RESUMO
<b>Objective: </b>We analyzed the characteristics of ligands of G-protein coupled receptor (GPCR) of new drugs approved, and the time dependent changes of these new drug approvals over three decades from 1980 to 2009 in Japan.<br><b>Methods: </b>The receptor therapeutic targets of 185 new drugs were distributed 20 receptor families of GPCR. Most of new drugs which targeted GPCR were the ligands of class A receptors. Among the class A receptors, the receptors of amine family, such as adrenaline, dopamine, histamine, serotonin and muscarinic receptor were the targets of new drugs. One hundred and ten of 185 new drugs were the antagonist and other 75 were the agonist of GPCR. Whether the new drug is agonist or antagonist depended on the receptor subtype. The time dependent changes of new drug approval were different among the drugs depending on which GPCR was targeted. Approval of new drugs which targeted some GPCR decreased time dependently. In contrast, approval of new drugs which targeted other GPCR increased time dependently or continuously retained.<br><b>Results: </b>The results obtained in this study indicated characteristics of targeted GPCR, and time dependent changes of new drugs approvals, and suggest the future aspect of new drugs.