Selective Androgen Receptor Modulators (SARMs)

LIGANDROL AND OSTARINE

SARMs were discovered in the late 1990s. They may have applications in treating various conditions, 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 and activate the AR to trigger cellular signaling.

SARMs are not currently approved by the FDA for human use. At TransformYou, they are prescribed through licensed pharmacies and administered under physician-supervised hormone optimization care.

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 and increased DHT). By binding to and stimulating the androgen receptor, SARMs can produce a therapeutic outcome similar to androgen therapy without increasing androgen levels. SARMs have the potential to take the place of androgens, exerting 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 reduced impact on prostate and cardiovascular health
• 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, allowing it to complete potency testing in-house and verify the authenticity and assay of everything it makes. All raw ingredients are accompanied by certificates of analysis, and each is quarantined, tested, and required to reach an assay greater than 98% before use.

Ligandrol (LGD-4033) — available in 1, 2, 5, and 10 mg capsules

Ligandrol is a SARM discovered by Ligand Pharmaceuticals. It's administered orally and, unlike most oral steroids, is not liver-toxic. It binds to the androgen receptor with high affinity and selectivity, producing pronounced anabolic effects in muscle and bone.

LGD-4033 has an anabolic/androgenic ratio of around 10:1; for comparison, the same ratio for pure testosterone is 1:1, meaning its anabolic potential is roughly 10 times stronger than testosterone.

In studies, Ligandrol has shown a dose-dependent suppression of total testosterone from baseline through 21 days. It didn't always result in fat loss, but it consistently promoted muscle growth and a dose-related increase in lean body mass. One study also found improvements in strength, measured by stair-climbing speed and power.

LGD-4033 affected hormone levels almost immediately after administration, with gains in lean muscle mass showing up within the 21-day study period, and no adverse effects noted. It has a prolonged elimination half-life of 24-36 hours; upon discontinuation, hormone levels returned to baseline by day 56.

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

Ostarine (MK-2866, also known as Enobosarm) — currently available in 2, 5, 10, and 25 mg

Ostarine is the most well-known SARM and also the most research-backed. This selective androgen receptor modulator has been studied and shown to improve lean body mass and physical function. It also increases tendon strength, ligament health, bone density, and collagen turnover.

Ostarine is one of the least suppressive and minimally androgenic SARMs, making it a strong candidate for therapeutic use while helping preserve or build muscle without the more severe androgen-related side effects.

Studies involving Ostarine have been positive. Merck presented results from a phase 2 clinical trial evaluating Ostarine (MK-2866) in patients with cancer-induced muscle loss (cancer cachexia) at the Endocrine Society's Annual Meeting in Washington in 2009. In the trial, 159 cancer patients were randomized to receive a placebo, 1 mg of Ostarine, or 3 mg of Ostarine daily for 16 weeks. Ostarine treatment led to significant increases in lean body mass (LBM) and improved muscle performance, measured by stair-climbing ability.

A separate phase 2A study found similar improvements in healthy, elderly men and women, who saw better stair-climbing speed and power alongside significant increases in LBM and decreases in fat mass after only 86 days. Enobosarm is among the most clinically well-characterized SARMs, with consistent evidence of increased LBM and improved physical function across several populations, along with a lower mortality hazard ratio in cancer patients.

Ostarine (MK-2866) is mainly used for cutting (dropping body fat) while preserving muscle and strength, but it's also used for recomposition (gaining muscle and losing body fat at the same time). During cutting, the goal is muscle preservation rather than muscle growth; often, a calorie deficit for weight loss also causes some muscle loss, and Ostarine helps prevent that while also reducing water retention. During recomposition, calories should be adequate for weight maintenance, not weight loss.

Treatment Time

Most SARM cycles run 6-8 weeks. Suppression of natural testosterone can occur with both SARMs. Low-testosterone-related sexual dysfunction and other androgen-deficiency side effects are less likely with Ostarine; they're reported more often among Ligandrol users.

If you're already on testosterone replacement therapy, you'd simply continue that treatment alongside SARM therapy. A PCT (post-cycle therapy) protocol is recommended in both cases after the 6-8 week treatment period.

Differences and Side Effects Between Lgd-4033 and Ostarine

• Ostarine was developed to treat muscle wasting and osteoporosis, while LGD-4033 was developed primarily to address muscle loss related to various health complications.
• Ostarine is minimally suppressive, while LGD-4033 is comparatively more suppressive.
• Ostarine has a half-life of 20-24 hours, while LGD-4033 has a half-life of 24-36 hours.
• Ostarine use can lead to a slight increase in estrogen levels, while Ligandrol use can cause a slight reduction in sex hormone-binding globulin and testosterone levels.
• LGD-4033 is better suited for users who have already completed a few cycles of SARMs, while Ostarine is ideal for both beginners and experienced users.
• LGD-4033 primarily supports muscle recovery, while MK-2866 addresses muscle loss and osteoporosis.
• MK-2866 is ideal for cutting cycles, while LGD-4033 is best suited for bulking cycles.
• Both Ostarine (MK-2866) and Ligandrol (LGD-4033) offer distinct benefits, and the right choice between the two depends entirely on the specific needs of the user.

Considering SARM Therapy?

SARM therapy is one of several options TransformYou may consider as part of physician-supervised hormone optimization, based on a full evaluation of your health history, goals, and candidacy. Schedule a consultation with our care team to find out whether Ligandrol or Ostarine fits your treatment plan.

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 Society's 93rd Annual Meeting & Expo, June 4-7, Boston, USA.

Bhasin 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 aging. 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) Study 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.

Evans W, Smith MR, Morley JE, Barnette KG, Rodriguez D, Steiner MS, Dalton JT. Ostarine increases lean body mass and improves physical performance in healthy elderly subjects: Implications for cancer cachexia patients. 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 ML, Bohl CE, Jones A, Coss CC, Narayanan R, He Y, Hwang DJ, Dalton JT, Miller DD.