CNS Drugs

, Volume 15, Issue 12, pp 969–976 | Cite as

Frovatriptan

Adis New Drug Profile

Abstract

  • ▴ Frovatriptan, a new serotonin receptor agonist developed for the acute treatment of migraine, has high affinity for serotonin 5-HT1B and 5-HT1D receptor subtypes and is a potent stimulator of contraction in human basilar arteries.

  • ▴ Along terminal elimination half-life (≈26 hours) is a distinctive pharmacokinetic feature of frovatriptan which appears to be independent of dose, age, gender and renal function.

  • ▴ A single oral dose of frovatriptan 2.5mg was effective in the acute treatment of migraine providing meaningful relief within 2 hours to approximately twice as many recipients as placebo in clinical trials.

  • ▴ Consistent relief of migraine symptoms was achieved in patients who treated a number of consecutive attacks with frovatriptan and the incidence of 24-hour migraine recurrence was reduced.

  • ▴ Frovatriptan was well tolerated in clinical trials, with the overall incidence of adverse events occurring with frovatriptan 2.5mg only slightly higher than that reported with placebo. Mild to moderate fatigue, nausea and paraesthesia were the most commonly reported drug-related adverse events

References

  1. 1.
    Lipton RB, Stewart WF. The epidemiology of migraine. Eur Neurol 1994; 34 Suppl. 2: 6–11PubMedCrossRefGoogle Scholar
  2. 2.
    Diener H-C, Kaube H, Limmroth V. A practical guide to the management and prevention of migraine. Drugs 1998 Nov; 56(5): 811–24PubMedCrossRefGoogle Scholar
  3. 3.
    Goadsby PJ, Olesen J. Diagnosis and management of migraine. BMJ 1996 May 18; 312: 1279–83PubMedCrossRefGoogle Scholar
  4. 4.
    Longmore J, Shaw D, Smith D, et al. Differential distribution of 5HT1d- and 5HT1B-immunoreactivity within the human trigemino-cerebrovascular system: implications for the discovery of new antimigraine drugs. Cephalalgia 1997; 17: 833–42PubMedCrossRefGoogle Scholar
  5. 5.
    Brown AM, Parsons AA, Raval P, et al. SB 209509 (VML 251), a potent constrictor of rabbit basilar artery with high affinity and selectivity for human 5-HT1d receptors [abstract]. Br J Pharmacol 1996 Oct; 119 Proc Suppl.: 11OPGoogle Scholar
  6. 6.
    Brown AM, Ho M, Thomas DR, et al. Comparison of functional effects of frovatriptan* (VML 251), sumatriptan, and naratriptan on human recombinant 5-HT1 and 5-HT7 receptors [abstract]. Headache 1998 May; 38: 376Google Scholar
  7. 7.
    Eglen RM, Jasper JR, Chang DJ, et al. The 5-HT7 receptor: orphan found. TiPS 1997 Apr; 18: 104–7PubMedGoogle Scholar
  8. 8.
    Parsons AA, Raval P, Smith S, et al. Effects of the novel high-affinity 5-HT1B/1D-receptor ligand frovatriptan in human isolated basilar and coronary arteries. J Cardiovasc Pharmacol 1998 Aug; 32: 220–4PubMedCrossRefGoogle Scholar
  9. 9.
    Parsons AA, Parker SG, Raval P, et al. Comparison of the cardiovascular effects of the novel 5-HT1B/1Dreceptor agonist, SB 209509 (VML251), and sumatriptan in dogs. J Cardiovasc Pharmacol 1997 Jul; 30: 136–41PubMedCrossRefGoogle Scholar
  10. 10.
    Keywood C. The effects of ascending doses of oral frovatriptan* (VML 251 /SB 209509), a potent selective 5HT1b/1d agonist, for the acute treatment of migraine on the cardiovascular system of healthy male volunteers [abstract]. Headache 1998 May; 38(5): 388Google Scholar
  11. 11.
    Elkind A, McDaris HL, Satin L, et al. Cardiovascular safety of frovatriptan in patients at high risk of or with known coronary artery disease during a migraine attack [abstract]. Cephalalgia 1999 May; 19: 365Google Scholar
  12. 12.
    Buchan P, Keywood C, Ward C. The pharmacokinetics of frovatriptan (VML 251/SB 209509), a potent, selective 5-HT1B/1D agonist, following a single dose administration by oral and intravenous routes to healthy male and female volunteers [poster]. 40th Annual Scientific Meeting of the American Association for the Study of Headache; 1998 Jun 26–28; San Francisco.Google Scholar
  13. 13.
    Buchan P. The pharmacokinetics of frovatriptan* (VML 251/ SB 209509), a potent selective 5-HT1b/1dagonist, following single dose administration by oral and intravenous routes to healthy male and female volunteers [abstract]. Headache 1998 May; 38(5): 376Google Scholar
  14. 14.
    Buchan P. Can blood cell binding explain the long half-life of frovatriptan? [abstract P2076]. Eur J Neurol 2000; 7 Suppl. 3:86Google Scholar
  15. 15.
    Buchan P, Ward C, Zeig S. Frovatriptan pharmacokinetics are unaffected during a migraine attack [abstract P433]. Eur J Neurol 1999; 6 Suppl. 3: 137Google Scholar
  16. 16.
    Buchan P, Keywood C, Ward C. Pharmacokinetics of frovatriptan (VML 251/SB 209509) in healthy young and elderly male and female subjects [poster]. 3rd Congress of the European Federation of Neurological Societies; 1998 Sep 18–25; Seville.Google Scholar
  17. 17.
    Buchan P. In. vitro. metabolism of frovatriptan [abstract P2057]. Eur J Neurol 2000; 7 Suppl. 3: 81Google Scholar
  18. 18.
    Buchan P. Effects of alcohol, smoking and oral contraceptives on the pharmacokinetics of frovatriptan [abstract P2077]. Eur J Neurol 2000; 7 Suppl. 3: 86Google Scholar
  19. 19.
    Cohen AF, van der Post J, Sacks S, et al. Pharmacokinetics of frovatriptan in patients with renal impairment [abstract]. Cephalalgia 1999 May; 19: 365Google Scholar
  20. 20.
    Cohen AF, van der Post J, Sacks S, et al. Pharmacokinetics of frovatriptan in patients with renal impairment [poster]. 9th Congress of the International Headache Society; 1999 Jun 22-26; Barcelona.Google Scholar
  21. 21.
    Buchan P, Ward C, Oliver SD. Lack of clinically significant interactions between frovatriptan and ergotamine [abstract]. Cephalalgia 1999 May; 19: 364Google Scholar
  22. 22.
    Wade A, Buchan P, Mant T, et al. Frovatriptan has no clinically significant interaction with fluvoxamine [abstract]. Cephalalgia 2001; 21: 427Google Scholar
  23. 23.
    Buchan P, Ward C, Stewart AJ. Propranolol has minimal effects on the pharmacokinetics and safety of frovatriptan [abstract]. Cephalalgia 1999 May; 19: 364–5Google Scholar
  24. 24.
    Buchan P, Ward C, Stewart AJ. The effect of propanolol on the pharmacokinetic and safety profiles of frovatriptan [poster]. 9th Congress of the International Headache Society; 1999 Jun 22–26; Barcelona.Google Scholar
  25. 25.
    Buchan P, Ward C, Freestone S. Lack of interaction between frovatriptan and monoamine oxidase inhibitor [abstract]. Cephalalgia 1999 May; 19: 364Google Scholar
  26. 26.
    Buchan P, Ward C, Freestone S. Lack of interaction between frovatriptan and the monoamine oxidase inhibitor, moclo-bemide [poster]. 9th Congress of the International Headache Society; 1999 Jun 22–26; Barcelona.Google Scholar
  27. 27.
    Ryan R, Keywood C. A preliminary study of frovatriptan (VML251), a potent cerebroselective 5-hydroxytryptamine (5-HT)1b/1d agonist for the acute treatment of migraine [abstract MTH1]. Eur J Neurol 1998 Sep; 5 Suppl. 3: S46Google Scholar
  28. 28.
    Goldstein J, Elkind A, Keywood C, et al. A low-dose rangefinding study of frovatriptan, a potent selective 5HT1D agonist for the acute treatment of migraine [abstract]. Cephalalgia 1998 Jul–Aug; 18: 410Google Scholar
  29. 29.
    Ryan R, Keywood C. Frovatriptan: review of efficacy in acute treatment of migraine [abstract]. Headache 2000 May; 40: 429Google Scholar
  30. 30.
    Spierings ELH, Keywood C, on behalf of the VML 251/96/08 Investigators. Consistent migraine relief with frovatriptan, a novel 5HT1B/1Dagonist [abstract]. Cephalalgia 1999 May; 19: 367Google Scholar
  31. 31.
    Headache Classification Committee of the International Headache Society. Classification and diagnostic criteria for headache disorders, cranial neuralgias, and facial pain. Cephalalgia 1988; 8 Suppl. 7: 1–96Google Scholar
  32. 32.
    International Headache Society Committee on Clinical Trials in Migraine. Guidelines for controlled trials of drugs in migraine, 1st ed. Cephalalgia 1991 Feb; 11: 1–12CrossRefGoogle Scholar
  33. 33.
    Goldstein J, Keywood C, Hutchison J. Low 24-hour migraine recurrence during treatment with frovatriptan [abstract]. Cephalalgia 1999 May; 19: 365–6Google Scholar
  34. 34.
    Ryan R, Keywood C. Apreliminary study of frovatriptan (VML 251), a cerebroselective 5-HT1B/1Dagonist for the acute treatment of migraine [poster]. 3rd Congress of the European Federation of Neurological Societies; 1998 Sep 18–25; Seville.Google Scholar
  35. 35.
    Goldstein J, Keywood C. A study of the efficacy and safety of low doses of frovatriptan (VML 251), apotent, cerebroselective 5-HT1B/1Dagonist, in the acute treatment of migraine [poster]. 3rd Congress of the European Federation of Neurological Societies; 1998 Sep 18–25; Seville.Google Scholar
  36. 36.
    McDaris HL, Hutchison J on behalf of the frovatriptan PIII investigators. Frovatriptan — a review of overall clinical efficacy [poster]. 9th Congress of the International Headache Society; 1999 Jun 22–26; Barcelona.Google Scholar
  37. 37.
    Spierings ELH, KeywoodC, VML 251/96/08 Investigators. Frovatriptan, a novel 5-HTIB/ID agonist, provides consistent relief of migraine [abstract P437]. Eur J Neurol 1999 Sep; 6 Suppl. 3: 139Google Scholar
  38. 38.
    Geraud G. Migraine headache recurrence: relationship to clinical, pharmacological and pharmacokinetic properties of triptans [abstract]. Cephalalgia 2001; 21: 406Google Scholar
  39. 39.
    MacGregor EA, Keywood C. Frovatriptan is effective in men-strually associated migraine [poster]. Headache World 2000; 2000 Sep 3–7; London.Google Scholar
  40. 40.
    Spierings ELH, Hutchison J. Frovatriptan — a review of safety and tolerability [poster]. 9th Congress of the International Headache Society; 1999 Jun 22–26; Seville.Google Scholar
  41. 41.
    Geraud G, Keywood C. Tolerability of frovatriptan during short-and long-term use for migraine and comparison with sumatriptan [poster]. Headache World 2000; 2000 Sep 3–7; LondonGoogle Scholar
  42. 42.
    Elan Corporation plc. Press release: FDA approves Elan’s migraine drug Frova™ (frovatriptan succinate). 9 Nov 2001. Available from URL: http://www.elancorp.com/news/display. asp?id=195 [Accessed 2001 Nov 13]
  43. 43.
    Vernalis Group plc. Press release: French regulatory approval advised for Migard™ (frovatriptan). 21 July 2000. Available from URL: http://www.vanguardmedica.com/r_d_portfolio/index.htm [Accessed 2001 Sep 14]

Copyright information

© Adis International Limited 2001

Authors and Affiliations

  1. 1.Adis International LimitedMairangi Bay, Auckland 10New Zealand

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