To learn about some of the side effects listed here and how to manage them, see Managing Cancer-related Side Effects. Megestrol (Megace) is a progesterone-like drug. Elacestrant and imlunestrant can also increase cholesterol and fat levels in the blood. These drugs are taken daily as pills.
Initially, clomifene was synthesized, and tamoxifen was developed subsequently. The long half-lives of tamoxifen and afimoxifene are attributed to their high plasma protein binding as well as to enterohepatic recirculation. Another active metabolite, norendoxifen (4-hydroxy-N,N-didesmethyltamoxifen), is formed via N-demethylation of endoxifen or 4-hydroxylation of N,N-didesmethyltamoxifen. Following its formation, N-desmethyltamoxifen is oxidized into several other metabolites, the most notable of which is endoxifen. Conversely, 4-hydroxylation of tamoxifen into afimoxifene is responsible for only about 7% of tamoxifen metabolism. Conversion of tamoxifen by N-demethylation into N-desmethyltamoxifen, which is catalyzed primarily by CYP3A4 and CYP3A5, is responsible for approximately 92% of tamoxifen metabolism.
Using an AI on the cycle can combat these effects. You might see this referred to as "super Clomid" because it’s somewhat based on Clomid, but Enclomiphene is considered superior to Clomid with fewer side effects. Enclomiphene has become very popular with bodybuilders, not least because of its superb ability to increase testosterone levels.
Mazzola and colleagues12 reported that men with hypogonadism and LH values ≤ 6 IU/mL are the ideal candidates for treatment with clomiphene. This is evidenced by a recent American Urological Association (AUA) survey in which 25% of practicing urologists admitted administering testosterone to infertile men with hypogonadism in an effort to treat their infertility.8 Most of the time the prescriber in this setting is unaware of the inhibitory effect that exogenously administered testosterone has on spermatogenesis via its inhibition of both FSH and LH secretion by the pituitary gland. The most recognized and well researched role of estradiol is its effect on bone metabolism.1 However, lesser known is the effect that estradiol has on the regulation of testosterone biosynthesis and spermatogenesis.2 Estradiol, normally considered a female hormone, appears to play a significant role in men in a variety of physiologic functions, such as bone metabolism, cardiovascular health, and testicular function.
To learn more about how hormone therapy is used to treat cancer, see Hormone Therapy. The side effects of orchiectomy are largely due to lower levels of testosterone and are generally the same as those for LHRH agonists (see above). AIs are effective in treating breast cancer in women, but they have not been well studied in men. Aromatase inhibitors (AIs) stop estrogen production by blocking an enzyme (aromatase) in fat tissue that converts male hormones from the adrenal glands into estrogen.
Tamoxifen needs to block growth factor proteins such as ErbB2/HER2 because high levels of ErbB2 have been shown to occur in tamoxifen resistant cancers. It is a nonsteroidal agent with potent antiestrogenic properties which compete with estrogen for binding sites in breast and other tissues. A beneficial side effect of tamoxifen is that it prevents bone loss by acting as an ER agonist (i.e., mimicking the effects of estrogen) in this cell type. In breast tissue, tamoxifen acts as an ER antagonist so that transcription of estrogen-responsive genes is inhibited. That difference translates to a 120% increase in the risk of breast cancer recurrence. Therefore, endometrial changes, including cancer, are among tamoxifen's side effects.
The fact that this can be caused by both high DHT or estrogen levels means you need to mitigate both unless you’re confident of one or the other being the main culprit. Excess water retention is a dead giveaway to anyone who is using steroids. Though Gynectrol is not limited to on-cycle use, its benefits go beyond being an anti-gyno formula. This is not PCT – it is proactive on-cycle gyno prevention. Men need some estrogen, so you don’t want to kill your levels completely – that’s not your goal.