Olcegepant

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Olcegepant (also known as BIBN 4096) is a peptide that is used in the treatment of migraines. 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.

History[edit | edit source]

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.

Mechanism of Action[edit | edit source]

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.

Clinical Trials[edit | edit source]

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.

Future Development[edit | edit source]

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.

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Contributors: Prab R. Tumpati, MD