Levetiracetam is a multiple action drug that primarily acts through an interaction with the synaptic vesicle protein 2A. Levetiracetam is the first drug of its kind to be approved for the treatment of epilepsy and is now the most prescribed among the newer antiepileptic drugs. The discovery process identifying levetiracetam's antiepileptic potential was unique because it challenged several dogmas of antiepileptic drug discovery, and thereby encountered skepticism from the epilepsy community. This was contrasted by a very successful development programme leading to rapid regulatory approval by the FDA. The history of levetiracetam proves that a small core group of committed scientists and physicians, who dare to challenge the conventional scientific doctrine, can be successful in bringing to market a truly novel therapy for epilepsy patients.