Migraine represents a recent growth area due to the development of improved treatment strategies such as the 5HT1D receptor agonist Imigran (sumatriptan), and the increased awareness and changing attitudes to the condition that this advance has brought about. Indeed, migraine is now known to affect 4-16% of the global population, representing a 60% increase over the past decade. Consequently, the antimigraine market sector has increased by five-fold to a current global value in excess of $2 billion since the mid-1990’s. Resurgent interest in migraine has led to fresh research into its pathophysiology, as well as the development of treatments with fewer side effects. The triptans such as sumatriptan are acute therapies of migraine aborting an attack once it has started rather than preventing it. According to current guidelines 15% of sufferers would benefit from prophylactic treatment however the availability of molecules that effectively prevent migraine attacks with an acceptable tolerability profile is extremely limited. The development of migraine prophylactics therefore represents an unmet clinical need with considerable commercial potential. As a result, new therapeutic classes such as 5-HT7 receptor antagonists are starting to emerge as candidates for the treatment of migraine (click here for access to our recent analysis of this area).

Here we focus on recent research investigating the therapeutic potential of a second candidate target for migraine prophylaxis, the histamine H3 receptor. In a recent study, Millan-Guerrero and colleagues evaluated the safety and efficacy the histaminergic H3 agonist, Nalpha-methylhistamine in migraineurs. In the first part of their study this group determined undesirable symptomatic effects of Nalpha-methylhistamine in healthy human volunteers and failed to identify adverse effects at doses of under 10ng. In the second part of this study Nalpha-methylhistamine, at doses of 1 to 3 ng was found to significantly reduce the frequency, intensity, and duration of migraine attacks, as well as the need for rescue analgesics in 18 patients with migraine. However, at doses greater than 3 ng, patients experienced intense headache. Hence at carefully controlled doses H3 receptor agonist may offer an approach to migraine prophylaxis.

Entry date Wednesday, April 23, 2003

Adapted from Millan-Guerrero et al, Headache 2003 Apr;43(4):389-94 - Interested in collaborating with this group? Contact LeadDiscovery or the authors direct.

Interested in collaborating with this group? Contact leaddiscovery@bioportfolio.co.uk