Re: E4 estetrol protective

[Guest guest]

Vliet apparently mentioned in one of her radio blogs that new research is coming out on a fourth estrogen called E4 or estetrol, which appears to inhibit breast cancer in pregnant women. Interesting. Madeleen http://www.endocrine-abstracts.org/ea/0014/ea0014S16.2.htm The pharmacological properties of oral E4 as investigated by Pantarhei Bioscience can be summarised as follows. Estetrol is orally bioavailable in the rat and acts as an estrogen on bone, brain, vagina and endometrium. Estetrol suppresses hot flushes and inhibits ovulation. Surprisingly, E4 acts as an estrogen antagonist on the breast since it was shown to prevent development of breast tumors and to remove pre-existing breast tumors in

the DMBA rat model. In phase I studies in early postmenopausal women E4 showed high oral absorption, full dose linearity, high bioavailability, low inter-subject variability and a long elimination half-life with a mean of 28 hours. Estetrol appeared to be efficacious, safe and without side-effects up to a dose of 20 mg per day for 28 days. Estetrol will be developed further for the treatment of breast cancer, prostate cancer, osteoporosis and for those Th2-mediated auto-immune diseases, that are known to improve during pregnancy. http://www.pantarheibio.com/ The Lead compound of Pantarhei Bioscience is estetrol (E4). Estetrol may be suitable for several clinical applications such as: the treatment of breast cancer (phase IIA) the treatment of prostate cancer (combined phase IB and IIA) the treatment of auto-immune diseases (Sjögren’s Syndrome in phase IIA) the replacement of ethinylestradiol (EE) in oral contraceptives (phase IIA) prevention of osteoporosis (ready to start phase IIB) Other projects are: a method to treat metastasised ovarian cancer a natural and orally bioavailable androgen a project to diagnose, prevent and treat vaginal HIV transmission (AIDS) At present more than 50 patents are in different stages of processing. Preclinical and clinical studies supporting the new treatment concepts are ongoing. http://www.pantarheibio.com/pipeline/estetrol.htm

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