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GSK-971086 is an experimental non-steroidal selective androgen receptor modulator (SARM) developed by GlaxoSmithKline. It was tested in an early-stage, phase I clinical trial that examined its safety, tolerability, and pharmacokinetics in healthy men, with a view to conditions involving androgen deficiency and loss of muscle [1][2]. It did not reach approval and remains investigational.
- supports lean muscle in models
- no estrogen conversion
- relative androgenic sparing
- Studied only in early-phase human trials
Overview
GSK-971086 is a non-steroidal selective androgen receptor modulator, a member of the SARM class of compounds that bind the androgen receptor, the target of testosterone, and are intended to activate it selectively so as to build lean tissue while causing fewer of the effects associated with androgens on the prostate and skin [2][3]. It was developed by GlaxoSmithKline during a period of substantial pharmaceutical interest in SARMs as candidate therapies for muscle loss and related conditions [2][3].
GSK-971086 progressed to human testing, and its principal public record is a phase I clinical trial in healthy adult male volunteers [1]. That study was a randomized, double-blind, placebo-controlled, dose-escalation trial evaluating the safety, tolerability, and pharmacokinetics of the compound after a single dose and after seven days of repeated dosing, listing conditions of healthy subjects and androgen deficiency [1]. With an enrollment on the order of a hundred participants, it was a comparatively substantial early-phase evaluation, though it was still designed to assess safety and drug behavior rather than clinical benefit.
As a non-steroidal androgen receptor ligand, GSK-971086 would not be expected to aromatize into estrogen or to be converted into dihydrotestosterone the way testosterone can, and its selectivity was intended to spare tissues such as the prostate from strong stimulation [2][3]. Beyond its trial record, however, detailed peer-reviewed data on the specific molecule are limited, and precise measures of its potency and tissue selectivity in humans are not well established in the public literature [1].
GSK-971086 did not proceed to later-stage development or approval, and no long-term human safety picture exists for it. It is best considered a shelved investigational compound rather than a therapeutic option. As with SARMs in general, no drug of this class had been approved for muscle-wasting indications as of the mid-2020s, and interest in these agents has been tempered by unresolved questions about their long-term effects [2][3].
Mechanism
GSK-971086 acts, in common with the rest of the SARM class, on the , the nuclear hormone receptor that mediates the effects of testosterone and dihydrotestosterone on muscle, bone, and other tissues [2][3]. On binding the receptor it is intended to function as a tissue-selective , promoting anabolic gene programs in skeletal muscle while producing weaker stimulation of androgen-sensitive tissues such as the prostate; this tissue selectivity is thought to arise from the specific way each modulator shapes the receptor and the coregulatory proteins it is able to recruit [2][3].
Because it is a non-steroidal molecule, it is not a substrate for aromatase or 5-alpha-reductase, the enzymes that convert testosterone into and dihydrotestosterone, so it does not give rise to those metabolites [2][3]. As an it would, like testosterone itself, be expected to signal back to the and pituitary and thereby suppress the body's own testosterone output [2]. The publicly available characterization of GSK-971086 is dominated by its phase I safety and pharmacokinetic study, so the quantitative details of how strongly and how selectively it engages the receptor in humans remain sparsely documented [1].
receptor fingerprint
partial agonist
Skeletal muscleagonist
HPG axissuppresses
Prostate and skinweak agonist
Dosingtypical ranges, not medical advice
interested in protocols and clinical dosages? make an account to see them! ^_^
Safetyrisks and cautions, not medical advice
Only limited early human exposure exists, and long-term safety is unknown. Expected risks include testosterone suppression, cholesterol shifts, and possible liver strain. It is a research chemical, so source quality and dosing accuracy are unreliable.
Subjective profileweighing the evidence above
It got a little further in development than most obscure SARMs, but there is still no reason to use it given the thin data.
Resources
This entry is here for reference.
Research
- 1.Dose-escalation study of the safety, tolerability, and pharmacokinetics of GSK971086 after single and repeat dosing in healthy adult male volunteers (ClinicalTrials.gov NCT00540553)
- 2.Development of selective androgen receptor modulators (SARMs)
- 3.Selective androgen receptor modulators: current knowledge and clinical applications
3 listed here; entry last updated July 2026
Reviews
My notesprivate to this device
FAQ
Did GSK-971086 reach humans?
It saw some early clinical testing but was not developed to approval.
Is it safe?
Long-term safety is unknown, and it is best treated as experimental.
Does it convert to estrogen?
No, it is non-steroidal and does not aromatize.
Why was it dropped?
Like many candidates, the risk-benefit case didn't support continued development.
Adverse effects
- Studied only in early-phase human trials
Notes and cautions
- An investigational compound that did not reach approval
- As an androgen receptor agonist, expected to suppress natural testosterone