GynoFiles

For the Woman Who Thought She had Everything, Gynos Trying To Build That Perfect Estrogen A Rose may be a Rose by any other name, not so An Estrogen is not necessarily an Estrogen. And it’s pointed out in the January2011  issue of Menopause that there are two forms of the ‘ ER’ or Estrogen receptor. We have Estrogen receptor alpha and beta: ER- α and ER- β . ER- β is the receptor of the ovary, lung, the bowel, and our brain. ER- α predominates in the breast, the bones, the heart and the brain axis including the pituitary. Actually the compound estradiol, the bioidentical estrogen we talk about in many of our blog posts about menopause, is that perfect compound binding to both the receptors. Scientists have exploited the partial action potential and created a class you know well that only binds mostly alpha receptors. Those medications are tamoxifen, which we use for breast cancer treatment and prevention; and raloxifene (Evista) we use for osteoporosis treatment a...

The FDA has now reworked some of the terms we use to describe the compounds we use for infertility, osteoporosis, and breast cancer treatments. These compounds were designed to act like estrogen on some tissues and like anti-estrogen on other tissue. Thus the effect can be inducing ovulation such as we can with clomid, prevention of breast cancer as we can accomplish with tamoxifen or the improvement of bone health with raloxifene. Understanding the action of these compounds has gotten just a bit more complex. In the past the compounds were given the group name "SERMS" for Selective Estrogen Receptor Modulators, and which were called in lay terms "designer estrogen". The FDA now prefers the term "estrogen agonist/antagonist." It has to do with the way the receptors are activated and therefor how much estrogen or anti-estrogen action the compound will produce. So when selecting your compound "formerly known as a SERM" discuss the biology wit...