Navigation Links
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 Rimonabant was withdrawn from the European market following a recommendation by the European Medicines Agency in late 2008, while further development of other similar products was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 these results indicate its development as a potential new treatment should be advanced."

In the rodent studies, the researchers conducted an extensive panel of studies with mice and rats to assess the weight-loss and anti-diabetic potential of the as-yet unnamed drug, TM38837, and to demonstrate the lack of exposure in the brain.

The researchers treated obese rats and mice with rimonabant, the new drug, or a placebo drug once a day for five weeks and measured their body weight and food intake daily. Animals lost an equal amount of body weight when treated with similar doses of rimonabant and TM38837. At the end of the treatment period, drug treated mice had 22-26% lower body weights than placebo treated mice while drug treated rats had 14% lower body weights than placebo treated rats.

Other animal studies provided substantial evidence that the drug has a markedly lower propensity than rimonabant to cross the blood-brain barrier. These studies included brain tissue examination, behavioural tests and other studies to demonstrate where in the body the drug was distributed.

For their human study of the drug, the researchers reported that in a phase 1 clinical trial of 48 healthy normal-weight adults, the drug was well tolerated even at the highest dose, with seven of the volunteers experiencing brief, mild drug-related side effects such as abdominal discomfort, nausea and diarrhoea.

On the basis of these results, development of the drug is continuing. The researchers expect to report the results of further animal and human studies this autumn.


'/>"/>

Contact: Emma Ross
rosswrite@mac.com
International Association for the Study of Obesity
Source:Eurekalert

Related medicine news :

1. Experimental nonsteroidal treatment of asthma shows promise
2. Experimental targeted therapy shows early promise against medulloblastomas
3. Experimental Vaccine Shields Monkeys Against Ebola
4. Experimental Drug Offers Hope for Cystic Fibrosis Patients
5. Childhood Obesity Boosts Risk of GERD
6. Inactivity no contributor to childhood obesity epidemic
7. New Book Helps Combat America's Child Obesity Epidemic
8. Zone Diet Creator Dr. Sears Discusses Obesity Causes and Solutions on Mel Robbins Radio Show
9. Obesity in America: World-Renowned Health Educator Offers Solutions to Obesity Epidemic
10. The Quantum Scale Helps in the Fight Against Childhood Obesity
11. Obesity Rates Jump in 28 States, Report Shows
Post Your Comments:
*Name:
*Comment:
*Email:
(Date:5/24/2016)... ... May 24, 2016 , ... Loma Linda University Health (LLUH) ... hospital and expanded Children’s Hospital. Over 3,000 people looked on as the shovels hit ... the event photo slidehsow. , During the program, Richard H. Hart, MD, DrPH, ...
(Date:5/24/2016)... Los Angeles, CA (PRWEB) , ... May 24, ... ... devoted to everything egg freezing, today announced the official relaunch of its community ... to use their frozen eggs. Eggsurance's mission is to create a safe and ...
(Date:5/24/2016)... Orion, Michigan (PRWEB) , ... May 24, 2016 , ... ... Yoga. , The Yoga practice enhanced with Young Living Essential Oils, taught by ... - 8pm at the Lake Orion location. Yoga Flow is 6:30pm - 7:15pm followed ...
(Date:5/24/2016)... ... , ... In light of recent heavy flooding in Houston, Texas, Pelican Water ... throughout the Houston area. , Heavy floodwaters have led to destroyed waterways and flooded ... may not even be aware of the contamination of their water supply and thus, ...
(Date:5/24/2016)... California (PRWEB) , ... May 24, 2016 , ... "ProText ... times," said Christina Austin - CEO of Pixel Film Studios. , ProText Layouts Vol. ... within Final Cut Pro X . With ProText Layouts, video editors can create ...
Breaking Medicine News(10 mins):
(Date:5/23/2016)... May 23, 2016 According ... Share, Development, Growth and Demand Forecast to 2022 ... Other), by Application (Drug Discovery and Development, Proteomics, ... (Pharmaceuticals, Life Science and Biotechnology, Academic and Research ... Research, the global mass spectrometry market ...
(Date:5/23/2016)... , May 23, 2016 ... for detection of multiple diseases; ,Technology to be presented ... Yissum Research Development Company of the Hebrew ... into a research agreement with Aurum Ventures MKI, the technology ... development of a new diagnostic approach for early detection ...
(Date:5/23/2016)... -- The global  reprocessed medical devices market ... according to a new study by Grand View Research, ... the lack of centralized support for waste disposal in ... for reprocessed medical devices market. Additionally, the long-term cost-efficiency ... the original device is the high impact rendering driver ...
Breaking Medicine Technology: