The foundation of developing drugs for retinal diseases by pharmaceutical drug-repositioning screening based on the distribution manner via the blood-retinal barrier

2018 Fiscal Year Final Research Report

• Project/Area Number: 16H05110
• Research Category: Grant-in-Aid for Scientific Research (B)
• Allocation Type: Single-year Grants
• Section: 一般
• Research Field: Medical pharmacy
• Research Institution: University of Toyama
• Principal Investigator: Hosoya Ken-ichi 富山大学, 大学院医学薬学研究部(薬学), 教授 (70301033)
• Co-Investigator(Kenkyū-buntansha): 赤沼 伸乙 富山大学, 大学院医学薬学研究部(薬学), 助教 (30467089)
• Research Collaborator: MATSUYA Yuji ; ABE Hajime ; ANDO Tsugunobu ; KUBO Yoshiyuki
• Project Period (FY): 2016-04-01 – 2019-03-31
• Keywords: 血液網膜関門 / カチオン性薬物輸送 / 薬物輸送担体 / 内側血液網膜関門 / ドラッグリポジショニング

Outline of Final Research Achievements

The purpose of this study was to establish the foundation of retinal drug discovery based on the cationic drug transport systems at the blood-retinal barrier. To evaluate the transport of drugs as candidates for the use of retinal diseases, the labeling reaction of cyanocobalamin, a model compound, with a fluorescent substrate was tested. Since receptor-mediated transcytosis manner of fluorescent cyanocobalamin was observed, it is indicated that the optimization of this labeling reaction with a fluorescent substrate is completed. Through the pharmaceutical drug-repositioning screening, several kinds of candidates for the treatment of retinal diseases were discovered. We continue to perform the pharmacological and pharmaceutical studies to judge whether these drugs could be applied for the retinal diseases.

Free Research Field

医療系薬学、薬物動態学、網膜疾患創薬学

Academic Significance and Societal Importance of the Research Achievements

ヒット薬物について、本報告書提出時点にて追加での薬理学的・薬物動態学的な評価を継続している。本評価が完了することで、革新的な網膜疾患治療薬が世に出るものと期待される。また、その薬物について治療標的を発見するための実験系構築に向けた各種検討結果も成果として挙げており、今後の創薬に向けた基礎の一部を本課題は築いたと言える。