Literature DB >> 33572689

Mirogabalin-A Novel Selective Ligand for the α2δ Calcium Channel Subunit.

Renata Zajączkowska1, Joanna Mika2, Wojciech Leppert3, Magdalena Kocot-Kępska4, Małgorzata Malec-Milewska5, Jerzy Wordliczek1.   

Abstract

The efficacy of neuropathic pain control remains unsatisfactory. Despite the availability of a variety of therapies, a significant proportion of patients suffer from poorly controlled pain of this kind. Consequently, new drugs and treatments are still being sought to remedy the situation. One such new drug is mirogabalin, a selective ligand for the α2δ subunits of voltage-gated calcium channels (VGCC) developed by Sankyo group for the management of neuropathic pain. In 2019 in Japan, mirogabalin was approved for peripheral neuropathic pain following the encouraging results of clinical trials conducted with diabetic peripheral neuropathic pain (DPNP) and postherpetic neuralgia (PHN) patients. The ligand selectivity of mirogabalin for α2δ-1 and α2δ-2 and its slower dissociation rate for α2δ-1 than for α2δ-2 subunits of VGCC may contribute to its strong analgesic effects, wide safety margin, and relatively lower incidence of adverse effects compared to pregabalin and gabapentin. This article discusses the mechanism of action of mirogabalin, presents data on its pharmacodynamics and pharmacokinetics, and reviews the available experimental and clinical studies that have assessed the efficacy and safety of the drug in the treatment of selected neuropathic pain syndromes.

Entities:  

Keywords:  adverse effects; clinical indications; drug interactions; mechanism of action; mirogabalin besylate; neuropathic pain; pharmacodynamics; pharmacokinetics; α2δ voltage-gated calcium channel subunit ligand

Year:  2021        PMID: 33572689      PMCID: PMC7911728          DOI: 10.3390/ph14020112

Source DB:  PubMed          Journal:  Pharmaceuticals (Basel)        ISSN: 1424-8247


  45 in total

1.  Analgesic effects of the novel α₂δ ligand mirogabalin in a rat model of spinal cord injury.

Authors:  Y Domon; Y Kitano; M Makino
Journal:  Pharmazie       Date:  2018-11-01       Impact factor: 1.267

2.  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.

Authors:  Mendel Jansen; Steven Warrington; Victor Dishy; Shoichi Ohwada; Lisa Johnson; Karen Brown; Hitoshi Ishizuka
Journal:  Clin Pharmacol Drug Dev       Date:  2018-04-17

3.  Anxiolytic effects of the novel α2δ ligand mirogabalin in a rat model of chronic constriction injury, an experimental model of neuropathic pain.

Authors:  Hiroyasu Murasawa; Hiroyuki Kobayashi; Kensuke Saeki; Yutaka Kitano
Journal:  Psychopharmacology (Berl)       Date:  2019-09-12       Impact factor: 4.530

Review 4.  Presynaptic NMDA receptors control nociceptive transmission at the spinal cord level in neuropathic pain.

Authors:  Meichun Deng; Shao-Rui Chen; Hui-Lin Pan
Journal:  Cell Mol Life Sci       Date:  2019-02-20       Impact factor: 9.261

Review 5.  Neuropathic pain in the general population: a systematic review of epidemiological studies.

Authors:  O van Hecke; Sophie K Austin; Rafi A Khan; B H Smith; N Torrance
Journal:  Pain       Date:  2013-11-26       Impact factor: 6.961

6.  Adverse drug reactions to gabapentin and pregabalin: a review of the French pharmacovigilance database.

Authors:  Régis Fuzier; Isabelle Serres; Emmanuelle Guitton; Maryse Lapeyre-Mestre; Jean-Louis Montastruc
Journal:  Drug Saf       Date:  2013-01       Impact factor: 5.606

7.  The increased trafficking of the calcium channel subunit alpha2delta-1 to presynaptic terminals in neuropathic pain is inhibited by the alpha2delta ligand pregabalin.

Authors:  Claudia S Bauer; Manuela Nieto-Rostro; Wahida Rahman; Alexandra Tran-Van-Minh; Laurent Ferron; Leon Douglas; Ivan Kadurin; Yorain Sri Ranjan; Laura Fernandez-Alacid; Neil S Millar; Anthony H Dickenson; Rafael Lujan; Annette C Dolphin
Journal:  J Neurosci       Date:  2009-04-01       Impact factor: 6.167

8.  Short-term outcomes of mirogabalin in patients with peripheral neuropathic pain: a retrospective study.

Authors:  Tomoko Tetsunaga; Tomonori Tetsunaga; Keiichiro Nishida; Haruo Misawa; Tomoyuki Takigawa; Kentaro Yamane; Hironori Tsuji; Yoshitaka Takei; Toshifumi Ozaki
Journal:  J Orthop Surg Res       Date:  2020-05-26       Impact factor: 2.359

9.  Abuse potential of mirogabalin in recreational polydrug users.

Authors:  Jeanne Mendell; Naama Levy-Cooperman; Ed Sellers; Bradley Vince; Debra Kelsh; James Lee; Vance Warren; Hamim Zahir
Journal:  Ther Adv Drug Saf       Date:  2019-04-05

Review 10.  Neuropathic pain: an updated grading system for research and clinical practice.

Authors:  Nanna B Finnerup; Simon Haroutounian; Peter Kamerman; Ralf Baron; David L H Bennett; Didier Bouhassira; Giorgio Cruccu; Roy Freeman; Per Hansson; Turo Nurmikko; Srinivasa N Raja; Andrew S C Rice; Jordi Serra; Blair H Smith; Rolf-Detlef Treede; Troels S Jensen
Journal:  Pain       Date:  2016-08       Impact factor: 7.926

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  4 in total

Review 1.  Effects of Gabapentin and Pregabalin on Calcium Homeostasis: Implications for Physical Rehabilitation of Musculoskeletal Tissues.

Authors:  Perla C Reyes Fernandez; Christian S Wright; Stuart J Warden; Julia Hum; Mary C Farach-Carson; William R Thompson
Journal:  Curr Osteoporos Rep       Date:  2022-09-23       Impact factor: 5.163

2.  The Evidence for Effective Inhibition of INa Produced by Mirogabalin ((1R,5S,6S)-6-(aminomethyl)-3-ethyl-bicyclo [3.2.0] hept-3-ene-6-acetic acid), a Known Blocker of CaV Channels.

Authors:  Chao-Liang Wu; Chao-Wei Chuang; Hsin-Yen Cho; Tzu-Hsien Chuang; Sheng-Nan Wu
Journal:  Int J Mol Sci       Date:  2022-03-31       Impact factor: 5.923

Review 3.  Pharmacotherapy of Painful Diabetic Neuropathy: A Clinical Update.

Authors:  Cornelius Fernandez James; Shiva Tripathi; Kyriaki Karampatou; Divya V Gladston; Joseph M Pappachan
Journal:  Sisli Etfal Hastan Tip Bul       Date:  2022-03-28

4.  Mirogabalin Decreases Pain-like Behaviours and Improves Opioid and Ketamine Antinociception in a Mouse Model of Neuropathic Pain.

Authors:  Renata Zajączkowska; Ewelina Rojewska; Agata Ciechanowska; Katarzyna Pawlik; Katarzyna Ciapała; Magdalena Kocot-Kępska; Wioletta Makuch; Jerzy Wordliczek; Joanna Mika
Journal:  Pharmaceuticals (Basel)       Date:  2022-01-13
  4 in total

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