Abstract

Context

Selective androgen receptor modulators (SARMs), because of their preferential muscle vs prostate selectivity, are being developed for muscle-wasting conditions. Oral SARMs suppress high-density lipoprotein cholesterol (HDL-C) but their effects on functional capacity and atherogenic potential of HDL particles are unknown.

Objective

To determine the effects of an oral SARM (OPK-88004) on cholesterol efflux capacity, HDL particle number and size, apolipoprotein particle number and size and HDL subspecies

Methods

We measured cholesterol efflux capacity (CEC); HDL particle number and size; APOB; APOA1; and protein-defined HDL subspecies associated with coronary heart disease (CHD) risk in men, who had undergone prostatectomy for low-grade prostate cancer during 12-week treatment with placebo or 1, 5, or 15 mg of an oral SARM (OPK-88004).

Results

SARM significantly suppressed HDL-C (P < .001) but HDL particle size did not change significantly. SARM had minimal effect on CEC of HDL particles (change + 0.016, –0.036, +0.070, and –0.048%/µmol-HDL/L–1 at 0, 1, 5, and 15 mg SARM, P = .045). SARM treatment suppressed APOAI (P < .001) but not APOB (P = .077), and reduced APOA1 in HDL subspecies associated with increased (subspecies containing α2-macroglobulin, complement C3, or plasminogen) as well as decreased (subspecies containing APOC1 or APOE) CHD risk; relative proportions of APOA1 in these HDL subspecies did not change. SARM increased hepatic triacylglycerol lipase (HTGL) (P < .001).

Conclusion

SARM treatment suppressed HDL-C but had minimal effect on its size or cholesterol efflux function. SARM reduced APOA1 in HDL subspecies associated with increased as well as decreased CHD risk. SARM-induced increase in HTGL could contribute to HDL-C suppression. These data do not support the simplistic notion that SARM-associated suppression of HDL-C is necessarily proatherogenic; randomized trials are needed to determine SARM’s effects on cardiovascular events.

Details

Title
Effect of Selective Androgen Receptor Modulator on Cholesterol Efflux Capacity, Size, and Subspecies of HDL Particles
Author
Guo, Wen 1 ; Pencina, Karol M 1 ; Furtado, Jeremy D 2 ; Sacks, Frank M 2 ; Vaisar, Tomas 3 ; Cheng, Ming 1 ; Sniderman, Allan D 4 ; Page, Stephanie T 3 ; Bhasin, Shalender 1 

 Research Program in Men’s Health: Aging and Metabolism ; Claude D. Pepper Older Americans Independence Center, Brigham and Women’s Hospital, Harvard Medical School , Boston, Massachusetts 02115 , USA 
 Department of Nutrition, Harvard TH Chan School of Public Health , Boston, Massachusetts 02115 , USA 
 Division of Metabolism, Endocrinology, and Nutrition, University of Washington , Seattle, Washington 98195 , USA 
 Mike and Valeria Rosenbloom Centre for Cardiovascular Prevention, Department of Medicine, McGill University Health Centre , Montreal, Quebec QCH4A , Canada 
Publication year
2022
Publication date
Aug 2022
Publisher
Oxford University Press
e-ISSN
24721972
Source type
Scholarly Journal
Language of publication
English
ProQuest document ID
3170014724
Copyright
© The Author(s) 2022. Published by Oxford University Press on behalf of the Endocrine Society. This work is published under https://creativecommons.org/licenses/by-nc-nd/4.0/ (the “License”). Notwithstanding the ProQuest Terms and Conditions, you may use this content in accordance with the terms of the License.