In the ever-evolving world of fitness and bodybuilding, Ligandrol has emerged as a powerful ally for those seeking to elevate their muscle growth and enhance performance. This selective androgen receptor modulator (SARM) is gaining attention for its ability to promote lean muscle gains while minimizing the risk of unwanted side effects often associated with traditional anabolic steroids.

Whether you’re a seasoned athlete or just starting your fitness journey, understanding the benefits of Ligandrol can be a game changer. This ultimate guide will explore how this compound works, its advantages, and how to incorporate it into your regimen safely and effectively.

Prepare to unlock your potential as we delve into the science behind Ligandrol and discover how it can transform your fitness aspirations into reality. Embrace the opportunity to elevate your training and redefine your limits!

SARMS or selective androgen receptor modulators are highly selective non-steroidal anabolic compounds. Commonly used by athletes, or bodybuilders studies have shown that SARMS and specifically Lingadrol, have high anabolic activity and can facilitate the growth of muscle

What Is Lingandrol, LGD-4033 

Ligandrol, or more commonly known as LGD-4033, is a non-steroidal selective androgen receptor modulator (SARM) currently under investigation for the treatment of muscle wasting, osteoporosis, and other clinical indications. Ligandrol was discovered and created by Ligland Pharmaceuticals and is currently under development by Viking Therapeutics and is now branded as VK5211.

How Does Ligandrol, LGD-4033 Work

Ligandrol, also known as LGD-4033, is a selective androgen receptor modulator (SARM) that has captivated the fitness community with its impressive potential for muscle growth and performance enhancement. Unlike traditional anabolic steroids, which can affect a broad range of tissues, Ligandrol specifically targets androgen receptors in muscle and bone, thereby minimizing undesirable side effects. The precision of SARMs in selectively modulating these receptors is what makes Ligandrol a promising alternative for athletes and bodybuilders.

At a molecular level, Ligandrol binds to the androgen receptors in muscle and bone tissues, just like natural testosterone. This binding activates the receptors, leading to an increase in protein synthesis and muscle growth. The process, known as anabolic activity, is crucial for anyone looking to build muscle and improve strength. The specificity of Ligandrol allows it to promote these anabolic effects without significantly impacting other tissues, such as the liver or prostate, which are commonly affected by anabolic steroids.

Moreover, Ligandrol has been shown to have a high oral bioavailability, meaning it can be effectively absorbed when taken in pill form, eliminating the need for injections. This convenience, combined with its potent muscle-building capabilities, makes Ligandrol a highly attractive option for those committed to improving their physical performance. The science behind Ligandrol underscores its potential as a game-changing supplement in the realm of fitness and bodybuilding.

Like other SARMS, Ligandrol binds androgen receptors with high affinity and selectivity. 

How Do SARMS Work?

SARMS were developed in the early 2000s, in an attempt to overcome the pharmacologic and pharmacokinetic limitations of steroidal androgen receptor agonists (i.e., testosterone and DHT), which have known associations with liver and heart disease [R]. SARMS have been investigated for several indications including muscle wasting (cachexia), sarcopenia, osteoporosis, stress urinary incontinence, erectile dysfunction, symptomatic benign prostatic hyperplasia, Alzheimer’s disease, muscular dystrophy, breast cancer [R].

SARMS are not anabolic steroids; rather, they are synthetic ligands that bind to androgen receptors. Depending on their molecular structure, they act as agonists, partial agonists, and antagonists. It is thus in a selective manner, that SARMS modulate or mediate coregulators and transcription factors or signaling cascade proteins to promote anabolic activity.

Unlike anabolic steroids which bind to androgen receptors in many tissues all over the body, individual SARMs selectively bind to androgen receptors in certain tissues, but not in others. Nonetheless, they are still exhibit androgenic and anabolic effects.

Androgen receptors are ubiquitous in muscle tissue and bone, thus making them highly receptive to activate or be inhibited my anabolic agents, creating undesirable systemic effects.  SARMS have a high binding affinity for muscle tissue and bone, in a dose dependent selective manner, thus limiting growth in undesirable tissue, such as the prostate.

Nonsteroidal SARMS serve as alternative to anabolic-androgenic steroids, with fewer limitations, also exhibiting high-bioavailability.

All SARMS bind to androgen receptors and display tissue-selective activation of androgenic signaling. Non-steroidal SARMS do not serve as substrates CYP19 aromatase or 5-alpha reductase, as full agonists in muscle and bone, and partial agonists in prostate.

Thus, SARMs do not undergo aromatization to estrogen or 5-alpha reduction which may contribute to their prostate-sparing effect. Nonsteroidal SARMs also exhibit diminished androgenic activity because they are not metabolized to dihydrotestosterone (DHT).

Unique interactions of SARM ligands with androgen receptor result in specific conformational change in the androgen receptor protein, recruitment of a unique repertoire of co-regulator proteins thus contributing to their tissue-specific transcriptional regulation of gene expression

Individual SARMS do, however, have different etiologies, to some degree.

Each SARM-AR complex possesses a different conformation, and various tissues (e.g., skeletal muscle, bone, prostate, brain, skin, liver) display a unique pattern of AR expression.

Ligandrol Benefits

Increases Lean Muscle Mass

One of the primary reasons Ligandrol has garnered attention is its ability to promote significant muscle growth. Users often report noticeable increases in lean muscle mass within just a few weeks of starting a Ligandrol cycle. This rapid muscle gain is attributed to the compound's ability to enhance protein synthesis, which is essential for muscle repair and growth. By accelerating this process, Ligandrol helps users achieve their muscle-building goals more efficiently than through training alone.

Of all investigational SARMS, preclinical trials have shown that Lingadrol has the highest anabolic activity, with greater than 500:1 anabolic to androgenic selectivity.

A Phase 1, 21 day study was completed to determine and evaluate the safety, tolerability, pharmacokinetics, and efficacy of ascending doses of LGD-4033,  lean body mass, muscle strength, stair-climbing power, and sex hormones [R].

76 healthy men, ages (21–50 years) were randomized to placebo or 0.1, 0.3, or 1.0 mg LGD-4033 daily for 21 days. Blood counts, chemistries, lipids, prostate-specific antigen, electrocardiogram, hormones, lean and fat mass, and muscle strength were measured during and for 5 weeks after intervention.

Results showed that doses of LGD-4033 were well tolerated with no adverse events. Hemoglobin, prostate-specific antigen, aspartate aminotransferase (AST), alanine aminotransferase (ALT), or QT intervals did not change significantly at any dose LGD-4033 administration was associated with dose-dependent suppression of total testosterone, sex hormone–binding globulin, high density lipoprotein cholesterol, and triglyceride levels. follicle-stimulating hormone and free testosterone showed significant suppression at 1.0-mg dose only. Lean body mass increased dose dependently, but fat mass did not change significantly. Hormone levels and lipids returned to baseline after treatment discontinuation.

Previous Phase 1 studies also established the safety of up to 22 mg LGD-4033. 

LGD-4033 displayed a prolonged elimination half-life (24–36 hours) FSH and free testosterone only showed significant suppression at the 1 mg per day dosage.

What was most impressive, is that LGD-4033 increased lean body mass on average 1.21 kg (2.67 pounds) at the 1 mg dosage [R]. The increase in lean body mass was directly correlated with dose.

In phase 2 trials, scope of treatment is focused on conditions to establish indications of treatment. The study was a randomized, double-blind, placebo-controlled, parallel group study designed to evaluate the efficacy, safety and tolerability of VK5211 in up to 120 patients recovering from hip fracture surgery.

Study design was to evaluate those recovering from hip fracture surgery. These patients are the perfect candidates for selective androgen receptor treatment, as mobility and movement are limited, resulting in muscle atrophy, bone degradation, and muscle wasting.

Within the first year after a hip fracture, body fat levels increase on average up to 7%,, while lean muscle mass decreases by up to 11% and bone mineral density by 4.6% [R, R]. Patients recovering from hip fractures are known to lose bone and muscle at accelerated rates, placing them at increased risk of further morbidity, re-fracture and prolonged disability.

LGD-4033 produced significant increases in lean body mass and appendicular lean mass following 12 weeks of daily dosing in all subjects.

Preserves Muscle Mass

Another benefit of Ligandrol is its ability to preserve muscle mass during cutting phases. When athletes reduce their caloric intake to shed body fat, they often risk losing muscle mass as well. Ligandrol's muscle-preserving properties help mitigate this risk, allowing users to maintain their hard-earned muscle while achieving a leaner physique. This dual benefit of muscle growth and preservation makes Ligandrol a versatile tool for both bulking and cutting cycles.

Improves Strength

Furthermore, Ligandrol's impact on muscle growth is not just limited to aesthetics. Increased muscle mass also contributes to improved strength and endurance, which can enhance overall athletic performance. Stronger muscles can lead to better performance in various physical activities, from weightlifting to endurance sports. The comprehensive muscle-building benefits of Ligandrol can therefore play a pivotal role in helping athletes reach new heights in their training and competition.

Ligandrol and Performance Enhancement: What to Expect

In addition to its muscle-building capabilities, Ligandrol is also known for its performance-enhancing effects. Users often experience increased strength, endurance, and overall athletic performance, which can be particularly beneficial for competitive athletes. The enhanced protein synthesis promoted by Ligandrol not only contributes to muscle growth but also supports faster recovery times, allowing athletes to train more frequently and intensely.

One of the key performance benefits of Ligandrol is its ability to increase strength. Users typically report significant gains in their lifting capacities, with improvements in both the amount of weight lifted and the number of repetitions performed. This increase in strength can translate to better performance in various sports and physical activities, giving users a competitive edge. Ligandrol's ability to enhance strength makes it a valuable asset for athletes aiming to push their limits and achieve new personal bests.

Endurance is another area where Ligandrol shines. By promoting lean muscle mass and improving overall strength, Ligandrol can help athletes sustain their performance over longer periods. This increased endurance can be particularly advantageous for endurance sports such as running, cycling, and swimming. Additionally, the faster recovery times facilitated by Ligandrol allow athletes to train more consistently, further boosting their endurance and overall performance.

Recommended Dosage and Cycle Length for Ligandrol

To maximize the benefits of Ligandrol while minimizing potential risks, it is crucial to follow recommended dosage guidelines and cycle lengths. For most users, a typical Ligandrol cycle lasts between 8 to 12 weeks. This duration allows the compound to exert its full effects on muscle growth and performance enhancement while reducing the risk of adverse side effects. It is important to note that exceeding the recommended cycle length can increase the likelihood of experiencing negative side effects.

The recommended dosage of Ligandrol varies depending on the user's experience level and goals. For beginners, a daily dose of 5 mg is usually sufficient to observe significant muscle gains and performance improvements. Intermediate users may increase the dosage to 10 mg per day, while advanced users might take up to 20 mg daily. It is essential to start with a lower dose and gradually increase it to assess the body's response and tolerance to the compound.

Post-cycle therapy (PCT) is an important consideration for anyone using Ligandrol. Since Ligandrol can suppress natural testosterone production, it is crucial to implement a PCT regimen to help restore hormonal balance after completing the cycle. A typical PCT regimen may include natural testosterone boosters, selective estrogen receptor modulators (SERMs), or other supplements designed to support hormonal recovery. Adhering to a proper PCT protocol is vital for maintaining the gains achieved during the Ligandrol cycle and ensuring long-term health and well-being.

Ligandrol, LGD-4033 Side Effects

While Ligandrol offers numerous benefits, it is important to be aware of potential side effects and risks associated with its use. One of the primary concerns is the suppression of natural testosterone production. Although Ligandrol is known to be less suppressive than traditional anabolic steroids, it can still impact the body's ability to produce testosterone. This suppression can lead to symptoms such as fatigue, decreased libido, and mood changes, which is why post-cycle therapy is essential.

Although clinical trials have shown that Lingandrol is very well tolerated and safe, SAMRS do exhibit several side effects. Without long-term efficacy and toxicity studies, it is impossible to know the long-term detriment, these compounds can create [R].

Studies show that Lingandrol does suppress high-density lipoproteins, (HDL) otherwise known as good cholesterol [R]. Negative effects are also notorious and associated with therapeutic application of all anabolic steroids and non-steroidal anabolics.

SARMs have shown to suppress luteinizing hormone (LH) and follicle stimulating hormone (FSH) through the hypothalamus-pituitary-testis axis, thus decreasing testosterone in a dose-dependent manner [R].

Studies also show a reduction in other hormones such as reduced levels of sex hormone-binding globulin (SHBG). Commonly reported symptoms and findings for all SARMs were headaches, dry mouth, and upper respiratory infections (URIs), constipation, dyspepsia, and nausea. 

Moreover, Lingandrol does not aromatize into Estrogen, yet it can still cause a systemic increase or decrease in Estrogen levels. LGD-4033, like other SARMS, suppresses natural Testosterone levels, which can result in an disparaging balance between Testosterone and Estrogen levels in the body. 

Another potential side effect of Ligandrol is an increase in liver enzymes, which can indicate liver stress or damage. While this side effect is relatively rare and often reversible, it is crucial to monitor liver function during a Ligandrol cycle. Regular blood tests can help detect any changes in liver enzyme levels, allowing users to take appropriate measures if necessary. It is also advisable to avoid alcohol and other substances that can strain the liver while using Ligandrol.

Other potential side effects of Ligandrol include headaches, nausea, and water retention. These side effects are generally mild and tend to resolve on their own as the body adjusts to the compound. However, if any side effects persist or worsen, it is important to discontinue use and consult a healthcare professional. By being aware of the potential risks and taking appropriate precautions, users can minimize the likelihood of experiencing negative side effects while benefiting from Ligandrol's muscle-building and performance-enhancing properties.

This can result in symptoms such as

• Acne
• Low Libido
• Lethargy
• Gynecomastia
• Depressive Mood State
• High Blood Pressure
• Change in testicular size

The average terminal half-life of S-4 in animals is four hours. After oral dosing, S-4 was rapidly absorbed and completely bioavailable.  

Pharmacokinetics studies show that the terminal half-life of SARMs range from 4.1 to 14.7 hours. Therefore, post cycle therapy is recommended to be started immediately after application has been concluded.   Any anabolic agent, SARMS or not, increase androgen activity. While ligandrol is selective for muscle and bone relative to androgen modulation there is still potential for androgen related side effects.

Anabolic agents are well known to cause liver damage which may manifest with elevated liver enzymes. Selective androgen receptor modulators (SARMs) have been heavily marketed as alternatives to androgenic anabolic steroids (AASs) for muscle gain and physical performance because of their perceived superior side-effect profile. 

LGD-4033 did not result in any significant changes in AST or ALT levels in human trials [R].

At therapeutic dosages, there appears to be a low risk associated with use and liver damage. However, it should be noted, that any anabolic modulator may have some degree of liver toxicity with ergogenic dosages. 

With doses higher than 1mg per day, it is possible, that ligandrol, will exhibit some some degree of liver toxicity, However, at therapeutic dosages, there appears to be a strong safety profile and the data suggests a complete absence of liver toxicity.

Ligandrol vs. Other Performance Enhancers: A Comparative Analysis

In the world of performance enhancement, Ligandrol is often compared to other SARMs and anabolic steroids. One of the primary differences between Ligandrol and traditional anabolic steroids is the specificity of their action. While anabolic steroids can affect a wide range of tissues, leading to numerous side effects, Ligandrol specifically targets androgen receptors in muscle and bone, minimizing the risk of unwanted side effects. This targeted action makes Ligandrol a safer alternative for those seeking muscle growth and performance enhancement.

Compared to other SARMs, Ligandrol is known for its potent muscle-building capabilities. While SARMs like Ostarine (MK-2866) and Andarine (S4) are also popular for their muscle-preserving and performance-enhancing effects, Ligandrol is often favored for its ability to promote significant lean muscle gains in a relatively short period. This potency makes Ligandrol an attractive option for users looking to achieve rapid and noticeable results.

Another factor to consider is the oral bioavailability of Ligandrol. Unlike injectable anabolic steroids, Ligandrol can be taken in pill form, offering a convenient and non-invasive option for users. This ease of administration, combined with its effectiveness, sets Ligandrol apart from other performance enhancers. When comparing Ligandrol to other options, it is clear that its targeted action, potent effects, and convenience make it a standout choice for athletes and bodybuilders.

Is Ligandrol Legal 

Legal Status and Regulations Surrounding Ligandrol

The legal status of Ligandrol varies by country, and it is important for users to be aware of the regulations in their region. In the United States, Ligandrol is not approved by the Food and Drug Administration (FDA) for human use, and its sale is restricted to research purposes only. Despite this, Ligandrol is widely available through various online vendors, though users should exercise caution and ensure they are purchasing from reputable sources to avoid counterfeit products.

In some countries, Ligandrol is classified as a controlled substance, meaning its possession, sale, and use are subject to strict regulations. For example, in Australia, Ligandrol is classified as a Schedule 4 substance, requiring a prescription for legal use. In contrast, other countries may have more lenient regulations, allowing for the purchase and use of Ligandrol without a prescription. It is crucial for users to research and understand the specific legal status of Ligandrol in their country to avoid legal repercussions.

Athletes should also be aware that Ligandrol is banned by most major sports organizations, including the World Anti-Doping Agency (WADA). Testing positive for Ligandrol can result in disqualification, suspension, and other penalties. Therefore, competitive athletes should carefully consider the risks and benefits of using Ligandrol, keeping in mind the potential impact on their careers. Understanding the legal and regulatory landscape surrounding Ligandrol is essential for making informed decisions about its use.

Ligandrol, LGD-4033 is classified as experimental and used for research purposes.

Ligandrol is classified as an investigational new drug by the FDA, meaning that it is still being studied and has not been approved for human use. As such, it is illegal to sell or distribute ligandrol in the U.S. for any purpose other than FDA-approved clinical trials. 

Thus, it is legal to sell and buy SARMs that are marketed for research purposes, which commonly occurs online. However, it is illegal to sell and buy those that are packaged in capsules for human consumption and/or labeled as dietary supplements. Furthermore, SARMS cannot be marketed to the public as dietary supplements and claims regarding their benefits cannot be made.

SARMs were banned by the World Anti-Doping Agency in January 2008, despite no drugs from this class yet being in clinical use, and blood tests for all known SARMs have been developed.

Ligandrol is still under investigation, however at this point, it seems the drugs progression into Phase 3 clincal trials, has come to a halt. 

Per the FDA requirement for Phase 3, an “approvable endpoint” for a Phase 3 trial would require showing a functional benefit, rather than just an increase in muscle mass. This requirement, makes it more challenging to design a trial with confidence since it becomes nearly impossible to account for the uncontrollable aspects of such things like a patient’s willpower to push forward. Finding investment to take on the possibility or risk of potentially failure to get approval, seems unlikely.

Conclusion: Is Ligandrol Right for You?

Ligandrol has emerged as a powerful ally for those seeking to elevate their muscle growth and enhance performance. Its ability to promote significant lean muscle gains, improve strength, and enhance endurance makes it a compelling option for athletes and bodybuilders. However, like any supplement, Ligandrol is not without its potential risks and side effects. It is important for users to carefully consider these factors and make informed decisions about its use.

For those who are committed to their fitness goals and are looking for an effective way to achieve rapid muscle growth and performance enhancement, Ligandrol may be worth considering. By following recommended dosage guidelines, adhering to proper cycle lengths, and implementing post-cycle therapy, users can maximize the benefits of Ligandrol while minimizing potential risks. Additionally, understanding the legal status and regulations surrounding Ligandrol is crucial to ensure compliance and avoid legal issues.

Clinical research shows that Ligandrol is a promising new compound, in relation to increasing lean body mass, with minimal side effects as compared to steroidal anabolic agents. Studies show, well tolerated safety and efficacy profile, while meeting primary and secondary endpoints, without increases in liver enzymes, AST, and ASL. 

At therapeutic dosages, there appears to be a low risk associated with use and liver damage. However, it should be noted, that any anabolic modulator may have some degree of liver toxicity with ergogenic dosages.

Results show that Ligandrol, has the highest anabolic capabilities of any known SARM. Pre-clinical trials showed that VK5211 demonstrated greater than 500-fold selectivity for maintaining muscle weight. 

Phase 1 studies showed a 2.67 gain in lean muscle mass. LGD-4033 therefore, is significantly more potent than many very well known testosterone analogs [R].

Ultimately, the decision to use Ligandrol should be based on individual goals, health considerations, and a thorough understanding of the compound's benefits and risks. Consulting with a healthcare professional or fitness expert can provide valuable guidance and help determine if Ligandrol is the right choice for you. By unlocking the potential of Ligandrol, users can transform their fitness aspirations into reality and redefine their limits.