Is GSK2881078 approved as a medicine, and where?

No. GSK2881078 is investigational: it is being studied in human clinical trials but is not approved by any regulator and is not available as a licensed medicine.

What is GSK2881078 studied for?

GSK2881078 is most often discussed in the context of muscle & growth hormone. Research has examined muscle-growth-hormone. Being studied for an area does not mean it is proven or approved for it.

Does GSK2881078 have human clinical trials?

Yes. GSK2881078 is currently being studied in human clinical trials, but it is not yet approved.

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Androgen Receptor Modulators (SARMs)

GSK2881078

GSK2881078; GSK-2881078; GSK 2881078

10 min read · Updated July 10, 2026 · 8 references

Curated by PeptideInfo Wikilast reviewed July 10, 2026how we verify

Explored forMuscle & growth hormone

In brief · TL;DR

Investigational — active human trials· Not approved — investigational (reached Phase 2)

GSK2881078 is a nonsteroidal, orally active SARM developed by GlaxoSmithKline — not a peptide and not a steroid. It reached Phase 2 for muscle wasting and weakness: a first-in-human study and a 13-week COPD trial, where it raised lean body mass by roughly 2 kg with a quadriceps-strength signal that reached statistical support in men but not women. The same trials documented the class risks — transient liver-enzyme (transaminase) elevations including ALT >3x the upper limit of normal, reversible drops in HDL cholesterol and SHBG, and dose-dependent testosterone suppression in men. It is not approved for any use, has a very long (>100 h) half-life so effects persist for weeks, and is WADA-prohibited at all times. It is not a milder or safer alternative to steroids.

Evidence: In human clinical trials; not yet approved.

Nonsteroidal selective androgen receptor modulator (SARM) — a true SARM, NOT a peptide and NOT an anabolic steroid
Developed by GlaxoSmithKline (GSK) for muscle wasting and weakness; reached Phase 2 — not approved anywhere
In a 13-week Phase 2 COPD trial (NCT03359473) it raised lean body mass ~2 kg, with a quadriceps-strength signal statistically supported in men but not women, and no improvement in patient-reported outcomes
Same trials documented transient liver-enzyme (transaminase) elevations — including ALT >3x the upper limit of normal that resolved after stopping — plus reversible HDL-cholesterol and SHBG reductions and dose-dependent testosterone suppression in men
Very long half-life (>100 h) means exposure and any adverse effects persist for weeks after dosing stops
WADA-prohibited at all times under S1.2 (Anabolic Agents / SARMs); validated urine and hair detection methods exist

↓ Read the full referenced entry below

Facts at a glance

GSK2881078

2D structure · PubChem (public domain)

Class: Nonsteroidal selective androgen receptor modulator (SARM) — a true SARM, an orally active small-molecule androgen receptor ligand — NOT a peptide, NOT an anabolic steroid, and NOT an approved medicine.
Status: Investigational (reached Phase 2); not approved anywhere. GSK appears to have discontinued active development after Phase 2 (not confirmed in sources reviewed).
Mol. weight: 330.33 g/mol (approximate, from formula C14H13F3N2O2S); CAS 1539314-06-1; PubChem CID 86709174
Half-life: Long terminal half-life reported as >100 hours in the first-in-human study (Clark et al., Br J Clin Pharmacol 2017, PMID 28449232)
Form: Orally active small molecule; no approved pharmaceutical formulation exists

Dosing

No established dose. No approved dose exists. The compound is in active human trials, so doses under study exist but remain investigational — they are protocol-defined and subject to change, not an authorised regimen. Trial doses, where relevant, are described with their citation in the research section.

Research areas

muscle-growth-hormone

A nonsteroidal, orally active selective androgen receptor modulator (SARM) developed by GlaxoSmithKline as an investigational treatment for muscle wasting and weakness — NOT a peptide and NOT an anabolic steroid. It reached Phase 2 (first-in-human study, Clark et al., Br J Clin Pharmacol 2017, PMID 28449232; and a 13-week Phase 2 trial in COPD, Thorax 2022, PMID 36283827, NCT03359473), where it raised lean body mass by ~2 kg with a strength signal in men — while the same trials documented the class-defining risks: transient liver-enzyme (transaminase) elevations, reduced HDL cholesterol and SHBG, and dose-dependent testosterone suppression in men. It is NOT an approved medicine for any use.

Contents9

Section 1 of 9Overview

Overview

GSK2881078 (also written GSK-2881078 or GSK 2881078) is a nonsteroidal, orally active selective androgen receptor modulator (SARM) developed by GlaxoSmithKline (GSK) as an investigational treatment for muscle wasting and weakness. It is a true SARM — a small-molecule androgen receptor ligand. It is NOT a peptide (it is not an amino-acid chain) and NOT an anabolic steroid (its scaffold is nonsteroidal).

Unlike most SARMs sold on the grey market, GSK2881078 has a genuine clinical development history: a first-in-human Phase 1 study (Clark et al., Br J Clin Pharmacol 2017) and a 13-week Phase 2 randomized, placebo-controlled trial in patients with COPD and muscle weakness (Thorax 2022; NCT03359473). In those trials it increased lean body mass by roughly 2 kg and produced a signal toward increased quadriceps strength (statistically supported in men, not women). It appears on this peptide reference because it is frequently discussed and stacked alongside peptides in the fitness and "research chemical" community — not because it is one.

Not approved — investigational, with documented hepatic and hormonal risks

GSK2881078 is not approved by any regulator (FDA, EMA, or otherwise) for any use. It reached Phase 2 and appears to have gone no further. The same trials that showed lean-mass gains also documented the risks that define this drug class: transient liver-enzyme (transaminase) elevations — including cases of ALT >3x the upper limit of normal that resolved after stopping — plus reversible reductions in HDL cholesterol and SHBG and dose-dependent suppression of testosterone in men. Its very long half-life (>100 h) means exposure and any adverse effects persist for weeks after dosing stops. It is WADA-prohibited at all times. This page is educational and is not medical, legal, or dosing advice; nothing here endorses or guides human use. This is not a "milder, safer, or legal alternative" to anabolic steroids.

Section 2 of 9Chemistry and structure

Chemistry and structure

GSK2881078 is a nonsteroidal small molecule — an amino-acid chain it is not.

Property	Value
Name	GSK2881078 (GSK-2881078 / GSK 2881078)
Class	Nonsteroidal selective androgen receptor modulator (SARM) — not a peptide, not a steroid
Molecular formula	C14H13F3N2O2S
Molecular weight	330.33 g/mol (approximate, from formula; verify against PubChem CID 86709174)
CAS number	1539314-06-1
PubChem CID	86709174
Route	Orally active
Elimination half-life	>100 h reported in the first-in-human study (Clark et al. 2017, PMID 28449232)

Section 3 of 9Mechanism of action

Mechanism of action

Androgen receptor (AR) agonism — tissue-selective by design. GSK2881078 is a nonsteroidal small-molecule ligand of the androgen receptor that acts as a tissue-selective modulator: it is designed to drive anabolic (muscle-building) signaling while sparing the androgenic effects on other tissues typical of testosterone and anabolic steroids. It has been reported to show greater than 100-fold selectivity for the androgen receptor over the glucocorticoid, mineralocorticoid, and progesterone receptors. As a nonsteroidal small molecule it is fundamentally NOT a peptide. [In vitro] / [Human]
Anabolic effect in muscle (human). AR agonism in muscle is reflected by increased lean body mass (~2 kg over 13 weeks) and a strength signal in the quadriceps in the Phase 2 COPD trial (Thorax 2022, PMID 36283827; NCT03359473). [Human]
Systemic androgenic / anti-gonadotropic activity (human). Evidenced by dose-dependent suppression of endogenous testosterone in men and reductions in sex-hormone-binding globulin (SHBG) — consistent with suppression of the hypothalamic-pituitary-testicular (HPTA) axis. This is an on-target androgenic effect, not a benign one (Clark et al., Br J Clin Pharmacol 2017, PMID 28449232). [Human]
Lipid effect (human). A dose-dependent lowering of HDL ("good") cholesterol was observed — a metabolic/lipid change characteristic of androgenic compounds, seen in both the Phase 1 and Phase 2 trials (PMID 28449232, PMID 36283827). [Human]

Section 4 of 9Research and evidence

Research and evidence

GSK2881078 has real, though limited, human data. It reached Phase 2 and there are no Phase 3 trials and no regulatory approval.

Finding	Model	Source
First-in-human Phase 1 (single + repeat oral dosing) in healthy young men (n~~65 across parts) and postmenopausal women (n~~24); dose-proportional exposure, long (>100 h) half-life, and dose-dependent reductions in testosterone (men), SHBG, and HDL; concluded acceptable tolerability supporting further study	[Human] — Phase 1, healthy volunteers	Clark RV et al., Br J Clin Pharmacol 2017 (PMID 28449232); NCT02045940 (first-in-human program)
Phase 2A randomized, double-blind, placebo-controlled trial in COPD with muscle weakness (97 randomized: 47 postmenopausal women at 1.0 mg/day, 50 men at 2.0 mg/day) for 13 weeks with a home-exercise program; total lean body mass rose ~2.1 kg in both sexes; quadriceps 1-RM strength signal reached statistical support in men but not women; no improvement in patient-reported outcomes; main treatment-related findings were reversible HDL reductions and transient transaminase elevations	[Human] — Phase 2, COPD patients	Thorax 2022 (PMID 36283827); NCT03359473
Anti-doping detection: GSK2881078 and its hydroxy-metabolites detectable in urine (peak ~920 pg/mL at 8 h, falling to detection limit by ~day 42) and in hair (peak ~1.7 pg/mg) after a single oral dose — establishing sport testing protocols	[Human] — controlled single-dose administration	Drug Testing and Analysis 2021 (PMID 33037775)

Human evidence in context. The efficacy signal is real but modest: about 2 kg of lean mass over 13 weeks and a strength signal in men only, with no improvement in how patients actually felt or functioned (patient-reported outcomes). There are no Phase 3 trials, no approval, and no long-term (beyond 13 weeks) safety data. Full reversibility and the time-course of testosterone/HPTA suppression after stopping are not fully characterized in the published trials.

Section 5 of 9Status and regulation

Status and regulation

Regulatory approval: None. GSK2881078 is not approved by the FDA, the EMA, or any other regulator for any indication. It is investigational — it reached Phase 2 and appears to have gone no further; GSK appears to have discontinued active development after Phase 2 (current development status not confirmed in sources reviewed).
Anti-doping: Prohibited by the World Anti-Doping Agency (WADA) at all times (in- and out-of-competition), listed under S1.2 (Anabolic Agents — Other Anabolic Agents, SARMs). Validated urine and hair detection methods exist (PMID 33037775). The precise sub-code should be confirmed against the current-year WADA Prohibited List, which is revised annually. WADA is a sport-eligibility axis and is separate from any question of legality.
Market reality: Outside clinical research it is sold only as an unregulated "research chemical" of unknown identity, purity, and potency.

Section 6 of 9Safety

Safety

The trials that showed benefit also documented the harms

GSK2881078's own clinical trials define its risk profile. The Phase 2 COPD trial reported transient elevations of hepatic transaminases (liver enzymes) as a main treatment-related finding — including cases of ALT (a liver enzyme) more than 3x the upper limit of normal that resolved after discontinuation [PMID 36283827] [Human]. This mirrors the class-wide drug-induced liver injury (DILI) concern for nonsteroidal SARMs, and the FDA has warned that products marketed as SARMs are associated with serious liver injury, including acute liver failure. The trials also documented dose-dependent testosterone suppression in men with reduced SHBG (HPTA suppression) [PMID 28449232] and reversible HDL-cholesterol reductions [PMID 28449232, PMID 36283827] [Human].

Documented and expected safety signals (tagged by evidence type):

Hepatotoxicity / transient transaminase elevation [Human]. Transient liver-enzyme (transaminase) elevations were a main treatment-related finding in the Phase 2 COPD trial, including ALT >3x the upper limit of normal that resolved after stopping. This reflects the class-wide DILI concern; the mechanism and predictors of these elevations, and long-term hepatic safety, are not established. Sources: Thorax 2022 (PMID 36283827); FDA SARM safety communications; NIH LiverTox.
Testosterone / HPTA suppression [Human]. Dose-dependent reductions in endogenous testosterone in men, with reduced SHBG — indicating suppression of the hypothalamic-pituitary-testicular axis. This is an on-target androgenic effect, not a benign one. No dosing, "cycle," or post-cycle guidance is given here. Source: Br J Clin Pharmacol 2017 (PMID 28449232).
HDL-cholesterol reduction [Human]. Dose-dependent, reversible lowering of HDL ("good") cholesterol in both the Phase 1 and Phase 2 trials — a cardiovascular-relevant lipid change; the consequences of chronic HDL lowering with this compound are not established. Sources: PMID 28449232, PMID 36283827.
Not an approved medicine; very long half-life [Human]. GSK2881078 is investigational only, approved by no regulator for any indication, and its very long half-life (>100 h) means exposure and any adverse effects persist for weeks after dosing stops. It must not be framed as a milder, safer, or legal alternative to anabolic steroids.

Contamination reality — a 'SARM' label is not a statement of contents

Van Wagoner et al. (JAMA 2017;318(20):2004-2010, PMID 29183075) chemically analyzed 44 products sold online as SARMs: only 52% actually contained the labeled SARM, 39% contained a different unapproved drug, and 9% contained no active compound at all; the labeled amount matched the analysis in only 41%. A "SARM" label — including one reading "GSK2881078" — is therefore not a reliable statement of what is inside the product. This is an independent hazard on top of the drug's own risks and a common source of inadvertent anti-doping violations.

Section 7 of 9Legal status

Legal status

Legality not assessed here

This page does not assess the legality of buying or possessing GSK2881078 in any specific country. What is documented: it is not an approved medicine, supplement, or food ingredient anywhere, it is an investigational drug sold otherwise only as a research reagent, and it is not legal to sell for human consumption as a supplement (the FDA has issued warnings and warning letters on SARMs marketed as "dietary supplements"). Separately, it is prohibited in sport by WADA at all times. "Research chemical" status is a legal and safety gray zone — it is not a signal of safety or approval, and this is not a "milder, safer, or legal alternative" to steroids. This is not legal advice; check your own jurisdiction.

Section 8 of 9How it compares

How it compares

GSK2881078 is often grouped with other SARMs and with non-SARM "research chemicals." The honest framing:

Ostarine, ligandrol (LGD-4033), andarine, testolone (RAD-140) — other nonsteroidal SARMs that share GSK2881078's mechanism (AR agonism), testosterone- suppression risk, WADA S1.2 status, and lack of approval. GSK2881078 stands out for having a published, GSK-run Phase 1 and Phase 2 program, whereas most grey-market SARMs never had a sponsor take them through controlled human trials.
Cardarine (GW-501516) and stenabolic (SR9009) — frequently sold alongside SARMs but are NOT SARMs; cardarine is a PPARδ agonist and stenabolic is a Rev-ErbA agonist, with different mechanisms and their own risks.
MK-677 (ibutamoren) — frequently grouped with SARMs but is a growth-hormone secretagogue / ghrelin agonist, not a SARM.

The decisive point: GSK2881078 is investigational, reached only Phase 2, is not approved for anything, and its efficacy signal (~2 kg lean mass, strength in men only, no patient-reported-outcome benefit) came hand in hand with liver-enzyme, hormonal, and lipid risks. See the Muscle, growth & hormones overview.

Section 9 of 9Common misconceptions

Common misconceptions

"GSK2881078 is a peptide." No. It is a nonsteroidal small molecule (C14H13F3N2O2S, ~330.33 g/mol). It is covered here only because it is discussed and stacked with peptides.
"A big pharma company developed it, so it must be safe/effective for muscle." No. GSK took it to Phase 2 and no further; it is not approved, showed only a modest lean-mass gain with no patient-reported-outcome benefit, and the same trials documented liver-enzyme, testosterone, and HDL risks.
"It's a milder, safer, legal alternative to steroids." No. It suppresses natural testosterone, lowers HDL, caused transient liver-enzyme elevations, and is not approved. "SARM" does not mean "safe."
"Buying it as a 'research chemical' means it's clean and correctly dosed." No. Independent testing (JAMA 2017) found most products sold as SARMs were mislabeled, contained a different drug, or contained nothing.

This entry is educational and summarizes published research and public regulatory information as of the "updated" date above. It is not medical advice, not legal advice, a recommendation, or a guide to obtaining or using any substance.

References8

References

1.
Safety, pharmacokinetics and pharmacological effects of the selective androgen receptor modulator, GSK2881078, in healthy men and postmenopausal women — Clark RV, Walker AC, Andrews S, et al., British Journal of Clinical Pharmacology, 2017. source
2.
Selective androgen receptor modulation for muscle weakness in chronic obstructive pulmonary disease: a randomised control trial — Thorax (research article), Thorax, 2022. source
3.
Study to Evaluate the Safety and Efficacy of 13 Weeks of the SARM GSK2881078 in COPD (NCT03359473) — GlaxoSmithKline, ClinicalTrials.gov, 2022. source
4.
Detection of the selective androgen receptor modulator GSK2881078 and metabolites in urine and hair after single oral administration — Drug Testing and Analysis (research article), Drug Testing and Analysis, 2021. source
5.
Chemical Composition and Labeling of Substances Marketed as Selective Androgen Receptor Modulators and Sold via the Internet — Van Wagoner RM, Eichner A, Bhasin S, Deuster PA, Eichner D., JAMA, 2017. source
6.
PubChem Compound Summary: GSK2881078 (CID 86709174) — National Library of Medicine (PubChem), PubChem, 2026. source
7.
Selective Androgen Receptor Modulators — LiverTox: Clinical and Research Information on Drug-Induced Liver Injury — National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK), LiverTox (NCBI Bookshelf), 2023. source
8.
FDA Warns of Use of Selective Androgen Receptor Modulators (SARMs) Among Teens, Young Adults — U.S. Food and Drug Administration, FDA Consumer Updates, 2026. source

Frequently asked questions4

Frequently asked questions

What is GSK2881078?: A nonsteroidal, orally active selective androgen receptor modulator (SARM) developed by GlaxoSmithKline as an investigational treatment for muscle wasting and weakness — NOT a peptide and NOT an anabolic steroid. It reached Phase 2 (first-in-human study, Clark et al., Br J Clin Pharmacol 2017, PMID 28449232; and a 13-week Phase 2 trial in COPD, Thorax 2022, PMID 36283827, NCT03359473), where it raised lean body mass by ~2 kg with a strength signal in men — while the same trials documented the class-defining risks: transient liver-enzyme (transaminase) elevations, reduced HDL cholesterol and SHBG, and dose-dependent testosterone suppression in men. It is NOT an approved medicine for any use.
Is GSK2881078 approved as a medicine, and where?: No. GSK2881078 is investigational: it is being studied in human clinical trials but is not approved by any regulator and is not available as a licensed medicine.
What is GSK2881078 studied for?: GSK2881078 is most often discussed in the context of muscle & growth hormone. Research has examined muscle-growth-hormone. Being studied for an area does not mean it is proven or approved for it.
Does GSK2881078 have human clinical trials?: Yes. GSK2881078 is currently being studied in human clinical trials, but it is not yet approved.

Educational disclaimer. This article summarizes published research for informational purposes and is not medical advice. GSK2881078 is a research chemical not approved for human use. Consult a qualified healthcare professional before making health decisions.

References

Frequently asked questions

Related in Androgen Receptor Modulators (SARMs)