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SARM: LGD-4033

SARM: LGD-4033

Androgens are natural steroid hormones, that is, synthesized by our body, which are secreted by the testes (testosterone and estradiol) but also by the ovaries in women (androstenedione) and by the adrenal cortex (only by 10%).

The so-called anabolic androgens are steroids in which the aim is to reduce androgenic and virilizing effects and increase anabolic actions chemically. While some progress has been made these two key actions were not completely separated, and that is why anabolic androgens retain their virilizing effects more evident in women and with prolonged use.

Myotrophic action: increase in muscle mass is often sought by athletes, on occasion causing possible health hazards.

The indiscriminate use of androgens can have several consequences, including the premature closure of bone epiphyses and growth arrest in adolescents. Following the inhibition of gonadotropin secretion (FSH and LH hormones), spermatogenesis (formation of spermatozoa), hypotrophy and testicular atrophy, gynecomastia ( increase in breast size) and feminization in man can be reduced.

The anabolic effects of testosterone on muscle mass and strength are directly related to the dose of testosterone. Therefore, the impact of muscle gain and strength are substantial at the dose; It has been observed that the administration of supraphysiological doses of testosterone is associated with several adverse effects such as erythrocytosis, leg edema and, prostate problems.

The modification (esterification) of testosterone increases its absorption and prolongs its action.

Supplementation with testosterone increases skeletal muscle mass and strength in healthy men with androgen deficiency, young with normal gonads, the elderly and people with other chronic disorders.

Despite the drawbacks of testosterone supplementation, potential benefits in chronic diseases associated with age and osteoporosis have also been discovered, prompting pharmaceutical companies to develop SARMs. Structurally, SARMs can be classified into steroids or non-steroids, the former is formed by modifying the chemical structure of testosterone.

The development of these drugs was motivated by the specialists’ concerns about the possible adverse effects of testosterone in the prostate when it is consumed exogenously in a prolonged treatment and to treat the severe problem of muscle wasting that occurs in patients with a variety of disorders, including cancer cachexia and sarcopenia in the elderly or merely the atrophy and loss of muscle fibers that occurs physiologically with age, which predisposes to increased muscle fragility and therefore increased bone exposure to falls and thus higher production of fractures.

Ligandrol, LGD-4033 or VK5211 is a representative of the family of SARMS that are selective modulators of the androgen receptor. That is, they show the selective activation of androgenic signaling in tissues.

LGD-4033 is a SARM for an oral, novel, non-steroidal use, which with very high affinity and selectivity binds to the androgen receptor, and differs from others, mainly because of its selectivity in muscle tissues and not in prostate tissues, which provides a category of high security, admissibility, and acceptance.

LGD-4033 has demonstrated anabolic activity in muscle, antiresorptive and anabolic in bone.

It is very popular in amateur athletes, bodybuilders and weightlifters, due to its ability to produce results similar to steroids and the various beneficial effects: such as the increase of lean muscle mass, the accompanying improvement of strength and endurance for the exercises, in addition to your more significant ability to burn fat without the dreaded side effects of steroids.

In the Article in The Journals of Gerontology Series A Biological Sciences and Medical Sciences in March 2012, they published the results of a phase 1 study that evaluated the safety and tolerability of LGD-4033, was a randomized, double-blind, clinical study placebo-controlled, where the drug was administered to healthy men orally for 21 days in doses of 0.1, 0.3 and 1 mg. Hormonal blood levels were measured consistently up to 35 days after administration of the substance, measured LH, FSH, adrenocorticotropic hormone, cortisol, free testosterone, total testosterone, and blood lipid levels: Cholesterol, HDL, LDL, and triglycerides. The results indicated that the incidence of adverse effects was similar in subjects who used LGD-4033 and those who consumed placebo, concluding that the drug does not produce serious adverse effects on liver function, hematological parameters, prostate-specific antigen (PSA) or the electrocardiogram.

 

References:

  1. Basaria, S., Collins, L., Dillon, E. L., Orwoll, K., Storer, T. W., Miciek, R., . & Gordon, G. (2013). The safety, pharmacokinetics, and effects of LGD-4033, a novel nonsteroidal oral, selective androgen receptor modulator, in healthy young men. The Journals of Gerontology Series A: Biological Sciences and Medical Sciences, 68, 87-95.
  2. Bhasin S , Calof OM , Storer TW , et al . Drug insight: Testosterone and selective androgen receptor modulators as anabolic therapies for chronic illness and aging . Nat Clin Practice Endocrinol Metab . 2006 ; 2 : 146 – 159 . Bhasin S , Storer TW , Berman N , et al . The effects of supraphysiologic doses of testosterone on muscle size and strength in normal men . N Engl J Med . 1996 ; 335 : 1 – 7 .
  3. Srinivas-Shankar U , Roberts SA , Connolly MJ , et al . Effects of testos￾terone on muscle strength, physical function, body composition, and quality of life in intermediate-frail and frail elderly men: a randomized, double-blind, placebo-controlled study . J Clin Endocrinol Metab . 2010 ; 95 : 639 – 650 .
  4. Page ST , Amory JK , Bowman FD , et al . Exogenous testosterone (T) alone or with finasteride increases physical performance, grip strength, and lean body mass in older men with low serum T . J Clin Endocrinol Metab . 2005 ; 90 : 1502 – 1510 .

For educational/research purposes only. This is not medical advice.


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