GSK2881078
GSK2881078 is a non-steroidal SARM developed by GlaxoSmithKline that reached early-phase human trials for muscle wasting and sarcopenia, including studies in older adults and patients with COPD. It produced modest measurable increases in lean mass and is one of the better-characterised experimental SARMs, though still far from approval.
01 Overview
GSK2881078 stands out among experimental SARMs because it advanced into Phase I/II clinical study. Trials in healthy older men and postmenopausal women, and in COPD patients with muscle wasting, showed small but measurable gains in lean body mass over weeks of dosing, alongside the expected reductions in HDL cholesterol and sex-hormone-binding globulin.
Development did not lead to approval, and long-term efficacy on physical function was not established. Still, the presence of real, if early, human pharmacokinetic and safety data places it above most SARMs in how well it is characterised. It is not a marketed product.
02 Mechanism
Non-steroidal androgen receptor agonist that selectively stimulates anabolic pathways in skeletal muscle, increasing lean mass while producing weaker androgenic effects elsewhere.
03 Dosing
| Tier | Dose | Route | Notes |
|---|---|---|---|
| Trial range | 0.75–10 mg/day | Oral | Doses studied in Phase I/II; not a validated physique protocol. |
Ester comparison
| Ester | Half-life | Injection freq. | Testosterone by mass |
|---|
04 Effects
| Effect | Magnitude | Evidence | |
|---|---|---|---|
| Increased lean body massSmall but measurable lean mass gains in early human trials over several weeks. | ~0.5-1.5 kg | Clinical | |
| Improved muscle in wasting conditionsLean mass increases seen in COPD patients with muscle wasting. | Clinical |
05 Side effects
| Effect | Severity | Frequency | Evidence | Countermeasures |
|---|---|---|---|---|
| Transient liver enzyme elevationMild elevations in transaminases observed in some subjects. | Mild | Reported | Clinical | |
| HDL cholesterol reductionLowered HDL cholesterol observed across dosing, a class effect of oral SARMs. | Moderate | Consistent in trials | Clinical | |
| HPTA suppression / SHBG reductionReduced sex-hormone-binding globulin and suppression of endogenous androgen signalling. | Moderate | Consistent in trials | Clinical |