Journal: Lancet
Team: Unspecified. "Lars Edvinsson (Lund University Hospital, Sweden) and Mattias Linde (St Olavs Hospital, Trondheim, Norway) "?
Telcagepant (formerly MK-0974, developed by Merck (U.S.)) acts on CGRP (Calcitonin gene-related peptide) . CGRP is a neuropeptide such as substance P, endorphins, neuropeptide Y (NPY). Neuropeptides generally act on GPCRs coupled receptors (G-protein) and have a medium-term modulatory action on neurons.
studies suggesting that a migraine attack is associated with release of CGRP from meningeal nociceptors in the trigeminal ganglion, the idea an antagonist of CGRP receptors directly came to the researcher, and Telcagepant is one. The effectiveness of this compound appears to be similar to triptans (which are currently used treatment of crisis, and act at serotonin receptors). Gold triptans, which in addition to being relatively expensive (Zomig: 30 € 6CP box), are formally cons-indicated in case a history of heart attack or angina pectoris, of history of stroke or peripheral, certain cardiac arrhythmias, or uncontrolled hypertension, as strongly vasoconstrictors, not to mention interactions with dihydroergotamine. And Telcagepant escapes these cons-indications and interactions, because there is no vasoconstrictor.
In contrast, phase II trials were halted in March 2009 because of liver toxicity apparently too strong, with high elevation of transaminases. It is on this toxicity is that the assessments currently being conducted by Merck. Moreover, the telcagepant induced side effects: nausea, dizziness, numbness or tingling skin.
Migraine affects 15% of the adult population in France.
Zolmitriptan (antimigraine major) is a global turnover of $ 158M in 2008.
Illustration: Pharmacorama
http://www.lesechos.fr/depeches/medecine-sante/afp_00246576.htm
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