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

The safety, pharmacokinetics, and effects of LGD-4033, a novel nonsteroidal oral, selective androgen receptor modulator, in healthy young men / Shehzad Basaria, Lauren Collins, E. Lichar Dillon, Katie Orwoll, Thomas W. Storer, Renee Miciek, Jagadish Ulloor, Anqi Zhang, Richard Eder, Heather Zientek, Gilad Gordon, Syed Kazmi, Melinda Sheffield-Moore, Shalender Bhasin. - (The Journals of Gerontology: Series A 68 (2013) 1 (January); p. 87–95)

  • PMID: 22459616
  • PMCID: PMC4111291
  • DOI: 10.1093/gerona/gls078

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.

Original document

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Study
Date
28 March 2012
People
Basaria, Shehzad
Bhasin, Shalender
Collins, Lauren
Dillon E. Lichar
Eder, Richard
Gordon, Gilad
Kazmi, Syed
Miciek, Renee
Orwoll, Katie
Sheffield-Moore, Melinda
Storer, Thomas W.
Ulloor, Jagadish
Zhang, Anqi
Zientek, Heather
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United States of America
Language
English
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Boston University School of Public Health (BUSPH)
University of Texas Medical Branch (UTMB)
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S1. Anabolic Agents
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LGD-4033 (ligandrol)
Selective androgen receptor modulators (SARMs)
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Health effects
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7 September 2020
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13 September 2020
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