Wednesday November 17, 10:59 am Eastern Time
Company Press Release
SOURCE: Hoffman-La Roche Inc.
New Compounds to Treat Obesity on the Horizon
NUTLEY, N.J., Nov. 17 /PRNewswire/ -- Two Hoffmann-La Roche Inc. (Roche) obesity
researchers caution that, while the recent reports of weight loss using the hormone leptin are
very promising, they should not lead people to believe that a drug, which acts in the brain to
fight fat, will be available from their doctors soon.
''Leptin results from the recent Journal of the American Medical Association (JAMA) study are a two-edged sword,'' stated
Keith Yagaloff, Ph.D., research leader, Metabolic Diseases at Roche, ''Leptin probably won't become a drug because of the
need for daily injections over several months, as well as the high doses needed for efficacy. However, the research does
validate the proof-of-concept for the leptin pathway.'' The article showed significant weight loss results among obese patients
injected with high doses of leptin, a hormone produced by fat cells that works in the brain to suppress appetite.
''The discovery of leptin is exciting because it opened a new area for research. As a result, we are finding greater success by
exploring drug targets within the leptin pathway that could lead to new orally active drugs,'' according to Joseph Grippo, Ph.D.,
director of Metabolic Diseases for Roche. Grippo said Roche hopes to begin early clinical trials in one to two years using other
drugs that influence biochemical pathways in the brain to promote weight loss.
Roche researchers have made significant contributions to understanding how leptin works. The positive results of weight loss
with leptin give researchers increased confidence in melanocortin 4 (MC4) discovery programs, one of the company's most
important programs. Roche has played a significant role in the study of obesity treatment by bringing understanding of the leptin
pathways and specifically leptin and its receptor as well as the MC4 receptor, a brain receptor that regulates appetite.
Roche's recent discovery of highly selective MC4 agonists demonstrates that MC4 causes weight loss in animals. Until recently,
it was unknown whether MC4 activation alone would cause weight loss. ''With this discovery, we now have increased
optimism that we can develop highly selective and safe MC4 agonists for obesity treatment,'' stated Grippo. In addition to the
MC4 receptor, other potential candidates for obesity treatments include CRH, corticosterone releasing hormone; NPY,
neuropeptide Y; AgRP, agouti-related protein; MCH, melonin-concentrating hormone and orexins.
In another recently published JAMA article, researchers point out that obesity in the U.S. has reached epidemic proportions,
with almost one out of five Americans meeting the medical definition of obesity. Both Grippo and Yagaloff note that Americans
who need to lose weight demand very safe and effective drugs.
About Xenical
As a world leader in obesity research, Roche currently markets Xenical® (orlistat), which through its fat-blocking mode of
action, works non-systemically in the gastrointestinal tract, and does not require entry into the bloodstream or brain. (snip)
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