Advantage and Core Benefit
- Safety of low dose small molecule DCA has been evaluated by clinical trial.
- administration of Nanoparticle can be localized in cancer tissue.
- Oral administration can maintain blood concentration for a long time.
Background and Technology
Dichloroacetic acid (DCA) is known to be a pyruvate dehydrogenase kinase inhibitor, which promotes mitochondrial electron transport chain and ROS generation, and result in cell death. DCA has been developed for cancer treatment and examined the effect of irradiation sensitizer. However, DCA is not easy to use in clinical settings because DCA is easily excreted from the body and has neurotoxicity at high concentration.
To overcome the drawback, the team of researchers has successfully synthesized prodrug, polyvinyl alcohol DCA ester and Polyethylene glycol block copolymer that forms micelles (NanoDCA), which accumulate in tumor tissues by extended permeation and release (EPR) effect, degrade and release DCA by endogenous enzyme (fig. L).
By oral administration, NanoDCA is trapped by the villi of the intestine and gradually release DCA and maintains the blood concentration for a long time, which could be useful for the mitochondrial disease treatment for example.
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Data
- 200mg/kg NanoDCA enhanced 5Gy x-ray radiation effect in tumor bearing mice (fig. R).
- DCA had some therapeutic effect, but not combination effects (data not shown).
- No weight loss observed.
Patent &Publications
Patent filed, not published.
Presented in the Japan Society of DDS.
Researchers
Dr. Yukio Nagasaki (University of Tsukuba)
Dr. Hironobu Yasui (Hokkaido University)
Expectations
We are seeking companies who can in-license and commercialize the technology.
Details can be disclosed under CDA.
Samples are available under material transfer agreement.
Project.KJ-05025