Ranirestat
From Wikipedia, the free encyclopedia
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| Preferred IUPAC name
(3R)-2′-[(4-Bromo-2-fluorophenyl)methyl]-1′H-spiro[pyrrolidine-3,4′-pyrrolo[1,2-a]pyrazine]-1′,2,3′,5(2′H)-tetrone | |
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| Properties | |
| C17H11BrFN3O4 | |
| Molar mass | 420.189 g/mol |
Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa).
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Ranirestat (also known as AS-3201) is an aldose reductase inhibitor being developed for the treatment of diabetic neuropathy by Dainippon Sumitomo Pharma and PharmaKyorin. It has been granted orphan drug status. The drug is to be used orally.
A Canadian Phase III clinical trial has been completed. Phase III trials in Europe and the US started in June 2009 and are expected to complete in April 2013.
Mechanism of action
Ranirestat is aldose reductase inhibitor that acts by reducing sorbitol accumulation in cells. Aldose reductase is an enzyme that catalyzes one of the steps in sorbitol (polyol) pathway which is responsible for formation of fructose from glucose. Aldose reductase activity is increased, parallel to glucose blood levels, in tissues that are not insulin sensitive, including lenses, peripheral nerves and renal glomeruli. Sorbitol does not diffuse through cell membranes easily and therefore accumulates in these tissues, causing osmotic damage, leading to retinopathy and neuropathy.
