A review of a new voltage-gated Ca²⁺ channel α₂δ ligand, mirogabalin, for the treatment of peripheral neuropathic pain

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 Ca²⁺ channel α₂δ ligand, mirogabalin, has a high specific binding affinity for the α₂δ subunit, with a slower dissociation rate for α₂δ-1 than α₂δ-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.

KEYWORDS:

• α₂δ subunits
• analgesic effect
• mirogabalin
• neuropathic pain
• voltage-gated Ca²⁺ channel α₂δ ligand

Declaration of interest

T Inoue, M Yokoyama, and M Kuroha are all employees of Daiichi Sankyo Co., Ltd. J Kato reports having received personal fees from Daiichi Sankyo Co., Ltd., Pfizer Japan Inc., Eisai Co., Ltd., and Mochida Pharmaceutical Co., Ltd. The authors have no other relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript apart from those disclosed.

Reviewer disclosures

One reviewer declares a financial relationship with Daiichi Sankyo Co., Ltd., Japan. Peer reviewers on this manuscript have no other relevant financial relationships or otherwise to disclose.

Additional information

Funding

This manuscript was funded by Daiichi Sankyo Co., Ltd.