Development of a tri-functional chelate for nuclear/fluorescence dual imaging

Research Project

Project/Area Number	18K19527
Research Category	Grant-in-Aid for Challenging Research (Exploratory)
Allocation Type	Multi-year Fund
Review Section	Medium-sized Section 52:General internal medicine and related fields
Research Institution	Kobe Pharmaceutical University
Principal Investigator	Mukai Takahiro 神戸薬科大学, 薬学部, 教授 (30284706)
Project Period (FY)	2018-06-29 – 2020-03-31
Project Status	Completed (Fiscal Year 2019)
Budget Amount *help	¥6,240,000 (Direct Cost: ¥4,800,000、Indirect Cost: ¥1,440,000) Fiscal Year 2019: ¥3,120,000 (Direct Cost: ¥2,400,000、Indirect Cost: ¥720,000) Fiscal Year 2018: ¥3,120,000 (Direct Cost: ¥2,400,000、Indirect Cost: ¥720,000)
Keywords	放射性医薬品 / イメージング / ガリウム / 蛍光 / 薬学
Outline of Final Research Achievements	The imaging probes applicable to both nuclear medical imaging and fluorescence imaging could provide identical information for both pre- and intra-operative diagnoses of cancers, leading to precise surgical therapy. In this study, since two free carboxylate groups of the radiogallium-DOTA complex could be used for coupling to functional moieties that recognize cancer-specific molecular targets, we introduced a fluorescence dye to a carboxylate group on DOTA, and furthermore, a folate derivative to an another carboxylate group. The new compound could detect ovarian cancers highly expressing folate receptors in vivo.
Academic Significance and Societal Importance of the Research Achievements	核医学診断と蛍光イメージングを同時に達成しうる薬剤骨格を開発できれば、がんの診断から治療への効率的ワークフローを構築でき、高効率な確定診断と、それに基づく効果的な治療法の迅速な選択・決定が可能になると考えられる。それにより、がんの早期における治療戦略決定が可能となり、最適な治療法選択と実施推進により治療効果の向上、必要な治療法の絞込みによる医療経済効果への寄与が期待できる。