Monoclonal antibodies for migraine: Preventing Calcitonin gene-related peptide activity

CNS Drugs

Volumn 28, Issue 5, 2014, Pages 389-399

  Bigal, Marcelo E ^a   Walter, Sarah ^a  

^a TEVA PHARMACEUTICALS   (Israel)

Author keywords

[No Author keywords available]

Indexed keywords

ALD 403; AMG 334; CALCITONIN GENE RELATED PEPTIDE; CALCITONIN GENE RELATED PEPTIDE RECEPTOR ANTAGONIST; LBR 101; LY 2951742; MONOCLONAL ANTIBODY; UNCLASSIFIED DRUG; CALCITONIN GENE RELATED PEPTIDE RECEPTOR;

ARTICLE; DRUG HALF LIFE; DRUG SAFETY; HEMODYNAMICS; HUMAN; LIVER TOXICITY; LONG TERM CARE; MIGRAINE; PATHOPHYSIOLOGY; PHASE 1 CLINICAL TRIAL (TOPIC); PRIORITY JOURNAL; PROPHYLAXIS; PROTEIN TARGETING; ANIMAL; ANTAGONISTS AND INHIBITORS; DRUG DEVELOPMENT; METABOLISM; MIGRAINE DISORDERS;

ANIMALS; ANTIBODIES, MONOCLONAL; CALCITONIN GENE-RELATED PEPTIDE; DRUG DISCOVERY; HUMANS; MIGRAINE DISORDERS; RECEPTORS, CALCITONIN GENE-RELATED PEPTIDE;

EID: 84901507463     PISSN: 11727047     EISSN: 11791934     Source Type: Journal    
DOI: 10.1007/s40263-014-0156-4     Document Type: Article

References (108)

1. Noguchi K, Senba E, Morita Y, et al. Alpha-CGRP and beta-CGRP mRNAs are differentially regulated in the rat spinal cord and dorsal root ganglion. Brain Res Mol Brain Res. 1990;7(4):299-304.
2. Tippins JR, Di Marzo V, Panico M, et al. Investigation of the structure/activity relationship of human calcitonin gene-related peptide (CGRP). Biochem Biophys Res Commun. 1986;134(3):1306-11.
3. Poyner DR. Molecular pharmacology of receptors for calcitonin-gene- related peptide, amylin and adrenomedullin. Biochem Soc Trans. 1997;25(3):1032-6.
4. Uddman R, Edvinsson L, Ekman R, et al. Innervation of the feline cerebral vasculature by nerve fibers containing calcitonin gene-related peptide: trigeminal origin and co-existence with substance P. Neurosci Lett. 1985;62(1):131-6.
5. Lundberg JM, Franco-Cereceda A, Hua X, et al. Co-existence of substance P and calcitonin gene-related peptide-like immunoreactivities in sensory nerves in relation to cardiovascular and bronchoconstrictor effects of capsaicin. Eur J Pharmacol. 1985;108(3):315-9.
6. McCulloch J, Uddman R, Kingman TA, et al. Calcitonin gene-related peptide: functional role in cerebrovascular regulation. Proc Natl Acad Sci USA. 1986;83(15):5731-5.
7. Lundberg JM, Franco-Cereceda A, Alving K, et al. Release of calcitonin gene-related peptide from sensory neurons. Ann N Y Acad Sci. 1992;657:187-93.
8. Edvinsson L, Eftekhari S, Salvatore CA, et al. Cerebellar distribution of calcitonin gene-related peptide (CGRP) and its receptor components calcitonin receptor-like receptor (CLR) and receptor activity modifying protein 1 (RAMP1) in rat. Mol Cell Neurosci. 2011;46(1):333-9.
9. Eftekhari S, Edvinsson L. Calcitonin gene-related peptide (CGRP) and its receptor components in human and rat spinal trigeminal nucleus and spinal cord at C1-level. BMC Neurosci. 2011;12:112.
10. Uddman R, Edvinsson L, Ekblad E, et al. Calcitonin gene-related peptide (CGRP): perivascular distribution and vasodilatory effects. Regul Pept. 1986;15(1):1-23.
11. Mulderry PK, Ghatei MA, Spokes RA, et al. Differential expression of alpha-CGRP and beta-CGRP by primary sensory neurons and enteric autonomic neurons of the rat. Neuroscience. 1988;25(1):195-205.
12. Goadsby PJ, Edvinsson L, Ekman R. Release of vasoactive peptides in the extracerebral circulation of humans and the cat during activation of the trigeminovascular system. Ann Neurol. 1988;23(2):193-6.
13. Silberstein SD, Edvinsson L. Is CGRP a marker for chronic migraine? Neurology. 2013;81(14):1184-5.
14. Emeson RB, Hedjran F, Yeakley JM, et al. Alternative production of calcitonin and CGRP mRNA is regulated at the calcitonin-specific splice acceptor. Nature. 1989;341(6237):76-80.
15. van Rossum D, Hanisch UK, Quirion R. Neuroanatomical localization, pharmacological characterization and functions of CGRP, related peptides and their receptors. Neurosci Biobehav Rev. 1997;21(5):649-78.
16. Yamamoto M, Kondo H. Calcitonin gene-related peptide (CGRP)- immunoreactive nerve varicosities in synaptic contact with sensory neurons in the trigeminal ganglion of rats. Neurosci Lett. 1989;104(3):253-7.
17. Messlinger K, Lennerz JK, Eberhardt M, et al. CGRP and NO in the trigeminal system: mechanisms and role in headache generation. Headache. 2012;52(9):1411-27.
18. Eftekhari S, Edvinsson L. Possible sites of action of the new calcitonin gene-related peptide receptor antagonists. Ther Adv Neurol Disord. 2010;3(6):369-78.
19. Ho TW, Edvinsson L, Goadsby PJ. CGRP and its receptors provide new insights into migraine pathophysiology. Nat Rev Neurol. 2010;6(10):573-82.
20. Raddant AC, Russo AF. Calcitonin gene-related peptide in migraine: intersection of peripheral inflammation and central modulation. Expert Rev Mol Med. 2011;13:e36.
21. Peroutka SJ. Clinical trials update - 2012: year in review. Headache. 2013;53:177-80.
22. 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(9656):2115-23.
23. 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(6):712-22.
24. Olesen J, Diener HC, Husstedt IW, et al. Calcitonin gene-related peptide receptor antagonist BIBN 4096 BS for the acute treatment of migraine. N Engl J Med. 2004;350(11):1104-10.
25. Silberstein SD. Emerging target-based paradigms to prevent and treat migraine. Clin Pharmacol Ther. 2013;93(1):78-85.
26. Hoffmann J, Goadsby PJ. New agents for acute treatment of migraine: CGRP receptor antagonists, iNOS inhibitors. Curr Treat Options Neurol. 2012;14(1):50-9.
27. Goadsby PJ, Lipton RB, Ferrari MD. Migraine - current understanding and treatment. N Engl J Med. 2002;346(4):257-70.
28. Akerman S, Holland PR, Goadsby PJ. Diencephalic and brainstem mechanisms in migraine. Nat Rev Neurosci. 2011;12(10):570-84.
29. Afridi SK, Matharu MS, Lee L, et al. A PET study exploring the laterality of brainstem activation in migraine using glyceryl trinitrate. Brain. 2005;128(Pt 4):932-9.
30. Moskowitz MA. Neurogenic inflammation in the pathophysiology and treatment of migraine. Neurology. 1993;43(6 Suppl 3):S16-20.
31. Moskowitz MA, Cutrer FM. CGRP: blood flow and more? Cephalalgia. 1996;16(5):287.
32. Bigal ME, Ferrari M, Silberstein SD, et al. Migraine in the triptan era: lessons from epidemiology, pathophysiology, and clinical science. Headache. 2009;49(Suppl 1):S21-33.
33. Edmeads J. What is migraine? Controversy and stalemate in migraine pathophysiology. J Neurol. 1991;238(Suppl 1):S2-5.
34. Lauritzen M. Pathophysiology of the migraine aura. The spreading depression theory. Brain. 1994;117:199-210.
35. Leao AA. The slow voltage variation of cortical spreading depression of activity. Electroencephalogr Clin Neurophysiol. 1951;3(3):315-21.
36. Leao AA. Further observations on the spreading depression of activity in the cerebral cortex. J Neurophysiol. 1947;10(6):409-14.
37. Haerter K, Ayata C, Moskowitz MA. Cortical spreading depression: a model for understanding migraine biology and future drug targets. Headache Curr. 2005;2:97-103.
38. Di Clemente L, Coppola G, Magis D, et al. Nitroglycerin sensitises in healthy subjects CNS structures involved in migraine pathophysiology: evidence from a study of nociceptive blink reflexes and visual evoked potentials. Pain. 2009;144(1-2):156-61.
39. Bahra A, Matharu MS, Buchel C, et al. Brainstem activation specific to migraine headache. Lancet. 2001;357(9261):1016-7.
40. Weiller C, May A, Limmroth V, et al. Brain stem activation in spontaneous human migraine attacks. Nat Med. 1995;1:658-60.
41. Afridi S, Giffin NJ, Kaube H, et al. A PET study in spontaneous migraine. Arch Neurol. 2005;62:1270-5.
42. Matharu MS, Bartsch T, Ward N, et al. Central neuromodulation in chronic migraine patients with suboccipital stimulators: a PET study. Brain. 2004;127:220-30.
43. Afridi S, Matharu MS, Lee L, et al. A PET study exploring the laterality of brainstem activation in migraine using glyceryl trinitrate. Brain. 2005;128:932-9.
44. Bahra A, Matharu MS, Buchel C, et al. Brainstem activation specific to migraine headache. Lancet. 2001;357:1016-7.
45. Raskin NH, Hosobuchi Y, Lamb S. Headache may arise from perturbation of brain. Headache. 1987;27:416-20.
46. Veloso F, Kumar K, Toth C. Headache secondary to deep brain implantation. Headache. 1998;38:507-15.
47. Haas DC, Kent PF, Friedman DI. Headache caused by a single lesion of multiple sclerosis in the periaqueductal gray area. Headache. 1993;33:452-5.
48. Goadsby PJ. Neurovascular headache and a midbrain vascular malformation - evidence for a role of the brainstem in chronic migraine. Cephalalgia. 2002;22:107-11.
49. Afridi S, Goadsby PJ. New onset migraine with a brainstem cavernous angioma. J Neurol Neurosurg Psychiatry. 2003;74:680-2.
50. Obermann M, Gizewski ER, Limmroth V, et al. Symptomatic migraine and pontine vascular malformation: evidence for a key role of the brainstem in the pathophysiology of chronic migraine. Cephalalgia. 2006;26:763-6.
51. Moskowitz MA, Nozaki K, Kraig RP. Neocortical spreading depression provokes the expression of c-fos protein-like immunoreactivity within trigeminal nucleus caudalis via trigeminovascular mechanisms. J Neurosci. 1993;13(3):1167-77.
52. Goadsby PJ. Calcitonin gene-related peptide antagonists as treatments of migraine and other primary headaches. Drugs. 2005;65:2557-67.
53. Moskowitz MA. Pathophysiology of headache - past and present. Headache. 2007;47(Suppl 1):S58-63.
54. Noseda R, Burstein R. Migraine pathophysiology: anatomy of the trigeminovascular pathway and associated neurological symptoms, CSD, sensitization and modulation of pain. Pain. 2013;154(Suppl):1.
55. Lafont AG, Dufour S, Fouchereau-Peron M. Evolution of the CT/CGRP family: comparative study with new data from models of teleosts, the eel, and cephalopod molluscs, the cuttlefish and the nautilus. Gen Comp Endocrinol. 2007;153(1-3):155-69.
56. Edvinsson L. Correlation between CGRP and migraine attacks. Cephalalgia. 2005;25(3):163-4.
57. Benarroch EE. CGRP: sensory neuropeptide with multiple neurologic implications. Neurology. 2011;77(3):281-7.
58. Lennerz JK, Ruhle V, Ceppa EP, et al. Calcitonin receptor-like receptor (CLR), receptor activity-modifying protein 1 (RAMP1), and calcitonin gene-related peptide (CGRP) immunoreactivity in the rat trigeminovascular system: differences between peripheral and central CGRP receptor distribution. J Comp Neurol. 2008;507(3):1277-99.
59. Sugimoto T, Fujiyoshi Y, Xiao C, et al. Central projection of calcitonin gene-related peptide (CGRP)- and substance P (SP)-immunoreactive trigeminal primary neurons in the rat. J Comp Neurol. 1997;378(3):425-42.
60. Goadsby PJ, Hargreaves RJ. Mechanisms of action of serotonin 5-HT1B/D agonists: insights into migraine pathophysiology using rizatriptan. Neurology. 2000;55(9 Suppl 2):S8-14.
61. Vause CV, Durham PL. Calcitonin gene-related peptide differentially regulates gene and protein expression in trigeminal glia cells: findings from array analysis. Neurosci Lett. 2010;473(3):163-7.
62. Edvinsson L, JansenOlesen I, Kingman TA, et al. Modification of vasoconstrictor responses in cerebral blood vessels by lesioning of the trigeminal nerve: possible involvement of CGRP. Cephalalgia. 1995;15(5):373-83.
63. Troltzsch M, Denekas T, Messlinger K. The calcitonin gene-related peptide (CGRP) receptor antagonist BIBN4096BS reduces neurogenic increases in dural blood flow. Eur J Pharmacol. 2007;562(1-2):103-10.
64. Eftekhari S, Warfvinge K, Blixt FW, et al. Differentiation of nerve fibers storing CGRP and CGRP receptors in the peripheral trigeminovascular system. J Pain. 2013;14(11):1289-303.
65. Markowitz S, Saito K, Buzzi MG, et al. The development of neurogenic plasma extravasation in the rat dura mater does not depend upon the degranulation of mast cells. Brain Res. 1989;477(1-2):157-65.
66. Mathew R, Andreou AP, Chami L, et al. Immunohistochemical characterization of calcitonin gene-related peptide in the trigeminal system of the familial hemiplegic migraine 1 knock-in mouse. Cephalalgia. 2011;31(13):1368-80.
67. Morara S, Rosina A, Provini L, et al. Calcitonin gene-related peptide receptor expression in the neurons and glia of developing rat cerebellum: an autoradiographic and immunohistochemical analysis. Neuroscience. 2000;100(2):381-91.
68. Pagani F, Guidobono F, Netti C, et al. Age-related increase in CGRP binding site densities in rat cerebellum. Pharmacol Res. 1989;21(Suppl 1):105-6.
69. Noseda R, Burstein R. Advances in understanding the mechanisms of migraine-type photophobia. Curr Opin Neurol. 2011;24(3):197-202.
70. Recober A, Kuburas A, Zhang Z, et al. Role of calcitonin gene-related peptide in light-aversive behavior: implications for migraine. J Neurosci. 2009;29(27):8798-804.
71. Lassen LH, Haderslev PA, Jacobsen VB, et al. CGRP may play a causative role in migraine. Cephalalgia. 2002;22(1):54-61.
72. Petersen KA, Birk S, Lassen LH, et al. The CGRP-antagonist, BIBN4096BS does not affect cerebral or systemic haemodynamics in healthy volunteers. Cephalalgia. 2005;25(2):139-47.
73. Eftekhari S, Salvatore CA, Chen TB, Zeng Z, Edvinsson L. Trigeminal ganglium - a site of action for CGRP receptor antagonists. Cephalalgia. 2013; Program Late Abstracts (Supplement): 1.
74. Hostetler ED, Joshi AD, Sanabria-Bohorquez S, et al. In vivo quantification of calcitonin gene-related peptide receptor occupancy by telcagepant in rhesus monkey and human brain using the positron emission tomography tracer [11C]MK-4232. J Pharmacol Exp Ther. 2013;347(2):478-86.
75. Bigal ME, Walter S, Rapoport AM. Calcitonin gene-related peptide (CGRP) and migraine current understanding and state of development. Headache. 2013;53(8):1230-44.
76. Salvatore CA, Moore EL, Calamari A, et al. Pharmacological properties of MK-3207, a potent and orally active calcitonin gene-related peptide receptor antagonist. J Pharmacol Exp Ther. 2010;333(1):152-60.
77. Pettypiece S. Merck halts testing of migraine drug on liver safety (update 2). http://www.bloomberg.com/apps/news?pid=newsarchive&sid= aKxzpNBZ2cbA. Accessed 10 Jan 2014.
78. Diener HC, Barbanti P, Dahlof 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(5):573-84.
79. 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. 2013.
80. Bigal ME. BMS-927711 for the acute treatment of migraine. Cephalalgia. 2013.
81. A dose-finding study of MK-1602 in the treatment of acute migraine (MK-1602-006 AM1); 2013. http://clinicaltrial.gov/ct2/show/NCT01613248?term= MK1602&rank=2. Accessed 10 Jan 2014.
82. Wu H, Dall'Acqua WF. Humanized antibodies and their applications. Methods. 2005;36(1):1-2.
83. Baumann A. Early development of therapeutic biologics - pharmacokinetics. Curr Drug Metab. 2006;7(1):15-21.
84. Tfelt-Hansen PC. Evidence-based guideline update: pharmacologic treatment for episodic migraine prevention in adults: report of the Quality Standards Subcommittee of the American Academy of Neurology and the American Headache Society. Neurology. 2013;80(9):869-70.
85. Services, U.D.o.H.a.H., F.a.D. Administration, C.f.D.E.a.R. (CDER), et al. Guidance for industry, S6 preclinical safety evaluation of biotechnology-derived pharmaceuticals; 1997. http://www.fda.gov/downloads/ regulatoryinformation/guidances/ucm129171.pdf. Accessed 10 Jan 2014.
86. Berton E. Safety pharmacology: similarities and differences between small molecules and novel biotherapeutics. In: Cavagnaro J, editor. Preclinical safety evaluation of biopharmaceuticals. New York: Wiley; 2008.
87. Vargas HM, Bass AS, Breidenbach A, et al. Scientific review and recommendations on preclinical cardiovascular safety evaluation of biologics. J Pharmacol Toxicol Methods. 2008;58(2):72-6.
88. Conolan S, Taylor DA. Antagonism by some ergot derivatives of 5-HT-induced vasoconstriction. Eur J Pharmacol. 1986;123(2):299-302.
89. Maassen VanDenBrink A, Bax WA, Ferrari MD, et al. Augmented contraction of the human isolated coronary artery by sumatriptan: a possible role for endogenous thromboxane. Br J Pharmacol. 1996;119(5):855-62.
90. Longmore J, Hargreaves RJ, Boulanger CM, et al. Comparison of the vasoconstrictor properties of the 5-HT1D-receptor agonists rizatriptan (MK-462) and sumatriptan in human isolated coronary artery: outcome of two independent studies using different experimental protocols. Funct Neurol. 1997;12(1):3-9.
91. Feuerstein G, Willette R, Aiyar N. Clinical perspectives of calcitonin gene related peptide pharmacology. Can J Physiol Pharmacol. 1995;73(7):1070-4.
92. Poyner D. Pharmacology of receptors for calcitonin gene-related peptide and amylin. Trends Pharmacol Sci. 1995;16(12):424-8.
93. Zhang M, Fukuyama H. CGRP immunohistochemistry in wound healing and dentin bridge formation following rat molar pulpotomy. Histochem Cell Biol. 1999;112(5):325-33.
94. Young S. Preventing migraines with a new kind of antibody; 2013. http://medcitynews.com/2013/05/preventing-migraines-with-a-new-kind-of-antibody/ . Accessed 10 Jan 2014.
95. Alder Biopharmaceuticals, I. Safety tolerability and pharmacokinetics of ALD403. http://clinicaltrial.gov/ct2/show/NCT01579383?term=ALD403&rank=1. Accessed 10 Jan 2014.
96. Stone I, Schull D. First patients dosed in proof-of-concept clinical study of Alder Biopharmaceuticals' lead therapeutic candidate for treatment of migraine, ALD403; 2013. http://www.prnewswire.com/news-releases/first-patients- dosed-in-proof-of-concept-clinical-study-of-alder-biopharmaceuticals-lead- therapeutic-candidate-for-treatment-of-migraine-ald403-199135511.html. Accessed 10 Jan 2014.
97. Safety, efficacy and pharmacokinetics of ALD403; 2013. http://clinicaltrials.gov/ct2/show/NCT01772524?term=ald403&rank=2. Accessed 10 Jan 2014.
98. de Hoon J, Montieth D, Vermeersch S, et al. Safety, pharmacokinetics, and pharmacodynamics of LY2951742: a monoclonal antibody targeting CGRP; 2013. http://cep.sagepub.com/content/33/8-suppl/1.full.pdf+html. Accessed 10 Jan 2014.
99. The Arteaus Therapeutics Story: R&D Externalization with Eli Lilly; 2014. http://www.forbes.com/sites/brucebooth/2014/01/13/the-arteaus- therapeutics-story-rd-externalization-with-eli-lilly/.
100. Amgen-Science-Pipeline; 2013. http://www.amgen.com/science/pipe.html. Accessed 10 Jan 2014.
101. Ascending single doses of AMG 334 in healthy subjects and migraine patients; 2013. http://clinicaltrial.gov/ct2/show/NCT01688739?term= AMG334&rank=1. Cited 4 Oct 2013.
102. Ascending multiple-doses of AMG 334 in healthy subjects and in migraine patients; 2013. http://clinicaltrial.gov/ct2/show/NCT01723514?term= AMG334&rank=2. Accessed 10 Jan 2014.
103. Amgen. A phase 2 study to evaluate the efficacy and safety of AMG 334 in migraine prevention; 2013. http://clinicaltrial.gov/ct2/show/NCT01952574?term= AMG+334&rank=4. Accessed 10 Jan 2014.
104. Bigal ME, Walter S, Bronson M, et al. Cardiovascular and hemodynamic parameters in women following prolonged CGRP inhibition using LBR-101, a monoclonal antibody against CGRP. Cephalalgia (submitted).
105. Bigal ME, Escandon R, Bronson M, et al. Safety and tolerability of LBR-101, a humanized monoclonal antibody that blocks the binding of CGRP to its receptor: results of the phase 1 program. Cephalalgia. 2013.
106. Bigal ME, Escandon R, Bronson M, Walter S, Sudworth M, Huggins JP, Garzone P. Safety and tolerability of LBR-101, a humanized monoclonal antibody that blocks the binding of CGRP to its receptor - results of the phase 1 program. Cephalalgia (in press).
107. Ho TW, Mannix LK, Fan X, et al. Randomized controlled trial of an oral CGRP receptor antagonist, MK-0974, in acute treatment of migraine. Neurology. 2008;70(16):1304-12.
108. Connor KM, Shapiro RE, Diener HC, et al. Randomized, controlled trial of telcagepant for the acute treatment of migraine. Neurology. 2009;73(12):970-7.