Telcagepant, a calcitonin gene-related peptide antagonist for the treatment of migraine.
Telcagepant is an oral calcitonin-gene related peptide (CGRP) receptor antagonist that is being developed by Merck & Co Inc for the treatment of migraine. This compound blocks CGRP receptors and may block the dilation of dural vessels and reduce neurotransmission in the CNS, resulting in pain relief. Telcagepant does not cause vasoconstriction, one of the major limitations in the use of triptans, which are considered to be the standard of care for migraine. Data from phase II and III clinical trials suggest that the use of telcagepant for the acute treatment of migraine was comparable with the use of triptan compounds and was superior to placebo in all primary endpoints, including pain relief and freedom from pain at 2 h. However, recent data reported elevated transaminase levels when telcagepant was dosed daily rather than acutely. It was concluded that, if these hepatic toxicities are not observed in ongoing/future trials of the acute use of telcagepant, then this agent may offer an alternative to triptan therapy for the treatment of migraine.
Tepper
Stewart J
SJ
Cleveland Clinic, Center for Headache and Pain, Department of Neurology, Neurological Institute, 9500 Euclid Avenue, Cleveland, OH 44195, USA. sjtepper@aol.com
Cleves
Catalina
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D018712:Analgesics, Non-Narcotic / Q000627:therapeutic use*; D001381:Azepines / Q000009:adverse effects / Q000493:pharmacokinetics / Q000627:therapeutic use*; D000077221:Calcitonin Gene-Related Peptide Receptor Antagonists; D002986:Clinical Trials as Topic; D015507:Drugs, Investigational / Q000627:therapeutic use*; D006801:Humans; D007093:Imidazoles / Q000009:adverse effects / Q000493:pharmacokinetics / Q000627:therapeutic use*; D008881:Migraine Disorders / Q000188:drug therapy*; D015394:Molecular Structure; D010330:Patents as Topic; D013329:Structure-Activity Relationship
D018712:Analgesics, Non-Narcotic; D001381:Azepines; D000077221:Calcitonin Gene-Related Peptide Receptor Antagonists; D015507:Drugs, Investigational; D007093:Imidazoles; C525458:telcagepant