calcitonin gene-related peptide receptor antagonist Archives

22 September 2010

Telcagepant to be Sublingual

On Monday the announcement came from Global Health Ventures, Inc., that they would be developing a sublingual version of migraine drug telcagepant.

Telcagepant, a calcitonin gene-related peptide receptor antagonist, has had a rocky beginning. Hailed in 2008 as the beginning of a new era in migraine treatment, the trials faltered over concerns about preventative use. Researchers were concerned when some patients developed high levels of liver enzymes (transaminases).

The drug’s developer, Merck, was cautious about the continued development of the drug, even as an abortive. Then, earlier this year, they announced that they would continue safety trials.

This past Monday, Global Health Ventures in Vancouver Canada, expressed their confidence in the future of telcagepant by announcing their commitment to developing a sublingual version. A special type of sublingual technology is one of the specialties of the company.

Global Health Ventures Inc. (the “Company”), a Specialty Pharma with focus on sublingual drug delivery, is pleased to announce that, it has initiated the development of a sublingual formulation of Telcagepant. Telcagepant is believed to be a powerful anti-migraine drug developed by Merck & Company. The drug blocks the recently discovered clacitonin-gene related hormone receptor (CGRP), a powerful vasodilator protein believed to be a key player in migraine.
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13 October 2009

New Migraine Drug Telcagepant – Not Dead Yet

James Discoveries & Stats, Medications, News 4

The pharmaceutical company Merck & Co., Inc was at the 14th International Headache Congress in September, talking again about the migraine drug Telcagepant. And hopes that Telcagepant will see the light of day aren’t dead yet.

After concerns about using Telcagepant as a migraine preventative, Merck has moved ahead with trials using the new drug as an abortive. Researchers were originally concerned when some patients developed high levels of liver enzymes (transaminases). (more on the background of Telcagepant here)

In one of the new trials, none of the patients had high levels of liver enzymes apparently caused by the drug (you caught that, right? Some did have the problem, but investigators felt it was not drug related.).

Two trials were reported on. First, compared with rizatriptan (Maxalt, Rizaliv, Rizalt), how many "adverse events" would patients experience?

Investigators didn’t look for any side effect here, they only measured events from a predetermined list. The adverse events were not too serious with either group, and there tended to be fewer with Telcagepant.

The problems more common with Telcagepant included nasopharyngitis, upper abdominal pain, and nausea and vomiting. In the other study, patients on telcagepant were more likely to feel sleepy (than those on a placebo). In an earlier study, Telcagepant was less likely to cause nausea than zolmitriptan, so we’ll see how it continues to compare with the triptans on this one.

But did Telcagepant fight symptoms of migraine? Yes, the results still look positive. In a large trial of 1,677 patients, researchers used doses of 140mg or 280mg and measured symptoms after 2 hours. They were interested in pain freedom or pain relief (reduction to mild or none). These charts show the percentage of patients helped at either dose, compared to a placebo:

Merck is preparing to have some major discussions regarding Telcagepant later this year with regulatory agencies. It remains to be seen if this drug will be the next big one for Merck and migraine, though it’s still showing promise.

The bad news is that Merck has shelved MK-3207, it’s other possible oral calcitonin gene-related peptide (CGRP) receptor antagonist for migraine treatment. So research on this type of drug continues to be stop and go for Merck.

However, Dr. David Michelson, vice president of clinical neurosciences, said Merck is still committed to this type of research: "Merck believes that the blocking of CGRP receptors remains an exciting pathway to address the underlying pathophysiology of migraine. We are continuing our efforts to offer patients a new treatment approach."

via: Merck Updates Status of Clinical Development Programs for Investigational CGRP Receptor Antagonist Treatments for Acute Migraine; MK-3207 Clinical Development Discontinued