mirogabalin-free-base

Description: Mirogabalin (DS-5565) is a potent, selective and orally bioavailable alpha2delta-1 ligand under development for treating pain associated with diabetic peripheral neuropathy, fibromyalgia, and postherpetic neuralgia. It has affinities for the alpha2delta subunit of voltage-gated calcium channels with Kds of 13.5 nM, 22.7 nM, 27 nM, and 47.6 nM for human alpha2delta-1, human alpha2delta-2, rat alpha2delta-1, and rat alpha2delta-2, respectively. Mirogabalin was estimated to be 17-fold more potent than pregabalin. Mirogabalin is being developed by Daiichi Sankyo and related to drugs such as gabapentin and pregabalin. Similarly to these drugs, mirogabalin binds to the alpha2delta calcium channels (1 and 2), but with significantly higher potency than pregabalin. It has shown promising results in Phase II clinical trials for the treatment of diabetic peripheral neuropathic pain.

References: Domon Y, et al. Binding Characteristics and Analgesic Effects of Mirogabalin, a Novel Ligand for the alpha2delta Subunit of Voltage-Gated Calcium Channels. J Pharmacol Exp Ther. 2018 Jun; 365(3):573-582.; Calandre EP, Rico-Villademoros F, Slim M. Alpha(2)delta ligands, gabapentin, pregabalin and mirogabalin: a review of their clinical pharmacology and therapeutic use. Expert Rev Neurother. 2016 Nov; 16(11):1263-1277.

Related CAS #: 1138245-21-2 (besylate) 1138245-13-2 (free base)