Calcitonin Gene-Related Peptide Receptor Antagonists

Pharmacologic agents that block NOCICEPTIVE PAIN signaling from CALCITONIN GENE-RELATED PEPTIDE RECEPTORS. They may be useful for the treatment of pain associated with MIGRAINE DISORDERS and OSTEOARTHRITIS.

Also Known As:

CGRP Receptor Antagonists; GEPANTS; Antagonist, CGRP Receptor; Antagonists, CGRP Receptor; CGRP R Inhibitor; CGRP R Inhibitors; Calcitonin Gene Related Peptide Receptor Antagonist; Calcitonin Gene Related Peptide Receptor Antagonists; Inhibitor, CGRP-R; Inhibitors, CGRP-R; Receptor Antagonist, CGRP; Receptor Antagonists, CGRP; CGRP Receptor Antagonist; CGRP-R Inhibitor; CGRP-R Inhibitors; Calcitonin Gene-Related Peptide Receptor Antagonist; GEPANT

Networked: 470 relevant articles (76 outcomes, 82 trials/studies)

Relationship Network

Bio-Agent Context: Research Results

Chemical Actions and Uses
- Pharmacologic Actions: 160

Experts

1.	Goadsby, Peter J: 38 articles (03/2022 - 03/2004)
2.	Edvinsson, Lars: 24 articles (10/2022 - 01/2002)
3.	Olesen, Jes: 16 articles (01/2021 - 03/2004)
4.	Dodick, David W: 15 articles (04/2022 - 02/2011)
5.	Lipton, Richard B: 15 articles (04/2022 - 04/2011)
6.	Salvatore, Christopher A: 14 articles (11/2015 - 10/2006)
7.	Russo, Andrew F: 12 articles (12/2021 - 01/2006)
8.	Conway, Charles M: 11 articles (01/2021 - 04/2012)
9.	Burgey, Christopher S: 11 articles (01/2020 - 10/2006)
10.	Ho, Tony W: 11 articles (02/2016 - 01/2010)

Related Diseases

1.	Migraine Disorders (Migraine) 04/01/2005 - "Recent evidence that a CGRP receptor antagonist was effective in the treatment of migraine attack supports the hypothesis that neurogenic vasodilatation is a major underlying mechanism of migraine." 12/01/2016 - "First tested were CGRP receptor antagonists; they proved effective in acute migraine treatment in several trials, but were discontinued due to liver toxicity in long-term administration. " 01/01/2022 - "CGRP receptor antagonists are effective for acute migraine treatment and are expected to be used clinically as emerging therapeutic agents." 01/01/2020 - "Gepants were effective for abortive treatment of migraine. " 01/01/2017 - "However, a peripheral site of action is indicated by the ability of intravenous CGRP to trigger migraine in humans and the efficacy of CGRP receptor antagonists that evidently do no penetrate the CNS in effective amounts. "
2.	Pain (Aches) 01/01/2022 - "Our work suggests that CGRP receptor antagonists could be tested for efficacy in women for a broader variety of pain conditions." 11/01/2015 - "Increased mechanosensitivity in OA knees and pain behaviour can be reduced by peripherally acting CGRP receptor antagonists. " 09/01/2022 - "Randomized placebo-controlled trials demonstrated gepants efficacy in treating acute attacks to obtain 2 h pain freedom in about 20% of patients and pain relief in about 60%, while up to 60% of treated patients with episodic migraine may experience a 50% reduction in monthly migraine days. " 08/01/2014 - "CGRP receptor antagonists recently developed for migraine pain should be investigated for their efficacy against pain in OA." 07/01/2012 - "CGRP receptor antagonists reduce migraine pain in clinical trials and spinal trigeminal activity in animal experiments. "
3.	Headache (Headaches) 09/01/2023 - "This review will illustrate how gepants will continue to revolutionize the acute and preventive treatment of headaches. " 03/30/2023 - "It is tempting to speculate what the effect would be if patients were instructed to take a gepant as needed (PRN) or even prior to headache onset. " 12/01/2012 - "Moreover, administration of CGRP receptor antagonists aborts the headache. " 07/01/2010 - "CGRP receptor antagonists will provide an additional and valuable therapeutic option for the treatment of headaches." 08/01/2004 - "The purpose of this review is to describe the role of CGRP in the intracranial circulation and to elucidate a possible role for a specific CGRP receptor antagonist in the treatment of primary headaches. "
4.	Nausea 01/01/2020 - "Random-effects meta-analysis was conducted to estimate the overall efficacy of gepants for nausea treatment. " 01/01/2020 - "An overall combined effect size with an odds ratio of 1.29 (95% CI 1.18, 1.40, P = .001; I2 = 42.8%) showed the efficacy of gepants for the treatment of nausea in episodic migraine. " 01/01/2020 - "Cumulative meta-analysis indicated that the effect size remained stable for studies conducted after 2011, with accumulating evidence continuing to favor efficacy of gepants for the treatment of nausea in episodic migraine. " 01/01/2020 - "There is sufficient evidence to support the efficacy of gepants for the treatment of nausea in episodic migraine. " 01/01/2022 - "A pooled analysis demonstrated that CGRP receptor antagonists significantly increased freedom from pain (odds ratio [OR] = 2.066, 95% confidence interval [CI] 1.766-2.418, I2 = 0%) and from bothersome symptoms in general (OR = 1.606, 95% CI = 1.408-1.830, I2 = 0%); reduced the intensity of pain (OR = 1.791, 95% CI = 1.598-2.008, I2 = 0%); and increased freedom from nausea (OR = 1.361, 95% CI = 1.196-1.548, I2 = 0%) compared to a placebo. "
5.	Cluster Headache (Cluster Headaches) 01/01/2020 - "The role of CGRP in cluster headache supports ongoing trials of the remaining CGRP pathway monoclonal antibodies and gepants for preventive and acute treatment. " 01/01/2011 - "CGRP and VIP have been found at increased concentrations in jugular venous plasma during attacks of migraine or cluster headache, and CGRP receptor antagonists have recently been shown to be effective in migraine therapy. " 08/01/2004 - "The data suggest that there are non-presynaptic CGRP receptors in the trigeminocervical complex that can be inhibited by CGRP receptor blockade and that a CGRP receptor antagonist would be effective in the acute treatment of migraine and cluster headache." 01/01/2021 - "Importantly, the work summarizes and discusses the role of genetic polymorphisms regarding their impact on metabolism safety and the effect of therapeutics that are used to treat migraine, cluster headache, and TTH exploring drug classes such as nonsteroidal anti-inflammatory drugs, triptans, antidepressants, anticonvulsants, calcium channel blockers, drugs with effect on the renin-angiotensin system, and novel headache therapeutics such as ditans, anti-calcitonin-gene-related peptide antibodies, and gepants. "

Related Drugs and Biologics

1.	Calcitonin Gene-Related Peptide Receptor Antagonists
2.	Calcitonin Gene-Related Peptide
3.	olcegepant
4.	Monoclonal Antibodies
5.	telcagepant
6.	rimegepant sulfate
7.	Calcitonin Gene-Related Peptide Receptors (Calcitonin-Gene Related Peptide Receptor)
8.	ubrogepant
9.	Tryptamines (Triptans)
10.	erenumab

Related Therapies and Procedures

1.	Therapeutics
2.	Contraindications
3.	Ligation
4.	Intravenous Injections
5.	Denervation