The Fall of SARMs

The Fall of SARMs

The Fall of (SARMs)

Top 4 Supplement Alternatives You Can Take.

Written by naturopathy and formulation expert Bryce La Grange

 

We’ve all heard of SARMs. They popped up a few years ago online and in stores, and have been making the rounds sold as ‘side effect free steroids’. But how much do we really know about them? Not much, actually. They are research chemicals after all, and most have been dropped by the pharmaceutical companies making them, for reasons we may never know. In this article we'll have a look at three popular SARMs and two popular ergogenics, which are usually branded under the SARM category.

What is a SARM?

Selective androgen receptor modulators (SARMs) are non-steroidal compounds that produce anabolic effects in bone and muscle without the side effects that typically come with using testosterone or synthetic androgens. A perfect SARM – one that binds only to androgen receptors and nothing else – would improve muscle strength and size without adversely affecting the prostate, blood markers or blood pressure, keeping a healthy head of hair and no other nasties. It should also mitigate any effect on the endocrine system, leaving gonadal function and fertility intact.

Are SARMs legal?

Yes, if you obtain a prescription. They reside in a legal grey area, since they are technically research chemicals, but they are still subject to WADA anti-doping rules. A doctor’s prescription is required for most.

Are SARMs effective?

SARMs have been proven to be effective, however they are currently banned from sale over the counter. Luckily supplements are so advanced that you can achieve similar results using natural raw ingredients such as Turkesterone - without resorting to banned substances. Despite this there are still a number of SARMs making the rounds today. Few have been tested even in animal models, let alone human models. Two compounds that have been human tested are Ligandrol (LGD-4033) and enobosarm (ostarine, MK-2866, S-22).

Enobosarm (ostarine, MK-677, S22)

Enobosarm tested in elderly subjects produced an average lean mass increase of a 1.2kg and lost 0.3kg of fat mass. The highest-dose group performed best in the stair-climb challenge, while the lowest-dose group performed even worse than placebo. Enobosarm reduced serum HDL, FSH, LH, estradiol, and the reduction in SHBG exceeds the reduction observed in men taking 600mg testosterone.[1][3][9] It's unclear what the implications of this may be, since SHBG is not just a carrier or a “deactivator”, and plays an important role in tissue-selective delivery of steroids.[10] Side effects such as diarrhoea, nasopharyngitis and headache were the most common, which is not so surprising given the structural likeness SARMs have to so many other drugs. 

Ligandrol (LGD-4033)

Similar results to Enobosarm were seen with Ligandrol. The suppression of natural hormones is a persistent problem with administering exogenous hormones in younger males, and the same problem emerged here. Healthy male adults given the highest dose of Ligandrol experienced an average lean mass gain of 1.2kg, but they also lost half of their total testosterone, half of their free testosterone, 30% of their LH and almost all of their SHBG. A decrease in HDL and an increase in LDL was also observed. All values returned to normal 5 weeks after the last dose.[3]

RAD140

No human studies are available to reference however anecdotal evidence shows that this SARM is similar to the ones mentioned above as it causes significant shut down of natural hormone production.

Cardarine (Endurobol, GW501516)

Cardarine is known as the ‘fat loss’ and ‘endurance enhancing’ compound. Cardarine acts on the PPAR receptor family, increasing energy expenditure and fatty acid oxidation in muscle tissue. Results were promising, as Cardarine decreased adipose tissue and favorably altered lipid profiles by increasing HDL and lowering VLDL. Trials were halted and the drug was abandoned in 2007 due to fibrosis of liver tissue and aggressive, multi-organ tumor growth in rodents.

Ibutamoren (MK-677)

Known as “the poor man's HGH”, this is an oral, long-acting GH secretagogue. Similar to SARMs, the drug was intended for use in elderly or GH-deficient populations. Unlike rHGH with its single 191aa isoform, these pulsed secretions include all the natural GH isoforms, some of which we know little about, and the frequency and amplitude of each pulse is further increased by Ibutamoren. Basal IGF-1 is elevated, however the elevation is not outside of normal parameters.[4]

The use of Ibutamoren in individuals without GH deficiencies may create excessive elevations of GH and IGF-1 throughout the day. GH powerfully stimulates lipolysis, filling the blood with fatty acids that interfere with blood sugar signaling, and IGF-1 is both anti-apoptotic and mitogenic, two things that you really don't need if you want to stay away from diabetes and reduce cancer risk.[5][6][7]

Do SARMs work?

SARMs definitely make elderly subjects stronger, and they undoubtedly demonstrate tissue selectivity[2], but beyond that it is clear that these current SARMs – at least those tested – has little to offer the healthy adult and too many down sides, especially to those looking for a performance edge or something to increase muscle mass. Both adult and elderly subjects received side effects that were similar to testosterone usage, with only 15% of the lean mass gains.

Alternatives to SARMs

A better approach is to increase natural androgens (testosterone, decrease estrogen). Small things like getting to sleep early and getting plenty of daylight exposure are not small things at all (refer to my blog 'Premature Aging'). Attack all three areas and you will see significant improvements in energy, stamina, strength, mood and recovery. So what else is there? What is the safe alternative which will help me achieve my goals.

What legal alternatives to SARMs can I take? 

Gen-Tech Male Fuel

Male Fuel is quite possibly the best natural replacement for a SARM, particularly Ostarine or GH-Pep. Male fuel provides you with clinically dosed ZMA to better sleep quality plus huge amounts of herbal blend to increase your natural testosterone production. One of the best on the market due to all ingredients being clinically dosed
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ATP Science Alpha Jupiter
 
Alpha Jupiter is next level. All ingredients have been TGA approved prior to production and as you know ATP Science offers the most advanced and researched naturopathic formula’s on the market. Try this phenomenon now and boost your testosterone by 20%, increase energy, improve mental clarity and focus, anti oxidant, anti inflammatory and boost immune support
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Emrald Labs Turkesterone

Turkesterone is a naturally occurring extract that mimics the effects of anabolic steroids, but without the negative side effects. While it is not a testosterone booster, we included it on this list due to it's muscle building properties.


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Switch Nutrition – Vitality Switch
This product is not marketed as a testosterone booster, however, it does exactly switch-nutrition-vitalityas the product says – increases vitality. While not directly increasing testosterone, this product will work to optimize liver function, increase the rate of detoxification, improve gut health, oppose estrogen synthesis, enhance nutrient absorption from food, and favourably alter your gut bacteria. By doing this, the bodily systems will vastly improve, indirectly increasing testosterone, balancing and detoxifying estrogen, cleansing the liver and nourishing the body with all the required nutrients that we need.



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REFERENCES

  1. Dalton J T, et al. (2011) The selective androgen receptor modulator GTx‐024 (enobosarm) improves lean body mass and physical function in healthy elderly men and postmenopausal women: results of a double‐blind, placebo‐controlled phase II trial, The Journal of Cachexia Sarcopenia and Muscle, Vol 2 Issue 1, pages 153-161
  2. Miner J N, et al. (2007) An Orally Active Selective Androgen Receptor Modulator Is Efficacious on Bone, Muscle, and Sex Function with Reduced Impact on Prostate, Endocrinology, Vol 148 Issue 1, pages 363-373
  3. Basaria S, et al. (2010) The Safety, Pharmacokinetics, and Effects of LGD-4033, a Novel Nonsteroidal Oral, Selective Androgen Receptor Modulator, in Healthy Young Men, The Journals of Gerontology, Vol 68 Issue 1, pages 87-95
  4. 4Copinschi G, et al. (1996) Effects of a 7-day treatment with a novel, orally active (GH) secretagogue, MK-677, on 24-hour GH profiles, IGF-1, and adrenocortical function in normal young men, The Journal of Clinical Endocrinology & Metabolism, Vol 81 Issue 8, pages 2776-2782
  5. Chhabra Y, Waters M J, Brooks A J (2011) Role of the GH–IGF-1 axis in cancer, Expert Review of Endocrinology & Metabolism, Vol 6 Issue 1, pages 71-84 DOI: 10.1586/eem.10.73
  6. Tentori L, Graziani G (2007) Doping with GH/IGF-1, anabolic steroids or erythropoietin: is there a cancer risk?, Pharmacological Research, Vol 55 Issue 5, pages 359-369
  7. Yakar S, et al. (2004) Inhibition of GH action improves blood sugar sensitivity in liver IGF-1-deficient mice, The Journal of Clinical Investigation, Vol 113 Issue 1, pages 96-105
  8. Salgado R M, et al. (2017) Effect of oral administration of Tribulus terrestris extract on semen quality and body fat index of infertile men, Andrologia, Vol 49 Issue 5, org/10.1111/and.12655
  9. Bhasin S, et al. (1996) The Effects of Supraphysiologic Doses of Testosterone on Muscle Size and Strength in Normal Men, The New England Journal of Medicine, DOI: 10.1056/NEJM199607043350101
  10. Fortunati N (1999) SHBG: not only a transport protein. What news is around the corner?, Journal of Endocrinological Investigation, Vol 22 Issue 3, pages 223-234 
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