7TM Pharma completes positron emission tomography preclinical research program to successfully demonstrate peripheral restriction of its CB1 receptor antagonist TM38837
Monday, July 12, 2010
7TM Pharma today announced positive preclinical Positron Emission Tomography (PET) data in non human primates with their proprietary drug candidate TM38837, which was discovered at 7TM Pharma and is being developed for treatment of obesity, type 2 diabetes and related metabolic disorders. In line with a full range of other experiments, the data clearly demonstrate the principle feature of this first in class compound, namely that it is peripherally restricted. A direct comparison between TM38837 and rimonabant, a brain penetrant CB1 receptor antagonist, importantly exhibited a clear difference between their propensities to cross the blood brain barrier in favor of TM38837.
TM38837 is a first in class, peripheral CB1 receptor antagonist. It was designed to avoid the risk of psychiatric side effects through its restriction to peripherally located CB1 receptors in the body. This approach is in contrast to the first generation CB1 receptor antagonists, which also targeted CB1 receptors within the central nervous system. Although clinically effective, these had an unfavorable psychiatric side effect profile including depression and anxiety.
Christian E. Elling, Vice President, commented: "Our first in class peripheral CB1 antagonist TM38837 continues to return very promising distribution data, validating that it is restricted to CB1 receptors outside the CNS, at what have been demonstrated to be relevant efficacious doses in various models of obesity and type 2 diabetes. These results have encouraged us to move TM38837 forward in clinical development. We intend to partner the program during clinical development to further accelerate the program to the benefit of the growing number of obese and diabetic patients requiring safe and effective medicines."