GSK2881078
Muscle Growth & Body CompositionAlso known as: GSK-2881078, GSK SARM
Mechanism
GSK2881078 is a non-steroidal SARM developed by GlaxoSmithKline for muscle wasting in COPD and other chronic conditions. It completed Phase 2 trials showing increased lean body mass with a manageable side effect profile, though development appears to have been deprioritized.
Technical detail
GSK2881078 is a non-steroidal SARM that entered Phase 2 clinical trials for chronic obstructive pulmonary disease (COPD)-associated muscle wasting. In healthy volunteer studies, it produced dose-dependent increases in lean body mass with expected suppression of total testosterone, SHBG, and HDL cholesterol. The Phase 2 COPD trial demonstrated modest improvements in appendicular lean mass. Adverse effects included dose-dependent HDL reduction and hepatic transaminase elevations. Development status is unclear following GlaxoSmithKline pipeline reprioritization.
Evidence
- moderate
GSK2881078, a SARM, Produces Dose-Dependent Increases in Lean Mass in Healthy Older Men and Women
Neil et al. (2018) — J Clin Endocrinol Metab — PMID: 29982690
In healthy older men and postmenopausal women, repeat dosing of GSK2881078 produced dose-dependent increases in lean mass relative to placebo, with transient ALT elevations and greater apparent sensitivity in women at lower doses.
- moderate
Clark et al. (2017) — Br J Clin Pharmacol — PMID: 28449232
Across single-dose and repeat-dose randomized cohorts in healthy men and postmenopausal women, GSK2881078 showed dose-proportional exposure with a long half-life, mild drug-related adverse events, and dose-related reductions in HDL and SHBG; women appeared more sensitive at lower doses than men.