Telcagepant
File:Telcagepant structure.svg | |
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 | |
Clinical data | |
Routes of administration | Oral |
Legal status | |
Legal status |
|
Pharmacokinetic data | |
Biological half-life | 5-8 hours |
Identifiers | |
CAS Number | 781649-09-0 |
ATC code | none |
PubChem | CID 11319053 |
IUPHAR/BPS | 703 |
Chemical data | |
Formula | C26H27F5N6O3 |
Molar mass | 566.5283[[Script error: No such module "String".]] |
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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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- ↑ Lua error in package.lua at line 80: module 'Module:Citation/CS1/Suggestions' not found.
- ↑ Lua error in package.lua at line 80: module 'Module:Citation/CS1/Suggestions' not found.
- ↑ Molecule of the Month February 2009
- ↑ ClinicalTrials.gov NCT00797667 MK0974 for Migraine Prophylaxis in Patients With Episodic Migraine
- ↑ Merck & Co.: Memo to all US study locations involved in protocol MK0974-049
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