2018 年 35 巻 3 号 p. 313-318
Migraine is a common and debilitating neurological disorder. With the advent of triptans, migraine therapy has much improved. Nevertheless, alternative therapy is required to treat those who are intractable to triptans or who have a cardiovascular complication(s). Calcitonin gene–related peptide (CGRP) is abundantly expressed in trigeminal ganglion neurons. Blood CGRP concentrations are increased in some migraine patients, and intravenous administration with CGRP has been shown to induce delayed migraine–like headache attacks almost exclusively in migraineurs. Hence, attempts have been made to develop CGRP–targeted migraine therapy. Initially, an injectable small–molecule CGRP receptor antagonist termed BIBN 4096 BS (Olcegepant) was found to abort migraine attacks. Subsequently, oral CGRP receptor antagonists demonstrated significant efficacy for migraine attacks. However, some of them have been abandoned because of hepatotoxicity. Recently, monoclonal antibodies against CGRP or its receptor have been shown to be effective in migraine prophylaxis with minimal side effects. Moreover, it has been made clear that such antibody therapy is able to ameliorate chronic migraine, which is extremely disabling and generally drug–resistant. In this article, recent advance in CGRP–based migraine therapy and its perspective are discussed.