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Research and Development of Donepezil Hydrochloride, a New Type of Acetylcholinesterase Inhibitor
Hachiro Sugimoto, Hiroo Ogura, Yasuo Arai, Youichi Iimura, Yoshiharu Yamanishi. The Japanese Journal of Pharmacology, 2002-01-01
Topic: Drug trials: efficacy and safety
Plain-language summary
A wide range of evidence shows that cholinesterase (ChE) inhibitors can interfere with the progression of Alzheimer's disease (AD). The earliest known ChE inhibitors, namely, physostigmine and tacrine, showed modest improvement in the cognitive function of AD patients. However, clinical studies show that physostigmine has poor oral activity, brain penetration and pharmacokinetic parameters, while tacrine has hepatotoxic liability. Studies were then focused on finding a new type of acetylcholinesterase (AChE) inhibitor that would overcome the disadvantages of these two compounds. During the study, by chance we found a seed compound. We then conducted a structure-activity relationship study of this compound. After four years of exploratory research, we found donepezil hydrochloride (donepezil). Donepezil showed several positive characteristics including the following: 1) It has a novel structure compared to other conventional ChE inhibitors; 2) It shows strong anti-AChE activity and has long lasting efficacy; 3) The inhibitory characteristic of donepezil shows that it is highly selective for AChE as compared to butyrylcholinesterase (BuChE) and showed reversibility; 4) The results of clinical studies on donepezil show a very high significant difference on ADAS cog and CIBIC plus scores of AD patients. Donepezil is currently marketed in 56 countries all over the world.
Cite this study APA, Vancouver, BibTeX · download .bib or .ris
APA 7th
Sugimoto, H., Ogura, H., Arai, Y., Iimura, Y., & Yamanishi, Y. (2002). Research and Development of Donepezil Hydrochloride, a New Type of Acetylcholinesterase Inhibitor. The Japanese Journal of Pharmacology. https://doi.org/10.1254/jjp.89.7
Vancouver
Sugimoto H, Ogura H, Arai Y, Iimura Y, Yamanishi Y. Research and Development of Donepezil Hydrochloride, a New Type of Acetylcholinesterase Inhibitor. The Japanese Journal of Pharmacology. 2002. doi:10.1254/jjp.89.7. PMID: 12083745.
BibTeX
@article{sugimoto2002-12083745,
author = {Sugimoto, Hachiro and Ogura, Hiroo and Arai, Yasuo and Iimura, Youichi and Yamanishi, Yoshiharu},
title = {{Research and Development of Donepezil Hydrochloride, a New Type of Acetylcholinesterase Inhibitor}},
journal = {The Japanese Journal of Pharmacology},
year = {2002},
doi = {10.1254/jjp.89.7},
pmid = {12083745},
url = {https://doi.org/10.1254/jjp.89.7}
}
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Key findings
- During the study, by chance we found a seed compound.
- After four years of exploratory research, we found donepezil hydrochloride (donepezil).
- Donepezil showed several positive characteristics including the following: 1) It has a novel structure compared to other conventional ChE inhibitors; 2) It shows strong anti-AChE activity and has long lasting efficacy; 3) The inhibitory characteristic of donepezil shows that it is highly selective for AChE as compared to butyrylcholinesterase (BuChE) and showed reversibility; 4) The results of clinical studies on donepezil show a very high significant difference on ADAS cog and CIBIC plus scores of AD patients.
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Study details
- Evidence strengthLow
How this study scored 40/100
Published in a peer-reviewed journal. Scored zero for study design, sample size, effect reported, studied in people and randomized / blinded because the record does not state it. We have no data on journal's citation record, times cited, citations per year, impact for its field and year, cited by studies here, still being cited, senior author's track record, institution's track record and multicenter collaboration, so those were left out: it earned 23 of the 58 points we could judge it on, which is 40 out of 100.
| Component | Points | Why |
|---|---|---|
| Journal tier | 7 / 10 | Tier 3 — peer-reviewed journal (The Japanese Journal of Pharmacology) |
| Journal's citation record | — / 4 | No journal record from OpenAlex — left out of this score |
| Study design | 0 / 12 | No study design recorded — scores zero, not guessed (not stated in the record — scored 0) |
| Strength of evidence | 1 / 5 | Rated “low” in our summary |
| Peer-review validation | 10 / 10 | Peer-reviewed. Published as an article in a named peer-reviewed journal. |
| How recent | 1 / 5 | 2002 — older than 20 years, still counted |
| Sample size | 0 / 4 | Participant count not stated — scores zero (not stated in the record — scored 0) |
| Effect reported | 0 / 3 | No effect size reported — scores zero (not stated in the record — scored 0) |
| Studied in people | 0 / 3 | Not stated whether this was studied in people — scores zero (not stated in the record — scored 0) |
| Randomized / blinded | 0 / 2 | No randomization or blinding stated — scores zero (not stated in the record — scored 0) |
| Times cited | — / 7 | No citation count (not found in OpenAlex) — left out of this score |
| Citations per year | — / 5 | No citation count or no year — left out of this score |
| Impact for its field and year | — / 6 | No field-weighted citation impact (OpenAlex has none yet) — left out of this score |
| Cited by studies here | — / 6 | Not yet checked against this library's citation graph — left out of this score |
| Still being cited | — / 4 | No yearly citation counts — left out of this score |
| Senior author's track record | — / 4 | Senior author's record not available — left out of this score |
| Institution's track record | — / 3 | No institution listed in OpenAlex — left out of this score |
| Multicenter collaboration | — / 3 | Institutions not listed — left out of this score |
| Indexed in PubMed | 2 / 2 | Indexed in PubMed (PMID 12083745) |
| Free to read | 2 / 2 | Free to read |
| Points | 23 / 58 | Scored on 11 of 20 parts. We have no data for the rest, so they are left out: 23 of the 58 points we could judge it on is 40 out of 100. |
| Total | 40 / 100 | — |
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