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SARMs

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SARMs were discovered in the late 1990’s.They may have an application in treatments of various diseases, including muscle wasting, cancer cachexia, breast cancer, osteoporosis, andropause and sarcopenia. The androgen receptor (AR) is a member of the steroid hormone receptor family that plays important roles in the physiology and pathology of various tissues. AR ligands, which include circulating testosterone and dihydrotestosterone bind to activate the AR to cause cellular signaling.

SARMs provide the benefits of traditional anabolic/androgenic steroids such as testosterone (including increased muscle mass, fat loss, and bone density) while having a lower tendency to produce the unwanted side effects of steroids (aromatization / increased DHT). By acting/stimulating on the androgen receptor, SARMs can provide a similar therapeutic outcome to androgen therapy without any increase in androgen levels. SARMs have the potential to take the place of the androgens, and therefore exert many of the same positive effects on muscle tissue as anabolic steroids like testosterone. 

Benefits of SARMs:

  • Provides benefits of anabolic/androgenic steroids such as testosterone
  • Increased fat loss
  • Increased lean muscle mass
  • Increased bone density
  • Fewer side effects compared to steroids, including prostate and cardiovascular outcomes
  • Not liver toxic like other oral steroids
  • Anabolic effect noted to be similar to testosterone
  • Used for rehab of injuries, particularly bone and tendon related injuries

There are two SARMs available for prescription. Our pharmacy is one of the only facilities in the world equipped with an HPLC and mass spectrometer that allows them to complete potency testing in house and verify the authenticity and assay of everything that they make. All of their raw ingredients are accompanied with certificates of analysis. They are all quarantined, tested and must achieve an assay greater than 98% prior to use.

Ligandrol (LGD 4033)

Ligandrol is a SARM discovered by Ligand Pharmaceuticals. It is administered orally and is not liver toxic like most oral steroids are. It binds to the androgen receptor with an extremely high affinity and selectivity, and once it does this it exerts exceptional anabolic effects in muscle and bone. LGD-4033 has an anabolic/androgenic ratio of around 10:1 ratio. For the sake of comparison, the same ratio for pure testosterone is 1:1. That means the anabolic potential is 10 times stronger than testosterone. 

In studies Ligandrol has shown a dose-dependent suppression of total testosterone from baseline to 21 days. Ligandrol did not always result in fat loss in the studies, it mainly promoted muscle growth and a dose related increase in lean body mass. From one study the increase in strength measured by stair climbing speed and power also showed improvement. LGD-4033 displayed an immediate effect on hormones in the body from the time it was taken. The research showed gains in lean muscle mass within the 21 days of the study. Adverse effects were not noted. LGD-4033 displayed a prolonged elimination half- life of 24-36 hours. Upon discontinuation of LGD- 4033 the hormone levels returned to baseline by day 56.

LGD-4033 is mostly used for size and strength gains/bulking. It has an unmatched ability to build muscle mass relative to other SARMs. Milligram for milligram, it even outperforms many of the most potent anabolic androgenic steroids.

Ostarine (MK-2866) (Enobosarm)

Ostarine is the most well-known SARM, and it is also the most research backed. This selective androgen receptor modulator (SARM) has been studied and proven to improve lean body mass and physical function. It also increases tendon strength, ligament health, bone density and encourages collagen turn-over. It is one of the least suppressive and minimally androgenic, making it a prime candidate for therapeutic purposes moving forward, and assisting in muscle retention/growth without the ramifications of severe androgen related side effects. 

Studies involving Ostarine have been positive. Merck presented the results of a phase 2 clinical trial evaluating Ostarine (MK-2866) in patients with cancer induced muscle loss (cancer cachexia) at the Endocrine Society Annual Meeting in Washington in 2009. 159 cancer patients were randomized and received placebo, 1mg or 3mg Ostarine daily for 16 weeks. Ostarine treatment led to significant increases in lean body mass (LBM) and improvement in muscle performance measured by stair climbing in patients. Another study showed significant improvement in the ability of healthy, elderly men and women to climb stairs in a phase2A study. Elderly men and women improved climbing stairs in speed and power, accompanied by significant increases in LBM and decreases in fat mass after only 86 days. Enobasarm is the most well characterized clinically and has consistently demonstrated increases in LBM and better physical function across several populations, along with a lower hazard ratio for survival in cancer patients.

Ostarine (MK-2866) is mainly used for cutting (dropping body fat) with muscle and strength preservation but also for re-composition (gaining muscle and losing body fat simultaneously). Muscle preservation is the goal while cutting, not building muscle and strength. Often times when we are at a calorie deficit for weight loss we also lose some muscle mass. Ostarine helps prevent this from happening while at the same time helping prevent water retention. During re-composition, calories should be adequate for weight maintenance, not weight loss. 

Treatment time:

Most SARM cycles are done for 6-8 weeks. Suppression of natural testosterone can occur with both SARMS. Low-Testosterone related sexual dysfunction and other androgen deficiency related side effects are less likely to occur with Ostarine, they are reported more often from Ligandrol users. If you are already on testosterone therapy, you would simply continue that treatment at the same time. Completing a PCT (post cycle therapy) protocol is recommended in both cases after completing the 6-8 weeks of treatment.

Differences and side effects between LGD-4033 And Ostarine:

  • Ostarine is a SARM that was developed for treating both muscle-wasting and osteoporosis. On the other hand, LGD-4033 was developed to treat muscle mass because of different health related complications.
  • Ostarine is minimal suppressive and LGD-4033 is comparatively more suppressive.
  • Ostarine has a half-life of 20-24 hours while LGD-4033 has a half-life of 24-26 hours.
  • Ostarine use can lead to a slight hike in the levels of estrogen while Ligandrol use can cause a slight reduction in the levels of Sex hormone-binding globulin and testosterone.
  • LGD-4033 is more suited for users who have already dabbed into a few cycles of SARMs. Ostarine, on the other hand, is ideal for both beginners as well as experienced users.
  • LGD-4033 includes ingredients for the processes of muscle recovery while MK-2866 treats muscle loss as well as osteoporosis.
  • MK-2866 is ideal for cutting cycles and LGD-4033 is best suited for bulking cycles.
  • Both Ostraine (MK-2866) and Ligandrol (LGD-4033) are remarkable for their own benefits and the final selection between the two entirely depends on the specific requirements of users. 

Research:

J Gerontol A Biol Sci Med Sci. 2013 Jan;68(1):87-95. doi: 10.1093/gerona/gls078. Epub 2012 Mar 28.The safety, pharmacokinetics, and effects of LGD-4033, a novel nonsteroidal oral, selective androgen receptor modulator, in healthy young men.

Basaria S, Collins L, Sheffield MM, Dillon EL, Orwoll K, et al. (2011) Safety and Tolerability of LGD-4033, a Novel-Non-Steroidal Selective Androgen Receptor Modulator (SARM) in Healthy Men. The Endocrine Societys 93rd Annual Meeting & Expo June 4-7 Boston, USA.

Bhasia S, Calof OM, Storer TW, Martin L, Norman AM, et al. (2006) Drug insight:Testosterone and selective androgen receptor modulators as anabolic therapies for chronic illness and ageing. Nature Clinical Practice Endocrinology & Metabolism 2(3): 146-159.

Dalton JT, Taylor RP, Mohler M, Steiner MS (2013) Selective androgen receptor modulators for the prevention and treatment of muscle wasting associated with cancer. Curr Opin Support Palliat Care 7(4): 345-351.

Dalton JT (2007) Therapeutic Promise of Selective Androgen Receptor Modulators (SARMs): Preclinical and Clinical Proof-of –Concept Studies. Annual Meeting of the Endocrine Society 41-42.

Crawford J, Prado CM, Johnston MA, Richard JG, Ryan PT, et al. (2016) Stydy Design and Rationale for the Phase 3 Clinical DEvelopment Program of Enobosarm, a Selective Androgen Receptor Modulator for the Prevention and Treatment of Muscle Wasting in Cancer Patients (POWER Trials). Curr Oncol Rep 18: 37.

Miner JN, Chang W, Chapman MS, Finn PD, Hong MH, et al. (2007) An orally active selective androgen receptor modulator is efficacious on bone,muscle and sex function with reduced impact on prostate. Endocrinology 148(1): 363-373.

Ostarine increases lean body mass and improves physical performance in healthy elderly subjects: Implications for cancer cachexia patients. W. Evans, M. R. Smith, J. E. Morley, K. G. Barnette, D. Rodriguez, M. S. Steiner, and J. T. Dalton. Journal of Clinical Oncology 2007 25:18_suppl, 9119-9119. J Med Chem. 2009 Jun 25;52(12):3597-617. doi: 10.1021/jm900280m.

Nonsteroidal selective androgen receptor modulators (SARMs): dissociating the anabolic and androgenic activities of the androgen receptor for therapeutic benefit. Mohler ML1, Bohl CE, Jones A, Coss CC, Narayanan R, He Y, Hwang DJ, Dalton JT, Miller DD.