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Further Information
In early 2008, dosing began in a randomised, double-blind, placebo controlled Phase I study to assess the safety, tolerability and pharmacokinetic profile of single rising doses of oral BGC20-1531 in healthy volunteers.

Migraine headache is estimated to affect 10-20% of the world population and is listed by the World Health Organisation in the top 20 causes of disabling conditions, and in the top four neurological disabling conditions. The most common current therapies for acute migraine are non-steroidal anti-inflammatory drugs (NSAIDs) and triptans. However, many migraine sufferers do not experience sufficient relief from these treatments or cannot tolerate their gastrointestinal, cardiovascular and other side-effects.

Prostaglandin PGE2-induced sensory nerve sensitisation, neuropeptide release and cerebral vascular dilatation is thought to underlie migraine pain, particularly via activation of the EP4 receptor subtype. BGC20-1531 is an EP4 receptor antagonist that has been shown to competitively antagonise PGE2-induced vasodilatation of human middle cerebral and meningeal arteries in vitro, supporting its potential use as a treatment for migraine and other pain conditions. Furthermore, since EP4 receptors are discretely localised, the overall safety profile of EP4 receptor antagonists may be improved compared to triptans and NSAIDs.