Novel drug, known under the brand name Lyrica and produced by Pfizer, has recently been approved for the management of neuropathic pain associated with diabetic peripheral neuropathy, postherpetic neuralgia and adjunctive treatment of partial seizures in adults with epilepsy. It is currently available in about 25 countries and 25 more countries have approved it and should be selling it by summer this year. Lyrica shows also high efficacy in the treatment of generalized anxiety disorder, fibromyalgia, as well as in sleep quality disorder. The story of a novel medication started in the late 1980s, when the author of this presentation came to Northwestern University in Evanston, near Chicago, to begin his post doctoral studies in R. Silverman laboratory in the Department of Chemistry. The project started with the synthesis of a series of substituted γ-amino butyric acid (GABA) derivatives and L-glutamic acid analogues which, then, were tested as GABA g-aminotransferase inhibitors. Moreover, these compounds, showed, unexpectedly, in vitro activation of brain L-glutamic acid decarboxylase (GAD) and anticonvulsant activity in mice. One of the selected compounds, i.e. (S)-3-isobutyl-4-aminobutyric acid exerted exceptionally high anticonvulsant activity and has been selected for clinical trials in Parke-Davis, then, in Pfizer and became known as pregabalin.

After intensive clinical trials, Pfizer in 2004 received approval from the European Medicines Agency (EMEA) to market Lyrica in all European Union member states, then in 2005 received the similar approval from the US Food and Drug Administration (FDA) to sell Lyrica in the US. This drug has a newly definied mechanism of action. In this short presentation some aspects of the discovery of the active compound will be presented.

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