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Telcagepant
Systematic (IUPAC) name
N-[(3R,6S)-6-(2,3-Difluorophenyl)hexahydro-2-oxo-1-(2,2,2-trifluoroethyl)-1H-azepin-3-yl]-4-(2,3-dihydro-2-oxo-1H-imidazo[4,5-b]pyridin-1-yl)-1-piperidinecarboxamide
Identifiers
CAS number 781649-09-0
ATC code none
PubChem 11319053
Chemical data
Formula C26H27F5N6O3 
Mol. mass 566.5283
SMILES eMolecules & PubChem
Pharmacokinetic data
Half life 5-8 hours
Therapeutic considerations
Pregnancy cat.  ?
Legal status Experimental
Routes Oral

Telcagepant (formerly MK-0974) is an investigational drug for the acute treatment and prevention of migraine, developed by Merck & Co. In the acute treatment of migraine, it was found to have equal potency to rizatriptan[1] and zolmitriptan[2] in two Phase III clinical trials.

Mechanism of action

The calcitonin gene-related peptide (CGRP) is a strong vasodilator primarily found in nervous tissue. Since vasodilation in the brain is thought to be involved in the development of migraine and CGRP levels are increased during migraine attacks, this peptide may be an important target for potential new antimigraine drugs.

Telcagepant acts as a calcitonin gene-related peptide receptor (CRLR) antagonist and blocks this peptide. It is believed to constrict dilated blood vessels within the brain.[3]

Termination of a clinical trial

A Phase IIa clinical trial studying telcagepant for the prophylaxis of episodic migraine was stopped on March 26, 2009 after the "identification of two patients with significant elevations in serum transaminases"[4]. A memo to study locations stated that telcagepant had preliminarily been reported to increase the hepatic liver enzyme alanine transaminase (AST) levels in "11 out of 660 randomized (double-blinded) study participants." All study participants were told to stop taking the medication.[5]

References

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