EMERYVILLE, Calif., Feb. 21 /PRNewswire/ -- Bionovo, Inc. Scientific Advisory Board member Dr. Dale Leitman’s laboratory at the University of California, San Francisco, Department of Obstetrics, Gynecology and Reproductive Sciences, Cellular and Molecular Pharmacology and Center for Reproductive Sciences published recent findings on the role of estrogen receptors in the regulation of inflammatory genes in the journal Molecular Cell, February 17, 2006.
The amount of estrogen in a woman’s body declines dramatically during the menopausal transition resulting in symptoms such as hot flashes, insomnia, vaginal dryness and mood changes. The prolonged loss of the reproductive hormone, estrogen is associated with a significant increase in the incidence of osteoporosis, cardiovascular disease, and dementia in the years following the menopausal transition. These conditions are linked to excessive production of proteins known as cytokines that cause inflammation. Ultimately, the inflammatory cytokines lead to tissue injury, a hallmark feature of these conditions.
While it has been thought that only the decline of estrogen levels contributes to inflammation processes, Dr. Aleksandra Cvoro, of Dr. Leitman’s laboratory, has shown that the estrogen receptor without estrogen increases the activity of inflammatory genes. When estrogen is introduced, the activity of the same inflammatory genes decreases in a process called transcriptional repression. Moreover, this repressive activity is dependent on the ability of the bound estrogen and the receptor to recruit regulatory proteins that were previously not thought to be involved in the repression of these inflammatory genes. According to Dr. Cvoro, this new activity of the unbound estrogen receptor could explain how the loss of estrogens can increase inflammatory activity and damage tissue after menopause.
Recent large clinical trials have suggested that estrogens used in hormone therapy increase the risk of cardiovascular disease and dementia. According to Dr. Leitman, this is likely due to the high amounts of estrogen used and their not selective action on the estrogen receptors.
“Our studies suggest that low levels of more selective estrogens may be key to combat the negative action of the unbound receptor on the inflammatory processes that occur in the cardiovascular system, bone and brain after menopause,” said Dr. Leitman. “Since estrogen has been shown to increase the risk of breast and uterine cancer by activating growth promoting genes, it also illustrates the need to discover drugs that will be selective transcriptional repressors that will prevent the inflammation and probably will not cause cancer.”
“Dr. Leitman’s work demonstrates the complexity of estrogen receptor regulation and its implications in the post-menopausal state. It underlines the need that in order to develop safer more selective estrogens one has to be able to probe deeper into the specifics of estrogen regulation,” said Dr. Isaac Cohen, president and CEO of Bionovo. “Bionovo’s selective estrogen receptor modulators program is committed to discovering safe and effective drugs for women’s health. That is why we are utilizing Dr. Leitman’s techniques in its discovery and development process, and therefore reaching greater selectivity for our pipeline of products.”
Bionovo recently launched a phase 2 randomized placebo controlled trial of its first selective estrogen receptor beta modulating drug MF101 for the treatment of menopausal hot flashes.
Bionovo, Inc.
Bionovo is a drug development company focusing on the discovery of novel pharmaceutical agents for cancer and women’s health. The company is working simultaneously on two distinct discovery approaches, one focusing on pro- apoptotic agents for cancer and a second, in the area of selective estrogen receptor modulators (SERMS) to treat severe menopausal symptoms. The company’s lead candidate drug, MF101 is in Phase 2 clinical testing and a second drug, BZL101, designed to treat advanced breast cancer is ready to enter Phase 2. The company is developing its products in close collaboration with leading U.S. academic research centers including the University of California, San Francisco; University of Colorado Health Sciences Center; University of California, Berkeley; and the University of Texas, Southwestern. For further information please visit: http://www.bionovo.com.
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Bionovo, Inc.
CONTACT: Jim Stapleton, Chief Financial Officer of Bionovo, Inc.,+1-510-601-2000, jim@bionovo.com; or Antima “Taz” Sadhkuhan of InvestorRelations Group for Bionovo, +1-212-825-3210
Web site: http://www.bionovo.com/
