Bob P's (New Med) Post.

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Posted by drummer ( on April 09, 2000 at 09:51:07:

Here's the article, that I believe Bob P was typing about, in his post down the message board a bit (from Reauters Medical News/Medscape):

Experimental Compounds for Migraine Designed to Avoid Cardiovascular Risks

SAN FRANCISCO, CA Apr 04 (Reuters Health) - Selective serotonin agonists for the treatment of migraine should be more potent with fewer side effects than currently available drugs, according to a presentation here at the national meeting of the American Chemical Society.

Sumatriptan and similar triptans currently indicated for migraine are non-selective agonists for 5-HT1D/1B serotonin receptors. Being potent vasoconstrictors, these drugs can cause transient chest heaviness or even pain, and are contraindicated in those with a history of ischemic heart disease, myocardial infarction or angina.

The adverse cardiovascular effect of triptans is believed to be mediated by the 5-HT1B receptor, not the 5-HT1D receptor that is involved in migraine. A drug with high affinity for the 5-HT1D, coupled with low affinity for 5-HT1B, would allow physicians to push dose in order to enhance efficacy and eliminate or significantly reduce rebound headache, according to Dr. A. Malik Slassi, of Allelix Biopharmaceuticals Inc., Mississauga, Ontario, Canada.

The firm has four or five potent and selective 5-HT1B/5-HT1D 5-thienyltryptamine derivatives under development. In a guinea pig model of migraine, these new triptans showed efficacy about 17-fold greater than sumatriptan, with about 16-fold less tendency to cause vasoconstriction, Dr. Slassi said.

Dr. Slassi also told Reuters Health that Allelix has a second generation of migraine compounds, which are not triptans, under development. "In vivo profiling shows that these are much better than triptans in general," he said, citing their higher degree of receptor selectivity. "If we had a non-triptan with efficacy and safety in animal models, it would fly."

The principal impediment to further development of either the triptan or the non-triptan series is not scientific, according to Dr. Slassi. "We are a small biotech company, we can't do everything by ourselves," he said. The company's ALX-0646 migraine drug, the selective triptan that is furthest along, has completed phase IA trials and the company is actively seeking collaborators to continue its development.

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