MK-0974 (Telcagepant) is a potent and selective antagonist of the human and rhesus CGRP receptors.

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2019-12-07 What does telcagepant mean? (medicine) A particular drug under investigation in the treatment of migraine. (noun) Telcagepant is a new migraine drug being developed by Merck. This drug is potentially very exciting for migraine patients because it works by a totally new mechanism. Telcagepant works by blocking the dilation of blood vessels surrounding the brain during a migraine. Telcagepant does this by blocking calcitonin gene-related peptide.

Telcagepant

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Methods: In this randomized, double-blind, placebo-controlled, multicenter trial ([ClinicalTrials.gov][1] [NCT00797667][2]), patients experiencing 3–14 migraine days during a 4-week baseline were randomized to telcagepant 140 mg, telcagepant Telcagepant is an oral calcitonin gene‐related peptide receptor antagonist with acute antimigraine efficacy comparable to oral triptans. It is currently unknown whether migraine patients who cannot be adequately helped with triptans might benefit from treatment with telcagepant. Methods.— Characterization of the CGRP receptor antagonist telcagepant in human isolated coronary artery of different caliber Chan, K. Y.; Edvinsson, Lars LU; Telcagepant (Synonyms: MK-0974) Telcagepant (MK-0974) is an orally active calcitonin gene-related peptide (CGRP) receptor antagonist with Kis of 0.77 nM  22 Apr 2010 Telcagepant represents a new class of antimigraine drug—the calcitonin gene- related peptide receptor blockers. This compound exerts its  25 Jan 2017 Telcagepant, MK-0974 Molecular FormulaC26H27F5N6O3 Average mass566. 523 Da 1-piperidinecarboxamide, N-[(3R,6S)-6-(2  Introduction. Merck & Co was developing telcagepant, an orally delivered antagonist of the calcitonin gene related peptide (CGRP) receptor, for the treatment of  30 May 2017 Telcagepant (10-6 M) inhibited both vasorelaxation and drop in intracellular calcium levels. Both functional components of the CGRP receptor,  11 Sep 2009 However things are looking much more promising for its other CGRP receptor antagonist telcagepant, or MK-0974.

TELCAGEPANT MK 0974 pubchem.compound:11319053 chemidplus:781649-09-0 drugbank:12228 chembl:CHEMBL236593 Drug Info: ChemblDrugs ChemblInteractions TTD DrugBank (0 Telcagepant 140 mg was administered once daily at bedtime for 7 consecutive days each month, beginning at the onset of menses, for up to 6 months.

Telcagepant (MK0974) (Fig. 1) is one of several CGRP antagonists in development as a potential treatment for acute migraine attacks and is the first orally available drug in this class. Mechanism of Action, Metabolism and Pharmacokinetic Profile Mechanism of action Telcagepant antagonises CGRP-induced relaxation,

It is an antagonist of the receptor for calcitonin gene-related peptide (CGRP), a primary neuropeptide involved in the pathophysiology of migraine. Definition of telcagepant in the Definitions.net dictionary. Meaning of telcagepant.

Telcagepant (MK-0974) is an orally administered antagonist of the calcitonin gene related peptide (CGRP) receptor. CGRP is a neuropeptide that is believed to 

Telcagepant Accession Number DB12228 Description. Telcagepant has been investigated for the treatment of Migraine. It is an antagonist of the receptor for calcitonin gene-related peptide (CGRP), a primary neuropeptide involved in the pathophysiology of migraine.

Merck & Co was developing telcagepant, an orally delivered antagonist of the calcitonin gene related peptide (CGRP) receptor, for the treatment of pain. The telcagepant was generally well-tolerated for the acute treatment of migraine. Most clinical adverse events occurred within 48 h of dosing. Both doses of telcagepant 150 mg and 300 mg were associated with fewer clinical adverse events than zolmitriptan, suggesting that telcagepant might offer tolerability advantages over current triptan treatments. Telcagepant is rapidly absorbed and plasma concentrations decrease biphasic way, with a terminal half-life of about 6 h. Telcagepant has non-linear pharmacokinetics after oral doses with greater than dose-proportional increases in AUC 0–∞.
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128 Development was terminated when elevated levels of the liver enzyme alanine transaminase were found in treated patients. Identification Name Telcagepant Accession Number DB12228 Description.

Telcagepant did not reduce monthly headache frequency, but did reduce perimenstrual headaches. BACKGROUND: Telcagepant is an oral calcitonin gene-related peptide receptor antagonist which is being evaluated for the acute treatment of migraine. Combining telcagepant with analgesics that have a different mechanism of action could produce greater efficacy. METHODS: Randomized, double-blind, placebo-controlled study.
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TELCAGEPANT D42O649ALL Investigational Source: NCT00442936: Phase 3 Migraine (2007

Telcagepant (MK0974) is one of several calcitonin-gene-related peptide antagonists in development as a potential treatment for acute migraine attacks and is the first orally available drug in this Telcagepant (INN) (tên mã MK-0974) là một chất đối kháng thụ thể peptide liên quan đến gen calcitonin, một loại thuốc điều trị trong điều trị cấp tính và phòng ngừa chứng đau nửa đầu, được phát triển bởi Merck & Co.. Telcagepant 140 mg taken perimenstrually for seven days was generally well tolerated, but was associated with transaminase elevations. Telcagepant did not reduce monthly headache frequency, but did reduce perimenstrual headaches. BACKGROUND: Telcagepant is an oral calcitonin gene-related peptide receptor antagonist which is being evaluated for the acute treatment of migraine. Combining telcagepant with analgesics that have a different mechanism of action could produce greater efficacy. METHODS: Randomized, double-blind, placebo-controlled study. telcagepant was generally well-tolerated for the acute treatment of migraine.