Nalfurafine
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Intravenous |
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| Biological half-life | 14 hours (acute); 25–28 hours (chronic) |
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| Synonyms | TRK-820, AC-820, MT-9938 |
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| Formula | C28H32N2O5 |
| Molar mass | 476.564 g/mol |
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Nalfurafine (INN, USAN) (brand name Remitch; former developmental code names TRK-820, AC-820, MT-9938) is an antipruritic (anti-itch drug) that is marketed in Japan for the treatment of uremic pruritus in individuals with chronic kidney disease undergoing hemodialysis. It acts as a potent, selective, centrally-penetrant κ-opioid receptor (KOR) agonist, and is the first and currently the only selective KOR agonist to have been approved for clinical use. It has also been referred to as the "first non-narcotic opioid drug" in history.
Nalfurafine was derived from structural modification of the opioid antagonist naltrexone. It was first synthesized and characterized in 1998, and was approved for clinical use in Japan as an intravenous drug under the brand name Remitch in 2009. The developer of nalfurafine also sought approval in Europe under the brand name Winfuran, but the Marketing Authorization Application was declined by the European Medicines Agency.[1] The drug was originally developed as an analgesic in surgery, but while effective in animal models of nociception, it was repurposed as an antipruritic at lower treatment doses due to an apparently unacceptable incidence of sedative effects in humans. As of 2015, nalfurafine is also in clinical trials for the treatment of cholestatic pruritus in Japan for patients with chronic liver disease, and for the treatment of uremic pruritus in the United States.[2]
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