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Telcagepant
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Telcagepant

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Telcagepant
Telcagepant structure.svg
Telcagepant-3D-balls.png
Clinical data
Routes of
administration
Oral
ATC code
  • none
Legal status
Legal status
  • Development terminated
Pharmacokinetic data
Elimination half-life 5–8 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
ChemSpider
UNII
KEGG
ChEMBL
CompTox Dashboard (EPA)
Chemical and physical data
Formula C26H27F5N6O3
Molar mass 566.533 g·mol−1
3D model (JSmol)
  • C1C[C@H](C(=O)N(C[C@@H]1C2=C(C(=CC=C2)F)F)CC(F)(F)F)NC(=O)N3CCC(CC3)N4C5=C(NC4=O)N=CC=C5
  • InChI=1S/C26H27F5N6O3/c27-18-4-1-3-17(21(18)28)15-6-7-19(23(38)36(13-15)14-26(29,30)31)33-24(39)35-11-8-16(9-12-35)37-20-5-2-10-32-22(20)34-25(37)40/h1-5,10,15-16,19H,6-9,11-14H2,(H,33,39)(H,32,34,40)/t15-,19-/m1/s1 checkY
  • Key:CGDZXLJGHVKVIE-DNVCBOLYSA-N checkY
 ☒NcheckY (what is this?)  (verify)

Telcagepant (INN) (code name MK-0974) is a calcitonin gene-related peptide receptor antagonist which was 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 and zolmitriptan.

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". A memo to study locations stated that telcagepant had preliminarily been reported to increase the hepatic liver enzyme alanine transaminase (ALT) levels in "11 out of 660 randomized (double-blinded) study participants." All study participants were told to stop taking the medication.

In July 2011, Merck announced that it had discontinued development of telcagepant.

See also


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