GLPG0492 (DT-200)

Overview

GLPG0492 (also known as DT-200) is a nonsteroidal selective androgen receptor modulator (SARM) — specifically an aryl-hydantoin (diarylhydantoin) small molecule — developed by Galapagos NV. It is a small-molecule research compound, not a peptide, and it has never been an approved medicine for any purpose.

It was investigated for muscle-wasting conditions (cachexia) and Duchenne muscular dystrophy (DMD). Like other SARMs, it binds the androgen receptor (AR) with tissue-selective activity — in animal models it acted as an anabolic agent on skeletal muscle while relatively sparing reproductive tissue such as the prostate. Its most advanced human testing was Phase 1: three registered studies in healthy volunteers — a first-in-human single-ascending-dose study (completed around December 2010), a multiple-ascending-dose study, and a muscle-protein-synthesis pharmacodynamic study (completed April 2012). Development did not advance to later-phase trials, and no regulator ever approved it.

Chemistry and structure

The IUPAC name and full synonym list were not retrieved from PubChem in this session, so they are recorded as not established / not found in sources.

Mechanism of action

GLPG0492 acts on the androgen receptor rather than through any peptide/hormone-receptor pathway.

• [Animal] Binds the androgen receptor as a nonsteroidal ligand with tissue-selective activity. After oral dosing, GLPG0492 produced robust anabolic activity on the levator ani muscle comparable to testosterone propionate, dissociated from androgenic activity on the ventral prostate. (Cozzoli et al., Pharmacol Res 2013; hindlimb-immobilization mouse study, PMC4167280.)
• [Animal] Improves muscle performance and reduces muscle loss in a Duchenne muscular dystrophy disease model. Tested in the exercised-mdx mouse model over 4 weeks at 30 mg/kg (6 days/week, subcutaneous); it improved muscle strength and running performance, compared against α-methylprednisolone and nandrolone. (Cozzoli et al., Pharmacol Res 2013, PMID 23523664.)
• [Hypothesis] Tissue selectivity is the general SARM rationale — muscle anabolism without full androgenic effect — but this dissociation is demonstrated in animals and is not established in humans for this compound. The claimed avoidance of cardiovascular, prostate, or virilizing effects derives from preclinical and mechanistic reasoning, not from controlled human efficacy/safety trials. (Galapagos press materials; SARM review PMC7108998.)

Research and evidence

Human exposure was limited to Phase 1 across three registered healthy-volunteer studies. No Phase 2/3 trial and no published efficacy readout in a target patient population were located.

Honest read on endpoints: the human data are early-phase safety, pharmacokinetics, and short-term pharmacodynamics only, not efficacy in patients. The disease-relevant benefit (muscle strength, running performance) was shown in mice, not people.

Status and regulation

GLPG0492 is not approved by any regulator for any indication. Its development did not progress beyond Phase 1. Three Phase 1 studies in healthy volunteers are registered on ClinicalTrials.gov — NCT01130818 (single-ascending-dose), NCT01397370 (multiple-ascending-dose), and NCT01538420 (muscle-protein-synthesis pharmacodynamics, completed April 2012) — but no Phase 2/3 trial is registered and no target-population efficacy readout was located. The reason and exact date development was discontinued are not established / not found in sources.

In sport, GLPG0492 is an androgen-receptor agonist and is prohibited under WADA code S1.2 (Other Anabolic Agents — SARMs), at all times, in and out of competition. WADA status is a separate axis from any question of legality.

Safety

The safety story dominates here because human data are thin and this is a high-harm compound class. Signals are tagged by evidence type.

• [Hypothesis] Androgen-receptor-mediated HPTA / endogenous testosterone suppression. As an AR agonist, class effects include suppression of the hypothalamic-pituitary-testicular axis and endogenous testosterone. No GLPG0492-specific human suppression data were located; the Phase 1 studies reported no severe adverse events but were not designed to characterize chronic endocrine effects. (Severity: class risk.)
• [Human] Hepatotoxicity / drug-induced liver injury (SARM class). The FDA has warned that SARMs sold to consumers are associated with serious liver injury, including cases of acute liver failure. This is a class-level warning; no GLPG0492-specific DILI case was located, and it was never marketed. (Severity: class risk.)
• [Human] No characterized long-term or chronic-dose human safety. Human exposure was limited to short Phase 1 studies (single dose and up to ~2 weeks multiple-dose in healthy volunteers). Long-term safety, cardiovascular effects, and effects in patient populations are not established. (Severity: unknown — data absent.)
• [Human] Product contamination and mislabeling reality. (Severity: high — consumer reality.)

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. A "SARM" label — including any product claiming to be GLPG0492 — is not a reliable statement of contents.

Legal status

This page does not assess the legality of possession, sale, or personal use in any jurisdiction — legal status varies and changes. The honest framing is research-reagent only: GLPG0492 is an investigational compound with no approved human use. WADA prohibition (S1.2) is a separate axis from national legality and applies to athletes regardless of local law. Nothing here is legal advice (dated 2026-07-10).

How it compares

GLPG0492 belongs to the same nonsteroidal-SARM class as the more widely discussed research compounds Ostarine, Ligandrol, Andarine, and Testolone — all androgen-receptor modulators, all unapproved for physique or performance use, all prohibited in sport. GLPG0492 is distinguished mainly by how little human data exists: it never got past Phase 1, whereas some of those compounds reached later-phase trials. It is unrelated to non-androgen "SARM-adjacent" compounds that are sometimes grouped together in the marketplace but work through entirely different pathways, such as Cardarine (a PPARδ agonist) and Stenabolic (a Rev-ErbA agonist) — neither of which is a SARM.

Common misconceptions

• "It's a peptide." No. GLPG0492 is a small-molecule aryl-hydantoin (C19H14F3N3O3), not a peptide.
• "It's an approved or clinically proven muscle drug." No. It never advanced beyond Phase 1 and was never approved; the muscle-benefit data are from mice.
• "Tissue selectivity means it's safe." The muscle-versus-prostate dissociation is an animal finding; human safety, including testosterone suppression and liver effects, is not established, and the SARM class carries FDA-warned liver-injury risk.
• "It's a legal way to get steroid-like gains." It is unapproved, WADA-prohibited (S1.2), and the products sold as SARMs are usually mislabeled or contaminated.
• "If I buy 'GLPG0492' online I'm getting GLPG0492." Per JAMA 2017, most products sold as SARMs do not contain what the label claims.