Jenrin discovery reveals peripherally restricted cb1 program at national obesity conference
NON-BRAIN PENETRANT CB1 ANTAGONISTS FROM JENRIN DISCOVERY SHOW BENEFICIAL EFFECTS IN TREATING DIABETES AND OBESITY Results presented at Annual Scientific Meeting of the Obesity Society indicate Jenrin CB1 antagonists could play a role in treatment of metabolic disorders while reducing risks of OCTOBER 30, 2008 (Philadelphia PA) – Research shows that proprietary non-brain
penetrant cannabinoid subtype 1 (CB1) receptor antagonists developed by Jenrin
Discovery are able to produce metabolically favorable effects in peripheral tissues,
including fat and liver. The research also showed for the first time that these results are
achievable when CB1 antagonists are modified so that they do not cross the blood-brain
barrier, thereby reducing the risk of psychiatric side effects associated with the use of
CB1 antagonists that are brain-penetrant. Results were presented in a plenary session at
the 2008 Annual Scientific Meeting of the Obesity Society.
Peripheral CB1 antagonists developed at Jenrin have been shown to help reduce body
weight, decrease fatty liver, and lower serum levels of insulin and triglycerides in mice
exposed to a high-fat diet. The modified CB1 antagonists were also shown to have a very
favorable psychiatric side effect profile compared to brain-penetrant CB1 antagonists.
Jenrin is working to develop non-brain penetrant CB1 antagonists for the treatment of a
range of metabolic disorders including diabetes and cardiovascular and fatty liver
“By using known and approved CB1 antagonists as a starting point in our research, we
have been able to capitalize on years of medicinal chemistry used to optimize the original
drug, reducing the time and investment required to take lead molecules into preclinical
and clinical testing. These findings further validate both our approach and our platform
targeting development of CB1 antagonists to treat a range of metabolic disorders,” said
Robert Chorvat, PhD, vice president of chemistry at Jenrin Discovery.
Many development programs associated with CB1 antagonists have been halted because
of the risk of psychiatric side effects. “With the recent removal of rimonabant from
European markets and the announced discontinuation of Merck’s phase III clinical
development program for taranabant, the market need is clear,” said Dr. Steven Smith of
the Pennington Biomedical Research Center and head of Jenrin’s Scientific Advisory
Board. “These exciting results indicate that blockade of peripheral CB1 receptors is
sufficient to produce beneficial metabolic effects, so Jenrin’s non-brain penetrant CB1
antagonists may represent a safer alternative to treating serious health problems including
Jenrin has a total of eight patents filed and pending for its CB1 program. The company is
positioned to move forward with development programs for CB1 in 2009 and will
consider opportunities in partnership and collaboration.
“The company’s technology platform also has potential applications for use in a wide
range of drugs where restriction to peripheral tissue can help to improve efficacy and
safety profiles,” said John McElroy, PhD, president and chief scientific officer at Jenrin
Jenrin Discovery, based in Philadelphia, PA, is a privately-held, emerging pharmaceutical
company focused on developing a pipeline of small molecule drugs designed to target
peripheral tissue. The company’s strategic approach begins with the identification of
drugs with dose-limiting side effects. Using Jenrin’s peripherally-restricting technology
and know-how, drugs are modified to prevent transfer across the blood-brain barrier. The
redesigned drugs retain pharmacological and other essential properties, but carry little or
no risk of psychiatric and neurological side effects. The company has received venture
funding from Research Corporation Technologies and Themelios Venture Partners, and
seed-stage funding from Ben Franklin Technology Partners of Southeastern Pennsylvania
and BioAdvance. For more information, visit www.jenrindiscovery.com.
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SKIN AND COAT DISORDERS IN DALMATIANS Study Group on Skin & Allergic DisordersResearch Committee, Dalmatian Club of Americawhat is referred to as the “Dalmatian Bronzing Syndrome” ? Does the “Dalmatian Skin & Allergic Disorders is that all-too- Bronzing Syndrome” really exist as a diagnostic entity? The answers to most ofto by fanciers as “Dal crud.”