Migraine is a common illness affecting 4-16% of the global population. The migraine market has traditionally been a low growth, low value market, dominated by sales of aspirin/paracetamol and drugs in the ergotamine class, and suffering from poor awareness of the condition among patients and physicians. The market was revolutionized in the 1990s with the launch of Glaxo Wellcome's 5HT receptor agonist Imigran (sumatriptan), which was approved in the USA in 1992. The market sector has since increased by five fold to a current global value in excess of $2 billion. The activity in the market created by the triptans has drawn attention to migraine as a condition that can be treated with prescription drugs, and has also stimulated fresh research into the causes and mechanisms of migraine, as well as the development of treatments with fewer side effects. This research has demonstrated that 5-HT is able to produce vasodilatation of intra- and extra-cranial blood vessels through the serotonin 5-HT7 receptor, and that the mRNA encoding for this receptor is highly expressed in cranial vessels. Other lines of evidence have suggested that the 5-HT7 receptor may play an excitatory role in neuronal systems and that it may be involved in hyperalgesic pain and neurogenic inflammation. On the basis of these observations, 5-HT7 receptors have been proposed to link abnormal 5-HT processing and neurotransmission, and the vascular and neurogenic alterations that account for migraine headache. This view is supported by the fact that most of the migraine prophylactic 5-HT receptor antagonists display relatively high affinity for the 5-HT7 receptor, which significantly correlates with their pharmaceutically active oral doses. Thus the 5-HT7 receptors represents an excellent target for the treatment of migraine. Despite this evidence few 5-HT7 receptor antagonists are currently in development for migraine and this target thus represents offers untapped opportunities.

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