Roidipedia.Compound reference & reporting
06 AUG 2026
CompoundsSARM GSK2881078
SARMNon-steroidalSARMExperimental

GSK2881078

Also known as GSK-2881078 · 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

TierDoseRouteNotes
Trial range0.75–10 mg/dayOralDoses studied in Phase I/II; not a validated physique protocol.

Ester comparison

EsterHalf-lifeInjection freq.Testosterone by mass

04 Effects

EffectMagnitudeEvidence
Increased lean body massSmall but measurable lean mass gains in early human trials over several weeks.~0.5-1.5 kgClinical
Improved muscle in wasting conditionsLean mass increases seen in COPD patients with muscle wasting.Clinical

05 Side effects

EffectSeverityFrequencyEvidenceCountermeasures
Transient liver enzyme elevationMild elevations in transaminases observed in some subjects.MildReportedClinical
HDL cholesterol reductionLowered HDL cholesterol observed across dosing, a class effect of oral SARMs.ModerateConsistent in trialsClinical
HPTA suppression / SHBG reductionReduced sex-hormone-binding globulin and suppression of endogenous androgen signalling.ModerateConsistent in trialsClinical

07 References

Safety, pharmacokinetics and pharmacodynamics of GSK2881078, a SARM, in healthy older subjectsBritish Journal of Clinical Pharmacology, 2018

08 Discussion0 comments

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