LGD-4033 and MK-677 use impacts body composition, circulating biomarkers, and skeletal muscle androgenic hormone and receptor content: A case report

Exp Physiol. 2022 Dec;107(12):1467-1476. doi: 10.1113/EP090741. Epub 2022 Nov 16.

Abstract

New findings: What is the main observation in this case? Co-administration of LGD-4033 and MK-677 increased body mass, lean mass and fat mass, while negatively impacting bone, serum lipids, liver enzymes, testosterone (total and free) and, probably, follicle-stimulating hormone. What insights does it reveal? Our cross-sectional data imply that these compounds might alter intramuscular androgenic hormone and receptor concentrations along with promoting muscular strength, when compared with previously published data from trained males.

Abstract: LGD-4033, a selective androgen receptor modulator, and MK-677, a growth hormone secretagogue, are being used increasingly amongst recreationally active demographics. However, limited data exist describing their effects on health- and androgen-related biomarkers. The purpose of this case study was to determine changes in body composition and biomarkers during and after continued co-administration of LGD-4033 and MK-677. We also aimed to examine muscular strength and intramuscular androgen-associated biomarkers relative to non-users. A 25-year-old male ingested LGD-4033 (10 mg) and MK-677 (15 mg) daily for 5 weeks. Blood and body composition metrics were obtained pre-, on- and post-cycle. One-repetition maximum leg and bench press, in addition to intramuscular androgens and androgen receptor content, were analysed on-cycle. We observed pre- to on-cycle changes in body composition (body mass, +6.0%; total lean body mass, +3.1%; trunk lean body mass, +6.6%; appendicular lean body mass, +4.3%; total fat mass, +15.4%; trunk fat mass, +2.8%; and appendicular fat mass, +14.8%), bone (bone mineral content, -3.60%; area, -1.1%; and bone mineral density, -2.1%), serum lipid-associated biomarkers (cholesterol, +14.8%; triglycerides, +39.2%; low-density lipoprotein-cholesterol, +40.0%; and high-density lipoprotein-cholesterol, -36.4%), liver-associated biomarkers (aspartate aminotransferase, +95.8%; and alanine aminotransferase, +205.0%) and androgen-associated biomarkers (free testosterone, -85.7%; total testosterone, -62.3%; and sex hormone-binding globulin, -79.6%); however, all variables returned to pre-cycle values post-cycle, apart from total fat mass, appendicular fat mass, bone area, total cholesterol and low-density lipoprotein-cholesterol. Follicle-stimulating hormone was below clinical reference values on- (1.2 IU/L) and post-cycle (1.3 IU/L). Intramuscular androgen receptor (-44.6%), testosterone (+47.8%) and dihydrotestosterone (+34.4%), in addition to one-repetition maximum leg press and bench press (+39.2 and +32.0%, respectively), were different in the case subject compared with non-users. These data demonstrate that LGD-4033 and MK-677 increase several body composition parameters, whilst negatively impacting bone and several serum biomarkers. Given the sparsity of data in recreationally using demographics, further research is warranted to elucidate the acute and chronic physiological effects of these anabolic agents.

Keywords: androgen receptor; ergogenic aid; growth hormone secretagogue; ibutamoren; ligandrol; muscle strength; performance-enhancing drug; selective androgen receptor modulator; testosterone.

Publication types

  • Case Reports
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adult
  • Androgens*
  • Biomarkers
  • Body Composition
  • Cross-Sectional Studies
  • Follicle Stimulating Hormone
  • Humans
  • Lipoproteins, LDL
  • Male
  • Muscle, Skeletal / physiology
  • Receptors, Androgen* / metabolism
  • Testosterone

Substances

  • Androgens
  • Receptors, Androgen
  • ibutamoren mesylate
  • 4-(2-(2,2,2-trifluoro-1-hydroxyethyl)pyrrolidin-1-yl)-2-(trifluoromethyl)benzonitrile
  • Testosterone
  • Biomarkers
  • Follicle Stimulating Hormone
  • Lipoproteins, LDL