Changes in body weight represent a major and increasing public health problem. The prevalence of obesity in the USA is 27.7% in men and 34% in women in the 20-74 year age group (source: National Health and Nutrition Examination Survey 1999-2000); whereas in most European countries it is approximately 10-20% in men and 15-25% in women (source: Danish National Board of Health Conference on Obesity, September 2002). Significant weight loss or cachexia is also an increasing cause of morbidity and mortality in the elderly, and persons with congestive heart failure or in some cancers.
Ghrelin is secreted by the stomach and stimulates the appetite. It has recently received media attention because high blood levels of ghrelin have been observed in individuals following weight loss from dieting, which may partially explain the difficulty in maintaining diet-induced weight loss. Ghrelin levels remain low in patients who have lost weight by undergoing gastric bypass surgery, and, again, this may partially explain the lack of appetite in these individuals. All these observations open the way to the research of new drugs which can treat weight pathologies such as the ghrelin agonists for cachexia and ghrelin antagonists for obesity.
Ghrelin also stimulates growth hormone and prolactin secretions by the pituitary gland, and cortisol and aldosterone secretion by the adrenal glands. If these additional effects can be desirable in certain pathologies, often they will lead to secondary effects in other pathologies (for example: augmentation of growth hormone is not desirable in the elderly with diabetes or in persons with cancer).
In this context, Ipsen research has for the first time synthesised a unique modified version of ghrelin analogues which conserves its regulator effect on appetite, but does not stimulate growth hormone secretion.
This discovery advances the possibility of producing ghrelin-based drugs for regulating appetite and body weight. For the first time this also suggests that differences may exist at the ghrelin receptor levels in different target tissues, which opens up a new field of research. This provides unique tools for researchers to increase the knowledge of ghrelin regulation and human body weight control.
This discovery has been made by Biomeasure Inc. (Boston, USA), one of four research centres of the Ipsen Group to discover drugs in neuroendocrinology. "This important discovery highlights the quality of our research in neuroendocrinology and our capacity to generate innovative molecules in this therapeutic area. At present, we are conducting pre-clinical tests on selected ghrelin analogues in order to enter them in the clinical evaluation phase in the near future" said Jacques-Pierre Moreau, Ipsen's CSO.
Ipsen
Present in over 110 countries with a total staff of nearly 3700, the Ipsen Group had a turnover of €718 million in 2002, 27.1% outside Western Europe.
The Group is focused on developing innovative products in targeted disease areas: oncology, endocrinology, neurology and hematology. Ipsen currently has over 20 products on the market, including those marketed to specialists in disease areas that represent the main source of Ipsen’s future growth, as well as predominantly natural-based products that represent the historical base of the Group’s business in other disease areas. In 2002, 18.2% of Ipsen’s turnover was reinvested in Research and Development, carried out from 4 centers Paris, Boston, Barcelona and London by an international network of about 550 scientists.
The Group’s website is www.ipsen.com
Source: Ipsen