LGD-4033 for sale online
LGD-4033 for sale online, a Novel Nonsteroidal Oral, Selective Androgen Receptor Modulator, in Healthy Young Men 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.
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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.
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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.
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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.
As men and women grow old, they lose muscle mass, muscle strength, and leg power (1,2,3,4,5,6), mostly due to the preferential loss of type II muscle fibers (5). Sarcopenia, the age-associated loss of muscle mass and strength, increases the risk of falls, fractures, physical disability, and poor quality of life (1,3,6,7). Similarly, the course of many illnesses, such as chronic obstructive lung disease, end-stage renal disease, and some types of cancer, is punctuated by the loss of muscle mass and physical function, which contributes to mobility limitation and disability (7,8). Thus, there is an unmet need for anabolic therapies that improve physical function and reduce the burden of disability in persons experiencing functional limitations due to aging or illness. Among the various candidate function-promoting anabolic therapies that are in development, androgens are the farthest along in development.
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Testosterone administration increases muscle mass and strength (9,10,11,12,13,14,15), but concerns regarding its potential adverse effects on the prostate have restrained enthusiasm for its use as an anabolic therapy and have motivated efforts to develop selective androgen receptor modulators (SARMs), a new class of androgen receptor ligands that are tissue selective (8,16,17,18,19). The last decade has witnessed substantial pharmaceutical efforts to develop nonsteroidal SARMs to treat muscle wasting and functional limitations associated with acute and chronic illness and aging (8,16,17,18,19). LGD-4033 is a novel nonsteroidal, oral SARM that binds to androgen receptor with high affinity (Ki of ∼1 nM) and selectivity. In animal models, LGD-4033 has demonstrated anabolic activity in the muscle, anti-resorptive and anabolic activity in bone, and robust selectivity for muscle versus prostate.
Here we report the results of a randomized, double-blind, placebo-controlled, ascending-dose study, which evaluated the safety, tolerability, and pharmacokinetics (PK) of LGD-4033 in healthy men. We also evaluated the effects of graded doses of LGD-4033 on lean body mass (LBM), muscle strength, and physical function. LGD-4033 doses of 0.1, 0.3, and 1.0 mg were selected for multiple dosing over 21 days because a previous phase I single ascending-dose study had established the safety of up to 22 mg LGD-4033. We also tested the hypothesis that the LGD-4033 increases muscle mass by stimulating fractional synthetic rate (FSR) of mixed-muscle proteins, measured using continuous steady state infusion of labeled phenylalanine in men randomized to either placebo or 0.3-mg daily dose of LGD-4033. This dose was selected for FSR study because preclinical data suggested that this dose was the most likely to increase LBM.
