Telcagepant, a calcitonin gene-related peptide antagonist for the treatment of migraine

Current Opinion in Investigational Drugs

Volumn 10, Issue 7, 2009, Pages 711-720

  Tepper, Stewart J ^a   Cleves, Catalina ^a  

^a NEUROLOGICAL INSTITUTE   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

AMINOTRANSFERASE; CALCITONIN GENE RELATED PEPTIDE RECEPTOR; CALCITONIN GENE RELATED PEPTIDE RECEPTOR ANTAGONIST; IBUPROFEN; MK 0974; MK 974; RIZATRIPTAN; SUMATRIPTAN; TELCAGEPANT; TRIPTAN DERIVATIVE; UNCLASSIFIED DRUG; ZOLMITRIPTAN;

AREA UNDER THE CURVE; ASTHENIA; BRAIN BLOOD VESSEL; CENTRAL NERVOUS SYSTEM; CHEST TIGHTNESS; CLINICAL TRIAL; DISEASE SEVERITY; DIZZINESS; DRUG EFFICACY; DRUG ELIMINATION; DRUG HALF LIFE; DRUG METABOLISM; DRUG RECEPTOR BINDING; DRUG SAFETY; DYSESTHESIA; FATIGUE; HUMAN; HYPERESTHESIA; HYPESTHESIA; LABORATORY TEST; MIGRAINE; NAUSEA; NEUROTRANSMISSION; NONHUMAN; PARESTHESIA; REVIEW; SIDE EFFECT; SINGLE DRUG DOSE; SOMNOLENCE; THORAX PAIN; TREATMENT RESPONSE; UPPER ABDOMINAL PAIN; VASOCONSTRICTION; XEROSTOMIA;

ANALGESICS, NON-NARCOTIC; AZEPINES; CLINICAL TRIALS AS TOPIC; DRUGS, INVESTIGATIONAL; HUMANS; IMIDAZOLES; MIGRAINE DISORDERS; MOLECULAR STRUCTURE; PATENTS AS TOPIC; RECEPTORS, CALCITONIN GENE-RELATED PEPTIDE; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 68149083001     PISSN: 14724472     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Review

References (69)

1. 358225 Neuropeptide changes in a case of chronic paroxysmal hemicrania - Evidence for trigemino-parasympathetic activation. Goadsby PJ, Edvinsson L CEPHALALGIA 1996 16 6 448-450
2. 358274 Release of vasoactive peptides in the extracerebral circulation of humans and the cat during activation of the trigeminovascular system. Goadsby PJ, Edvinsson L, Ekman R ANN NEUROL 1988 23 2 193-196
3. 358282 Human in vivo evidence for trigeminovascular activation in cluster headache. Neuropeptide changes and effects of acute attacks therapies. Goadsby PJ, Edvinsson L BRAIN 1994 117 Pt 3 427-434
4. 548040 CGRP receptor antagonists: A new choice for acute treatment of migraine? Durham PL CURR OPIN INVEST DRUGS 2004 5 7 731-735
5. 552258 Prevalence and burden of migraine in the United States: Data from the American Migraine Study II. Lipton RB, Stewart WF, Diamond S, Diamond ML, Reed M HEADACHE 2001 41 7 646-657
6. 552424 Increase in plasma calcitonin gene-related peptide from the extracerebral circulation during nitroglycerin-induced cluster headache attack. Fanciullacci M, Alessandri M, Figini M, Geppetti P, Michelacci S PAIN 1995 60 2 119-123
7. 552427 Calcitonin gene-related peptide receptor antagonist BIBN 4096 BS for the acute treatment of migraine. Olesen J, Diener HC, Husstedt IW, Goadsby PJ, Hall D, Meier U, Pollentier S, Lesko LM N ENGL J MED 2004 350 11 1104-1110
8. 552466 Calcitonin gene-related peptide in the regulation of cardiac function. Goto K, Miyauchi T, Homma S, Ohshima N ANN NY ACAD SCI 1992 657 194-203
9. 552467 Calcitonin gene-related peptide levels are elevated in patients with sepsis. Joyce CD, Fiscus RR, Wang X, Dries DJ, Morris RC, Prinz RA SURGERY 1990 108 6 1097-1101
10. 552468 Neuroendocrine, immune, and local responses related to temporomandibular disorders. Kopp S J OROFACIAL PAIN 2001 15 1 9-28
11. 552470 New insights into peripheral chemical mediators of temporomandibular pain and inflammation. Sessle BJ J OROFACIAL PAIN 2001 15 1 5
12. 552472 Dynamic plasticity of dental sensory nerve structure and cytochemistry. Byers MR ARCH ORAL BIOL 1994 39 Suppl 13S-21S
13. 552473 Neural basis of sensation in intact and injured corneas. Belmonte C, Acosta MC, Gallar J EXP EYE RES 2004 78 3 513-525
14. 559660 Calcitonin gene-related peptide (CGRP) antagonists: Blockers of neuronal transmission in migraine. Brain SD BR J PHARMACOL 2004 142 7 1053-1054
15. 687272 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. Rudolf K, Eberlein W, Engel W, Pieper H, Entzeroth M, Hallermayer G, Doods H J MED CHEM 2005 48 19 5921-5931
16. 777729 American Chemical Society 233rd National Meeting (Part I)- OVERNIGHT REPORT, First Time Disclosure of Clinical Candidates, Chicago, IL, USA, 25-29 March 2007 Turner B IDDB MEETING REPORT 2007 March 25-29
17. 789706 Consensus statement: Cardiovascular safety profile of triptans (5-HT agonists) in the acute treatment of migraine. Dodick D, Lipton RB, Martin V, Papademetriou V, Rosamond W, MaassenVanDenBrink A, Loutfi H, Welch KM, Goadsby PJ, Hahn S, Hutchinson S et al HEADACHE 2004 44 5 414-425
18. 800471 GPCR modulation by RAMPs. Hay DL, Poyner DR, Sexton PM PHARMACOL THER 2006 109 1-2 173-197
19. 820081 Calcitonin gene-related peptide receptor antagonists for the treatment of migraine. Williams TM, Burgey CS, Paone DV, Shaw AW, Bell IM, Deng JZ, deSolms J, Gallicchio SN, Nguyen DN, Potteiger CM, Stump CA et al AM CHEM SOC NATL MEET EXPOSITION 2007 234 Abs MEDI 219
20. 845805 Potent, orally bioavailable calcitonin gene-related peptide receptor antagonists for the treatment of migraine: Discovery of N-[(3R,6S)-6-(2,3-difluorophenyl)-2-oxo-1-(2,2,2-trifluoroethyl) azepan-3-yl]-4-(2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridin-1-yl) piperidine-1-carboxamide (MK-0974). Paone DV, Shaw AW, Nguyen DN, Burgey CS, Deng JZ, Kane SA, Koblan KS, Salvatore CA, Mosser SD, Johnston VK, Wong BK et al J MED CHEM 2007 50 23 5564-5567
21. 875024 GSK reports 2007 business performance EPS of 99.1p up 10% CER. GlaxoSmithKline plc PRESS RELEASE 2008 February 07
22. 875166 Pharmacological characterization of MK-0974 [A/-[(3R,6S)- 6-(2,3-difluorophenyl)-2-oxo-1-(2,2,2-trifluoroethyl)azepan-3-yl]- 4-(2-oxo-2,3-dihydro-1 H-imidazo[4,5-b]pyridin-1-yl)piperidine- 1-carboxamide], a potent and orally active calcitonin gene- related peptide receptor antagonist for the treatment of migraine. Salvatore CA, Hershey JC, Corcoran HA, Fay JF, Johnston VK, Moore EL, Mosser SD, Burgey CS, Paone DV, Shaw AW, Graham SL et al J PHARMACOL EXP THER 2008 324 2 416-421
23. 875167 Efficacy and tolerability of a novel, oral CGRP antagonist, MK-0974, in the acute treatment of migraine. Assaid C, Fan X, Furtek C, Ho T, Jones C, Mannix L, Rapoport A CEPHALALGIA 2007 27 6 Abs ScS6-7
24. 875168 Inhibition of capsaicin-induced increase in dermal microvascular blood flow by the oral CGRP antagonist, MK-0974. de Hoon J, de Lepeleire I, Hickey L, Kane SA, Murphy MG, Palcza J, Sinclair S, Vanmolkot F, Willson K, Xiao A, Xu Y CEPHALALGIA 2007 27 6 738-739
25. 875169 The novel oral CGRP antagonist, MK-0974, exhibits similar pharmacokinetics during and between migraine attacks. Sinclair S, Boyle JE, Murphy MG, de Lepeleire I, Kane SA, Blanchard R, Willson K, Xu Y, Agrawal N, Palcza J, de Hoon J CEPHALALGIA 2007 27 6 Abs F060
26. 875174 MK-0974 oral CGRP antagonist inhibits capsaicin-induced increase in dermal microvascular blood flow. Sinclair SR, Kane SA, Xiao A, Willson KJ, Xu Y, Hickey L, Palcza J, de Lepeleire I, Vanmolkot FHM, de Hoon JNJ NEUROLOGY 2007 68 12 Abs P07.064
27. 875175 Efficacy and tolerability of a novel, oral CGRP antagonist, MK-0974, in the acute treatment of migraine: Results from a phase 2 randomized, controlled, clinical trial. Ho T, Mannix L, Fan X, Assaid C, Furtek C, Jones C, Rapoport A HEADACHE 2007 47 5 Abs 0R19
28. 875177 MK-0974 oral CGRP antagonist inhibits capsaicin-induced increase in dermal microvascular blood flow. Sinclair SR, Kane SA, Xiao A, Willson KJ, Xu Y, Hickey L, Palcza J, de Lepeleire I, Vanmolkot FHM, de Hoon JNJM, Murphy MG HEADACHE 2007 47 5 Abs S68
29. 875178 MK-0974, a novel oral CGRP antagonist, exhibits similar pharmacokinetics during and between migraine attacks. Sinclair SR, Boyle JE, de Lepeleire I, Kane SA, Blanchard R, Willson K, Xu Y, Agrawal N, Palcza J, de Hoon J, Murphy MG HEADACHE 2007 47 5 Abs S69
30. 882577 Annual report 2007 - GlaxoSmithKline plc. GlaxoSmithKline plc ANNUAL REPORT 2008 February 28
31. 902111 Randomized controlled trial of an oral CGRP receptor antagonist, MK-0974, in acute treatment of migraine. Ho TW, Mannix LK, Fan X, Assaid C, Furtek C, Jones CJ, Lines CR, Rapoport AM NEUROLOGY 2008 70 16 1304-1312
32. 914065 Acute antimigraine efficacy and tolerability of the novel oral CGRP receptor antagonist MK-0974: A phase III clinical trial versus placebo and zolmitriptan. Ho TW, Ferrari MD, Dodick DW, Galet V, Kost P, Fan X, Leibensperger H, Froman S, Assaid C, Koppen H, Winner P HEADACHE 2008 48 Suppl 1 Abs OR17
33. 914205 "Sustained pain freedom and no adverse events" as an endpoint in clinical trials of acute migraine treatments: Application to patient-level data from a trial of the CGRP receptor antagonist, MK-0974, and zolmitriptan. Dodick DW, Galet V, Kost J, Assaid C, Ho TW HEADACHE 2008 48 Suppl 1 Abs S6
34. 916496 Pain Therapeutics - SMi's Eighth Annual Conference - Conference Presentation Book SMI CONF - PAIN THERAPEUTICS 2008 8th 09-10 June
35. 941337 Merck & Co Inc's investigational migraine treatment telcagepant relieved migraine pain and symptoms in latest phase III study. Merck & Co Inc PRESS RELEASE 2008 September 06
36. 968193 Synthesis of the (3R,6S)-3-amino-6-(2,3-difluorophenyl) azepan-2-one of telcagepant (MK-0974), a calcitonin gene-related peptide receptor antagonist for the treatment of migraine headache. Burgey CS, Paone DV, Shaw AW, Deng JZ, Nguyen DN, Potteiger CM, Graham SL, Vacca JP, Williams TM ORG LETT 2008 10 15 3235-3238
37. 974993 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. Ho TW, Ferrari MD, Dodick DW, Galet V, Kost J, Fan XY, Leibensperger H, Froman S, Assaid C, Lines C, Koppen H et al LANCET 2008 372 9656 2115-2123
38. 985635 Boehringer Ingelheim scales up production of CGRP antagonist BI-44370, phase II back-up to olcegepant. Thomson Reuters IDDB ALERT 2009 February 20
39. 986404 Discovery of a novel, orally bioavailable CGRP receptor antagonist for the treatment of migraine. Bell IM AM CHEM SOC NATL MEET EXPOSITION 2009 237 Abs MEDI 028
40. 987255 The pharmacokinetics, safety, and tolerability of telcagepant, a novel calcitonin gene related peptide (CGRP) receptor antagonist, in healthy subjects and migraineurs. Han TH, Blanchard RL, Palcza J, De Lepeleire I, Laethem T, Martucci A, Willson K, Xu Y, Boyle J, Butterfield K, Mahon C et al CLIN PHARMACOL THER 2009 85 Suppl 1 Abs PII-08
41. 987508 Challenges in the development of orally bioavailable antagonists of the calcitonin gene-related peptide receptor, a family B GPCR: Discovery of telcagepant (MK-0974) for the treatment of migraine. Burgey C AM CHEM SOC NATL MEET EXPOSITION 2009 237 Abs MEDI 174
42. 1001845 Merck announces first-quarter 2009 financial results. Merck & Co Inc PRESS RELEASE 2009 April 21
43. 1003858 Chapter 6: Migraine: Diagnosis and treatment. Silberstein SD, Lipton RJ, Goadsby PJ HEADACHE CLIN PRACT (EDS: SILBERSTEIN SD, UPTON RJ, GOADSBY PJ) 2002 Martin Dunitz Ltd, London, UK 2nd Edition 69-112
44. 1003907 Calcitonin gene-related peptide receptor antagonist human CGRP-(8-37). Chiba T, Yamaguchi A, Yamatani T, Nakamura A, Morishita T, Inui T, Fukase M, Noda T, Fujita T AM J PHYSIOL - ENDOCRINOL METAB 1989 256 2 Pt 1 E331-E335
45. 1004050 Preclinical pharmacokinetics of MK-0974, an orally active calcitonin-gene related peptide (CGRP)-receptor antagonist, mechanism of dose dependency and species differences. Roller S, Cui D, Laspina C, Miller-Stein C, Rowe J, Wong B, Prueksaritanont T XENOBIOTICA 2009 39 1 33-45
46. 1004302 Examining the binding properties of MK-0974: A CGRP receptor antagonist for the acute treatment of migraine. Moore EL, Burgey CS, Paone DV, Shaw AW, Tang YS, Kane SA, Salvatore CA EUR J PHARMACOL 2009 602 2-3 250-254
47. 1004317 Assessment of the effect of MK-0974, an oral CGRP receptor antagonist, on spontaneous ischemia in patients with stable cardiovascular disease. Behm MO, Blanchard RL, Murphy MG, Chodakewitz JA, Palcza JS, Harris DE, Butterfield KL, Smith WB, Haynes EM, Sackner-Bernstein J, Preston RA et al HEADACHE 2008 48 Suppl 1 Abs S1
48. 1004325 Effect of MK-0974, an oral CGRP antagonist, on the hemodynamic response to subligual nitroglycerin. Van der Schueren BJ, Blanchard R, Murphy MG, Palcza J, De Lepeleire I, Van Hecken A, Depre M, de Hoon JN HEADACHE 2008 48 Suppl 1 Abs S58
49. 1004615 The global burden of disease study: Implications for neurology. Menken M, Munsat TL, Toole JF ARCH NEUROL 2000 57 3 418-420
50. 1004648 Intravital microscope studies on the effects of neurokinin agonists and calcitonin gene-related peptide on dural vessel diameter in the anaesthetized rat. Williamson DJ, Hargreaves RJ, Hill RG, Shepheard SL CEPHALALGIA 1997 17 4 518-524
51. 1004650 Calcitonin gene-related peptide (CGRP) antagonists and migraine: Is this a new era? Goadsby PJ NEUROLOGY 2008 70 16 1300-1301
52. 1004660 An adaptive two-stage design in a phase 2 dose-finding trial to treat acute migraine. Fan X, Assaid CA, Ho T NEUROLOGY 2007 68 Suppl 1 Abs S25.003
53. 1004774 Efficacy and safety of rizatriptan wafer for the acute treatment of migraine. Rizatriptan Wafer Protocol 049 Study Group. Ahrens SP, Farmer MV, Williams DL, Willoughby E, Jiang K, Block GA, Visser WH CEPHALALGIA 1999 19 5 525-530
54. 1004775 Clinical profile of the novel oral CGRP receptor antagonist telcagepant for the acute treatment of migraine in two phase 3 randomized placebo-controlled trials. Ho TW, Ferrari MD, Dodick DW, Shapiro RE, Diener H-C, Lucas S, Galet V, Kost J, Fan X, Leibensperger H, Froman S et al NEUROLOGY 2009 72 Suppl 3 Abs IN4-1.006
55. 1004786 Topographic localization of calcitonin gene-related peptide in the rat brain: An immunohistochemical analysis. Kawai Y, Takami K, Shiosaka S, Emson PC, Hillyard CJ, Girgis S, MacIntyre I, Tohyama M NEUROSCIENCE 1985 15 3 747-763
56. 1004794 Localization of binding sites for calcitonin gene-related peptide in rat brain by in vitro autoradiography. Sexton PM, McKenzie JS, Mason RT, Moseley JM, Martin TJ, Mendelsohn FA NEUROSCIENCE 1986 19 4 1235-1245
57. 1004803 Regional and cellular localization of calcitonin gene-related peptide-receptor component protein mRNA in the guinea-pig central nervous system. Oliver KR, Wainwright A, Kinsey AM, Heavens RP, Sirinathsinghji DJ, Hill RG BRAIN RES MOL BRAIN RES 1999 66 1-2 205-210
58. 1004805 Localization and modulation of calcitonin gene-related peptide-receptor component protein-immunoreactive cells in the rat central and peripheral nervous systems. Ma W, Chabot JG, Powell KJ, Jhamandas K, Dickerson IM, Quirion R NEUROSCIENCE 2003 120 3677-694
59. 1004833 A pathophysiological view of primary headaches. Edvinsson L FUNCT NEUROL 2000 15 Suppl 3 50-60
60. 1004933 Ramping it up: RAMP1 and the implications for migraine. Russo AF PHARMACOGENOMICS 2007 8 7 687-690
61. 1009255 Hyperbaric oxygen treatment of active cluster headache: A double-blind placebo-controlled cross-over study. Nilsson Remahl AI, Ansjon R, Lind F, Waldenlind E CEPHALALGIA 2002 22 9 730-739
62. 1009264 Acute treatment of cluster headaches. Sandrini G, Ward TN THE HEADACHES (EDS: OLESEN J, GOADSBY PJ, RAMADAN NM, TFELT- HANSEN P, WELCH KMA) 2005 Lippincott Williams & Wilkins, Philadelphia, PA, USA 803-807
63. 1010888 Caprolactams as potent CGRP receptor antagonists for the treatment of migraine. Shaw AW, Paone DV, Nguyen DN, Stump CA, Burgey CS, Mosser SD, Salvatore CA, Rutledge RZ, Kane SA, Koblan KS, Graham SL et al BIOORG MED CHEM LETT 2007 17 17 4795-4798
64. 1014237 The pathophysiology of primary headache. Schreiber CP PRIMARY CARE 2004 31 2 261-276
65. 1014241 The triptans. Bigal ME, Krymchantowski AV, Hargreaves R EXPERT REV NEUROTHERAPEUTICS 2009 9 5 649-659
66. 1014246 Advances in pharmacological treatment of migraine. Diener HC, Limmroth V EXPERT OPIN INVEST DRUGS 2001 10 10 1831-1845
67. 1014262 Regulation of calcitonin gene-related peptide secretion by a serotonergic antimigraine drug. Durham PL, Russo AF J NEUROSCI 1999 19 9 3423-3429
68. 1014301 Calcitonin gene-related peptide (CGRP) and migraine. Durham PL HEADACHE 2006 46 Suppl 1 S3-S8
69. 1014308 Trigeminal autonomic cephalalgias: Current and future treatments. Cohen AS, Matharu MS, Goadsby PJ HEADACHE 2007 47 6 969-980