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

References

• Japan Society of Pain Clinicians, eds. Guidelines for the pharmacologic management of neuropathic pain. 2nd. Tokyo, Japan: Shinko Trading Co., Ltd.; 2016. [cited 2020 Jul 22]. Japanese/English. Available from. http://minds4.jcqhc.or.jp/minds/Pharmacologic-management-of-neuropathic-pain/Pharmacologic-management-of-neuropathic-pain.pdf
   Google Scholar
• Colloca L, Ludman T, Bouhassira D, et al. Neuropathic pain. Nat Rev Dis Primers. 2017;3:17002.
   PubMed Web of Science ®Google Scholar
• Freynhagen R, Bennett MI. Diagnosis and management of neuropathic pain. BMJ. 2009;339:b3002.
   PubMed Web of Science ®Google Scholar
• Baron R. Neuropathic pain: a clinical perspective. Handb Exp Pharmacol. 2009;194:3–30.
   PubMedGoogle Scholar
• International Diabetes Federation, eds. IDF diabetes atlas. 9th. [cited 2020 Nov 27]. Available from: https://www.idf.org/e-library/epidemiology-research/diabetes-atlas/159-idf-diabetes-atlas-ninth-edition-2019.html
   Google Scholar
• Abbott CA, Malik RA, Van Ross ER, et al. Prevalence and characteristics of painful diabetic neuropathy in a large community-based diabetic population in the U.K. Diabetes Care. 2011;34:2220–2224.
   PubMed Web of Science ®Google Scholar
• Bouhassira D, Letanoux M, Hartemann A. Chronic pain with neuropathic characteristics in diabetic patients: a French cross-sectional study. PLoS One. 2013;8:e74195.
   PubMed Web of Science ®Google Scholar
• Alleman CJ, Westerhout KY, Hensen M, et al. Humanistic and economic burden of painful diabetic peripheral neuropathy in Europe: a review of the literature. Diabetes Res Clin Pract. 2015;109:215–225.
   PubMed Web of Science ®Google Scholar
• Sloan G, Shillo P, Selvarajah D, et al. A new look at painful diabetic neuropathy. Diabetes Res Clin Pract. 2018;144:177–191.
   PubMed Web of Science ®Google Scholar
• Schmader KE. Epidemiology and impact on quality of life of postherpetic neuralgia and painful diabetic neuropathy. Clin J Pain. 2002;18:350–354.
   PubMed Web of Science ®Google Scholar
• Ministry of Health, Labour and Welfare. Summary results of the national health and nutrition survey in Japan, 2017. [cited 2021 Jun 22]. Japanese. Available from: https://www.mhlw.go.jp/file/04-Houdouhappyou-10904750-Kenkoukyoku-Gantaisakukenkouzoushinka/kekkagaiyou_7.pdf
   Google Scholar
• Hanaoka K, Ogawa S, Hotta N, et al. Current status and future prospects for neuropathic pain treatment in Japan: a proposal from the expert consensus conference. Japanese. Pain Clinic. 2009;30:1395–1408.
   Google Scholar
• Pinchinat S, Cebrián-Cuenca AM, Bricout H, et al. Similar herpes zoster incidence across Europe: results from a systematic literature review. BMC Infect Dis. 2013;13:170.
   PubMed Web of Science ®Google Scholar
• Kawai K, Yawn BP, Wollan P, et al. Increasing Incidence of herpes zoster over a 60-year period from a population-based study. Clin Infect Dis. 2016;63:221–226.
   PubMed Web of Science ®Google Scholar
• Klompas M, Kulldorff M, Vilk Y, et al. Herpes zoster and postherpetic neuralgia surveillance using structured electronic data. Mayo Clin Proc. 2011;86:1146–1153.
   PubMed Web of Science ®Google Scholar
• Toyama N, Shiraki K. Epidemiology of herpes zoster in Miyazaki prefecture (Miyazaki study). Japanese. IASR. 2013;34:298–300.
   Google Scholar
• Inada E, eds. Herpes zoster up-to-date - from herpes zoster to PHN. Japanese. Tokyo, Japan: SHINDAN TO CHIRYO SHA, Inc.; 2012. p. 64–67.
   Google Scholar
• Inoue S, Kobayashi F, Nishihara M, et al. Chronic pain in the Japanese community–prevalence, characteristics and impact on quality of life. PLoS One. 2015;10:e0129262.
   PubMed Web of Science ®Google Scholar
• Schaefer C, Sadosky A, Mann R, et al. Pain severity and the economic burden of neuropathic pain in the United States: BEAT neuropathic pain observational study. Clinicoecon Outcomes Res. 2014;6:483–496.
   PubMedGoogle Scholar
• Sommer C, Cruccu G. Topical treatment of peripheral neuropathic pain: applying the evidence. J Pain Symptom Manage. 2017;53:614–629.
   PubMed Web of Science ®Google Scholar
• de Leon-Casasola O. New developments in the treatment algorithm for peripheral neuropathic pain. Pain Med. 2011;12(Suppl 3):S100–108.
   PubMedGoogle Scholar
• Ushida T, Matsui D, Inoue T, et al. Recent prescription status of oral analgesics in Japan in real-world clinical settings: retrospective study using a large-scale prescription database. Expert Opin Pharmacother. 2019;20:2041–2052.
   PubMed Web of Science ®Google Scholar
• Finnerup NB, Attal N, Haroutounian S, et al. Pharmacotherapy for neuropathic pain in adults: a systematic review and meta-analysis and updated NeuPSIG recommendations. Lancet Neurol. 2015;14:162–173.
   PubMed Web of Science ®Google Scholar
• Yang M, Qian C, Liu Y. Suboptimal treatment of diabetic peripheral neuropathic pain in the United States. Pain Med. 2015;16:2075–2083.
   PubMed Web of Science ®Google Scholar
• Obrosova IG. Diabetic painful and insensate neuropathy: pathogenesis and potential treatments. Neurotherapeutics. 2009;6:638–647.
   PubMed Web of Science ®Google Scholar
• Ushida T, Inoue T, Matsui D, et al. Cross-sectional study of patient satisfaction with oral analgesics in patients with chronic pain in Japan. Expert Opin Pharmacother. 2020;21:983–991.
   PubMed Web of Science ®Google Scholar
• Deeks ED Mirogabalin: first global approval. Drugs. 2019;79:463–468.
   PubMed Web of Science ®Google Scholar
• Daiichi Sankyo Co., Ltd. Tarlige® (mirogabalin) Tablets, 2.5 mg, 5mg, 10mg, 15 mg, package insert. Japanese. [ cited 2021 Jun 22]. Available from: https://www.info.pmda.go.jp/go/pdf/430574_1190026F1028_1_05
   Google Scholar
• Daiichi Sankyo Co., Ltd. Tarlige® (mirogabalin) Tablets 2.5 mg∙5 mg∙10 mg∙15 mg, Drug interview form. Japanese. [ cited 2021 Jun 22]. Available from: https://www.info.pmda.go.jp/go/interview/1/430574_1190026F1028_1_TL6_1F.pdf
   Google Scholar
• Taiwan Food and Drug Administration. Assessment Report. TARLIGE ® F.C. Tablets 15 mg. [ cited 2020 Dec 23]. Available from: https://www.fda.gov.tw/tc/includes/GetFile.ashx?id=f637368791343691781
   Google Scholar
• Jansen M, Warrington S, Dishy V, et al. A randomized, placebo-controlled, double-blind study of the safety, tolerability, pharmacokinetics, and pharmacodynamics of single and repeated doses of mirogabalin in healthy Asian volunteers. Clin Pharmacol Drug Dev. 2018;7:661–669.
   PubMed Web of Science ®Google Scholar
• Baba M, Kuroha M, Ohwada S, et al. Results of mirogabalin treatment for diabetic peripheral neuropathic pain in Asian subjects: a phase 2, double-blind, randomized, placebo-controlled, study. Pain Ther. 2020;9:261–278.
   PubMed Web of Science ®Google Scholar
• Vinik A, Rosenstock J, Sharma U, et al. Efficacy and safety of mirogabalin (DS-5565) for the treatment of diabetic peripheral neuropathic pain: a randomized, double-blind, placebo- and active comparator–controlled, adaptive proof-of-concept phase 2 study. Diabetes Care. 2014;37:3253–3261.
   PubMed Web of Science ®Google Scholar
• Kato J, Matsui N, Kakehi Y, et al. Mirogabalin for the management of postherpetic neuralgia: a randomized, double-blind, placebo-controlled phase 3 study in Asian patients. Pain. 2019;160:1175–1185.
   PubMed Web of Science ®Google Scholar
• Baba M, Matsui N, Kuroha M, et al. Mirogabalin for the treatment of diabetic peripheral neuropathic pain: a randomized, double-blind, placebo-controlled phase III study in Asian patients. J Diabetes Investig. 2019;10:1299–1306.
   PubMed Web of Science ®Google Scholar
• Amorim D. Pharmacological treatment of neuropathic pain: review of oral and topical therapy recommendations. Int J Clin Neurosci Ment Health. 2015;2:4.
   Google Scholar
• Vink S, Alewood PF. Targeting voltage-gated calcium channels: developments in peptide and small-molecule inhibitors for the treatment of neuropathic pain. Br J Pharmacol. 2012;167:970–989.
   PubMed Web of Science ®Google Scholar
• Cavalli E, Mammana S, Nicoletti F, et al. The neuropathic pain: an overview of the current treatment and future therapeutic approaches. Int J Immunopathol Pharmacol. 2019;33:1–10.
   Web of Science ®Google Scholar
• Japan Society of Pain Clinicians, eds. Guidelines for the pharmacologic management of neuropathic pain. 2nd. Supplementary edition. Tokyo, Japan: Shinko Trading Co., Ltd.; 2016. [cited 2020 July 22]. Japanese. Available from: https://www.jspc.gr.jp/Contents/public/kaiin_guideline09.html
   Google Scholar
• Domon Y, Arakawa N, Inoue T, et al. Binding characteristics and analgesic effects of mirogabalin, a novel ligand for the α2δ subunit of voltage-gated calcium channels. J Pharmacol Exp Ther. 2018;365:573–582.
   PubMed Web of Science ®Google Scholar
• Daiichi Sankyo Co., Ltd. An Asian, multicenter, randomized, double-blind, placebo-controlled, 14-week study of mirogabalin in participants with central neuropathic pain followed by a 52-week, open-label extension (NCT03901352). 2019. [cited 2020 Jul 22]. Available from: https://clinicaltrials.gov/ct2/show/NCT03901352
   Google Scholar
• Copeland RA, Pompliano DL, Meek TD. Drug-target residence time and its implications for lead optimization. Nat Rev Drug Discov. 2006;5:730–739.
   PubMed Web of Science ®Google Scholar
• Kitano Y, Wakimoto S, Tamura S, et al. Effects of mirogabalin, a novel ligand for the α2δ subunit of voltage-gated calcium channels, on N-type calcium channel currents of rat dorsal root ganglion culture neurons. Pharmazie.2019;74:147–149
   PubMed Web of Science ®Google Scholar
• Taylor CP. Mechanisms of analgesia by gabapentin and pregabalin – alpha2-delta [Cavalpha2-delta] ligands. Pain. 2009;142:13–16.
   PubMed Web of Science ®Google Scholar
• Burgess J, Javed S, Frank B, et al. Mirogabalin besylate in the treatment of neuropathic pain. Drugs Today. 2020;56:135–149.
   PubMed Web of Science ®Google Scholar
• Seltzer Z, Dubner R, Shir Y. A novel behavioral model of neuropathic pain disorders produced in rats by partial sciatic nerve injury. Pain. 1990;43:205–218.
   PubMed Web of Science ®Google Scholar
• Newton RA, Bingham S, Case PC, et al. Dorsal root ganglion neurons show increased expression of the calcium channel alpha2delta-1 subunit following partial sciatic nerve injury. Brain Res Mol Brain Res. 2001;95:1–8.
   PubMedGoogle Scholar
• Boroujerdi A, Zeng J, Sharp K, et al. Calcium channel alpha-2-delta-1 protein upregulation in dorsal spinal cord mediates spinal cord injury-induced neuropathic pain states. Pain. 2011;152:649–655.
   PubMed Web of Science ®Google Scholar
• Li CY, Song YH, Higuera ES, et al. Spinal dorsal horn calcium channel alpha2delta-1 subunit upregulation contributes to peripheral nerve injury-induced tactile allodynia. J Neurosci. 2004;24:8494–8499.
   PubMed Web of Science ®Google Scholar
• Domon Y, Arakawa N, Inoue T, et al. Analgesic effect of mirogabalin via the α2δ-1 subunit of voltage-gated calcium channels – evidence from α2δ-1 (R217A) and α2δ-2 (R282A) mutant mice. Japanese. Jpn Pharmacol Ther. 2019;47:585–591.
   Google Scholar
• Field MJ, Cox PJ, Stott E, et al. Identification of the α2δ-1 subunit of voltage-dependent calcium channels as a molecular target for pain mediating the analgesic actions of pregabalin. Proc Natl Acad Sci USA. 2006;103:17537–17544.
   PubMed Web of Science ®Google Scholar
• Oyama M, Watanabe S, Iwai T, et al. Mirogabalin activates the descending noradrenergic system by binding to the α2δ-1 subunit of voltage-gated Ca2+ channels to generate analgesic effects. J Pharmacol Sci. 2021;146:33–39.
   PubMed Web of Science ®Google Scholar
• Barclay J, Balaguero N, Mione M, et al. Ducky mouse phenotype of epilepsy and ataxia is associated with mutations in the Cacna2d2 gene and decreased calcium channel current in cerebellar Purkinje cells. J Neurosci. 2001;21:6095–6104.
   PubMed Web of Science ®Google Scholar
• Brill J, Klocke R, Paul D, et al. Entla, a novel epileptic and ataxic Cacna2d2 mutant of the mouse. J Biol Chem. 2004;279:7322–7330.
   PubMed Web of Science ®Google Scholar
• Donato R, Page KM, Koch D, et al. The ducky2J mutation in Cacna2d2 results in reduced spontaneous Purkinje cell activity and altered gene expression. J Neurosci. 2006;26:12576–12586.
   PubMed Web of Science ®Google Scholar
• Ivanov SV, Ward JM, Tessarollo L, et al. Cerebellar ataxia, seizures, premature death, and cardiac abnormalities in mice with targeted disruption of the Cacna2d2 gene. Am J Pathol. 2004;165:1007–1018.
   PubMed Web of Science ®Google Scholar
• Brown K, Mendell J, Ohwada S, et al. Tolerability, pharmacokinetics, and pharmacodynamics of mirogabalin in healthy subjects: results from phase 1 studies. Pharmacol Res Perspect. 2018;6(5):e00418.
   PubMed Web of Science ®Google Scholar
• Tachibana M, Yamamura N, Atiee GJ, et al. Coadministration of probenecid and cimetidine with mirogabalin in healthy subjects: a phase 1, randomized, open-label, drug–drug interaction study. Br J Clin Pharmacol. 2018;84:2317–2324.
   PubMed Web of Science ®Google Scholar
• Jansen M, Mendell J, Currie A, et al. Pharmacokinetics, pharmacodynamics, safety, and tolerability of mirogabalin when coadministered with lorazepam, zolpidem, tramadol, or ethanol: results from drug-drug interaction studies in healthy subjects. Clin Pharmacol Drug Dev. 2018;7:597–612.
   PubMed Web of Science ®Google Scholar
• Kitano Y, Kai K, Yamamura N, et al. Pharmacological, pharmacodynamics, and clinical profile of mirogabalin besylate (Tarlige® tablets 2.5 mg∙5 mg∙10 mg∙15 mg). Japanese. Nihon Yakurigaku Zasshi. 2019;154:352–361.
   PubMedGoogle Scholar
• Kato J, Matsui N, Kakehi Y, et al. Long-term safety and efficacy of mirogabalin in Asian patients with postherpetic neuralgia: results from an open-label extension of a multicenter randomized, double-blind, placebo-controlled trial. Medicine (Baltimore). 2020;99:e21976.
   PubMed Web of Science ®Google Scholar
• Pharmaceuticals and Medical Device Agency. Common technical document of mirogabalin (module 1). Japanese. [ cited 2020 Dec 23]. Available from: https://www.pmda.go.jp/drugs/2019/P20190122001/430574000_23100AMX00014_B100_1.pdf
   Google Scholar
• Baba M, Matsui N, Kuroha M, et al. Long‐term safety and efficacy of mirogabalin in Asian patients with diabetic peripheral neuropathic pain. J Diabetes Investig. 2020;11:693–698.
   PubMed Web of Science ®Google Scholar
• Baba M, Kuroha M, Wasaki Y, et al. Effects of mirogabalin on tingling or pins & needles in a phase 3 study of diabetic peripheral neuropathy. J Japan Soc Pain Clin. 2020;27:287–295.
   Google Scholar
• Pfizer Japan Inc. Lyrica® (pregabalin) OD Tablets 25 mg, 75 mg, 150 mg, package insert. Japanese. [ cited 2020 Oct 10]. Available from: https://www.pmda.go.jp/PmdaSearch/iyakuDetail/ResultDataSetPDF/672212_1190017F1029_2_02
   Google Scholar
• Kato M, Tajima N, Shimizu T, et al. Pharmacokinetics and safety of a single oral dose of mirogabalin in Japanese subjects with varying degrees of renal impairment. J Clin Pharmacol. 2018;58:57–63.
   PubMed Web of Science ®Google Scholar
• Baba M, Takatsuna H, Matsui N, et al. Mirogabalin in Japanese patients with renal impairment and pain associated with diabetic peripheral neuropathy or post-herpetic neuralgia: a phase III, open-Label, 14-week study. J Pain Res. 2020;13:1811–1821.
   PubMed Web of Science ®Google Scholar
• Fuji Pharma Co., Ltd. Gabapen® (gabapentin) Tablets 200 mg, 300 mg, 400 mg, package insert. Japanese. [ cited 2020 Aug 10]. Available from: https://www.info.pmda.go.jp/go/pdf/670109_1139007F1022_3_01
   Google Scholar
• Kimura Y, Yamaguchi S, Suzuki T, et al. Switching from pregabalin to mirogabalin in patients with peripheral neuropathic pain: a multi-center, prospective, single-arm, open-label study (MIROP Study). Pain Ther. 2021;10:711–727.
   PubMed Web of Science ®Google Scholar