Enhancer of Anticancer Drug Taxanes

Advantages

• Small molecules that are promising as anticancer enhancers
• Low cytotoxicity
• Possible to reduce the dosage by synergistically enhancing the effects of taxanes

Current Stage and Key Data

• Discovery and optimization research stage
• Fluorescence and electron microscopy observations revealed that the present invented compounds enhanced the microtubule polymerization-promoting effect of taxanes.
• These compounds do not exhibit cytotoxicity, but synergistically enhances the cancer cell proliferation inhibitory activity of paclitaxel in combination (IC₅₀ value reduced to 1/6).

Partnering Model

• Currently seeking partners for joint research and development of the enhancer compounds.
• Examples of potential partners: companies that manufacture, sell, and develop taxane-based anticancer drugs, and companies that develop anticancer drug delivery systems.

Background and Technology

Taxane compounds, including paclitaxel (Taxol^®), a well-known anticancer drug, bind to the inside of polymerized microtubules and stabilize them, thereby inhibiting depolymerization and suppressing mitosis and cell division.
While taxane compounds have a high therapeutic effect, they cause severe side effects such as peripheral neuropathy, bone marrow suppression, gastrointestinal symptoms (nausea, vomiting, diarrhea), and hair loss. They also cause neuropathy, such as numbness and pain in the hands and feet, significantly reducing the patient’s quality of life (QOL). They also suppress the production of normal blood cells, leading to a weakened immune system, anemia, and an increased risk of infection.
Clinical development of a combination drug (plinabulin) that reduces the side effects of taxanes is progressing, but to develop combination drugs that reduce the dosage of anticancer drug is important.

Principal Investigator

Prof. Masaki Kita (Graduate School of Bioagricultural Sciences, Nagoya University, Tokai National Higher Education and Research System)

Reference

• Paper submitted
• Patent pending (unpublished)

Project ID:BK-05172