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Estradiol Balance in Testosterone Replacement Therapy.

Medications like AIs and SERMs can often help treat patients with hypogonadism. NovaGenix in Jupiter can help patients with Low T optimize their hormone levels in Palm Beach County.

Estradiol or E2, is normally considered a female hormone, however it plays a very important role in males in several physiologic functions, like bone metabolism, cardiovascular health, and as well testicular functioning. Due to its significance in men’s health and hormonal balance, estradiol has been studied by male reproductive and sexual medicine experts and medical specialists to help treat conditions like hypogonadism infertility.

The various medications that are used to regulate E2 levels are often referred to as SERM’s which is short for selective estrogen receptor modulators. There are also AI’s which is short for aromatase inhibitors. In some men who may be infertile, in particular ones that also suffer from hypogonadism, or men with low total testosterone to E2 ratios, there is good evidence showing that SERMs and AIs can increase free testosterone levels or the imbalance between testosterone levels to E2 ratios. They can also improve infertility issues in males as the signal spermiogenesis, which is the production of sperm as well as testosterone.

In men, most of the estradiol flowing through our bloodstream and tissues comes from the peripheral aromatization of testosterone by specialized cells that store fat in the connective tissue called adipocytes which are located all throughout the body.


So, it’s understood that for men, the circulating testosterone (which is mostly produced by the testes), will get taken up by non-testicular tissue through a process known as passive diffusion. Passive diffusion is when molecules can move across cell membranes without active transport, or the utilization of energy. After uptake, testosterone is then synthesized within that specific tissue into estradiol, which now allows the new formed E2 to begin affecting the tissue systems.

Much like with what happens with circulating free testosterone, it’s thought that estradiol which had been produced in these peripheral cells is now circulating within the blood stream and being taken up by certain tissue through estrogen receptor sites located within the surface membrane of the tissues which then become influenced hormonally by the estradiol.


One can look to the hypothalamus to provide an example of how both estradiol and testosterone both exhibit similar effects. Both can modulate the negative feedback inhibition of LH, short for luteinizing hormone and FSH or follicle stimulating hormone by the pituitary.  Through these mechanisms of action, the modulation of selective estrogen receptor modulators, or SERM’s and Aromatase inhibitors, AI’s and the feedback loop created between the testosterone and estrogen interaction with the testiscular-hypothalamic-pituitary axis that allows providers the ability to prescribe and treat for hypogonadism and infertility with medications like HcG, or human chorionic gonadotropin and AI’s like Anastrozole or E2RA, estrogen receptor antagonists like Clomiphene. Some clinics are now using gonadorelin to replace hCG . The problem with using Gonadorelin to replace hCG stems from the short half-life of gonadorelin and the need for frequent injections, making it terribly inconvenient for TRT patients. But because of recent FDA changes regarding the regulations on 503 a and b compounding pharmacies and their need for a biologics license to manufacture hCG, there is a shortage of medications. This has certainly made it more difficult for patients to find hCG, however we are still able to prescribe and help patients obtain it from licensed US pharmacies for our TRT patients. (Click this link to learn more about how to get a prescription for hCG)Through their own actions each of the medications can play a role in regulation of estradiol levels, production of testosterone and biogenesis of sperm. Understanding the differences in these medications is important in developing a TRT protocol that is effective for men with sub optimal hormone levels. If you feel as if your testosterone levels are low and are experienced the telltale signs of low T, visit us at NovaGenix in Jupiter, Florida to get tested, diagnosed and treated for andropause. Call us at 561-277-8260 to learn more and visit us online at


Once you fill out and submit the intake form, we can schedule a consultation to speak with our physician, Dr. Mackey who has been helping men with hormone optimization and testosterone therapy for years. Check out our patient reviews on Google!


609 N. Hepburn Ave Suite 106 Jupiter, Florida 33458


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