LGD-4033 (LIGANDROLE) DESCRIPTION
LGD-4033 (often called Ligandrol) is an oral, nonsteroidal and potent selective androgen receptor modulator (SARM). It was developed to increase anabolic activity and reduce muscle wasting in people with severe diseases associated with catabolic conditions and critical loss of muscle mass. In clinical studies, LGD-4033 has shown significant anabolic activity in muscles and antiresorptive anabolic activity in bones, along with a high selectivity to act in those tissues (appropriate and desirable) and minimally in other tissues and organs, where it is undesirable. LGD-4033 binds to the androgen receptor with high affinity (Ki ‘1 nM) and selectivity, chemical formula C14H12F6N2O, molecular mass 338,253 g mol−1, long elimination half-life 24-36 hours, and linear pharmacokinetics.
LGD-4033 DEVELOPMENT AND HISTORY
SARM LGD-4033 (Ligandrol) was discovered by Ligand Pharmaceuticals and is currently under development (under the new designation VK5211) by Viking Therapeutics, which does not manufacture any pharmaceutical products but develops several products for the treatment of metabolic and endocrine disorders. Viking Therapeutics incurred the largest spend in 2014 from Research and Development costs ($21.2M), which may be related to the purchase of equipment and facilities necessary to develop licensed drug candidates by Ligand Pharmaceuticals, including LGD-4033. Another promising drug candidate, VK2809, is expected to cap the Viking Therapeutics market and drive a large shift in market share for TRβ agonists. In the United States, LGD-4033 is currently a research compound.
LIGANDROL, RESEARCH, AND POTENTIAL CLINICAL USE IN THE FUTURE
SARM LGD-4033 is a nonsteroidal selective androgen receptor modulator expected to offer the therapeutic benefits of testosterone with enhanced safety, tolerability and patient acceptance due to tissue-selective mechanisms of action and oral routes of administration. Research indicates that LGD-4033 appears to be a promising candidate for the treatment of serious diseases associated with muscle wasting in the future, however, the long-term effects of LGD-4033 are not fully known and have been researched so far, and more research is still needed.
LGD-4033 AND PHASE 1 & 2 CLINICAL STUDIES
Administration of LGD-4033 to cynomolgus monkeys at daily doses ranging from 0 to 75 mg/kg for 13 weeks showed significant body weight gain in both males and females. After 48 days, the 75 mg/kg dose test was discontinued due to toxicity concerns, but this did not adversely affect the improvement as the dose was significantly higher than those used in the Phase 2 clinical trial.
The first clinical study in phase 1 is the first human study of LGD-4033 and evaluated the safety, tolerability, and pharmacokinetic profiles of the molecule in a single incremental dose, double-blind, placebo-controlled 48 healthy volunteers. LGD-4033 was also tolerated by healthy male volunteers after single oral doses of 22 mg. No serious adverse events (SAEs) or clinically significant dose-related adverse events were reported. LGD-4033 systemic exposure increased proportionally with dose level after a single oral dose. Continuous systemic exposure, with significant plasma levels of Igd-4033, was dose determinable after one week. The half-life of LGD-4033 was compatible with a daily oral dosing regimen.
In another Phase 1 clinical study with 76 adult men taking low doses of LGD-4033 at 0.1, 0.3, and 1 mg per day, a dose-dependent increase in muscle mass was observed, with no significant side effects, for 21 days, and a dose of Ligandrol 1 mg per day of approximately 3 pounds was enough to increase lean muscle mass. However, it had no effect at low doses.
The Phase 2 clinical trial, initiated on November 3, 2016, consists of 120 patients who recovered after hip fracture surgery. Randomized study participants will receive either a placebo or varying dose sizes of LGD-4033 over a 12-week period, with improved lean body mass as the primary endpoint. Other extremes include satisfactory results in terms of quality of life, safety, and pharmacokinetics.
LGD-4033 Stimulates STRONG MUSCLE MASS GROWTH
Results of clinical studies conducted by the Boston Medical Center Department of Endocrinology also show that LGD-4033 can help significantly increase muscle mass and muscle strength in serious diseases associated with muscle wasting, and without significant side effects (which can result in the treatment of these diseases with androgenic drugs – steroids). Similarly, another study in January 2013 confirmed that Ligandrol can help increase muscle mass in muscle tissue, and its use was well tolerated by the subjects.
LGD-4033 AND BODYBUILDING
Like anabolic androgenic steroids (AAS), LGD-4033 also has a very powerful ability to induce significant muscle gains. However, unlike AAS, LGD-4033 as a Selective Androgen Receptor Modulator (SARM) provides potent anabolic effects and can bind to androgen receptors in the body only when desired, muscles and bones (the action is selectively targeted to that tissue only). And, conversely, it does not act (or minimally in comparison with AAS) in tissues and organs (prostate, liver, sebaceous glands, etc.), which can cause undesirable and serious side effects.
So we summarize: LGD-4033 (Ligandrol) has a very strong anabolic activity that makes it possible to help bodybuilders and athletes achieve muscle gains most effectively comparable to those that can be achieved using “bulking” anabolic steroids, but dangerous and unpleasant side effects. Many without such steroids cause. Thus, Ligandol is a great full-fledged alternative to the most effective anabolic steroids for muscle gains, while much safer, less harmful and less risky using steroids.
This is why LGD-4033 is so popular and well known among bodybuilders and strength athletes. However, it should be emphasized here that the use of LGD-4033 as a nutritional supplement or sports performance stimulant is illegal in many countries. It is an experimental substance that is still under research, its long-term effects are not fully known and have not been investigated so far, and more research is still needed. Note also that LGD-4033, like all our other products, is sold for scientific and research clinical use only.
LIGANDROLE AND DOPING
The World Anti-Doping Agency (WADA) banned all SARMs (including Ligandrol) as early as 2008. Since then, there have been several key cases where professional athletes have tested positive for LGD-4033:
In 2015, Florida Gators quarterback Will Grier was suspended after testing positive for Ligandrol. In 2017, Joakim Noah was banned from 20 games by the NBA because he tested positive for LGD-4033. In 2019, Australian swimmer Shayna Jack also tested positive for Ligandrol; she purposely denies taking the substance. In August 2019, it was revealed that Canadian sprint kayaker Laurence Vincent Lapointe tested positive for Ligandrol. Athlete refuses to knowingly take a prohibited substance. In January 2020, Chilean ATP tennis singles competitor Nicolás Jarry tested positive for both Ligandrol and Stanozolol.
However, despite the bans and negative media coverage, bodybuilders and athletes in many internet forums and discussions argue that LGD 4033 is the most effective SARM on the market and is simply functional and a much safer way to gain massive muscle gains simultaneously without using anabolic steroids.
POSSIBLE BENEFITS OF LGD-4033 SCIENTIFICALLY RESEARCHED
Significant and selective anabolic activity in muscles and bones, without strong androgenic adverse effects and adverse effects on other organs
Promising candidate for the treatment of serious diseases associated with muscle wasting
Promising candidate for the treatment of osteoporosis and fractures
Helps build lean muscle mass very effectively
It has strong anti-catabolic effects and the ability to preserve muscle mass even with reduced calorie intake
Increases bone density and helps prevent bone loss
ADVANTAGES OF LGD-4033 OVER ANABOLIC-ANDROGENIC STEROIDS
SARM LGD-4033 is highly selective and is primarily aimed at acting on muscles and bones. Due to this selectivity, it does not cause strong androgenic side effects and adverse effects on other organs, unlike anabolic steroids.
LGD-4033 has anabolic activity completely comparable to anabolic steroids, is able to help achieve similar results muscle mass growth, but without many of the adverse effects and health risks that result from the use of anabolic steroids:
LGD-4033 does not interact with CYP19 aromatase or 5α-reductase enzymes (LGD-4033 does not convert on Estrogen or Dihydrotestosterone (DHT)
LGD-4033 does not cause gynecomastia (abnormal development of mammary glands in men causing breast enlargement)
LGD-4033 does not cause significant retention of water and salts in the body.
LGD-4033 does not cause increased Cortisol and Estrogen production
LGD-4033 does not cause heavy load and damage to the liver
LGD-4033 does not cause prostate enlargement
LGD-4033 does not cause kidney disease
LGD-4033 does not cause acne and oily skin
LGD-4033 does not cause hair loss and baldness
LGD-4033 does not cause swollen face
LGD-4033 does not cause excessive facial or body hair (hirsutism)
LGD-4033 does not cause sudden changes in mood and behavior
LGD-4033 does not cause irritability, irritability, depression, restlessness
LGD-4033 does not cause aggression, explosiveness and psychological problems
LGD-4033 is extremely effective when administered orally (no injection required)
LGD-4033 (LIGANDROL) FAQ
What is LGD-4033 (Ligandrol)?
LGD-4033 (Ligandrol) is an oral, nonsteroidal and potent selective androgen receptor modulator (SARM), expected to offer the therapeutic benefits of testosterone with improved safety, tolerability and patient acceptance due to tissue-selective mechanisms of action and oral routes of administration.
What does LGD-4033 do?
LGD-4033 binds to the androgen receptor with high affinity (Ki and 1 nM) and selectivity in muscle and bone tissues. This novelty has strong anabolic effects on building muscle mass, and strong anti-catabolic effects and the ability to maintain muscle mass even with reduced caloric intake.
What is Ligandrol used for?
LGD-4033, a selective androgen receptor modulator (SARM), is currently under investigation as a drug therapy for muscle wasting and aging-related weakness.
Does LGD-4033 Ligandrol build muscle?
The results of clinical studies have confirmed that LGD-4033 can significantly help increase muscle mass, has strong anabolic properties, and moreover, it acts selectively only in necessary tissues, in muscles and bones.
LGD-4033 powerful SARM for building muscle mass?
Bodybuilders and athletes in many internet forums and discussions argue that LGD 4033 is the most effective SARM on the market and is just a functional and at the same time a much safer way to gain massive muscle gains without the use of anabolic steroids.
Does LGD-4033 Ligandrol have strong side effects?
LGD-4033 was safe and well tolerated in clinical studies. It is highly selective and binds to androgen receptors in the body only where it is desired, in muscles and bones. Due to this selectivity, it is also many times milder, less dangerous and less dangerous than anabolic steroids with possible side effects.
Does LGD-4033 cause gynecomastia?
LGD-4033 does not cause gynecomastia (abnormal development of mammary glands in men causing breast enlargement), because it does not interact with CYP19 aromatase enzymes.
Is LGD-4033 dangerous for the prostate?
LGD-4033 is highly selective only for muscle and bone action, does not interact with 5α-reductase enzymes (does not convert dihydrotestosterone), therefore, unlike anabolic steroids, it does not pose a risk to the prostate (enlargement or cancer)
Does LGD-4033 cause increased cortisol production?
No, LGD-4033 does not affect cortisol levels and does not increase its production in the body
Is Ligandrol sports forbidden?
Yes, the World Anti-Doping Agency (WADA) banned all SARMs as early as 2008, including Ligandrol (LGD-4033).
Is LGD-4033 Ligandrol legal to use in the USA?
Because LGD-4033 Ligandrol is still an investigational new compound, it has not yet been approved as marketed for human consumption in the United States. However, it has been used experimentally in some bodybuilding community.
Is LGD-4033 Ligandrol low testosterone?
LGD-4033 suppresses production and reduces natural Testosterone levels in the body, but much less than some anabolic steroids. The effect on reducing testosterone production is also affected by the size of the dose and the length of use.
How safe is LGD 4033?
In clinical studies, LGD-4033 was safe, had a favorable pharmacokinetic profile, and increased lean body mass with no change in prostate-specific antigen even in this short period. Longer randomized trials need to evaluate its effectiveness in improving physical function and health outcomes in specific populations.
One phase 1 clinical trial found that even a low dose of 1mg LGD-4033 (Ligandrol) led to an increase in daily muscle mass, another phase 1 clinical trial also found LGD-4033 was tolerated by healthy male volunteers after a single oral dose as much as 22mg .
However, in addition to increasing its overall anabolic effect, LGD-4033’s negative effect on suppressing endogenous testosterone production may be increased if used in higher doses (over 20 mg). Therefore, a dose of 10-20 mg per day may be considered optimal. Due to the long half-life of LGD-4033, 1 dose per day is sufficient.
We emphasize that LGD-4033 is not an approved nutritional supplement or stimulant for athletes. It is an experimental substance still under investigation and not all of its side effects are known. Note that LGD-4033, like all our other products, is sold for scientific and research clinical use only.