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From Basic Science to Blockbuster Drug: The Discovery of Lyrica
Author(s) -
Silverman Richard B.
Publication year - 2008
Publication title -
angewandte chemie international edition
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 5.831
H-Index - 550
eISSN - 1521-3773
pISSN - 1433-7851
DOI - 10.1002/anie.200704280
Subject(s) - glutamate receptor , neurotransmitter , excitatory postsynaptic potential , glutamate decarboxylase , chemistry , inhibitory postsynaptic potential , neurotransmitter agents , pharmacology , drug , anticonvulsant , gamma aminobutyric acid , glutamic acid , neuroscience , biochemistry , biology , epilepsy , amino acid , receptor , enzyme
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.
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