GSK-2881078

Overview

GSK-2881078 is a nonsteroidal selective androgen receptor modulator (SARM) of the indole-5-carbonitrile chemotype, developed by GlaxoSmithKline to produce tissue-selective anabolic effects in skeletal muscle with reduced activity in androgen-sensitive tissues. It has been studied in three human clinical trials (Phase I and Phase IIa) but has never been approved for any indication and is not in active further development. SARMs as a pharmacological class are prohibited in sport at all times under WADA category S1.2 (Other Anabolic Agents), though GSK-2881078 is not individually named in reviewed WADA documents.

Mechanism of Action

GSK-2881078 is a nonsteroidal small molecule built on an indole-5-carbonitrile scaffold that binds the androgen receptor to produce tissue-selective anabolic effects in skeletal muscle, with intended reduced activity in prostate and other androgen-sensitive tissues relative to testosterone. No published crystal structure or binding-affinity (Ki/EC50) data for the androgen receptor were located, so the precise selectivity mechanism versus other tissues is not independently confirmed beyond the class description used in clinical trial publications.

Research Summary

Human data are the most extensive of any compound in the SARM class: a Phase I first-in-human study in healthy men and postmenopausal women (Clark 2017) established dose-proportional systemic exposure and a long half-life (>100 hours) supporting once-daily dosing; a Phase I dose-escalation study in adults ≥50 years (Neil 2018) showed dose-dependent lean body mass gains (~3.39 kg in women, ~1.76 kg in men versus placebo at 8 weeks) accompanied by transient ALT elevations and 30–45% HDL-cholesterol reductions at the highest doses, both reversible on stopping treatment; and a Phase IIa randomized controlled trial in 97 COPD patients with muscle weakness (Mohan 2023) demonstrated increased lean body mass and leg-press strength (more consistently in men) over 13 weeks, with reversible HDL-C reduction and transient ALT increases as the main treatment-related safety signals. No peer-reviewed animal or in-vitro pharmacology/toxicology data for GSK-2881078 were located via PubMed or PubChem.

Vendors selling GSK-2881078

Scored vendors carrying GSK-2881078, ranked by trust grade. Grades are computed from indexed Certificates of Analysis. Full $/mg pricing is on the comparison page.

Reported Side Effects

• Reversible HDL-cholesterol reductions (30–45% at highest doses)
• Transient ALT elevations (modeled as limited, reversible hepatocyte turnover)
• Reversible reductions in testosterone and SHBG in men
• Exercise-related CPK elevation (two cases in Phase I)
• Drug rash (one withdrawal in Phase I)

Compare GSK-2881078 with Others

Research References

• Safety, pharmacokinetics and pharmacological effects of the selective androgen receptor modulator, GSK2881078, in healthy men and postmenopausal women. 2017. PMID 28449232.
• GSK2881078, a SARM, Produces Dose-Dependent Increases in Lean Mass in Healthy Older Men and Women. 2018.
• Selective androgen receptor modulation for muscle weakness in chronic obstructive pulmonary disease: a randomised control trial. 2023. PMID 36283827.
• Study to Evaluate the Safety and Efficacy of 13 Weeks of GSK2881078 in COPD — NCT03359473. 2018.

Frequently asked questions

Has GSK-2881078 been independently lab-tested?

Disclosed Labs has collected 2 Certificates of Analysis (COA) for GSK-2881078 from 2 independent testing labs. 1 vendor has submitted material for testing. Products average 99.6% tested purity across the corpus. Full testing data is available at https://www.disclosedlabs.com/peptides/gsk-2881078/testing.

Where can researchers source GSK-2881078?

1 vendor with Disclosed Labs trust grades currently list GSK-2881078, including Kimera Chems. Compare live prices and lab-verified COAs at https://www.disclosedlabs.com/prices/gsk-2881078.

How does GSK-2881078 work?

GSK-2881078 is a nonsteroidal small molecule built on an indole-5-carbonitrile scaffold that binds the androgen receptor to produce tissue-selective anabolic effects in skeletal muscle, with intended reduced activity in prostate and other androgen-sensitive tissues relative to testosterone. No published crystal structure or binding-affinity (Ki/EC50) data for the androgen receptor were located, so the precise selectivity mechanism versus other tissues is not independently confirmed beyond the class description used in clinical trial publications.

What does the research say about GSK-2881078?

Human data are the most extensive of any compound in the SARM class: a Phase I first-in-human study in healthy men and postmenopausal women (Clark 2017) established dose-proportional systemic exposure and a long half-life (>100 hours) supporting once-daily dosing; a Phase I dose-escalation study in adults ≥50 years (Neil 2018) showed dose-dependent lean body mass gains (~3.39 kg in women, ~1.76 kg in men versus placebo at 8 weeks) accompanied by transient ALT elevations and 30–45% HDL-cholesterol reductions at the highest doses, both reversible on stopping treatment; and a Phase IIa randomized controlled trial in 97 COPD patients with muscle weakness (Mohan 2023) demonstrated increased lean body mass and leg-press strength (more consistently in men) over 13 weeks, with reversible HDL-C reduction and transient ALT increases as the main treatment-related safety signals. No peer-reviewed animal or in-vitro pharmacology/toxicology data for GSK-2881078 were located via PubMed or PubChem.