GLPG-0492

GLPG-0492
Legal status
Legal status
Identifiers
  • 4-[(4R)-4-(hydroxymethyl)-3-methyl-2,5-dioxo-4-phenylimidazolidin-1-yl]-2-(trifluoromethyl)benzonitrile
CAS Number
PubChem CID
ChemSpider
ChEMBL
Chemical and physical data
FormulaC19H14F3N3O3
Molar mass389.334 g·mol−1
3D model (JSmol)
  • CN1C(=O)N(C(=O)[C@]1(CO)C2=CC=CC=C2)C3=CC(=C(C=C3)C#N)C(F)(F)F
  • InChI=1S/C19H14F3N3O3/c1-24-17(28)25(14-8-7-12(10-23)15(9-14)19(20,21)22)16(27)18(24,11-26)13-5-3-2-4-6-13/h2-9,26H,11H2,1H3/t18-/m0/s1
  • Key:VAJGULUVTFDTAS-SFHVURJKSA-N

GLPG-0492 (DT-200) is a drug which acts as a selective androgen receptor modulator (SARM). It has been investigated for the treatment of cachexia and muscular dystrophy.[1][2][3][4][5][6]

  1. ^ Nique F, Hebbe S, Triballeau N, Peixoto C, Lefrançois JM, Jary H, et al. (October 2012). "Identification of a 4-(hydroxymethyl)diarylhydantoin as a selective androgen receptor modulator". Journal of Medicinal Chemistry. 55 (19): 8236–8247. doi:10.1021/jm300281x. PMID 22957947.
  2. ^ Cozzoli A, Capogrosso RF, Sblendorio VT, Dinardo MM, Jagerschmidt C, Namour F, et al. (June 2013). "GLPG0492, a novel selective androgen receptor modulator, improves muscle performance in the exercised-mdx mouse model of muscular dystrophy". Pharmacological Research. 72: 9–24. doi:10.1016/j.phrs.2013.03.003. hdl:11586/62855. PMID 23523664.
  3. ^ Blanqué R, Lepescheux L, Auberval M, Minet D, Merciris D, Cottereaux C, et al. (September 2014). "Characterization of GLPG0492, a selective androgen receptor modulator, in a mouse model of hindlimb immobilization". BMC Musculoskeletal Disorders. 15: 291. doi:10.1186/1471-2474-15-291. PMC 4167280. PMID 25185887.
  4. ^ Zierau O, Kolodziejczyk A, Vollmer G, Machalz D, Wolber G, Thieme D, Keiler AM (May 2019). "Comparison of the three SARMs RAD-140, GLPG0492 and GSK-2881078 in two different in vitro bioassays, and in an in silico androgen receptor binding assay". The Journal of Steroid Biochemistry and Molecular Biology. 189: 81–86. doi:10.1016/j.jsbmb.2019.02.014. PMID 30825507. S2CID 72334106.
  5. ^ Fonseca GW, Dworatzek E, Ebner N, Von Haehling S (August 2020). "Selective androgen receptor modulators (SARMs) as pharmacological treatment for muscle wasting in ongoing clinical trials". Expert Opinion on Investigational Drugs. 29 (8): 881–891. doi:10.1080/13543784.2020.1777275. PMID 32476495. S2CID 219174372.
  6. ^ Stacchini C, Botrè F, Comunità F, de la Torre X, Dima AP, Ricci M, Mazzarino M (February 2021). "Simultaneous detection of different chemical classes of selective androgen receptor modulators in urine by liquid chromatography-mass spectrometry-based techniques". Journal of Pharmaceutical and Biomedical Analysis. 195: 113849. doi:10.1016/j.jpba.2020.113849. PMID 33383501. S2CID 229941017.