Telcagepant: Difference between revisions

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| ATC_supplemental =
| ATC_supplemental =
| PubChem = 11319053
| PubChem = 11319053
| KEGG = D09391
| IUPHAR_ligand = 703
| IUPHAR_ligand = 703
| chemical_formula =
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Revision as of 04:55, 20 January 2011

Telcagepant
Clinical data
Routes of
administration		Oral
ATC code
  • none
Legal status
Legal status
  • Experimental
Pharmacokinetic data
Elimination half-life5-8 hours
Identifiers
  • 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
CAS Number
PubChem CID
IUPHAR/BPS
KEGG
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC26H27F5N6O3
Molar mass566.5283 g·mol−1
3D model (JSmol)
  • Fc1c(F)cccc1C(CN(C3=O)CC(F)(F)F)CCC3NC(=O)N5CCC(CC5)n2c4cccnc4nc2=O

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

  1. ^ Ho, TW (2008). "Randomized controlled trial of an oral CGRP receptor antagonist, MK-0974, in acute treatment of migraine". Neurology. 70 (16): 1304. doi:10.1212/01.WNL.0000286940.29755.61. PMID 17914062. {{cite journal}}: More than one of |author= and |last= specified (help); Unknown parameter |month= ignored (help)
  2. ^ Ho TW, Ferrari MD, Dodick DW; et al. (2008). "Efficacy and tolerability of MK-0974 (telcagepant), a new oral antagonist of calcitonin gene-related peptide receptor, compared with zolmitriptan for acute migraine: a randomised, placebo-controlled, parallel-treatment trial". Lancet. 372 (9656): 2115–23. doi:10.1016/S0140-6736(08)61626-8. PMID 19036425. {{cite journal}}: Explicit use of et al. in: |author= (help); Unknown parameter |month= ignored (help)CS1 maint: multiple names: authors list (link)
  3. ^ Molecule of the Month February 2009
  4. ^ Clinical trial number NCT00797667 for "MK0974 for Migraine Prophylaxis in Patients With Episodic Migraine" at ClinicalTrials.gov
  5. ^ Merck & Co.: Memo to all US study locations involved in protocol MK0974-049


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