scholarly journals A CGRP receptor antagonist peptide formulated for nasal administration to treat migraine

2020 ◽  
Author(s):  
Bengt Mentzer ◽  
Andrew F. Russo ◽  
Zhongming Zhang ◽  
Adisa Kuburas ◽  
Patrick M. Killoran ◽  
...  
Keyword(s):  
Receptor Antagonist ◽  
Nasal Administration ◽  
Cgrp Receptor ◽  
Cgrp Receptor Antagonist

scholarly journals A Short on Ubrogepant

2021 ◽  
pp. 79-81
Author(s):  
S. Padmaja ◽  
J. Mohan
Keyword(s):  
Receptor Antagonist ◽  
Research Process ◽  
Calcitonin Gene Related Peptide ◽  
Review Article ◽  
Acute Migraine ◽  
Cgrp Receptor ◽  
Related Peptide ◽  
Calcitonin Gene ◽  
Acute Attacks ◽  
Cgrp Receptor Antagonist

Migraine is a mysterious disorder characterized by pulsating head ache, which is actually characterized to one side and comes in attacks which will be lasting for about 3-48 hours and can be associated with nausea,vomiting,sensitivity to sound,flashes of light,vertigoand diarrhoea [1]. Most of the drugs which are in current use for actue migraine like triptans, treats the disorder symptomatically. A novel group of drugs has been in research for the migraine which treats the disorder pathologically. Calcitonin gene – related peptide (CGRP) has a major role in the pathophysiology of the disorder and hence CGRP receptor antagonist, known as Gepants are in the research process [2]. Gepants are being studied for the efficacy of treating acute migraine [2]. This article will be a review article about the drug – Ubrogepant, which is approved for treatment of migraine with acute attacks in adults [3].

Zavegepant. Calcitonin gene-related peptide (CGRP) receptor antagonist, Treatment of migraine

2021 ◽  
Vol 46 (4) ◽  
pp. 281
Author(s):  
F. Cipolla ◽  
M. Capi ◽  
L. Lionetto ◽  
D. De Bernardini ◽  
V. De Angelis ◽  
...  
Keyword(s):  
Receptor Antagonist ◽  
Calcitonin Gene Related Peptide ◽  
Cgrp Receptor ◽  
Related Peptide ◽  
Calcitonin Gene ◽  
Cgrp Receptor Antagonist

scholarly journals Discovery of BMS-846372, a Potent and Orally Active Human CGRP Receptor Antagonist for the Treatment of Migraine

2012 ◽  
Vol 3 (4) ◽  
pp. 337-341 ◽  
Author(s):  
Guanglin Luo ◽  
Ling Chen ◽  
Charles M. Conway ◽  
Rex Denton ◽  
Deborah Keavy ◽  
...  
Keyword(s):  
Receptor Antagonist ◽  
Cgrp Receptor ◽  
Cgrp Receptor Antagonist ◽  
Orally Active

Randomized controlled trial of the CGRP receptor antagonist telcagepant for prevention of headache in women with perimenstrual migraine

Cephalalgia ◽  
2015 ◽  
Vol 36 (2) ◽  
pp. 148-161 ◽  
Author(s):  
Tony W Ho ◽  
Andrew P Ho ◽  
Yang (Joy) Ge ◽  
Christopher Assaid ◽  
Regina Gottwald ◽  
...  
Keyword(s):  
Adverse Event ◽  
Adverse Events ◽  
Receptor Antagonist ◽  
Alanine Aminotransferase ◽  
Controlled Trial ◽  
Cgrp Receptor ◽  
Double Blind ◽  
Treatment Difference ◽  
Clinical Adverse Event ◽  
Cgrp Receptor Antagonist

Aim The aim of this article is to evaluate the safety and efficacy of perimenstrual telcagepant, a CGRP receptor antagonist, for headache prophylaxis. Methods We conducted a randomized, double-blind, placebo-controlled, six-month trial in women with migraine for ≥3 months who experienced perimenstrual headaches. Women were randomized to telcagepant 140 mg or placebo (2:1 ratio) for seven consecutive days perimenstrually. Safety was assessed by adverse events and laboratory tests. The primary efficacy endpoint was mean monthly headache days in the subset of women reporting perimenstrual migraine (−2 days to +3 days of menses onset) and ≥5 moderate or severe migraines per month prior to entering the trial. Results Telcagepant was generally well tolerated: 66/2660 (2.5%) on telcagepant and 36/1326 (2.7%) on placebo discontinued because of a clinical adverse event. The percentages of patients with clinical adverse events, laboratory adverse events, or discontinuation because of a laboratory adverse event were also similar between treatments. Alanine aminotransferase elevations ≥3× normal occurred in 0.6% of women on telcagepant and 0.4% on placebo. Three women on telcagepant vs none on placebo had alanine aminotransferase elevations ≥8× normal. In the efficacy subset there was no significant effect of telcagepant ( n = 887) vs placebo ( n = 447) in mean monthly headache days (treatment difference −0.5 day (95% CI: −1.1, 0.1)). However, telcagepant was associated with a reduction in on-drug headache days (treatment difference −0.4 day (95% CI: –0.5, –0.2), nominal p < 0.001). Conclusions 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.

Serendipitous oxidation product of BIBN4096BS: A potent CGRP receptor antagonist

2014 ◽  
Vol 24 (12) ◽  
pp. 2744-2748 ◽  
Author(s):  
Bireshwar Dasgupta ◽  
Edward Kozlowski ◽  
Daniel R. Schroeder ◽  
John R. Torrente ◽  
Cen Xu ◽  
...  
Keyword(s):  
Receptor Antagonist ◽  
Oxidation Product ◽  
Cgrp Receptor ◽  
Cgrp Receptor Antagonist

scholarly journals Inhibition of capsaicin-induced increase in dermal blood flow by the oral CGRP receptor antagonist, telcagepant (MK-0974)

2010 ◽  
Vol 69 (1) ◽  
pp. 15-22 ◽  
Author(s):  
Simon R. Sinclair ◽  
Stefanie A. Kane ◽  
Bart J. Van der Schueren ◽  
Alan Xiao ◽  
Kenneth J. Willson ◽  
...  
Keyword(s):  
Blood Flow ◽  
Receptor Antagonist ◽  
Cgrp Receptor ◽  
Cgrp Receptor Antagonist ◽  
Dermal Blood Flow

Randomized controlled trial of the CGRP receptor antagonist telcagepant for migraine prevention

Neurology ◽  
2014 ◽  
Vol 83 (11) ◽  
pp. 958-966 ◽  
Author(s):  
T. W. Ho ◽  
K. M. Connor ◽  
Y. Zhang ◽  
E. Pearlman ◽  
J. Koppenhaver ◽  
...  
Keyword(s):  
Randomized Controlled Trial ◽  
Receptor Antagonist ◽  
Controlled Trial ◽  
Migraine Prevention ◽  
Cgrp Receptor ◽  
Randomized Controlled ◽  
Cgrp Receptor Antagonist

scholarly journals CGRP receptor antagonist activity of olcegepant depends on the signalling pathway measured

Cephalalgia ◽  
2017 ◽  
Vol 38 (3) ◽  
pp. 437-451 ◽  
Author(s):  
Christopher S Walker ◽  
Ann C Raddant ◽  
Michael J Woolley ◽  
Andrew F Russo ◽  
Debbie L Hay
Keyword(s):  
Receptor Antagonist ◽  
Signalling Pathway ◽  
Cgrp Receptor ◽  
Trigeminovascular System ◽  
Antagonist Activity ◽  
Creb Phosphorylation ◽  
Signalling Molecules ◽  
Calcitonin Gene ◽  
Cgrp Receptor Antagonists ◽  
Cgrp Receptor Antagonist

Background Calcitonin gene-related peptide (CGRP) is a neuropeptide that acts in the trigeminovascular system and is believed to play an important role in migraine. CGRP activates two receptors that are both present in the trigeminovascular system; the CGRP receptor and the amylin 1 (AMY1) receptor. CGRP receptor antagonists, including olcegepant (BIBN4096BS) and telcagepant (MK-0974), can treat migraine. This study aimed to determine the effectiveness of these antagonists at blocking CGRP receptor signalling in trigeminal ganglia (TG) neurons and transfected CGRP and AMY1 receptors in Cos7 cells, to better understand their mechanism of action. Methods CGRP stimulation of four intracellular signalling molecules relevant to pain (cAMP, CREB, p38 and ERK) were examined in rat TG neurons and compared to transfected CGRP and AMY1 receptors in Cos7 cells. Results In TG neurons, olcegepant displayed signal-specific differences in antagonism of CGRP responses. This effect was also evident in transfected Cos7 cells, where olcegepant blocked CREB phosphorylation more potently than expected at the AMY1 receptor, suggesting that the affinity of this antagonist can be dependent on the signalling pathway activated. Conclusions CGRP receptor antagonist activity appears to be assay-dependent. Thus, these molecules may not be as selective for the CGRP receptor as commonly reported.

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