Department of Nuclear Medicine and Tracer Kinetics, Osaka University Graduate School of Medicine

Introduction

Research

  1. HOME
  2. Introduction
  3. Research
  4. 11C-donepezil

2) Diagnostic PET/SPECT【Mircodose PET】
11C-donepezil

In microdose PET, pharmacokinetics and receptor occupancy can be evaluated by administering a small amount of drug (less than 1/100 of drug efficacy and 100 μg or less) as a PET probe and acquiring images over time. 1)
Conducting microdose PET clinical trials in humans, especially in the early stages of new drug development, can dramatically improve development efficiency.
We performed Microdose PET Clinical research using donepezil hydrochloride (product name: Aricept), which is used as a therapeutic drug for Alzheimer's disease, labeled with C-11 and its pharmacokinetics was evaluated by PET. 2)
As a result, it was revealed that donepezil hydrochloride was distributed to non-target organs such as the myocardium and pancreas, and important findings in future drug development were obtained.

1) Raichle ME, et al. Proc Natl Acad Sci U S A. 2001.
2) Watabe T, et al. Front Neurosci. 2019.
3) Aoe J, et al. Ann Nucl Med. 2018.

11C-donepezil PET image （Group A: DNP oral administration group, Group B: DNP non-oral administration group)
11C-donepezil PET image
（Group A: DNP oral administration group, Group B: DNP non-oral administration group)