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Description
Tamoxifen is classed as a specific estrogen receptor modulator or SERM. It acts as an estrogen antagonist in the brain and the breast area meaning it prevents estrogen from exerting its normal effect in those areas. With respect to its action in the brain it inhibits the conversion of testosterone to estrogen which during a cycle can mean that estrogen levels remain low. Although low estrogen is often considered advantageous by bodybuilders it should be noted that estrogen helps both with the accrual of muscle mass and also helps to boost libido on cycle. In fact, when bodybuilders use testosterone enhancing compounds and run tamoxifen alongside it, they often lose out on some of the muscle gains and enhanced libido that normally accompanies testosterone elevation.


How does tamoxifen work?
Tamoxifen is a medication primarily used to treat and prevent breast cancer. Here's how it works:
Mechanism of Action:
Selective Estrogen Receptor Modulator (SERM):
Tamoxifen acts as a selective estrogen receptor modulator, meaning it can block or activate estrogen receptors in different tissues.
Inhibition of Estrogen Effects:
In breast tissue, tamoxifen blocks estrogen from binding to its receptors. Since many breast cancers rely on estrogen for growth, this blockade helps to slow down or stop the growth of hormone-sensitive tumors.
Partial Agonist Activity:
In other tissues (like the uterus), tamoxifen can act as a partial agonist, meaning it can mimic estrogen's effects. This dual action is beneficial for certain uses, but it also means tamoxifen can carry risks, such as an increased risk of uterine cancer.
Clinical Uses:
Breast Cancer Treatment:
Tamoxifen is often prescribed for women with estrogen receptor-positive breast cancer, particularly after surgery and radiation. It can be used in both premenopausal and postmenopausal women.
Prevention:
It is also used to reduce the risk of developing breast cancer in women with a family history or other risk factors.
Male Breast Cancer:
Occasionally, tamoxifen is used in men with breast cancer or conditions related to high estrogen levels.
Side Effects:
While tamoxifen is effective, it can have side effects, including:
Hot flashes
Vaginal discharge or bleeding
Mood swings
Increased risk of blood clots
Potential for uterine cancer with long-term use
Tamoxifen is generally well-tolerated, but it is essential to discuss potential risks and benefits with a healthcare provider.
What Are The Benefits Of Tamoxifen (Nolvadex)?
Tamoxifen, commonly known by its brand name Nolvadex, is primarily used in the treatment and prevention of breast cancer. Here are the main benefits of tamoxifen:
Benefits of Tamoxifen:
Breast Cancer Treatment:
Effective Against Hormone-Receptor-Positive Cancers: Tamoxifen is particularly effective for estrogen receptor-positive (ER+) breast cancers, helping to slow or stop the growth of tumors that rely on estrogen.
Cancer Prevention:
Reduces Risk in High-Risk Women: For women with a family history of breast cancer or other risk factors (like atypical hyperplasia), tamoxifen can significantly reduce the risk of developing breast cancer.
Improved Survival Rates:
Adjuvant Therapy: When used after surgery (adjuvant therapy), tamoxifen has been shown to improve survival rates and reduce recurrence in women treated for early-stage breast cancer.
Versatile Use:
Applicable for Different Stages: Tamoxifen can be used in various stages of breast cancer, including early-stage, metastatic, and as a preventive measure.
Male Breast Cancer:
Treats Breast Cancer in Men: Although rare, tamoxifen is also used to treat breast cancer in men, especially those with hormone-sensitive tumors.
Potential Fertility Benefits:
Improvement in Ovulation: In some cases, tamoxifen can induce ovulation in women with fertility issues, particularly those with polycystic ovary syndrome (PCOS).
Bone Health:
Bone Density Preservation: Tamoxifen may help maintain bone density in postmenopausal women, reducing the risk of osteoporosis, although this effect is more pronounced in premenopausal women.
Cost-Effectiveness:
Affordable Treatment Option: Tamoxifen is generally more affordable than some newer targeted therapies for breast cancer, making it accessible for many patients.
Summary:
Tamoxifen (Nolvadex) offers numerous benefits, particularly in treating and preventing hormone-sensitive breast cancer. Its ability to reduce the risk of recurrence and improve survival rates makes it a valuable medication in oncology. However, as with any medication, it is essential to discuss its use, benefits, and potential side effects with a healthcare provider.
Negatives Of Tamoxifen Use
Although classed as an estrogen antagonist it should be noted that in some parts of the body tamoxifen actually acts as an estrogen agonist meaning it actually acts in an estrogenic manner as opposed to how most think of it being which is an anti-estrogen. When it acts in an estrogenic fashion in the liver for instance, tamoxifen can increase levels of sex hormone binding globulin (SHGB) which acts to bind to testosterone thus lowering free testosterone in the body. Free testosterone is the amount of unbound testosterone in the system and it is the level of free testosterone which is strongly correlated to the positive effects of high testosterone such as increased muscle mass, strength, and libido.
By lowering free testosterone, tamoxifen has the potential to hurt our bodybuilding gains. This helps to explain why we never hear of people using tamoxifen on a standalone basis (similar to how a testosterone booster is used) and gaining any muscle mass despite the significant rise in testosterone it is capable of producing. Quite simply, a lot of the testosterone rise is cancelled out by the increase in SHGB. Another negative of tamoxifen's action in the liver is its ability to suppress production of the peptide hormone IGF-1. IGF-1 is broken down from growth hormone and is considered to be more potent than growth hormone itself for the purposes of building muscle tissue. High IGF-1 levels make a big contribution to the process of building a better physique and the ability of tamoxifen to suppress IGF-1 levels is another reason why tamoxifen use tends to be disappointing for the purposes of building muscle mass.
In fact, a recent study which showed a rise in total testosterone (they failed to measure free testosterone or levels of SHGB) and a reduction in IGF-1 levels after tamoxifen usage is a significant indicator as to why it can prove disappointing for the building or maintenance of muscle mass.(1,2) The fact that tamoxifen is referred to as an anti-estrogen overlooks the fact that outside of certain tissues it promotes estrogenic effects. A study published in the Journal of Endocrinology(3) showed that long term tamoxifen use increased serum testosterone levels by 50% which is certainly a healthy increase. However, at the same time serum estrogen levels increased by a massive 341%. In fact, in the control group in this study, which only used tamoxifen for a week, estrogen rose after just four days. Considering that the subjects in this trial used tamoxifen at a lower dose of just 10mg it begs the question of what would happen if used at the higher dosage typically seen in bodybuilding circles.
Tamoxifen and gyno in bodybuilders
Tamoxifen is of course frequently used to suppress estrogenic action in breast tissue to prevent gynecomastia for which it can work rather well during cycle. It will not totally eliminate the possibility of gyno though especially with those steroids that act in a progesterogenic fashion for which something that lowers prolactin such as the supplement Vitex will be required. Assuming though that your cycle went well and you ran a PCT and you battled through the suppressed sex drive, low IGF-1 levels and low free testosterone levels seen with tamoxifen usage. What happens when you remove tamoxifen? If we consider the study above which shows a profound rise in estrogen in the body during tamoxifen use, its removal is going to create a situation where we now have high estrogen levels in the body and with nothing to stop this estrogen from causing gyno in male bodybuilders. This creates a recipe for the kind of rebound gyno that you often hear people complaining about on bodybuilding forums. Adding insult to injury, high estrogen levels are suppressive in their own right which can cause delayed progress in the gym when coming off tamoxifen use..
Other Health Effects
Carcinogenic action - Tamoxifen has been shown in several studies 4,5,6) to increase the risk of cancer and is listed as a known carcinogen by the American Cancer Society. A 2006 study in The Lancet showed it increased mortality rate in women using tamoxifen. Studies in rats (7) add further weight to the argument supporting tamoxifen's carcinogenic potential with up to 80% of animals developing malignant tumours.
Liver damage - Tamoxifen has been studied for its effects on liver for some time with it being linked to fatty liver in women (8) as well as showing an increased likelihood in the formation of liver cancer.
Cataracts - Tamoxifen is acutely toxic to the eyes with more than one report on a bodybuilding forum showing a user who irreversibly damaged their eyesight. Studies (9,10) support the notion that tamoxifen can contribute to increasing susceptibility to cataracts.
Blood Clots - Tamoxifen usage is recognised as increasing the risk of blood clotting which if it occurs in a major artery or cardiac tissue can potentially be life threatening. For bodybuilders whose blood pressure may be high it makes tamoxifen use doubly dangerous.
Low libido - As previously noted the negative impact on free testosterone levels of tamoxifen can cause users to fail to experience the effects associated with elevated testosterone including libido. Compared to other compounds which increase testosterone, tamoxifen users tend to report poorer libido. In addition, the adverse effect on blood clots means it can make erectile dysfunction more likely as well. It is for this reason that many users will employ a testosterone booster in PCT to help address these shortcomings of tamoxifen usage.
Mood swings - Perhaps the most common complaint of all from bodybuilders using tamoxifen or other SERM's during PCT is they cause unbearable mood swings with frequent reports of tearfulness, and depression occurring among bodybuilders. While not everyone gets this it is notable that these effects don't get reported to anywhere the same extent with other PCT products making it feasible that this occurs as a consequence of the rise in serum estrogen seen during tamoxifen use.
Final thoughts on Tamoxifen for PCT
While many bodybuilders see tamoxifen as an essential hopefully this article helps to illustrate some of the potential negatives associated with its use. While it can be important in particular situations especially if used during cycles of aromatising compounds, it's overuse and usage in pct can cause a host of issues. A more sensible strategy for prohormone or AAS users is to employ the use of an aromatase inhibitor to lower estrogen levels significantly, making an SERM less important, as well as addressing other aspects of PCT which are commonly overlooked and discussed in our article on post cycle therapy. Finally, the use of aromatising products should be limited and if these are going to be used an AI as opposed to an SERM is a much better solution for managing estrogen levels on cycle. For those who insist on using tamoxifen during PCT it is important this is combined with an AI to help mitigate against the prospect of rebound gyno which could potentially occur with tamoxifen use. In addition the use of a testosterone booster to help combat the deleterious effects of tamoxifen on libido and mood is advisable with the use of a product such as Activate Xtreme a good tool to address both this aspect and also to boost free testosterone levels which are otherwise suppressed during tamoxifen use.
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