Drug General Information
Drug ID
D0G5ME
Former ID
DCL000245
Drug Name
Telcagepant
Synonyms
MK 0974; MK0974; N7R; MK-0974; Telcagepant (USAN); N-(6-(2,3-difluorophenyl)-2-oxo-1-(2,2,2-trifluoroethyl)azepan-3-yl)-4-(2-oxo-2,3-dihydro-1H-imidazo(4,5-b)pyridin-1-yl)piperidine-1-carboxamide
Drug Type
Small molecular drug
Indication Migraine; Cluster headaches [ICD9: 339.00, 339.01, 339.02, 346; ICD10:G43, G44.0] Phase 2 [531970], [542049]
Company
Merck
Structure
Download
2D MOL

3D MOL

Formula
C26H27F5N6O3
InChI
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
InChIKey
CGDZXLJGHVKVIE-DNVCBOLYSA-N
CAS Number
CAS 781649-09-0
PubChem Compound ID
PubChem Substance ID
Target and Pathway
Target(s) Calcitoningene-related peptide type 1 receptor Target Info Antagonist [537202], [537267], [537377]
KEGG Pathway Neuroactive ligand-receptor interaction
Vascular smooth muscle contraction
Reactome G alpha (s) signalling events
Calcitonin-like ligand receptors
WikiPathways GPCRs, Class B Secretin-like
Endothelin Pathways
GPCR ligand binding
GPCR downstream signaling
References
Ref 531970ACS chemical neuroscience molecule spotlight on Telcagepant (MK-0974). ACS Chem Neurosci. 2011 Jul 20;2(7):334-5.
Ref 542049(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 703).
Ref 537202A flexible and high throughput liquid chromatography-tandem mass spectrometric assay for the quantitation of telcagepant in human plasma. J Chromatogr B Analyt Technol Biomed Life Sci. 2009 May 15;877(14-15):1465-71. Epub 2009 Mar 18.
Ref 537267Elimination of diastereomer interference to determine Telcagepant (MK-0974) in human plasma using on-line turbulent-flow technology and off-line solid-phase extraction coupled with liquid chromatography/tandem mass spectrometry. J Chromatogr B Analyt Technol Biomed Life Sci. 2009 Jun 1;877(16-17):1634-42. Epub 2009 Apr 8.
Ref 537377CGRP antagonists: novel concept for treatment of migraine. Med Monatsschr Pharm. 2009 May;32(5):182-5.

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