New selective estrogen receptor modulator (SERM)
OHSU # 0725
- Martin Kelly, SM.Physiology & Pharmacology
- Oline Ronnekleiv, SM.Physiology & Pharmacology
- Jian Qiu, SM.Physiology & Pharmacology
- Thomas Scanlan, SM.Physiology & Pharmacology
- Sandra Tobias
Current hormone replacement therapy involving either estrogen alone or a combination of estrogen and progestin is fraught with serious side effects including increased susceptibility to breast cancer, endometrial cancer, and stroke. A novel SERM designed and synthesized by researchers at OHSU and UCSF has been shown to be devoid of many of the negative side effects arising from peripheral estrogen receptor activation since it does not bind to the classical nuclear estrogen receptors. The action of this compound is restricted to the non-genomic hypothalamic responses.
Using animal models, the Kelly laboratory at OHSU is characterizing the rapid signaling pathway activated by estrogen, and has demonstrated the efficacy of this novel SERM, STX, for treatment of obesity, hot flashes,anxiety, and memory and learning. Future work is slated to include toxicity testing, evaluation of other STX derivatives, and Phase 1 Clinical Trials.
Considering the nearly 42 million women over the age of fifty in the United States, the NIH stated that, “new medications with the benefits of HRT and fewer side effects are urgently needed.” In addition to menopause, thermoregulation and emotional symptoms are issues associated with pre-menstrual syndrome (PMS). The market value is estimated at $200 million in the US alone, with a projected growth rate of 15%. Likewise, men treated with HRT for prostate cancer suffer from some of the same symptoms as menopausal women. With one in six American men developing the illness in their lifetime, this market is as large as 250,000 new cases each year.
There are two basic classes of menopause therapies: HRT and SERMS. HRT drugs include Provera (Pharmacia & Upjohn), Premarin (Wyeth) and Delatestryl (Savient), while leading SERM treatments are Tamoxifen (marketed as Nolvadex by AstraZeneca) and Raloxifene (marketed as Evista by Eli Lilly). Additionally, antihypertensive drugs (such as Clonadine which is marketed as Catapres by Boehringher Ingelheim) are often prescribed to treat hot flashes alone. However, these drugs are not always prescribed specifically for symptoms of menopause and most carry with them undesirable side effects that may be avoided through STX's unique mode of action.
The differentiating factors between STX and current menopausal treatments give STX a substantial competitive advantage for the market associated with menopausal women. The end goal is for STX to be the ideal drug of choice for safe and effective treatment of many of the symptoms associated with menopause.
Patent rights are owned by OHSU and UCSF. Dr. Martin Kelly is a member of the OHSU faculty in the Program in Molecular and Cellular Biosciences.
Technology 0725 is currently available for exclusive licensing.
|Published||Patent Cooperation Treaty||WO 2005/041946|
|Issued||United States||7,196,119 B2|
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