Synonyms: Alredase® | AY-27,773 | AY-27773
tolrestat is an approved drug
Compound class:
Synthetic organic
Comment: Tolrestat is an aldose reductase inhibitor [1] that failed Phase 3 clinical trial in the US and never made it to the clinic. The manufacturer withdrew the drug from other markets due to toxicity concerns.
Ligand Activity Visualisation ChartsThese are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts. ✖ |
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No information available. |
Summary of Clinical Use |
This drug was approved for the control of certain diabetic complications but was discontinued due to severe side effects. |
Mechanism Of Action and Pharmacodynamic Effects |
Tolrestat is an aldose reductase (AR) inhibitor. The AR AKR1B1 has been implicated in the development of diabetic complications as it catalyzes the reduction of glucose to sorbitol. AR inhibitors decrease the diabetes-associated accumulation of sorbitol in insulin insensitive tissues (such as lense cells, peripheral nerves and the renal glomerulus) which causes damage in these tissues and which leads to diabetic retinopathy, neuropathy and kidney damage [3]. |