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GSK-2881078 is one of the best-documented SARMs in humans, which alone sets it apart in a class full of guesswork. Developed by GlaxoSmithKline as a non-steroidal, tissue-selective androgen receptor agonist, it produced clean, dose-dependent gains in lean mass in older men and women and was carried into a controlled trial in patients with COPD. For anyone seeking a selective androgen receptor modulator with genuine clinical evidence and a real pharmaceutical pedigree, GSK-2881078 sits near the top of the list.
- Real human trials, rare for a SARM
- Built lean mass in older men and women
- Added leg strength when paired with exercise
- Targets muscle selectively, not the whole body
- Well tolerated across short human trials
- Big pharma pedigree from GlaxoSmithKline
- Small, usually reversible liver enzyme rises
Overview
GSK-2881078 is a non-steroidal selective androgen receptor modulator (SARM) developed by GlaxoSmithKline for the treatment of reduced mobility and muscle weakness associated with chronic and acute illness. As a SARM it is designed to act as a tissue-selective androgen receptor agonist, directing androgen signaling toward muscle while limiting the broader effects of traditional anabolic steroids [1].
The compound reached phase 1 and phase 2 clinical testing, making it one of the better-characterized SARMs in human research, complete with documented pharmacokinetics and safety data that most compounds in the class lack [1][4]. It is an oral agent, an attractive feature for a muscle-directed therapy [2].
Its research applications focus on lean mass and physical function. A phase 1b dose-escalation study in healthy older men and postmenopausal women showed dose-dependent increases in lean mass, with women exhibiting greater sensitivity at lower exposures, and generally good tolerability [1]. A phase 2a randomized, double-blind, placebo-controlled trial paired GSK-2881078 with a home exercise program in men and women with COPD and impaired physical function, examining leg strength and lean body mass [2]. The compound also features in systematic reviews of SARMs, which report positive effects on body composition and physical performance across the class alongside mild-to-moderate adverse effects [3][4], and it is cited among emerging therapies for age-related sarcopenia [4].
GSK-2881078 is an experimental drug, not an approved medicine or a dietary supplement; it is encountered in clinical research and on the gray market. Its long-term safety has not been established, and it remains investigational.
- GSK-2881078 is one of very few SARMs ever carried into controlled human trials, including a Phase 2a study in patients with COPD.
- In that trial, men combining the drug with exercise gained about 11.8 kilograms more leg strength than those on placebo plus exercise.
- A recognized marker of its androgenic activity in people is the suppression of sex hormone-binding globulin, which its developers tracked as a pharmacodynamic readout.
Mechanism
GSK-2881078 stands out for a reason that is rare among SARMs; it has actual human data. Its appeal is muscle-selective androgen action delivered orally, producing dose-dependent gains in lean mass in older adults with a tolerability profile documented in real trials rather than inferred from anecdotes.
The mechanism is selective agonism of the . Like other SARMs it binds the androgen receptor and activates anabolic signaling preferentially in skeletal muscle, aiming to build lean mass while sparing the prostate and other tissues that full androgens strongly affect [1]. A recognized marker of its androgenic activity in humans is suppression of sex hormone-binding globulin, and its metabolism involves CYP3A4, which the developers characterized for potential drug interactions [1].
The human evidence carries concrete numbers. In the phase 1b study, all dose levels produced greater lean-mass accrual than placebo, with postmenopausal women responding at lower doses than men, and adverse events limited largely to transient rises in alanine aminotransferase [1]. In the phase 2a COPD trial, GSK-2881078 combined with exercise increased leg strength in men, with an adjusted mean gain of about 11.8 kilograms and roughly 7.0 percent of predicted over placebo, and it raised lean body mass, though patient-reported outcomes did not change and the strength effect was less consistent in women [2]. Systematic reviews place these findings in context, reporting generally favorable body-composition and performance effects for SARMs alongside moderate rates of mild-to-moderate adverse effects [3]. The main safety signals observed were reversible reductions in HDL cholesterol, transient hepatic transaminase elevations, and lowered sex hormone-binding globulin, and long-term safety remains unestablished [1][2].
receptor fingerprint
Selective tissue-selective agonist
Skeletal muscleAnabolic stimulation
Sex hormone binding globulinSuppression
Safetyrisks and cautions, not medical advice
GSK-2881078 is a selective androgen receptor modulator (SARM); early-phase human studies showed the expected class effects, including suppression of endogenous testosterone and sex-hormone-binding globulin, reductions in HDL cholesterol, and mild elevations in liver enzymes. As with other SARMs, HPTA and testosterone suppression and adverse lipid shifts are the principal concerns, and long-term safety is not established. It remains an investigational compound not approved for general use.
History
GSK-2881078 is a non-steroidal selective androgen receptor modulator (SARM) developed by GlaxoSmithKline as a potential treatment for muscle wasting and weakness in aging and chronic illness. Unlike the many research SARMs known only from anecdote, it was advanced through formal clinical development, beginning with a Phase 1b study in healthy older men and postmenopausal women that established dose-dependent gains in lean mass and characterized its metabolism via CYP3A4 and its suppression of sex hormone-binding globulin.
It then progressed to a Phase 2a randomized, double-blind, placebo-controlled trial in patients with chronic obstructive pulmonary disease, combining the drug with a home exercise program and reporting results in Thorax in 2022. That trial (NCT03359473) enrolled 97 patients and measured leg strength, lean body mass, and safety. Its documented clinical program distinguishes it sharply from the largely uncharacterized SARM landscape.
Reputation
GSK-2881078 stands out among selective androgen receptor modulators for the simple reason that it carries genuine human data and a real pharmaceutical pedigree. In its Phase 1b study every dose level produced greater lean-mass accrual than placebo, and in the Phase 2a COPD trial it increased leg strength in men, with an adjusted mean gain of roughly 11.8 kilograms over placebo, alongside rises in lean body mass.
As a tissue-selective androgen receptor agonist it is designed to build muscle while sparing tissues that full androgens strongly affect, and it was described as well tolerated over short-term dosing. Honesty requires noting the limits: patient-reported outcomes did not improve, the strength effect was less consistent in women, and safety signals included reversible drops in HDL cholesterol and transient elevations in liver transaminases, with long-term safety unestablished. Even so, for a SARM backed by controlled clinical evidence, it sits near the top of the class.
Subjective profileweighing the evidence above
The best-documented SARM in humans, which counts for something in a class built on guesswork, and the lean-mass gains in older adults were clean and dose-dependent. It still does what SARMs do: suppresses your own testosterone, drops HDL and nudges liver enzymes. It was never approved for anyone.
Where to buy
Suppliers
Vendors carrying GSK-2881078, with live product details and codes. Links are affiliate links that support the wiki at no cost to you.
Kimera Chems
GSK-2881078
Research
- 2017first citedThe long and winding road for selective androgen receptor modulators
- 2018controlled trialGSK2881078, a SARM, Produces Dose-Dependent Increases in Lean Mass in Healthy Older Men and Wom…
- 2026most recentSarcopenia in Aging: Pathogenesis, Diagnosis, and Emerging Therapeutic Frontiers
- 1.GSK2881078, a SARM, Produces Dose-Dependent Increases in Lean Mass in Healthy Older Men and Women
- 2.Selective androgen receptor modulation for muscle weakness in chronic obstructive pulmonary disease: a randomised control trial
- 3.Selective Androgen Receptor Modulators (SARMs) Effects on Physical Performance: A Systematic Review of Randomized Control Trials
- 4.The long and winding road for selective androgen receptor modulators
- 5.Sarcopenia in Aging: Pathogenesis, Diagnosis, and Emerging Therapeutic Frontiers
5 listed here; entry last updated August 2026
Reviews
My notesprivate to this device
FAQ
Was GSK-2881078 tested in humans?
Yes; it went through phase 1 and phase 2 trials, including studies in older adults and COPD patients, which is unusual for compounds in this class.
Did it build strength?
It reliably increased lean mass, but strength results were mixed and differed between men and women, especially in the COPD study.
Is it approved?
No; development did not lead to approval, and it remains an investigational compound.
Adverse effects
- Small, usually reversible liver enzyme rises
Notes and cautions
- Some drop in HDL cholesterol in trials
- Lowers sex hormone binding globulin
- Strength effects were inconsistent, especially in women
- Long-term safety not yet established