nalfurafine

Nalfurafine is a small molecule, centrally acting, highly potent and selective full agonist of the kappa opioid receptor (KOR). It is approved in Japan for the treatment of pruritus (itch) in patients undergoing hemodialysis who are resistant to conventional treatments, as well as for pruritus associated with chronic liver disease. Nalfurafine acts by selectively activating KORs, which suppresses itch when antihistamines or antiallergic drugs are ineffective. Unlike other KOR agonists, nalfurafine displays atypical pharmacological properties and may act as a biased agonist favoring G protein signaling over β-arrestin pathways. Preclinical studies suggest it also has weak partial agonist activity at the mu opioid receptor but with much lower affinity than for KOR. Nalfurafine has shown potential benefits beyond antipruritic effects, including analgesia without central nervous system adverse effects and possible neuroprotective actions such as promoting remyelination and reducing neuroinflammation in animal models of multiple sclerosis[1][2][3][5][6][7][8].

Brand names

Remitch

Other names

nalfurafine hydrochloride