Mirogabalin: First Global Approval
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ADISINSIGHT REPORT
Mirogabalin: First Global Approval Emma D. Deeks1
© Springer Nature Switzerland AG 2019
Abstract Mirogabalin besylate (hereafter mirogabalin) [ Tarlige®] is an orally administered gabapentinoid developed by Daiichi Sankyo for the treatment of peripheral neuropathic pain (PNP), including diabetic PNP and post-herpetic neuralgia. The drug binds to and modulates the α2δ-1 subunit of the voltage-gated calcium channels widely found in the nervous system in areas that mediate pain transmission and processing. Mirogabalin has a unique binding profile and long duration of action. The drug is approved in Japan for the treatment of PNP and is in clinical development for this indication elsewhere in Asia. Clinical development of the drug for fibromyalgia pain was discontinued in the USA and EU after the primary endpoint was not met in phase 3 trials. No recent reports of development have been identified for PNP in the USA or India or for fibromyalgia pain in Australia, India, New Zealand, Russia, Argentina, Belarus, Chile, Colombia, Israel, Mexico, Switzerland, Canada, Serbia or South Africa. This article summarizes the milestones in the development of mirogabalin leading to this first approval for PNP.
1 Introduction Neuropathic pain can be debilitating, leading to sleep problems and a reduced quality of life [1]. It can have various underlying causes and, depending on the location of the causative damage, can be peripheral [e.g. diabetic neuropathy, post-herpetic neuralgia (PHN), cancer/chemotherapy, surgery] and/or central (e.g. stroke, traumatic brain injury) [1]. Gabapentinoids are key components of neuropathic pain management [2–4], providing analgesia largely by reducing dorsal horn sensitivity via mechanisms that include voltage-gated calcium channel (VGCC) blockade [5]. VGCCs are vital for the electrical activity of neurons and other excitable cells [5] and thus facilitate sensory information processing, although their activity/ expression can become dysregulated and/or maladapted in various pathological conditions, possibly contributing
This profile has been extracted and modified from the AdisInsight database. AdisInsight tracks drug development worldwide through the entire development process, from discovery, through preclinical and clinical studies to market launch and beyond. * Emma D. Deeks [email protected] 1
to pain development [6]. High-voltage activated VGCCs comprise a channel-forming α1 subunit and various modulatory auxiliary subunits, including α2δ [5, 6]. By binding to α2δ-1 (one of the four known α2δ isoforms), gabapentinoids inhibit calcium-mediated neurotransmitter release in the dorsal horn that would otherwise promote neuronal excitation and sensory signalling [5, 6]. However, various other mechanisms not directly related to dorsal horn neurotransmitter release may also contribute to the analgesic effects of these drugs [5]. The gabapentinoid drug class includes gabapentin, pregabalin and, most recently, mirogabalin besylate (hereafter referred to as mirogabalin). In Januar
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