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SERMs 101 & How to Use Them as PCT for SARMs

SERMs 101 & How to Use Them as PCT for SARMs

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A PCT (post-cycle therapy) is a SERM protocol used to bring natural testosterone back to baseline after being suppressed or shut down from a SARM or steroid cycle.

This article is a comprehensive guide to doing one after a SARM cycle. It is based on the most widely accepted and proven-to-work protocol within the enhanced bodybuilding community, encompassing thousands of successful anecdotal reports as well as my own personal experiments with myself and over 500 lifetime clients. Rest assured, after this article, all of your questions regarding PCT and SARMs will be answered.

You will learn:

  • What are SERMs
  • (When) Do You Need PCT for SARMs
  • Best PCT for: Mildly, Moderately, Highly Suppressive SARMs

What are SERMs?

Selective Estrogen Receptor Modulators (SERMs) represent a unique class of medications that exhibit both antagonistic and sometimes agonistic effects on the estrogen receptor. These drugs play a vital role in treating estrogen-related conditions such as osteoporosis, infertility, and breast cancer in women.

Interestingly, SERMs have found an application in the realm of bodybuilding. Their use stems from the ability to stimulate endogenous testosterone production in males. This is achieved by blocking the hypothalamic estrogen receptor. As a result, the brain is led to believe that estrogen levels are low. Since estrogen is mainly produced through the conversion of testosterone, a decrease in perceived estrogen levels prompts the hypothalamus to release Gonadotropin-Releasing Hormone (GnRH). This in turn stimulates the pituitary gland to release Luteinizing Hormone (LH) and Follicle-Stimulating Hormone (FSH), thereby increasing testosterone levels and enhancing sperm production.

Furthermore, SERMs such as Tamoxifen and Raloxifene are utilized to prevent and treat gynecomastia, a potential side effect of Anabolic Androgenic Steroids (AAS) and Selective Androgen Receptor Modulators (SARMs). They achieve this by specifically blocking the estrogen receptor in breast tissue, which can both prevent and reverse the development of breast tissue.

The following sections will provide comprehensive insights into each SERM, particularly focusing on their usage in bodybuilding and Post-Cycle Therapy contexts.

Tamoxifen (Nolvadex)

Chemical Composition: 2-[4-[(Z)-1,2-diphenylbut-1-enyl]phenoxy]-N,N-dimethylethanamine

Pharmacokinetics and Dosage

  • Half-life: 5-7 days
  • Recommended Dose: 5-20 mg/day, taken in the morning
  • Suggested PCT Length: 4-6 weeks

Benefits:

Stimulates Testosterone Production: Research, including a specific scientific paper, highlights Tamoxifen’s ability to elevate testosterone levels through the stimulation of LH (Luteinizing Hormone) and FSH (Follicle-Stimulating Hormone) release. Its off-label use by bodybuilders supports this finding, with numbers in the thousands reporting successful reversal of testosterone suppression following Post-Cycle Therapy (PCT) with Tamoxifen. [1]

Treats Gynecomastia: Evidence from studies confirms the efficacy of Tamoxifen in both preventing and reducing existing gynecomastia. Its widespread use among bodybuilders—reaching into the thousands, if not millions—attests to its effectiveness in these contexts. Additional details on Tamoxifen’s use for gynecomastia can be found in the On-Cycle Therapy chapter. [2]

Reduces Cholesterol: Studies indicate Tamoxifen’s potential in reducing total and LDL cholesterol, albeit with unclear effects on HDL cholesterol. This property may counteract the negative impact of SARMs on lipid profiles, although it may elevate triglyceride levels. [3]

Side Effects:

Lower IGF-1: Tamoxifen is known to decrease IGF-1 (Insulin-like Growth Factor 1), an anabolic hormone crucial for muscle mass growth. To mitigate this effect, some users opt for MK-677. [4]

Mood Swings and Sexual Dysfunction: While lacking robust scientific backing, a minority of users report experiencing mood swings and sexual dysfunction. Brain fog is also a commonly reported issue, with some scientific evidence supporting this claim. [5]

Hot Flashes and Night Sweats: Although scientifically established in women with breast cancer, the occurrence of hot flashes and night sweats in men using Tamoxifen is primarily supported by anecdotal evidence. [6]

Blood Clots: Tamoxifen has been linked to an increased risk of deep vein thrombosis and pulmonary embolism, particularly in older women with breast cancer. Men with a family history of these conditions should exercise caution and limit the use of Tamoxifen. [7]

Mild Liver Toxicity: While Tamoxifen could potentially elevate AST and ALT liver enzyme levels, significant liver toxicity is rare. It is advisable to use NAC (N-Acetylcysteine) during PCT as a precautionary measure.

Take Away:

Tamoxifen is a strong SERM that can increase testosterone levels by stimulating LH and FSH release. It has been successfully used as a PCT thousands of times and is able to completely reverse testosterone suppression after a suppressive SARM cycle.

Clomiphene (Clomid)

Chemical Composition: 2-[4-(2-chloro-1,2-diphenylethenyl)phenoxy]-N,N-diethylethanamine

Pharmacokinetics and Dosage

  • Half-life: 5-6 days
  • Recommended Dose: 12.5-50 mg/day, taken in the morning
  • Suggested PCT Length: 4-6 weeks

Benefits:

Stimulates Testosterone Production Clomiphene is highly effective in increasing both Total and Free Testosterone levels. It is often used as an alternative to testosterone injections for men with hypogonadism. Compared to Tamoxifen, Clomiphene is more efficient at enhancing testosterone levels and improving fertility, making it a mainstay in Post-Cycle Therapy (PCT) protocols for many years. [8]

Potential in Treating Gynecomastia While Clomiphene may be beneficial in treating gynecomastia, it is not as effective as Raloxifene or Tamoxifen in this regard. [9]

Lowers IGF-1 Similar to Tamoxifen, Clomiphene decreases IGF-1 levels, potentially limiting muscle mass gains. This effect can be countered by using MK-677. [10]

Side Effects

Mood Swings and Sexual Dysfunction: Clomiphene is notably associated with severe mood swings, anxiety, and depression in a significant number of users. While it may modestly enhance sexual function in some, it can adversely affect sex drive and erectile function in others. [11] [12]

Hot Flashes and Night Sweats: A small proportion of Clomiphene users may experience hot flashes and night sweats. [13]

Mild Liver Toxicity: The potential elevation of liver enzymes AST and ALT by Clomiphene is noted, but significant liver toxicity is rare. The use of NAC (N-Acetylcysteine) during PCT is recommended as a precaution. [14]

Visual Disturbances: Studies have documented instances of visual disturbances, such as blurring, spots, and flashes, in a minority of Clomiphene users. These side effects typically subside after discontinuation of the drug. [15]

Take Away:

Clomiphene is extremely effective at boosting Total Testosterone and Free Testosterone levels. In fact, it is often prescribed as an alternative to testosterone injections in men with hypogonadism. Clomiphene is reportedly more effective than Tamoxifen at increasing Testosterone levels, and it is also more effective at improving fertility. It has been a staple of PCT protocols for decades.

Toremifene (Fareston)

Chemical Composition: 2-[4-[(Z)-4-chloro-1,2-diphenylbut-1-enyl]phenoxy]-N,N-dimethylethanamine

Pharmacokinetics and Dosage

  • Half-life: 5 days
  • Recommended Dose: 15-60 mg/day, taken in the morning
  • Suggested PCT Length: 4-6 weeks

Benefits:

Stimulates Testosterone Production: Research, including a specific scientific paper, has demonstrated that Toremifene can enhance testosterone levels by promoting the release of LH (Luteinizing Hormone) and FSH (Follicle-Stimulating Hormone). Anecdotal evidence suggests that while Toremifene may not be as potent as Tamoxifen or Clomiphene, it is sufficiently effective to restore testosterone levels following a cycle of mildly suppressive to moderately suppressive SARMs. [16]

Potential in Treating Gynecomastia: Toremifene can be beneficial in treating gynecomastia, although it is less effective compared to Tamoxifen and Raloxifene. Early intervention with Toremifene may reverse gynecomastia, but having Tamoxifen or Raloxifene as alternatives is advisable. [17]

Reduces Cholesterol: Studies indicate that Toremifene is capable of reducing total and LDL cholesterol while potentially increasing HDL cholesterol levels. This makes it advantageous in mitigating the adverse effects of SARMs on lipid profiles. [18]

Side Effects:

Lowers IGF-1: Like other SERMs, Toremifene can decrease levels of IGF-1, which could limit muscle mass gains. The use of MK-677 can help offset this effect. [19]

Mood Swings and Sexual Dysfunction: While these side effects are possible with any SERM, they are infrequently reported by Toremifene users, making it one of the least likely SERMs to cause such issues.

Hot Flashes and Night Sweats: Although rare, Toremifene can cause hot flashes and consequently night sweats in a small percentage of users. [20]

Mild Liver Toxicity: Toremifene has the potential to elevate AST and ALT liver enzymes, but significant liver toxicity is very unlikely. [21] Interestingly, a study highlighted Toremifene’s potential liver-protective effects in alcoholic rats. [22]

Take Away:

Toremifene can increase testosterone by stimulating the release of LH and FSH. Anecdotal information shows Toremifene is not as strong as Tamoxifen or Clomiphene, but it is strong enough to restore Testosterone levels after a mildly or moderately suppressive SARM cycle.

Raloxifene (Evista)

Chemical Composition: [6-hydroxy-2-(4-hydroxyphenyl)-1-benzothiophen-3-yl]-[4-(2-piperidin-1-ylethoxy)phenyl]methanone

Pharmacokinetics and Dosage

  • Half-life: 28-33 hours
  • Recommended Dose: 15-60 mg/day, taken in the morning
  • Suggested PCT Length: 6-12 weeks

Benefits:

Stimulates Testosterone Production: Raloxifene shows some effectiveness in boosting testosterone, but it is generally not considered strong enough for use as a primary Post-Cycle Therapy (PCT) agent. It may be suitable for PCT after a mildly or moderately suppressive cycle, though its primary strength lies in treating gynecomastia. [23]

Treats Gynecomastia Raloxifene is exceptionally effective in both preventing and reversing gynecomastia, outperforming Tamoxifen in this regard. It has shown efficacy in reversing long-standing pubertal gynecomastia. Further details on using Raloxifene for gynecomastia are available in the On-Cycle Therapy chapter. [24]

Reduces Cholesterol Studies have demonstrated Raloxifene’s ability to lower total and LDL cholesterol, contributing to a more favorable lipid profile. [25]

Take Away:

Raloxifene is somewhat effective at boosting Testosterone, but it isn’t strong enough to be used as a PCT. It could work as a PCT after a mildly/moderately suppressive cycle, but you are better off saving it for fighting gynecomastia.

Side Effects

Lowers IGF-1: Raloxifene decreases IGF-1 levels, which may impact muscle mass gains. This effect can be counterbalanced by using MK-677. [26]

Mood Swings and Sexual Dysfunction: Raloxifene does not significantly affect mood according to studies, and instances of sexual dysfunction in men are very rarely reported. [27]

Mild Liver Toxicity: Although Raloxifene may impact liver enzymes, significant liver toxicity is uncommon. [28]

Enclomiphene (Androxal)

Chemical Composition: 2-[4-(2-chloro-1,2-diphenylethenyl)phenoxy]-N,N-diethylethanamine

Pharmacokinetics and Dosage

  • Half-life: 10 hours
  • Recommended Dose: 6.25-25 mg/day, taken in the morning
  • Suggested PCT Length: 4-6 weeks

Benefits:

Stimulates Testosterone Production: Enclomiphene is a potent SERM currently being studied as a treatment for hypogonadism. It is highly effective in boosting testosterone levels and enhancing fertility and sperm count. Anecdotal data also suggest its efficacy as an excellent PCT option and for use during SARM cycles. [29]

Potential in Treating Gynecomastia Though there is no definitive scientific or anecdotal evidence on Enclomiphene’s impact on gynecomastia, its similarity to Clomiphene, which has mild anti-gynecomastia properties, suggests it may also be effective.

Muscle Gains While there is no direct scientific evidence of Enclomiphene inducing muscle growth, its substantial increase in testosterone levels could indirectly contribute to muscle gain, despite the decrease in IGF-1 levels.

Side Effects

Lowers IGF-1: Enclomiphene significantly reduces IGF-1 levels, which could be a limiting factor in muscle development. This side effect might be offset with MK-677. [29]

Mood Swings and Sexual Dysfunction: There is no concrete scientific data regarding Enclomiphene’s impact on mood and sexual function. However, anecdotal reports suggest it may cause mood changes such as increased aggression and impatience, often described as “Roid Rage,” along with a notable increase in libido.

Hot Flashes and Night Sweats: Currently, there is no scientific or anecdotal evidence to suggest that Enclomiphene causes hot flashes and night sweats.

Mild Liver Toxicity: There is no specific information available on Enclomiphene’s hepatotoxicity. However, given the general trend among SERMs and its potency, it is reasonable to assume that Enclomiphene may have a mild impact on liver enzymes. Therefore, monitoring and precautionary measures are advisable.

Take Away:

Enclomiphene is the best SERM to use as a PCT after a SARM cycle, as it is the strongest of the SERMs and very well tolerated.

Enclomiphene is the only SERM that is being seriously studied as a treatment for hypogonadism. It is remarkably effective at increasing testosterone levels, and more and more anecdotal data is coming out confirming that it is an outstanding PCT option. It is so effective that it can and very often does increase testosterone levels beyond the reference range.

NOTE: The previously mentioned SERM “Clomid” consists of two isomers: Zuclomiphene and Enclomiphene. Zuclomiphene causes moodiness, whereas Enclomiphene causes a boost in testosterone.

When is PCT Necessary?

Whether you need to do a PCT for your SARM cycle depends on the level of suppression the cycle has caused. In general, you will have to do a PCT for most SARM cycles, but there are a few exceptions.

The compounds that are known to be more mild or even moderate at testosterone suppression are a bit tricky to deal with when doing a PCT. The best way to determine if you need to run a PCT is by doing bloodwork, regardless of how you feel or how confident you are about your ability to recover naturally.

Mildly Suppressive SARMs Include:

  • Ostarine
  • Andarine
  • ACP-105
  • AC-262-536

Moderately Suppressive SARMs Include:

  • Testolone
  • Ligandrol

The table below illustrates how you should determine whether a PCT is necessary for you based on the bloodwork markers used to determine suppression and whether symptoms of testosterone suppression are present:

Bloodwork Shows:Symptoms of Suppression:PCT:
Total Testosterone & LH within reference range (even if close to bottom)NoNo
Total Testosterone & LH within reference range (even if close to bottom)YesYes
Total Testosterone & LH below reference rangeDoesn’t MatterYes
Can’t Do Bloodwork (For Whatever Reason)NoOptional
Can’t Do Bloodwork (For Whatever Reason)YesYes

Highly suppressive SARMs, will always require a PCT. These include:

  • LGD-3303
  • S-23
  • YK-11

Since these are strong enough to completely shut you down, you’ll also be doing a testosterone base.

If you use Enclomiphene as a test base and you feel good/bloodwork shows LH and Testosterone within the reference ranges only then can you get away with a 2-week post-cycle therapy. If not you will have to go through the full 4 weeks of PCT, although it is very rare.

If something else is used as a test base you will have to do a full 4-week PCT with a SERM.

NOTE: You must PCT if stacking multiple SARMs regardless of which you use!

How to take SERMs

All of the SERMs are administered orally, at the same time everyday. I recommend taking them first thing in the morning to keep the timing consistent.

As a PCT, start taking the SERM the first day after your cycle, and take it for 2, 3, or 4 weeks depending on the suppression level of your cycle.

For Mildly Suppressive SARMs

For mildly suppressive SARMs (Ostarine, Andarine, ACP-105, AC-262 536) any of the SERMs can work could work as a PCT. Though ideally Enclomiphene, Tamoxifen, and Toremifene.

Pick one:

 

WEEK 1

WEEK 2

WEEK 3

TAMOXIFEN

10mg/day

10mg/day

5mg/day

ENCLOMIPHENE

6.25mg/day

6.25mg/day

3.125mg/day

TOREMIFENE

30mg/day

30mg/day

15mg/day

CLOMIPHENE

25mg/day

25mg/day

12.5mg/day

RALOXIFENE

30mg/day

30mg/day

15mg/day

Clomiphene and Raloxifene will work, but I would avoid them as you would feel way better on any of the other ones.

Enclomiphene can even raise your testosterone levels above the reference range and help you build muscle even after the cycle. Not to mention that you’ll feel amazing.

For Moderately Suppressive SARMs

For moderately suppressive SARMs (RAD-140 or LGD-4033) you will still be using only one SERM, but at a higher dose and for a longer period of time. 

Any one of the SERMs will work, although I would avoid Raloxifene over any of the others.

The best options are Tamoxifen or Enclomiphene. Toremifene could still work although you will feel way better on the other two. Clomiphene could also work but if you have access to Enclomiphene I see no reason to use it.

Pick one:

 

WEEK 1

WEEK 2

WEEK 3

WEEK 4

TAMOXIFEN

20mg/day

20mg/day

20mg/day

10mg/day

ENCLOMIPHENE

12.5mg/day

12.5mg/day

12.5mg/day

6.25mg/day

TOREMIFENE

30mg/day

30mg/day

30mg/day

15mg/day

CLOMIPHENE

50mg/day

50mg/day

50mg/day

25mg/day

RALOXIFENE

60mg/day

60mg/day

60mg/day

30mg/day

For Highly Suppressive SARMs

For highly suppressive SARMs (LGD-3303, S-23, YK-11) you will need to run two SERMs. Although there is enough anecdotal evidence that just using Enclomiphene can also work, but only if it was also used as a testosterone base as well (on cycle to mitigate the suppression).

These kinds of cycles are usually followed by a Tamoxifen + Clomiphene PCT, but you can replace the Clomiphene with Enclomiphene.

Enclomiphene + Raloxifene or Toremifene combos may work, but I wouldn’t go with them since the better alternative exists. Avoid any other combination.

Pick one:

 

WEEK 1

WEEK 2

Week 3

Week 4

TAMOXIFEN

20mg/day

20mg/day

20mg/day

10mg/day

ENCLOMIPHENE

12.5mg/day

12.5mg/cay

12.5mg/day

6.25mg/day

 

WEEK 1

WEEK 2

Week 3

Week 4

TAMOXIFEN

20mg/day

20mg/day

20mg/day

10mg/day

CLOMIPHENE

50mg/day

50mg/cay

50mg/day

25mg/day

 

WEEK 1

WEEK 2

Week 3

Week 4

RALOXIFENE

60mg/day

60mg/day

60mg/day

30mg/day

ENCLOMIPHENE

12.5mg/day

12.5mg/cay

12.5mg/day

6.25mg/day

 

WEEK 1

WEEK 2

Week 3

Week 4

TOREMIFENE

30mg/day

30mg/day

30mg/day

15mg/day

ENCLOMIPHENE

12.5mg/day

12.5mg/cay

12.5mg/day

6.25mg/day

Conclusion

The first and most important thing is to have a SERM at your disposal even before you start your cycle, no matter how confident you are in your ability to naturally recover your testosterone levels.

Always do bloodwork, at the very least once per cycle, ideally twice. Once before and once after your cycle. This is the only way to accurately determine whether you need to PCT or not.

Finally, you know know how to effectively do a PCT after ANY SARM cycle based on the most effective and established PCT practices. Bookmarks this page and refer to the dosing tables when needed.

Happy cycling.

References

  1. The Role of Estrogen Modulators in Male Hypogonadism and Infertility
  2. Treatment of gynecomastia with tamoxifen: a double-blind crossover study
  3. Effect of tamoxifen on serum cholesterol and lipoproteins during chemohormonal therapy
  4. Effect of low dose tamoxifen on the insulin-like growth factor system in healthy women
  5. Mental Fog with Tamoxifen is Real; Scientists Find Possible Antidote
  6. Tamoxifen, hot flashes and recurrence in breast cancer
  7. Correlation of the tamoxifen use with the increased risk of deep vein thrombosis and pulmonary embolism in elderly women with breast cancer
  8. Clomiphene increases free testosterone levels in men with both secondary hypogonadism and erectile dysfunction: who does and does not benefit?
  9. Clomiphene in the treatment of adolescent gynecomastia. Clinical and endocrine studies
  10. Clomiphene citrate increases insulin-like growth factor binding protein-1 and reduces insulin-like growth factor-I without correcting insulin resistance associated with polycystic ovarian syndrome
  11. Clomiphene-lnduced Mood Swings
  12. Clomiphene increases free testosterone levels in men with both secondary hypogonadism and erectile dysfunction: who does and does not benefit?
  13. Use of clomiphene citrate in infertile women: a committee opinion
  14. Clomiphene has been linked to a low rate of transient serum aminotransferase elevations during therapy and to rare instances of clinically apparent liver injury, which can be severe and even fatal.
  15. Association between Clomiphene Citrate and Visual Disturbances with Special Emphasis on Central Retinal Vein Occlusion: A Review 
  16. The beneficial effects of toremifene administration on the hypothalamic-pituitary-testicular axis and sperm parameters in men with idiopathic oligozoospermia
  17. Phase III ADT trial demonstrates improvement in gynecomastia in men on toremifene 80 mg compared to placebo
  18. Toremifene improves lipid profiles in men receiving androgen-deprivation therapy for prostate cancer: interim analysis of a multicenter phase III study
  19. Effects of Toremifene, a Selective Estrogen Receptor Modulator, on Spontaneous and Stimulated GH Secretion, IGF-I, and IGF-Binding Proteins in Healthy Elderly Subjects
  20. Toremifene in postmenopausal breast cancer. Efficacy, safety and cost
  21. Toremifene Hepatoxicity
  22. The antiestrogen toremifene protects against alcoholic liver injury in female rats
  23. Effects of raloxifene on gonadotrophins, sex hormones, bone turnover and lipids in healthy elderly men
  24. Beneficial effects of raloxifene and tamoxifen in the treatment of pubertal gynecomastia
  25. Effects of raloxifene on lipid and lipoprotein levels in postmenopausal osteoporotic women with and without hypertriglyceridemia
  26. Raloxifene decreases serum IGF-I in male patients with active acromegaly
  27. Mood effect of raloxifene in postmenopausal women
  28. Serum enzyme elevations are uncommon during raloxifene therapy and are rarely dose limiting.
  29. Testosterone restoration using enclomiphene citrate in men with secondary hypogonadism: a pharmacodynamic and pharmacokinetic study

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