Telcagepant: Difference between revisions

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'''Telcagepant''' is a drug that was under development for the acute treatment of [[migraine]]s. It belongs to the class of drugs known as [[calcitonin gene-related peptide receptor]] (CGRP receptor) antagonists. Telcagepant was being developed by [[Merck & Co.]], but its development was discontinued in 2011 due to concerns about its potential to cause liver damage.
== Telcagepant ==


== History ==
[[File:Telcagepant_structure.svg|thumb|right|Structure of Telcagepant]]


Telcagepant was first synthesized by Merck & Co. in the early 2000s as part of their research into CGRP receptor antagonists. Early clinical trials showed promise, with the drug demonstrating efficacy in the treatment of acute migraines. However, in 2011, Merck announced that they were discontinuing the development of Telcagepant due to concerns about its potential to cause liver damage.
'''Telcagepant''' is a drug that was investigated for the treatment of [[migraine]]s. It belongs to a class of medications known as [[calcitonin gene-related peptide receptor antagonists]] (CGRP antagonists). Unlike traditional migraine treatments, which often involve [[triptans]] or [[nonsteroidal anti-inflammatory drugs]] (NSAIDs), telcagepant works by blocking the action of CGRP, a neuropeptide involved in the pathophysiology of migraines.


== Mechanism of Action ==
== Mechanism of Action ==


Telcagepant works by blocking the CGRP receptor. CGRP is a neuropeptide that plays a key role in the pathophysiology of migraines. By blocking this receptor, Telcagepant prevents the vasodilation and inflammation that are associated with migraines.
Telcagepant functions by selectively antagonizing the [[calcitonin gene-related peptide receptor]], which is implicated in the transmission of pain and the dilation of blood vessels in the brain during a migraine attack. By inhibiting this receptor, telcagepant aims to prevent the cascade of events that lead to migraine symptoms.
 
== Development and Clinical Trials ==
 
[[File:Telcagepant-3D-balls.png|thumb|left|3D ball model of Telcagepant]]


== Clinical Trials ==
Telcagepant was developed by [[Merck & Co.]] and underwent several phases of clinical trials. Initial studies showed promise, as telcagepant was effective in reducing migraine pain without the cardiovascular side effects associated with triptans. However, during later stages of development, concerns arose regarding liver toxicity, which ultimately led to the discontinuation of its development.


Several clinical trials were conducted to assess the efficacy and safety of Telcagepant. These trials showed that the drug was effective in treating acute migraines, with a similar efficacy to [[triptans]], the standard treatment for migraines. However, some patients in the trials experienced elevated liver enzymes, a potential sign of liver damage. This led to the discontinuation of the drug's development.
== Safety and Efficacy ==


== Potential Side Effects ==
In clinical trials, telcagepant demonstrated efficacy in relieving migraine symptoms, including headache pain, nausea, and sensitivity to light and sound. However, the emergence of liver enzyme elevations in some patients raised safety concerns. These adverse effects were significant enough to halt further development, as the risk-benefit profile was deemed unfavorable compared to existing treatments.


The most common side effects observed in clinical trials of Telcagepant were nausea, dizziness, and dry mouth. However, the potential for liver damage was the most significant concern, leading to the discontinuation of the drug's development.
== Comparison with Other Treatments ==


== See Also ==
Telcagepant was part of a new wave of migraine treatments targeting the CGRP pathway. Unlike triptans, which are [[serotonin receptor agonists]], telcagepant does not cause vasoconstriction, making it a potentially safer option for patients with cardiovascular risk factors. Despite its potential, the safety concerns prevented it from reaching the market.
 
== Future of CGRP Antagonists ==
 
The development of telcagepant paved the way for other CGRP antagonists, some of which have successfully reached the market. These newer agents, such as [[erenumab]], [[fremanezumab]], and [[galcanezumab]], have been approved for the prevention of migraines and have shown favorable safety profiles.
 
== Related Pages ==


* [[Calcitonin gene-related peptide receptor]]
* [[Migraine]]
* [[Migraine]]
* [[Triptans]]
* [[Calcitonin gene-related peptide]]
* [[CGRP receptor antagonist]]
* [[Triptan]]


[[Category:Drugs]]
[[Category:Migraine treatments]]
[[Category:Migraine]]
[[Category:Calcitonin gene-related peptide receptor antagonists]]
[[Category:Merck & Co.]]
{{Pharma-stub}}
<gallery>
File:Telcagepant_structure.svg|Structure of Telcagepant
File:Telcagepant-3D-balls.png|3D ball model of Telcagepant
</gallery>
== Telcagepant ==
<gallery>
File:Telcagepant_structure.svg|Chemical structure of Telcagepant
File:Telcagepant-3D-balls.png|3D ball model of Telcagepant
</gallery>

Latest revision as of 11:03, 23 March 2025

Telcagepant[edit]

Structure of Telcagepant

Telcagepant is a drug that was investigated for the treatment of migraines. It belongs to a class of medications known as calcitonin gene-related peptide receptor antagonists (CGRP antagonists). Unlike traditional migraine treatments, which often involve triptans or nonsteroidal anti-inflammatory drugs (NSAIDs), telcagepant works by blocking the action of CGRP, a neuropeptide involved in the pathophysiology of migraines.

Mechanism of Action[edit]

Telcagepant functions by selectively antagonizing the calcitonin gene-related peptide receptor, which is implicated in the transmission of pain and the dilation of blood vessels in the brain during a migraine attack. By inhibiting this receptor, telcagepant aims to prevent the cascade of events that lead to migraine symptoms.

Development and Clinical Trials[edit]

3D ball model of Telcagepant

Telcagepant was developed by Merck & Co. and underwent several phases of clinical trials. Initial studies showed promise, as telcagepant was effective in reducing migraine pain without the cardiovascular side effects associated with triptans. However, during later stages of development, concerns arose regarding liver toxicity, which ultimately led to the discontinuation of its development.

Safety and Efficacy[edit]

In clinical trials, telcagepant demonstrated efficacy in relieving migraine symptoms, including headache pain, nausea, and sensitivity to light and sound. However, the emergence of liver enzyme elevations in some patients raised safety concerns. These adverse effects were significant enough to halt further development, as the risk-benefit profile was deemed unfavorable compared to existing treatments.

Comparison with Other Treatments[edit]

Telcagepant was part of a new wave of migraine treatments targeting the CGRP pathway. Unlike triptans, which are serotonin receptor agonists, telcagepant does not cause vasoconstriction, making it a potentially safer option for patients with cardiovascular risk factors. Despite its potential, the safety concerns prevented it from reaching the market.

Future of CGRP Antagonists[edit]

The development of telcagepant paved the way for other CGRP antagonists, some of which have successfully reached the market. These newer agents, such as erenumab, fremanezumab, and galcanezumab, have been approved for the prevention of migraines and have shown favorable safety profiles.

Related Pages[edit]