Tolrestat
Tolrestat is an aldose reductase inhibitor that blocks the conversion of glucose to sorbitol via the polyol pathway, which is implicated in diabetic peripheral neuropathy, nephropathy, and retinopathy through osmotic, oxidative, and metabolic mechanisms. It was investigated for the treatment of diabetic complications but was withdrawn from clinical development due to hepatotoxicity observed in clinical trials. Its mechanism of polyol pathway inhibition represented a rational approach to preventing glucose-mediated tissue damage in diabetes.
Molecular Weight
357.3000 g/mol
LogP
3.70
TPSA
81.90 Ų
Lipinski RO5
Pass
Pharmacokinetics (PK)
Pharmacodynamics (PD)
2D Structure
Cite this structure
Embed this structure
SMILES
COc1ccc2c(C(=S)N(C)CC(=O)O)cccc2c1C(F)(F)F
InChI
InChI=1S/C16H14F3NO3S/c1-20(8-13(21)22)15(24)11-5-3-4-10-9(11)6-7-12(23-2)14(10)16(17,18)19/h3-7H,8H2,1-2H3,(H,21,22)
Molecular Formula
C16H14F3NO3S
HBD / HBA
1 / 7
Rotatable Bonds
4
Heavy Atoms
24
No targets recorded
Target interaction data is not yet available for this drug.
No interactions recorded
Drug interaction data is not yet available for this compound.
No side effects recorded
Side effect data is not yet available for this drug.
Frequently Asked Questions
Tolrestat is an aldose reductase inhibitor that blocks the conversion of glucose to sorbitol via the polyol pathway, which is implicated in diabetic peripheral neuropathy, nephropathy, and retinopathy through osmotic, oxidative, and metabolic mechanisms. It was investigated for the treatment of diabetic complications but was withdrawn from clinical development due to hepatotoxicity observed in clinical trials. Its mechanism of polyol pathway inhibition represented a rational approach to preventing glucose-mediated tissue damage in diabetes.
Yes, Tolrestat is an approved drug. It has reached clinical phase 4. It is classified as a Small molecule.
References & Data Sources
- ChEMBL — European Bioinformatics Institute (EBI). CHEMBL436. Open-access bioactivity database.
- PubChem — National Center for Biotechnology Information (NCBI). CID 53359. Chemical information database.
Data aggregated from publicly available pharmacological databases. Last updated 2026-03-28.
Embed This Widget
Add the script tag and a data attribute to embed this widget.
<script src="https://cdn.jsdelivr.net/npm/drugfyi-embed@1/dist/embed.min.js" defer></script>
<div data-drugfyi="drug" data-slug="tolrestat"></div>Embed via iframe for maximum compatibility.
<iframe src="https://drugfyi.com/iframe/drug/tolrestat/" width="420" height="400" frameborder="0" style="border:0;border-radius:10px;max-width:100%" loading="lazy"></iframe>Paste this URL in WordPress, Medium, or any oEmbed-compatible platform.
https://drugfyi.com/drug/tolrestat/Add a dynamic SVG badge to your README or docs.
[](https://drugfyi.com/drug/tolrestat/)Use the native HTML custom element.
<script src="https://cdn.jsdelivr.net/npm/drugfyi-embed@1/dist/embed.min.js" defer></script>
<drugfyi-drug slug="tolrestat"></drugfyi-drug>