From Basic Science to Blockbuster Drug: The Discovery of Lyrica

The anticonvulsant drug (S)-(+)-3-isobutyl-γ-aminobutyric acid ((S)-(+)-3-isobutyl-GABA, Lyrica; see structure) was developed from a study of fundamental science, which took an unexpected course. The activity of Lyrica was found to be unrelated to the originally anticipated activation of L-glutamic acid decarboxylase and the increase in the inhibitory neurotransmitter GABA; instead, it antagonizes a calcium ion channel, which inhibits the release of the excitatory neurotransmitter L-glutamate. The ultimate effect, however, is the same.