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Review

Pharmacokinetics and pharmacodynamics of new acute treatments for migraine

, , , &
Pages 189-198 | Received 19 Dec 2018, Accepted 01 Feb 2019, Published online: 12 Feb 2019

References

  • Dodick DW. Migraine. Lancet. 2018;391(10127):1315–1330.
  • Headache classification committee of the International Headache Society (IHS) the international classification of headache disorders, 3rd edition. Cephalalgia. 2018;38:1–211.
  • Noseda R, Burstein R. Migraine pathophysiology: anatomy of the trigeminovascular pathway and associated neurological symptoms, cortical spreading depression, sensitization, and modulation of pain. Pain. 2013;154(Suppl 1):S44–53.
  • Edvinsson L, Haanes KA, Warfvinge K, et al. CGRP as the target of new migraine therapies - successful translation from bench to clinic. Nat Rev Neurol. 2018;14(6):338–350.
  • GBD 2016 Headache Collaborators. Global, regional, and national burden of migraine and tension-type headache, 1990–2016: a systematic analysis for the global burden of disease study 2016. Lancet Neurol. 2018;17(11):954–976.
  • Linde M, Gustavsson A, Stovner LJ, et al. The cost of headache disorders in Europe: the Eurolight project. Eur J Neurol. 2012;19(5):703–711.
  • The Multinational Oral Sumatriptan and Cafergot Comparative Study Group. A randomized, double-blind comparison of sumatriptan and Cafergot in the acute treatment of migraine. Eur Neurol. 1991;31:314–322. The Multinational Oral Sumatriptan and Cafergot Comparative Study Group.
  • Diener HC, Jansen JP, Reches A, et al. Efficacy, tolerability and safety of oral eletriptan and ergotamine plus caffeine (Cafergot) in the acute treatment of migraine: a multicentre, randomised, double-blind, placebo-controlled comparison. Eur Neurol. 2002;47:99–107.
  • Goadsby PJ. The ‘Act when Mild’ (AwM) study: a step forward in our understanding of early treatment in acute migraine. Cephalalgia. 2008;28(Suppl 2):36–41.
  • Diener HC, Limmroth V. Advances in pharmacological treatment of migraine. Expert Opin Investig Drugs. 2001;10(10):1831–1845.
  • Jayamaha JE, Street MK. Fatal cerebellar infarction in a migraine sufferer whilst receiving sumatriptan. Intensive Care Med. 1995;21(1):82–83.
  • MaassenVanDenBrink A, Reekers M, Bax WA, et al. Coronary side-effect potential of current and prospective antimigraine drugs. Circulation. 1998;98(1):25–30.
  • Jähnichen S, Radtke OA, Pertz HH. Involvement of 5-HT1B receptors in triptan-induced contractile responses in guinea-pig isolated iliac artery. Naunyn Schmiedebergs Arch Pharmacol. 2004;370(1):54–63.
  • Bouchelet I, Case B, Olivier A, et al. No contractile effect for 5-HT1D and 5-HT1F receptor agonists in human and bovine cerebral arteries: similarity with human coronary artery. Br J Pharmacol. 2000;129(3):501–508.
  • Bouchelet I, Cohen Z, Case B, et al. Differential expression of sumatriptan-sensitive 5-hydroxytryptamine receptors in human trigeminal ganglia and cerebral blood vessels. Mol Pharmacol. 1996;50(2):219–223.
  • Amrutkar DV, Ploug KB, Hay-Schmidt A, et al. mRNA expression of 5-hydroxytryptamine 1B, 1D, and 1F receptors and their role in controlling the release of calcitonin gene-related peptide in the rat trigeminovascular system. Pain. 2012;153(4):830–838.
  • Goadsby PJ, Classey JD. Evidence for serotonin (5-HT)1B, 5-HT1D and 5-HT1F receptor inhibitory effects on trigeminal neurons with craniovascular input. Neuroscience. 2003;122(2):491–498.
  • Vila-Pueyo M. Targeted 5-HT1F therapies for migraine. Neurotherapeutics. 2018;15(2):291–303.
  • Ferrari MD, Färkkilä M, Reuter U, et al. Acute treatment of migraine with the selective 5-HT1F receptor agonist lasmiditan–a randomised proof-of-concept trial. Cephalalgia. 2010;30(10):1170–1178.
  • Ramadan NM, Skljarevski V, Phebus LA, et al. 5-HT1F receptor agonists in acute migraine treatment: a hypothesis. Cephalalgia. 2003;23(8):776–785.
  • Kuca B, Silberstein SD, Wietecha L, et al. Lasmiditan is an effective acute treatment for migraine: A phase 3 randomized study. Neurology. 2018;91(24):e2222–e2232.
  • Eli Lilly and Company. [webpage on the Internet]. Three doses of lasmiditan (50 mg, 100 mg and 200 mg) compared to placebo in the acute treatment of migraine (SPARTAN). NLM identifier: NCT02605174. [cited 2018 Dec 4]. Available from: https://clinicaltrials.gov/ct2/show/results/NCT02605174?term=SPARTAN+LASMIDITAN&rank=1&view=results
  • Eli Lilly and Company. [webpage on the Internet]. An open-label, long-term, safety study of lasmiditan for the acute treatment of migraine (GLADIATOR). NLM identifier: NCT02565186. [cited 2018 Dec 17]. Available from: https://clinicaltrials.gov/ct2/show/NCT02565186?term=lasmiditan+gladiator&rank=1
  • Eli Lilly and Company. [webpage on the Internet]. A study of lasmiditan (LY573144) over four migraine attacks. NLM identifier: NCT03670810. [cited 2018 Dec 17]. Available from: https://clinicaltrials.gov/ct2/show/NCT03670810?term=lasmiditan&phase=2&rank=1
  • Eli Lilly and Company. [webpage on the Internet]. Lilly submits new drug application to the FDA for lasmiditan for acute treatment of migraine, receives breakthrough therapy designation for emgality™ (galcanezumab-gnlm) for prevention of episodic cluster headache. [cited 2018 Dec 17]. Available from: https://investor.lilly.com/news-releases/news-release-details/lilly-submits-new-drug-application-fda-lasmiditan-acute
  • Nelson DL, Phebus LA, Johnson KW, et al. Preclinical pharmacological profile of the selective 5-HT1F receptor agonist lasmiditan. Cephalalgia. 2010;30(10):1159–1169.
  • Rubio-Beltran E, Kristian H, Labastida A, et al. Lasmiditan and sumatriptan: comparison of in vivo vascular constriction in the dog and in vitro contraction of human arteries. Cephalalgia. 2016;36(1S):104–105.
  • MaasseenVanDenBrink A, Labastida-Ramırez A, van Den Bogaerdt A, et al. In vitro characterization of agonist binding and activity at a panel of serotonin receptor subtypes for lasmiditan, triptans and other 5-HT receptor ligands and activity relationships for human isolated coronary artery contraction. Headache. 2018;58(S2):182.
  • Vila-Pueyo M, Strother L, Page K, et al. Lasmiditan inhibits trigeminovascular nociceptive transmission. Cephalalgia. 2016;36:152.
  • MaassenVanDenBrink A, Rubio-Beltràn E, Garrelds IM, et al. Lasmiditan inhibits CGRP release in the mouse trigeminovascular system. Headache. 2018;58(S2):64–65.
  • Färkkilä M, Diener HC, Géraud G, et al. COL MIG-202 study group. Efficacy and tolerability of lasmiditan, an oral 5-HT(1F) receptor agonist, for the acute treatment of migraine: a phase 2 randomised, placebo-controlled, parallel-group, dose-ranging study. Lancet Neurol. 2012;11(5):405–413.
  • Pilgrim A, Dussault B, Rupniak N, et al. COL-144, an orally bioavailable selective 5-HT1F receptor agonist for acute migraine therapy. Cephalalgia. 2009;29(1S):24–25.
  • Eli Lilly and Company. [webpage on the Internet]. Food-effect study in healthy participants. NLM identifier: NCT02233296. [cited 2018 Dec 17]. Available from: https://clinicaltrials.gov/ct2/show/results/NCT02233296?term=lasmiditan&rslt=With&rank=1&view=results
  • Bigal M, Rapoport A, Aurora S, et al. Satisfaction with current migraine therapy: experience from 3 centers in US and Sweden. Headache. 2007;47:475–479.
  • Aurora SK, Kori SH, Barrodale P, et al. Gastric stasis in migraine: more than just a paroxysmal abnormality during a migraine attack. Headache. 2006;46:57–63.
  • Dahlöf CG, Saiers J. Sumatriptan injection and tablets in clinical practice: results of a survey of 707 migraineurs. Headache. 1998;38(10):756–763.
  • Mathew NT, Dexter J, Couch J, et al. Dose ranging efficacy and safety of subcutaneous sumatriptan in the acute treatment of migraine US sumatriptan research group. Arch Neurol. 1992;49:1271–1276.
  • Cady RK, Munjal S, Cady RJ, et al. Randomized, double-blind, crossover study comparing DFN-11 injection (3 mg subcutaneous sumatriptan) with 6 mg subcutaneous sumatriptan for the treatment of rapidly-escalating attacks of episodic migraine. J Headache Pain. 2017;18(1):17.
  • Landy S, Munjal S, Brand-Schieber E, et al. Efficacy and safety of DFN-11 (sumatriptan injection, 3 mg) in adults with episodic migraine: a multicenter, randomized, double-blind, placebo-controlled study. J Headache Pain. 2018;19(1):69.
  • Landy S, Munjal S, Brand-Schieber E, et al. Efficacy and safety of DFN-11 (sumatriptan injection, 3 mg) in adults with episodic migraine: an 8-week open-label extension study. J Headache Pain. 2018;19(1):70.
  • Dahlöf CG. Sumatriptan: pharmacological basis and clinical results. Curr Med Res Opin. 2001;17:s35–s45.
  • Aggarwal R, Cardozo A, Homer JJ. The assessment of topical nasal drug distribution. Clin Otolaryngol. 2004;29:201–205.
  • Obaidi M, Offman E, Messina J, et al. Improved pharmacokinetics of sumatriptan with breath powered nasal delivery of sumatriptan powder. Headache. 2013;53:1323–1333.
  • Djupesland PG, Docekal P. Czech Migraine Investigators Group. Intranasal sumatriptan powder delivered by a novel breath-actuated bi-directional device for the acute treatment of migraine: a randomised, placebo-controlled study. Cephalalgia. 2010;30:933–942.
  • Cady RK, McAllister PJ, Spierings EL, et al. A randomized, double-blind, placebo-controlled study of breath powered nasal delivery of sumatriptan powder (AVP-825) in the treatment of acute migraine (the TARGET study). Headache. 2015;55(1):88–100.
  • Goadsby PJ. Therapeutic prospects for migraine. Ann Neurol. 2013;74:423–434.
  • Tepper SJ. Clinical implications for breath-powered powder sumatriptan intranasal treatment. Headache. 2013;53:1341–1349.
  • Silberstein SD, Marcus DA. Sumatriptan: treatment across the full spectrum of migraine. Expert Opin Pharmacother. 2013;14:1659–1667.
  • Tepper SJ, Cady RK, Silberstein S, et al. AVP-825 breath-powered intranasal delivery system containing 22 mg sumatriptan powder vs 100 mg oral sumatriptan in the acute treatment of migraines (the COMPASS study): a comparative randomized clinical trial across multiple attacks. Headache. 2015;55:621–635.
  • Silberstein S, Winner PK, McAllister PJ, et al. Early onset of efficacy and consistency of response across multiple migraine attacks from the randomized COMPASS Study: AVP-825 breath powered® exhalation delivery system (sumatriptan nasal powder) vs oral sumatriptan. Headache. 2017;57:862–876.
  • Lewis DW, Winner P, Hershey AD, et al. Adolescent Migraine Steering Committee. Efficacy of zolmitriptan nasal spray in adolescent migraine. Pediatrics 2007;120(2):390–396.
  • Winner P, Farkas V, Štillová H, et al. TEENZ Study Group. Efficacy and tolerability of zolmitriptan nasal spray for the treatment of acute migraine in adolescents: results of a randomized, double-blind, multi-center, parallel-group study (TEENZ). Headache 2016;56(7):1107–1119.
  • Tepper SJ, Chen S, Reidenbach F, et al. Intranasal zolmitriptan for the treatment of acute migraine. Headache. 2013;53(Suppl 2):62–71.
  • Garnock-Jones KP. Intranasal ketorolac: for short-term pain management. Clin Drug Investig. 2012;32:361–371.
  • Rao AS, Gelaye B, Kurth T, et al. A randomized trial of ketorolac vs sumatriptan vs placebo nasal spray (KSPN) for acute migraine. Headache. 2016;56:331–340.
  • Nagda CD, Chotai NP, Nagda DC, et al. Preparation and characterization of spray-dried mucoadhesive microspheres of ketorolac for nasal administration. Curr Drug Deliv. 2012;9(2):205–218.
  • Puri V, Bansal AK. In vitro-in vivo characterization of release modifying agents for parenteral sustained-release ketorolac formulation. Drug Dev Ind Pharm. 2004;30(6):619–626.
  • Spierings EL, Brandes JL, Kudrow DB, et al. Randomized, double-blind, placebo-controlled, parallel-group, multi-center study of the safety and efficacy of ADAM zolmitriptan for the acute treatment of migraine. Cephalalgia. 2018;38:215–224.
  • Kellerman DJ, Ameri M, Tepper SJ. Rapid systemic delivery of zolmitriptan using an adhesive dermally applied microarray. Pain Manag. 2017;7(6):559–567.
  • Tepper SJ. History and review of anti-Calcitonin Gene-Related Peptide (CGRP) therapies: from translational research to treatment. Headache. 2018;58(Suppl 3):238–275.
  • Olesen J, Diener HC, Husstedt IW, BIBN 4096 BS Clinical Proof of Concept Study Group, et al.. Calcitonin gene-related peptide receptor antagonist BIBN 4096 BS for the acute treatment of migraine. N Engl J Med. 2004;350:1104–1110.
  • Doods H, Hallermayer G, Wu D, et al. Pharmacological profile of BIBN4096BS, the first selective small molecule CGRP antagonist. Br J Pharmacol. 2000;129:420–423.
  • Rudolf K, Eberlein W, Engel W, et al. Development of human calcitonin gene-related peptide (CGRP) receptor antagonists. 1. Potent and selective small molecule CGRP antagonists. 1-[N2-[3,5-dibromo-N-[[4-(3,4-dihydro-2(1H)-oxoquinazolin-3-yl)-1-piperidinyl]carbonyl]-D-tyrosyl]-l-lysyl]-4-(4-pyridinyl)piperazine: the first CGRP antagonist for clinical trials in acute migraine. J Med Chem. 2005;48:5921–5931.
  • Hay DL, Walker CSCGRP. and its receptors. Headache. 2017;57(4):625–636.
  • Bigal ME, Walter S, Rapoport AM. Calcitonin gene-related peptide (CGRP) and migraine current understanding and state of development. Headache. 2013;53(8):1230–1244.
  • Li CC, Dockendorf M, Kowalski K, et al. Population PK analyses of ubrogepant (MK-1602), a CGRP receptor antagonist: enriching in-clinic plasma PK sampling with outpatient dried blood spot sampling. J Clin Pharmacol. 2017 Nov 14. DOI:10.1002/jcph.1021.
  • Tong G, Savant I, Jariwala N, et al. Phase I single and multiple dose study to evaluate the safety, tolerability, and pharmacokinetics of BMS-927711 in healthy subject. J Headache Pain. 2013;14(Suppl 1):P118.
  • Edvinsson L. Clinical data on the CGRP antagonist BIBN4096BS for treatment of migraine attacks. CNS Drug Rev. 2005;11:69–76.
  • Ho TW, Ferrari MD, Dodick DW, et al. Efficacy and tolerability of MK-0974 (telcagepant), a new oral antagonist of calcitonin gene-related peptide receptor, compared with zolmitriptan for acute migraine: A randomised, placebo-controlled, parallel-treatment trial. Lancet. 2008;372:2115–2123.
  • Connor KM, Shapiro RE, Diener HC, et al. Randomized, controlled trial of telcagepant for the acute treatment of migraine. Neurology. 2009;73:970–977.
  • Hewitt DJ, Aurora SK, Dodick DW, et al. Randomized controlled trial of the CGRP receptor antagonist MK-3207 in the acute treatment of migraine. Cephalalgia. 2011;31:712–722.
  • Diener HC, Barbanti P, Dahlöf C, et al. BI 44370 TA, an oral CGRP antagonist for the treatment of acute migraine attacks: results from a phase II study. Cephalalgia. 2011;31:573–584.
  • Marcus R, Goadsby PJ, Dodick D, et al. BMS-927711 for the acute treatment of migraine: A double-blind, randomized, placebo controlled, dose-ranging trial. Cephalalgia. 2014;34:114–125.
  • Voss T, Lipton RB, Dodick DW, et al. A phase IIb randomized, double-blind, placebo-controlled trial of ubrogepant for the acute treatment of migraine. Cephalalgia. 2016;36:887–898.
  • Ho TW, Connor KM, Zhang Y, et al. Randomized controlled trial of the CGRP receptor antagonist telcagepant for migraine prevention. Neurology. 2014;83:958–966.
  • Ho TW, Ho AP, Ge YJ, et al. Randomized controlled trial of the CGRP receptor antagonist telcagepant for prevention of headache in women with perimenstrual migraine. Cephalalgia. 2016;36:148–161.
  • Tfelt-Hansen P, Loder E. The emperor’s new gepants: are the effects of the new oral CGRP antagonists clinically meaningful? Headache. 2019;59:113-117.
  • Pascual J. Efficacy of BMS-927711 and other gepants vs triptans: there seem to be other players besides CGRP. Cephalalgia. 2014 Oct;34(12):1028–1029.
  • Monaghan DT, Bridges RJ, Cotman CW. The excitatory amino acid receptors: their classes, pharmacology, and distinct properties in the function of the central nervous system. Annu Rev Pharmacol Toxicol. 1989;29:365–402.
  • Traynelis SF, Wollmuth LP, McBain CJ, et al. Glutamate receptor ion channels: structure, regulation, and function. Pharmacol Rev. 2010;62(3):405–496.
  • Ramadan NM. The link between glutamate and migraine. CNS Spectr. 2003;8:446–449.
  • Xiao Y, Richter JA, Hurley JH. Release of glutamate and CGRP from trigeminal ganglion neurons: role of calcium channels and 5-HT1 receptor signaling. Mol Pain. 2008;4:12.
  • van Dongen RM, Zielman R, Noga M, et al. Migraine biomarkers in cerebrospinal fluid: A systematic review and meta-analysis. Cephalalgia. 2017;37(1):49–63.
  • Gomez-Mancilla B, Brand R, Jürgens TP, et al. Randomized, multicenter trial to assess the efficacy, safety and tolerability of a single dose of a novel AMPA receptor antagonist BGG492 for the treatment of acute migraine attacks. Cephalalgia. 2014;34:103–113.
  • Johnson KW, Dieckman DK, Phebus LA, et al. GluR5 antagonists as novel migraine therapies (abstract). Cephalalgia. 2001;21:268.
  • Weiss B, Alt A, Ogden AM, et al. Pharmacological characterization of the competitive GLUK5 receptor antagonist decahydroisoquinoline LY466195 in vitro and in vivo. J Pharmacol Exp Ther. 2006;318:772–781.
  • Sang CN, Ramadan NM, Wallihan RG, et al. LY293558, a novel AMPA/GluR5 antagonist, is efficacious and well-tolerated in acute migraine. Cephalalgia. 2004;24:596–602.
  • Johnson KW, Nisenbaum ES, Johnson MP, et al. Innovative drug development for headache disorders: glutamate. In: Olesen J, Ramadan NM, editors. Frontiers in headache research. New York: Oxford; 2008. p. 185–194.
  • TorreyPines Therapeutics. [webpage on the Internet]. Study to assess the safety, tolerance and efficacy of tezampanel in patients with acute migraine. NLM identifier: NCT00567086. [cited 2018 Dec 17]. Available from: https://clinicaltrials.gov/ct2/show/NCT00567086?term=tezampanel&draw=1&rank=1
  • Marin JC, Goadsby PJ. Glutamatergic fine tuning with ADX-10059: a novel therapeutic approach for migraine? Expert Opin Investig Drugs. 2010;19:555–561.
  • Waung MW, Akerman S, Wakefield M, et al. Metabotropic glutamate receptor 5: a target for migraine therapy. Ann Clin Transl Neurol. 2016;3:560–571.
  • Negro A, Curto M, Lionetto L, et al. A critical evaluation on MOH current treatments. Curr Treat Options Neurol. 2017;19(9):32.
  • Negro A, Koverech A, Martelletti P. Serotonin receptor agonists in the acute treatment of migraine: a review on their therapeutic potential. J Pain Res. 2018;11:515–526.
  • Depre C, Antalik L, Starling A, et al. A randomized, double-blind, placebo-controlled study to evaluate the effect of erenumab on exercise time during a treadmill test in patients with stable angina. Headache. 2018;58:715–723.
  • MaassenVanDenBrink A, Meijer J, Villalón CM, et al. Wiping out CGRP: potential cardiovascular risks. Trends Pharmacol Sci. 2016;37(9):779–788.

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