The Best Estrogen Blockers for Men: How Aromatase Inhibitors Work
Tamoxifen, a selective estrogen receptor modulator (SERM) with antiestrogenic activity in the breast tissue, was the previous standard of care for both pre- and postmenopausal, estrogen receptor–positive breast cancer patients. However, the drug’s efficacy was limited by the rate of breast cancer recurrence. Aromatase inhibitor research has demonstrated improved survival in postmenopausal women, postmenopausal women with metastasis, and premenopausal women under the age of 35 with ovarian ablation. In the Testis, the Leydig, Sertoli, and Germ cells are abundant in aromatase and oestrogen, where oestrogens serve to modulate testosterone production and sperm production and quality 1.
Arimidex Side Effects in Men
- Aromatase inhibitors (AI) have been used in males in idiopathic short stature, constitutional delay of puberty, precocious puberty, gynecomastia, oligospermia, hypogonadism related to obesity and ageing.
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- This is particularly relevant given that the greatest cause of death in women with early stage breast cancer is heart disease (Levi et al, 2002).
- Some experimental agents, such as selective aromatase modulators (SAMs), aim for tissue-specific inhibition, reducing estrogen synthesis in certain areas while preserving its function elsewhere.
- For example, lower estrogen levels can lead to the thinning and weakening of bones.
This makes it suitable for certain subsets of male patients with mild hypogonadism who have functional testes but experience infertility and hormonal imbalance with high estrogen. Anastrozole, more popular by the brand name Arimidex, is a prescription drug that’s become popular amongst men with low testosterone (T) because of its ability to affect the ratio between testosterone and estrogen (E) in the human body. While AIs are generally well tolerated, side effects may limit adherence in a number of women. The effectiveness of AIs is well documented, but they are not without concerns.
How quickly does Arimidex lower estrogen?
Patients and providers should be aware of any estrogen-containing products the patient is taking. These products should be avoided while on hormone deprivation therapy, as they could potentially counteract the benefits from AIs. Less significant is your intake of carbohydrates and protein, however, an increased protein intake tends to lead to improved fat loss during caloric restriction and more muscle mass, in addition to better controlled blood glucose 45,46. Naturally, serum oestrogens levels decrease with a lowered body fat percentage too, as there has been less available fat to produce aromatase enzyme.
So adult males on hormone therapy need to manage estrogen levels effectively because estrogen plays a key role in male physiology. There have been significant advancements in understanding the interaction between testosterone and estrogen and how these two hormones impact multiple physiologic functions in men. SERMs and AIs have been used off-label in men to increase testosterone levels while maintaining spermatogenesis. Though their use in idiopathic infertility is questionable, there are data to Steroids support their use in men with both hypogonadism and low sperm counts, and also in men who are symptomatic from low testosterone levels. AIs can also be used in these same subsets of men who have an imbalance between testosterone and estradiol. More recently, BCRF researchers have been studying why some breast cancers become resistant to these treatments, which can lead to metastasis.
Steroidal AIs, or suicide inhibitors, irreversibly bind to aromatase, leading to permanent enzyme inactivation. Exemestane, the most well-known steroidal AI, is structurally similar to androstenedione, allowing it to compete with natural substrates. Once bound, the enzyme degrades, resulting in prolonged estrogen suppression even after the drug clears from circulation. Limitations to our study include the retrospective design, but all data were collected prospectively.