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.
Andra läkemedelsnamn slutar i ”-gepant”, såsom olcegepant, telcagepant, ubrogepant, atogepant och rimegepant. Dessa är CGRP-receptor
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. 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 inhibits the increases in DBF induced by the topical application of capsaicin on the human forearm.
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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. Merck is presenting new Telcagepant (MK-0974) is a calcitonin gene-related peptide receptor Telcagepant is an extremely potent CGRP antagonist with a Ki = 0.77 (0.07 nM).
Methods: This study evaluated the calcitonin gene-related peptide (CGRP) receptor antagonist telcagepant (tablet formulation) for treatment of a migraine attack and across four attacks. Adults with migraine were randomized, doubleblind, to telcagepant 140 mg, telcagepant 280 mg, or control treatment sequences to treat four moderate-to-severe migraine attacks.
The non-linear pharmacokinetics is probably a result of saturation or inhibition of first-pass metabolism. Telcagepant might provide hope for those who have a poor response to, or are unable to use, older drugs. In patients who need prophylaxis because of frequent attacks of migraine, topiramate is a first-line drug for migraine prevention in many countries; it is generally safe and reasonably well tolerated. Telcagepant har i tester visat inga, eller väldigt få biverkningar, enligt tillverkaren.
Telcagepant är ett preparat som blockerar den så kallade CGRP-receptorn, Calcitonin gene-related peptide, och som vid ett begynnande
CGRP-receptorantagonister, som olcegepant och telcagepant, har undersökts både in vitro och i kliniska studier som behandling av migrän. År 2011 stoppade Många biverkningar. CGRP-receptorantagonister på gång: telcagepant dock stoppat i fas III. Även 5-HT1F-agonister, TRPV1-antagonister, EP4-antagonister.
29 Jul 2011 The company made its decision about telcagepant--a calcitonin gene-related peptide receptor antagonist--known in its quarterly earnings release
26 Nov 2008 Results of a randomized trial show that telcagepant, also known as MK-0974, is effective in the treatment of migraine, with efficacy similar to
Telcagepant (INN) (code name MK-0974) is a calcitonin gene-related peptide receptor antagonist which was an investigational drug for the acute treatment and
Telcagepant is a new migraine drug being developed by Merck.
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Although CGRP receptor antagonists seem devoid of direct vasoconstrictor activity, animal research suggests a role for CGRP in nitroglycerin (NTG) induced vasodilation.
This synthesis features the first application of iminium organocatalysis on an industrial scale. The key to the success of this organocatalytic transformation was the identification of a dual acid cocatalyst system, which allowed striking a balance of the
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