Olcegepant: Difference between revisions

Latest revision as of 03:40, 13 February 2025

Olcegepant[edit]

Olcegepant is a calcitonin gene-related peptide receptor antagonist that has been investigated for its potential use in the treatment of migraine. It is a small molecule drug that was developed to block the action of the calcitonin gene-related peptide (CGRP), a neuropeptide that plays a significant role in the pathophysiology of migraine.

Mechanism of Action[edit]

Olcegepant works by selectively binding to the CGRP receptor, thereby inhibiting the binding of CGRP. This prevents the vasodilation and neurogenic inflammation associated with migraine attacks. By blocking CGRP, olcegepant aims to reduce the frequency and severity of migraine headaches.

Development and Clinical Trials[edit]

Olcegepant was one of the first CGRP receptor antagonists to be developed and tested in clinical trials. Early studies demonstrated its efficacy in reducing migraine symptoms when administered intravenously. However, the development of an oral formulation proved challenging, and as a result, olcegepant did not progress to market.

Pharmacokinetics[edit]

Olcegepant is administered intravenously, which limits its use to clinical settings. The drug has a rapid onset of action, which is beneficial for acute migraine treatment. However, its short half-life necessitates frequent dosing, which is a limitation for its practical use.

Comparison with Other CGRP Antagonists[edit]

While olcegepant was a pioneering drug in the class of CGRP antagonists, other drugs such as erenumab, fremanezumab, and galcanezumab have since been developed and approved for the prevention of migraine. These newer agents are typically administered subcutaneously and have longer half-lives, making them more suitable for regular use.

Related Pages[edit]

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-'''Olcegepant''' (also known as '''BIBN 4096''') is a [[peptide]] that is used in the treatment of [[migraine]]s. It is a [[calcitonin gene-related peptide receptor]] antagonist, which means it works by blocking the action of a protein in the body that causes blood vessels in the brain to dilate. This dilation is thought to be a major cause of the pain associated with migraines.
+== Olcegepant ==
-== History ==
+[[File:Olcegepant.svg|thumb|right|Chemical structure of Olcegepant]]
-Olcegepant was first developed by the pharmaceutical company [[Boehringer Ingelheim]]. It was the first [[CGRP receptor antagonist]] to be investigated for the treatment of migraines. Early clinical trials showed promise, but development was halted due to concerns about the drug's method of administration.
+'''Olcegepant''' is a [[calcitonin gene-related peptide receptor antagonist]] that has been investigated for its potential use in the treatment of [[migraine]]. It is a small molecule drug that was developed to block the action of the [[calcitonin gene-related peptide]] (CGRP), a neuropeptide that plays a significant role in the pathophysiology of migraine.
-== Mechanism of Action ==
+=== Mechanism of Action ===
+Olcegepant works by selectively binding to the CGRP receptor, thereby inhibiting the binding of CGRP. This prevents the vasodilation and neurogenic inflammation associated with migraine attacks. By blocking CGRP, olcegepant aims to reduce the frequency and severity of migraine headaches.
-Olcegepant works by blocking the [[CGRP receptor]], a protein found on the surface of cells in the brain. CGRP (calcitonin gene-related peptide) is a molecule that is released in the body in response to inflammation or stress. When CGRP binds to its receptor, it causes blood vessels in the brain to dilate. This dilation is thought to be a major cause of the pain associated with migraines. By blocking the CGRP receptor, Olcegepant prevents this dilation and reduces migraine pain.
+=== Development and Clinical Trials ===
+Olcegepant was one of the first CGRP receptor antagonists to be developed and tested in clinical trials. Early studies demonstrated its efficacy in reducing migraine symptoms when administered intravenously. However, the development of an oral formulation proved challenging, and as a result, olcegepant did not progress to market.
-== Clinical Trials ==
+=== Pharmacokinetics ===
+Olcegepant is administered intravenously, which limits its use to clinical settings. The drug has a rapid onset of action, which is beneficial for acute migraine treatment. However, its short half-life necessitates frequent dosing, which is a limitation for its practical use.
-In clinical trials, Olcegepant was found to be effective at reducing the severity of migraine pain. However, the drug had to be administered intravenously, which is less convenient than oral administration. This led to the development of other CGRP receptor antagonists that can be taken orally, such as [[Telcagepant]] and [[Ubrogepant]].
+=== Comparison with Other CGRP Antagonists ===
+While olcegepant was a pioneering drug in the class of CGRP antagonists, other drugs such as [[erenumab]], [[fremanezumab]], and [[galcanezumab]] have since been developed and approved for the prevention of migraine. These newer agents are typically administered subcutaneously and have longer half-lives, making them more suitable for regular use.
-== Future Development ==
+== Related Pages ==
+* [[Migraine]]
+* [[Calcitonin gene-related peptide]]
+* [[CGRP receptor antagonist]]
+* [[Erenumab]]
+* [[Fremanezumab]]
+* [[Galcanezumab]]
-While development of Olcegepant was halted, research into CGRP receptor antagonists continues. These drugs represent a new class of treatment for migraines, and have the potential to provide relief for patients who do not respond to other treatments. Future research will likely focus on developing CGRP receptor antagonists that can be administered orally or through other convenient methods.
+[[Category:Pharmacology]]
-[[Category:Peptides]]
 [[Category:Migraine]]
-[[Category:Drugs]]
+[[Category:Calcitonin gene-related peptide receptor antagonists]]
-{{medicine-stub}}