suppressing cell division and inducing cell death.

Particularly notable is that BF-04 demonstrated anticancer activity even in cancer cells resistant to existing microtubule-targeting anticancer drugs, suggesting it could overcome a key limitation of current treatments.

The research team also succeeded in visualizing the location of tumor tissue and the distribution of the drug by attaching a fluorescent material (Cy5) and the radioactive isotope zirconium-89 (89Zr), used for imaging diagnostics, to BF-04.

Experiments using cancer cells, patient-derived cancer organoids and animal models confirmed both the anticancer effect and tumor-targeting properties of the compound. In animal experiments particularly, the drug was found to selectively accumulate in tumor tissue without the need for separate antibodies or nanoparticle delivery vehicles.

Using molecular imaging equipment, researchers were able to track how the drug remained in tumor tissue for up to four days after administration. The findings suggest the potential to confirm whether an anticancer drug is being properly delivered to a tumor and to predict treatment response.

The research is significant in that a single small-molecule compound can perform both cancer treatment and diagnostic functions at the same time. The team expects the approach could develop into a personalized precision medicine technology capable of evaluating drug delivery and therapeutic effectiveness tailored to each patient's tumor characteristics.

However, the research is currently at the preclinical stage, and additional verification of safety and efficacy will be required before it can be applied to actual patient treatment.

The team plans to pursue follow-up research attaching therapeutic radioactive isotopes — including lutetium-177 (Lu-177), yttrium-90 (Y-90) and actinium-225 (Ac-225) — to BF-04. To do so, the team will need to optimize the linker structure that stably binds the radioactive isotopes while maintaining the drug's tumor-targeting properties.

"This research is meaningful in that it has established a new integrated cancer diagnosis and treatment platform that allows real-time observation of how a drug works inside the body, as well as anticancer effects against resistant cancer cells," Seong said. "It will be able to be used in various ways in the future development of precision cancer treatments."

The findings were published in the September online edition of the international academic journal Acta Pharmaceutica Sinica B.