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GSK-2849466 is an experimental non-steroidal selective androgen receptor modulator (SARM) developed by GlaxoSmithKline. It was evaluated in an early-stage, phase I clinical trial that assessed its safety, tolerability, and pharmacological behavior in healthy men, in the context of possible use for muscle-wasting conditions such as cachexia [1][2]. It did not become an approved medicine and remains a research compound.
- potential tissue-selective anabolic effect
- distinct receptor engagement profile
- non-steroidal, no estrogen conversion
- As an androgen receptor agonist, expected to suppress natural testosterone
Overview
GSK-2849466 is a selective androgen receptor modulator, one of a class of non-steroidal compounds that bind the androgen receptor, the protein normally activated by testosterone, and are designed to stimulate it selectively so as to build muscle and bone with reduced effects on other androgen-sensitive tissues [2][3]. It was developed by the pharmaceutical company GlaxoSmithKline as part of broader industry interest in SARMs as potential treatments for disorders involving loss of muscle mass and strength [2][3].
The principal public record of GSK-2849466 is a phase I clinical study [1]. Conducted in healthy male volunteers, it was a single-center, randomized, placebo-controlled trial designed to examine the compound's safety, tolerability, pharmacokinetics, and pharmacodynamics when given in single and repeated doses, with and without food; it was framed around cachexia, the muscle-wasting syndrome that accompanies many serious illnesses [1]. Early-phase studies of this kind are meant to characterize how a drug behaves in the body rather than to prove that it treats a disease.
Within the scientific literature on SARMs, individual compounds are distinguished by how they bind the androgen receptor and by the receptor conformations and coregulator interactions they favor, features thought to underlie their tissue-selective effects [2][3]. Detailed, peer-reviewed characterization of GSK-2849466 specifically is scarce, and most of what is publicly documented about it derives from its clinical-trial record rather than from published laboratory studies [1]. As a result, precise figures for its potency and tissue selectivity in humans are not well established.
GSK-2849466 did not advance to become an approved drug and is best regarded as an investigational compound. As with the SARM class as a whole, no agent of this type had gained approval for muscle-wasting indications as of the mid-2020s, and the long-term safety of GSK-2849466 in humans has not been established [2][3]. It is not a licensed medicine and is encountered mainly as a footnote in the pharmacology of androgen receptor modulators.
Mechanism
As a selective modulator, GSK-2849466 is understood to act on the androgen receptor, the nuclear hormone receptor through which testosterone and dihydrotestosterone regulate the growth of muscle and bone [2][3]. Compounds of this class bind the receptor and activate it in a tissue-selective fashion, seeking to reproduce the anabolic, muscle-building effects of androgens while limiting stimulation of tissues such as the prostate; this selectivity is attributed to the particular conformation the receptor adopts when bound to a given modulator and to the set of coregulatory proteins it recruits, which differ from those engaged by natural steroids [2][3].
For GSK-2849466 in particular, the publicly available information is largely confined to its phase I evaluation of safety and pharmacology in healthy men, so the fine detail of its tissue selectivity and potency in people is not well documented [1]. Like other agonists, it would be expected to exert negative feedback on the hypothalamic-pituitary axis that governs the body's own testosterone production [2]. Being non-steroidal, it would not be converted into or dihydrotestosterone by the enzymes that normally act on testosterone, a general feature that separates the SARM class from anabolic steroids [3].
receptor fingerprint
modulator
Skeletal muscleagonist
conformationalters
HPG axissuppresses
Dosingtypical ranges, not medical advice
interested in protocols and clinical dosages? make an account to see them! ^_^
Safetyrisks and cautions, not medical advice
Human safety data is essentially absent. Standard SARM concerns apply: suppression of natural testosterone, unfavorable lipid shifts, and possible liver strain. Because it only exists through research suppliers, purity and dosing are unreliable.
Resources
This entry is here for reference.
Research
- 1.Study of the selective androgen receptor modulator GSK2849466 in single and repeat doses in healthy male subjects (ClinicalTrials.gov NCT01696604)
- 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
Is there human data on GSK-2849466?
Not really; it's known mostly from receptor pharmacology work.
Is it approved?
No, it never advanced to clinical use.
How is it different from other SARMs?
Its interest is in how it changes the androgen receptor's shape and gene activation, but the practical meaning of that is unclear.
Should I use it?
No; the data just isn't there to judge safety.
Limitations of the evidence
- An investigational compound, not an approved medicine
- Public data are limited mostly to a single early-phase trial
Adverse effects
- As an androgen receptor agonist, expected to suppress natural testosterone