Ubrogepant: An Oral Calcitonin Gene-Related Peptide (CGRP) Receptor Antagonist for Abortive Migraine Treatment

2021 ◽  
pp. 106002802110238
Author(s):  
Madell Nedd ◽  
Scott Garland ◽  
Nathan Falk ◽  
Ashley Wilk
Keyword(s):  
Receptor Antagonist ◽  
Data Extraction ◽  
Calcitonin Gene Related Peptide ◽  
Migraine Treatment ◽  
Efficacy And Safety ◽  
Related Peptide ◽  
Study Selection ◽  
Calcitonin Gene ◽  
Bothersome Symptom ◽  
Cgrp Receptor Antagonist

Objective To review the pharmacology, efficacy, and safety of ubrogepant as an abortive migraine treatment. Data Sources A literature search of MEDLINE and PubMed was performed (January 2006 through May 2021) using the following search terms: ubrogepant, calcitonin gene related peptide, and abortive migraine therapy. Study Selection and Data Extraction Relevant studies evaluating ubrogepant’s pharmacology, efficacy, and safety in humans for the treatment of migraine were considered Data Synthesis Ubrogepant is a calcitonin gene-related peptide receptor antagonist approved by the Food and Drug Administration for the acute treatment of migraine via data from ACHIEVE I and II. From ACHIEVE I, ubrogepant demonstrated superiority to placebo in freedom from migraine pain at 2 hours postdose (50-mg dose: odds ratio [OR] = 1.83, 95% CI = 1.25-2.66; 100-mg dose: OR = 2.04, 95% CI = 1.41-2.95) and freedom from most bothersome symptom (MBS; 50-mg dose: OR = 1.70, 95% CI = 1.27-2.28; 100-mg dose: OR = 1.63, 95% CI = 1.22-2.17). ACHIEVE II trial demonstrated efficacy of ubrogepant 50 mg compared with placebo (2-hour pain freedom: OR = 1.62, 95% CI = 1.14-2.29; 2-hour MBS freedom: OR = 1.65, 95% CI = 1.25-2.20). Relevance to Patient Care and Clinical Practice Ubrogepant is a viable option for patients who are unable to tolerate nonsteroidal anti-inflammatory drug or triptan therapy because of ineffective relief or contraindications that limit use. Conclusions Ubrogepant is a well-tolerated effective abortive migraine treatment that bridges a gap in therapy for many patients who previously could not tolerate other first-line treatments.

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

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

2019 ◽  
Vol 44 (8) ◽  
pp. 635 ◽  
Author(s):  
L. Lionetto ◽  
M. Capi ◽  
M. Curto ◽  
F. Cipolla ◽  
M. Guglielmetti ◽  
...  
Keyword(s):  
Receptor Antagonist ◽  
Calcitonin Gene Related Peptide ◽  
Cgrp Receptor ◽  
Related Peptide ◽  
Calcitonin Gene ◽  
Cgrp Receptor Antagonist

Calcitonin gene related peptide as inhibitory neurotransmitter in the ureter

1995 ◽  
Vol 73 (7) ◽  
pp. 986-990 ◽  
Author(s):  
C. A. Maggi ◽  
S. Giuliani ◽  
S. Meini ◽  
P. Santicioli
Keyword(s):  
Guinea Pig ◽  
Receptor Antagonist ◽  
Calcitonin Gene Related Peptide ◽  
K Channel ◽  
Organ Bath ◽  
Cgrp Receptor ◽  
Membrane Hyperpolarization ◽  
Related Peptide ◽  
Calcitonin Gene ◽  
Cgrp Receptor Antagonist

A dense plexus of calcitonin gene related peptide (CGRP) containing nerve fibres is present in the mammalian ureter, from which CGRP is released by depolarizing stimuli, including chemicals normally present in the urine. CGRP exerts a profound, receptor-mediated, inhibitory effect on the evoked motility of the ureter by suppressing latent pacemakers in the smooth muscle. This effect is largely glibenclamide sensitive, indicating the activation of potassium (K) channels in its genesis. Electrical stimulation of intramural nerves in the guinea-pig ureter produces a transient membrane hyperpolarization, which is blocked by glibenclamide or by capsaicin pretreatment, enhanced in a low-K medium, and inhibited by a CGRP receptor antagonist. Thus endogenous CGRP acts as a neurotransmitter K channel opener in the ureter. The refractory period of the guinea-pig ureter is markedly and similarly reduced by capsaicin pretreatment or administration of a CGRP receptor antagonist, indicating that endogenous CGRP can modulate the maximal frequency of ureteral peristalsis. Using a three-chamber organ bath that enabled the separate perfusion of the renal, middle, and bladder regions of the organ, evidence was obtained that CGRP blocks propagation of impulses along the ureter through a glibenclamide-sensitive mechanism. These findings indicate a role of CGRP in the local regulation of ureteral motility and peristalsis.Key words: guinea-pig ureter, calcitonin gene related peptide, sensory nerves, glibenclamide-sensitive potassium channels.

Effect of the calcitonin gene-related peptide (CGRP) receptor antagonist telcagepant in human cranial arteries

Cephalalgia ◽  
2010 ◽  
Vol 30 (10) ◽  
pp. 1233-1240 ◽  
Author(s):  
Lars Edvinsson ◽  
Kayi Y Chan ◽  
Sajedeh Eftekhari ◽  
Elisabeth Nilsson ◽  
René de Vries ◽  
...  
Keyword(s):  
Receptor Antagonist ◽  
Calcitonin Gene Related Peptide ◽  
Sensory Nerves ◽  
Cgrp Receptor ◽  
Response Curves ◽  
Related Peptide ◽  
Calcitonin Gene ◽  
Meningeal Arteries ◽  
Cgrp Receptor Antagonist ◽  
Cranial Arteries

Introduction: Calcitonin gene-related peptide (CGRP) is a neuronal messenger in intracranial sensory nerves and is considered to play a significant role in migraine pathophysiology. Materials and methods: We investigated the effect of the CGRP receptor antagonist, telcagepant, on CGRP-induced cranial vasodilatation in human isolated cerebral and middle meningeal arteries. We also studied the expression of the CGRP receptor components in cranial arteries with immunocytochemistry. Concentration response curves to αCGRP were performed in human isolated cerebral and middle meningeal arteries in the absence or presence of telcagepant. Arterial slices were stained for RAMP1, CLR and actin in a double immunofluorescence staining. Results: In both arteries, we found that: (i) telcagepant was devoid of any contractile or relaxant effects per se; (ii) pretreatment with telcagepant antagonised the αCGRP-induced relaxation in a competitive manner; and (iii) immunohistochemistry revealed expression and co-localisation of CLR and RAMP1 in the smooth muscle cells in the media layer of both arteries. Conclusions: Our findings provide morphological and functional data on the presence of CGRP receptors in cerebral and meningeal arteries, which illustrates a possible site of action of telcagepant in the treatment of migraine.

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