Mirogabalin: could it be the next generation gabapentin or pregabalin?
0
조회
0
다운로드
1
인용
0
참고문헌
키워드
초록
Except for carbamazepine for trigeminal neuralgia, gabapentinoid anticonvulsants have been the standard for the treatment of neuropathic pain. Pregabalin, which followed gabapentin, was developed with the benefit of rapid peak blood concentration and better bioavailability. Mirogabalin besylate (DS-5565, Tarlige®) shows greater sustained analgesia due to a high affinity to, and slow dissociation from, the α2δ-1 subunits in the dorsal root ganglion (DRG). Additionally, it produces a lower level of central nervous system-specific adverse drug reactions (ADRs), due to a low affinity to, and rapid dissociation from, the α2δ-2 subunits in the cerebellum. Maximum plasma concentration is achieved in less than 1 hour, compared to 1 hour for pregabalin and 3 hours for gabapentin. The plasma protein binding is relatively low, at less than 25%. As with all gabapentinoids, it is also largely excreted via the kidneys in an unchanged form, and so the administration dose should also be adjusted according to renal function. The equianalgesic daily dose for 30 mg of mirogabalin is 600 mg of pregabalin and over 1,200 mg of gabapentin. The initial adult dose starts at 5 mg, given orally twice a day, and is gradually increased by 5 mg at an interval of at least a week, to 15 mg. In conclusion, mirogabalin is anticipated to be a novel, safe gabapentinoid anticonvulsant with a greater therapeutic effect for neuropathic pain in the DRG and lower ADRs in the cerebellum.
Abstract
Except for carbamazepine for trigeminal neuralgia, gabapentinoid anticonvulsants have been the standard for the treatment of neuropathic pain. Pregabalin, which followed gabapentin, was developed with the benefit of rapid peak blood concentration and better bioavailability. Mirogabalin besylate (DS-5565, Tarlige®) shows greater sustained analgesia due to a high affinity to, and slow dissociation from, the α2δ-1 subunits in the dorsal root ganglion (DRG). Additionally, it produces a lower level of central nervous system-specific adverse drug reactions (ADRs), due to a low affinity to, and rapid dissociation from, the α2δ-2 subunits in the cerebellum. Maximum plasma concentration is achieved in less than 1 hour, compared to 1 hour for pregabalin and 3 hours for gabapentin. The plasma protein binding is relatively low, at less than 25%. As with all gabapentinoids, it is also largely excreted via the kidneys in an unchanged form, and so the administration dose should also be adjusted according to renal function. The equianalgesic daily dose for 30 mg of mirogabalin is 600 mg of pregabalin and over 1,200 mg of gabapentin. The initial adult dose starts at 5 mg, given orally twice a day, and is gradually increased by 5 mg at an interval of at least a week, to 15 mg. In conclusion, mirogabalin is anticipated to be a novel, safe gabapentinoid anticonvulsant with a greater therapeutic effect for neuropathic pain in the DRG and lower ADRs in the cerebellum.
참고문헌 (57)
- Dolphin AC, "The α2δ subunits of voltage-gated calcium channels", Biochim Biophys Acta, 1828, pp.1541~1549 (2013)
- Deeks ED, "Mirogabalin : first global approval", Drugs, 79, pp.463~468 (2019)
- Deeks ED, "Correction to : mirogabalin : first global approval", Drugs, 79, pp.469~ (2019)
- 김경훈, "All about pain pharmacology: what pain physicians should know", The Korean Journal of Pain, 33(2), pp.108~120 (2020), 대한통증학회[DOI]
- Hauser AS, "Trends in GPCR drug discovery: new agents, targets and indications", Nat Rev Drug Discov, 16, pp.829~842 (2017)
- Domon Y, "Binding characteristics and analgesic effects of mirogabalin, a novel ligand for the α2δ subunit of voltage-gated calcium channels", J Pharmacol Exp Ther, 365, pp.573~582 (2018)
- Dolphin AC, "Voltage-gated calcium channel α2δ subunits: an assessment of proposed novel roles", F1000Res, 7, pp.1830~ (2018)
- Dolphin AC, "Calcium channel auxiliary α2δ and β subunits : trafficking and one step beyond", Nat Rev Neurosci, 13, pp.542~555 (2012)
- Burnashev N, "Calcium permeability of ligand-gated channels", Cell Calcium, 24, pp.325~332 (1998)
- Catterall WA, "Voltage-gated calcium channels", Cold Spring Harb Perspect Biol, 3, pp.a003947~ (2011)
- D’Arco M, "The upregulation of α2δ-1 subunit modulates activity-dependent Ca2+signals in sensory neurons", J Neurosci, 35, pp.5891~5903 (2015)
- Hoppa MB, "α2δ expression sets presynaptic calcium channel abundance and release probability", Nature, 486, pp.122~125 (2012)
- Davies A, "Functional biology of the alpha(2)delta subunits of voltage-gated calcium channels", Trends Pharmacol Sci, 28, pp.220~228 (2007)
- Chincholkar M, "Analgesic mechanisms of gabapentinoids and effects in experimental pain models : a narrative review", Br J Anaesth, 120, pp.1315~1334 (2018)
- Patel R, "Mechanisms of the gabapentinoids and α 2 δ-1 calcium channel subunit in neuropathic pain", Pharmacol Res Perspect, 4, pp.e00205~ (2016)
- El-Awaad E, "Direct, gabapentin-insensitive interaction of a soluble form of the calcium channel subunit α2δ-1 with thrombospondin-4", Sci Rep, 9, pp.16272~ (2019)
- Brini M, "Neuronal calcium signaling : function and dysfunction", Cell Mol Life Sci, 71, pp.2787~2814 (2014)
- Alcántara Montero A, "Emerging therapies in clinical development and new contributions for neuropathic pain", Rev Esp Anestesiol Reanim, 66, pp.324~334 (2019)
- Javed S, "Mirogabalin and emerging therapies for diabetic neuropathy", J Pain Res, 11, pp.1559~1566 (2018)
- Reem Abdullah Alyoubi, "Efficacy and safety of mirogabalin treatment in patients with diabetic peripheral neuropathic pain: A systematic review and meta‐analysis of randomised controlled trials", International Journal of Clinical Practice, 75(5) (2021), Wiley[DOI]
- Calandre EP, "Alpha2delta ligands, gabapentin, pregabalin and mirogabalin: a review of their clinical pharmacology and therapeutic use", Expert Rev Neurother, 16, pp.1263~1277 (2016)
- Merante D, "The mirogabalin ALDAY phase 3 program in pain associated with fibromyalgia : the lessons learned", Curr Med Res Opin, 36, pp.661~666 (2020)
- Burgess J, "Mirogabalin besylate in the treatment of neuropathic pain", Drugs Today(Barc), 56, pp.135~149 (2020)
- Jansen M, "A randomized, placebo-controlled, doubleblind study of the safety, tolerability, pharmacokinetics, and pharmacodynamics of single and repeated doses of mirogabalin in healthy Asian volunteers", Clin Pharmacol Drug Dev, 7, pp.661~669 (2018)
- Tetsunaga T, "Short-term outcomes of mirogabalin in patients with peripheral neuropathic pain : a retrospective study", J Orthop Surg Res, 15, pp.191~ (2020)
- Kato J, "Longterm safety and efficacy of mirogabalin in Asian patients with postherpetic neuralgia: results from an open-label extension of a multicenter randomized, double-blind, placebocontrolled trial", Medicine (Baltimore), 99, pp.e21976~ (2020)
- Kato J, "Mirogabalin for the management of postherpetic neuralgia : a randomized, double-blind, placebo-controlled phase 3 study in Asian patients", Pain, 160, pp.1175~1185 (2019)
- Ye X, "Cost-effectiveness of mirogabalin for the treatment of post-herpetic neuralgia in Taiwan", J Med Econ, 23, pp.529~536 (2020)
- Baba M, "Mirogabalin for the treatment of diabetic peripheral neuropathic pain : a randomized, double-blind, placebo-controlled phase III study in Asian patients", J Diabetes Investig, 10, pp.1299~1306 (2019)
- Vinik A, "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 proofof-concept phase 2 study", Diabetes Care, 37, pp.3253~3261 (2014)
- Merante D, "DS-5565-A-U201US Phase 2 Study Investigators. Efficacy of mirogabalin (DS-5565) on patient-reported pain and sleep interference in patients with diabetic neuropathic pain: secondary outcomes of a phase II proof-of-concept study", Pain Med, 18, pp.2198~2207 (2017)
- Baba M, "Results of mirogabalin treatment for diabetic peripheral neuropathic pain in Asian subjects : a phase 2, double-blind, randomized, placebo-controlled, study", Pain Ther, 9, pp.261~278 (2020)
- Baba M, "Longterm safety and efficacy of mirogabalin in Asian patients with diabetic peripheral neuropathic pain", J Diabetes Investig, 11, pp.693~698 (2020)
- Hutmacher MM, "Exposure-response modeling of average daily pain score, and dizziness and somnolence, for mirogabalin(DS-5565)in patients with diabetic peripheral neuropathic pain", J Clin Pharmacol, 56, pp.67~77 (2016)
- Arnold LM, "Efficacy and safety of mirogabalin for the treatment of fibromyalgia:results from three 13-week randomized, double-blind, placebo- and active-controlled, parallel-group studies and a 52-week open-label extension study", Curr Med Res Opin, 35, pp.1825~1835 (2019)
- Kim Kyongsong, "Therapeutic Effect of Mirogabalin on Peripheral Neuropathic Pain due to Lumbar Spine Disease", Asian Spine Journal, 15(3), pp.349~356 (2021), 대한척추외과학회[DOI]
- Baba M, "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, 13, pp.1811~1821 (2020)
- Kato M, "Pharmacokinetics and safety of a single oral dose of mirogabalin in Japanese subjects with varying degrees of renal impairment", J Clin Pharmacol, 58, pp.57~63 (2018)
- Yin OQ, "Population pharmaco-kinetic modeling and simulation for assessing renal impairment effect on the pharmacokinetics of mirogabalin", J Clin Pharmacol, 56, pp.203~212 (2016)
- Duchin K, "Open-label single-dose study to assess the effect of mild and moderate hepatic impairment on the pharmacokinetics of mirogabalin", Clin Drug Investig, 38, pp.1001~1009 (2018)
- Dow J, "Effect of coadministration of metformin with mirogabalin : results from a phase 1, randomized, open-label, drug-drug interaction study", Int J Clin Pharmacol Ther, 56, pp.451~458 (2018)
- Tachibana M, "Coadministration of probenecid and cimetidine with mirogabalin in healthy subjects : a phase 1, randomized, open-label, drug-drug interaction study", Br J Clin Pharmacol, 84, pp.2317~2324 (2018)
- Jansen M, "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, 7, pp.597~612 (2018)
- Brown K, "Tolerability, pharmacokinetics, and pharmacodynamics of mirogabalin in healthy subjects : results from phase 1 studies", Pharmacol Res Perspect, 6, pp.e00418~ (2018)
- Mendell J, "Abuse potential of mirogabalin in recreational polydrug users", Ther Adv Drug Saf, 10, pp.2042098619836032~ (2019)
- Takahashi S, "A probable case of mirogabalin-induced neutropenia", Cureus, 12, pp.e10182~ (2020)
- Kazuki M. Matsuda, "A case of trigeminal trophic syndrome responding to mirogabalin", European Journal of Dermatology, 30(2), pp.206~207 (2020), John Libbey Eurotext[DOI]
- Kumar P, "Trigeminal trophic syndrome", Indian J Dermatol, 59, pp.75~76 (2014)
- Kitano Y, "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, 74, pp.147~149 (2019)
- Domon Y, "Analgesic effects of the novel α₂δ ligand mirogabalin in a rat model of spinal cord injury", Pharmazie, 73, pp.659~661 (2018)
- Murasawa H, "Anxiolytic effects of the novel α2δ ligand mirogabalin in a rat model of chronic constriction injury, an experimental model of neuropathic pain", Psychopharmacology (Berl), 237, pp.189~197 (2020)
- Murasawa H, "Anxiolytic-like effects of mirogabalin, a novel ligand for α2δ ligand of voltage-gated calcium channels, in rats repeatedly injected with acidic saline intramuscularly, as an experimental model of fibromyalgia", Pharmacol Rep, 72, pp.571~579 (2020)
- Saeki K, "Analgesic effects of mirogabalin, a novel ligand for α2δsubunit of voltage-gated calcium channels, in experimental animal models of fibromyalgia", Naunyn Schmiedebergs Arch Pharmacol, 392, pp.723~728 (2019)
- Iwai T, "Mirogabalin prevents repeated restraint stress-induced dysfunction in mice", Behav Brain Res, 383, pp.112506~ (2020)
- Kitano Y, "Pharmacological, pharmacodynamics, and clinical profile of mirogabalin besylate (Tarlige® tablets 2.5 mg∙5 mg∙10 mg∙15mg)", Nihon Yakurigaku Zasshi, 154, pp.352~361 (2019)
- Gong N, "Injury-induced maladaptation and dysregulation of calcium channel α2δ subunit proteins and its contribution to neuropathic pain development", Br J Pharmacol, 175, pp.2231~2243 (2018)
- Bockbrader HN, "A comparison of the pharmacokinetics and pharmacodynamics of pregabalin and gabapentin", Clin Pharmacokinet, 49, pp.661~669 (2010)
