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Thread: Lgd-4033

  1. #1
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    Lgd-4033






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    The safety, pharmacokinetics, and effects of "LGD-4033", a novel nonsteroidal oral, selective androgen receptor modulator, in healthy young men.


    AuthorsBasaria S, et al. Show all Journal
    J Gerontol A Biol Sci Med Sci. 2013 Jan;68(1):87-95. doi: 10.1093/gerona/gls078. Epub 2012 Mar 28.


    ABSTRACT


    BACKGROUND: Concerns about potential adverse effects of testosterone on prostate have motivated the development of selective androgen receptor modulators that display tissue-selective activation of androgenic signaling. "LGD-4033", a novel nonsteroidal, oral selective androgen receptor modulator, binds androgen receptor with high affinity and selectivity. Objectives. To evaluate the safety, tolerability, pharmacokinetics, and effects of ascending doses of "LGD-4033" administered daily for 21 days on lean body mass, muscle strength, stair-climbing power, and sex hormones.


    METHODS: In this placebo-controlled study, 76 healthy men (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: "LGD-4033" was well tolerated. There were no drug-related serious adverse events. Frequency of adverse events was similar between active and placebo groups. Hemoglobin, prostate-specific antigen, aspartate aminotransferase, alanine aminotransferase, or QT intervals did not change significantly at any dose. "LGD-4033" had a long elimination half-life and dose-proportional accumulation upon multiple dosing. "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.


    CONCLUSIONS:"LGD-4033" was safe, had favorable pharmacokinetic profile, and increased lean body mass even during this short period without change in prostate-specific antigen. Longer randomized trials should evaluate its efficacy in improving physical function and health outcomes in select populations.
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    LGD4033 is 12 times more anabolic than Ostarine.
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    This is the sarm I will try first
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    Key findings in Phase 1 Trial of LGD-4033:




    LGD-4033 was safe and well tolerated at all doses following daily oral administration for three weeks in young healthy males


    No clinically significant dose-related adverse events were reported


    No clinically significant changes in liver function tests, PSA, hematocrit or ECG were seen


    Positive dose-dependent trends in lean muscle mass increase were observed with drug-treated subjects


    Positive dose-dependent trends in functional exercise and strength measures were consistent with anabolic activity
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    There are not loads of studies on this but what I have found as been great so far. Although there are a lot of great logs all over the net though and it definitely lives up to it's rep of being the strongest SARM
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    LGD BENEFITS:


    *Effects similar to anabolics with size and strength
    *Minimal Side Effects
    *Excellent for recomping
    *Healing properties
    *Prevents muscle wasting
    *Works well as a stand alone or stacked with other SARMS
    *Great results in every aspect for different types of goals
    *Half life of 24-36 hours
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    I think I will be using this when I start my test c and deca run in the next few months. I might even kick start my cycle with it
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    *LGD-4033 is a selective androgen receptor modulator that is safe and well tolerated up to 22 mg, the highest tested dose, with no serious adverse events reported.
    *LGD-4033 has sustained systemic exposure and is amenable for once daily dosing with a half life of approximately 30 hours after a single oral dose.
    *1 mg of LGD-4033 achieved exposures in humans greater than the predicted efficacious exposure based upon pre-clinical data in the rat.
    *The projected therapeutic dose based on PK-PD modeling in rats is 0.2 mg with once-daily dosing.
    *Based upon its favorable profile, LGD-4033 initiated a Phase Ib multi-dose clinical trial in 2010.
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    Selective androgen receptor modulators as function promoting therapies.


    AuthorsBhasin S, et al. Show all Journal
    Curr Opin Clin Nutr Metab Care. 2009 May;12(3):232-40. doi: 10.1097/MCO.0b013e32832a3d79.


    Affiliation
    Abstract
    PURPOSE OF REVIEW: The past decade has witnessed an unprecedented discovery effort to develop selective androgen receptor modulators (SARMs) that improve physical function and bone health without adversely affecting the prostate and cardiovascular outcomes. This review describes the historical evolution, the rationale for SARM development, and the mechanisms of testosterone action and SARM selectivity.


    RECENT FINDINGS: Although steroidal SARMs have been around since the 1940s, a number of nonsteroidal SARMs that do not serve as substrates for CYP19 aromatase or 5alpha-reductase, act as full agonists in muscle and bone and as partial agonists in prostate are in development. The differing interactions of steroidal and nonsteroidal compounds with androgen receptor (AR) contribute to their unique pharmacologic actions. Ligand binding induces specific conformational changes in the ligand-binding domain, which could modulate surface topology and protein-protein interactions between AR and coregulators, resulting in tissue-specific gene regulation. Preclinical studies have demonstrated the ability of SARMs to increase muscle and bone mass in preclinical rodent models with varying degree of prostate sparing. Phase I trials of SARMs in humans have reported modest increments in fat-free mass.


    SUMMARY: SARMs hold promise as a new class of function promoting anabolic therapies for a number of clinical indications, including functional limitations associated with aging and chronic disease, frailty, cancer cachexia, and osteoporosis.
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