A review of a new voltage-gated Ca2+ channel α2δ ligand, mirogabalin, for the treatment of peripheral neuropathic pain. (22nd November 2021)

• Record Type: Journal Article
• Authors: Kato, Jitsu; Inoue, Teruyoshi; Yokoyama, Mizuka; Kuroha, Masanori
• Is Part Of: Expert opinion on pharmacotherapy. Volume 22:Number 17(2021)
• Page Start: 2311
• Page End: 2322
• Publication Date: 2021-11-22
• Subjects: α2δ subunits -- analgesic effect -- mirogabalin -- neuropathic pain -- voltage-gated Ca2+ channel α2δ ligand; Chemotherapy -- Periodicals; 615.5805
• DOI: 10.1080/14656566.2021.1958780
• Languages: English
• ISSNs: 1465-6566

Abstract

ABSTRACT: Introduction: Neuropathic pain (NeP) is a chronic and refractory condition in many patients, and its treatment is a challenge for physicians. A new voltage-gated Ca 2+ channel α2 δ ligand, mirogabalin, has a high specific binding affinity for the α2 δ subunit, with a slower dissociation rate for α2 δ-1 than α2 δ-2 compared to that of pregabalin. Mirogabalin was shown to be effective in NeP animal models, with a margin of safety between central nervous system side effects and the analgesic effect of the dose. It exerted a favorable analgesic effect, was well tolerated in patients with peripheral NeP (P-NeP), and was first approved in Japan in 2019 and subsequently in Korea and Taiwan in 2020. Areas covered: The purpose of this article is to review the pharmacological characteristics, pharmacokinetics, and efficacy and safety of mirogabalin for NeP based on the results of non-clinical and clinical studies. Expert opinion: Although there are several first-line therapies for NeP, insufficient efficacy and adverse drug reactions of NeP drugs often cause patient dissatisfaction. Mirogabalin was effective and well tolerated with a step-wise dose increase in clinical studies on P-NeP patients. Thus, mirogabalin is expected to be a useful treatment option for patients with P-NeP.