��UӺ�Mwm���c�t�@r����N5��D'�����s����Es �X��;���9�����I4m�W�6D4�f�v��uً2���=? Nalfurafine has been found in vitro to bind to the μ-opioid receptor and to possess weak partial agonist activity at this site, albeit with much lower affinity relative to the KOR. [5][14] In animals, nalfurafine produces anti-scratch, antinociceptive, sedative, and diuretic effects.[5]. [4][12], Unlike other KOR agonists, nalfurafine does not produce hallucinogenic effects in humans. 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. 8 0 obj QA Engineer of web and mobile applications, Creative Commons Attribution-ShareAlike 4.0. A review by EMA’s safety committee (PRAC) has confirmed that 5-mg ulipristal acetate (Esmya and generic medicines) used for the treatment of symptoms of uterine fibroids can cause liver injury, including the need for liver transplantation. [15] The drug is a 4,5-epoxymorphinan derivative, and is structurally unique relative to other KOR agonists. An IV Difelikefalin version of CR845 is ready for commercialization for use in post-op settings and another oral Difelikefalin version has completed Phase 3 clinical studies for chronic pain and is progressing to commercialization. [5] As touched on above, nalfurafine shows atypical properties as a KOR agonist relative to other drugs. [6][7] It has also been dubiously referred to as the "first non-narcotic opioid drug" in history. %���� [5], CN([C@@H]1CC[C@]2([C@H]3CC4=C5[C@]2([C@H]1OC5=C(C=C4)O)CCN3CC6CC6)O)C(=O)/C=C/C7=COC=C7, InChI=1S/C28H32N2O5/c1-29(23(32)7-4-18-9-13-34-16-18)20-8-10-28(33)22-14-19-5-6-21(31)25-24(19)27(28,26(20)35-25)11-12-30(22)15-17-2-3-17/h4-7,9,13,16-17,20,22,26,31,33H,2-3,8,10-12,14-15H2,1H3/b7-4+/t20-,22-,26+,27+,28-/m1/s1, "Nalfurafine hydrochloride to treat pruritus: a review", Statement on a Nonproprietary Name adopted by the USAN Council, "TRK-820, a Selective .KAPPA.-Opioid Agonist, Produces Potent Antinociception in Cynomolgus Monkeys", "Discovery of a structurally novel opioid kappa-agonist derived from 4,5-epoxymorphinan", "Kappa Opioid Receptor-Induced Aversion Requires p38 MAPK Activation in VTA Dopamine Neurons", "Nalfurafine hydrochloride, a selective κ opioid receptor agonist, has no reinforcing effect on intravenous self-administration in rhesus monkeys", https://en.wikipedia.org/w/index.php?title=Nalfurafine&oldid=963984474, Creative Commons Attribution-ShareAlike License, This page was last edited on 22 June 2020, at 22:44.