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Experimental obesity drug avoids brain effects that troubled predecessors
Date:7/12/2010

Stockholm, Sweden: A second-generation experimental anti-obesity and diabetes drug has shown promise in reducing body weight in rodents just as effectively as the predecessor rimonabant while avoiding the risk of psychiatric side effects that led to the withdrawal of rimonabant from the market and stopped further development of other brain-penetrating drugs of its type.

The first generation of anti-obesity drugs that targeted the cannabinoid receptor CB1 such as rimonabant - showed great promise as a therapy for obesity and related diseases such as diabetes. However, they were troubled by risk of psychiatric side effects. Rimonabant was withdrawn from the European market following a recommendation by the European Medicines Agency in late 2008, while further development of other similar products was halted.

However, in a study presented today (Monday) at the International Congress on Obesity in Stockholm, Sweden, Danish researchers demonstrated in rodents that a new first-in-class, second-generation CB1 receptor blocker induced the same degree of weight loss as rimonabant while not exposing the brain to significant levels of the drug. The drug was designed to act selectively in peripheral tissues and organs, in contrast with the first generation of CB1 receptor blockers, which also significantly affected the brain.

"These findings, together with what we have seen in our first human study regarding the safety and tolerability, make this drug candidate a promising therapy for obesity and diabetes. The lack of significant exposure in the brain seen in our preclinical experiments provides optimism that blockade of the CB1 receptor may still be an effective and safe approach to treat obesity and related diseases," said Christian E. Elling, Vice President at 7TM Pharma A/S in Hoersholm, Denmark, who presented the findings at the conference. "This is, to our knowledge, the first peripheral CB1 drug candidate being tested in humans and t
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Contact: Emma Ross
rosswrite@mac.com
International Association for the Study of Obesity
Source:Eurekalert

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