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GSK2881078
Legal status
Legal status
  • US: Investigational drug
Identifiers
  • 1-[(2R)-1-methylsulfonylpropan-2-yl]-4-(trifluoromethyl)indole-5-carbonitrile
CAS Number
PubChem CID
ChemSpider
UNII
Chemical and physical data
FormulaC14H13F3N2O2S
Molar mass330.33 g·mol−1
3D model (JSmol)
  • C[C@H](CS(=O)(=O)C)N1C=CC2=C1C=CC(=C2C(F)(F)F)C#N
  • InChI=1S/C14H13F3N2O2S/c1-9(8-22(2,20)21)19-6-5-11-12(19)4-3-10(7-18)13(11)14(15,16)17/h3-6,9H,8H2,1-2H3/t9-/m1/s1
  • Key:SKDVMPZQJMZEAC-SECBINFHSA-N

GSK2881078 is a drug which acts as a selective androgen receptor modulator (SARM). It was developed for the prevention of muscle wasting and sarcopenia in elderly people.[1][2][3]

In a phase II trial the drug was shown to be well tolerated and increased muscle strength in men with COPD.[4]

See also

References

  1. ^ Clark RV, Walker AC, Andrews S, Turnbull P, Wald JA, Magee MH (October 2017). "Safety, pharmacokinetics and pharmacological effects of the selective androgen receptor modulator, GSK2881078, in healthy men and postmenopausal women". British Journal of Clinical Pharmacology. 83 (10): 2179–2194. doi:10.1111/bcp.13316. PMC 5595940. PMID 28449232.
  2. ^ Neil D, Clark RV, Magee M, Billiard J, Chan A, Xue Z, Russell A (September 2018). "GSK2881078, a SARM, Produces Dose-Dependent Increases in Lean Mass in Healthy Older Men and Women". The Journal of Clinical Endocrinology and Metabolism. 103 (9): 3215–3224. doi:10.1210/jc.2017-02644. PMID 29982690.
  3. ^ 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.
  4. ^ Mohan D, Rossiter H, Watz H, Fogarty C, Evans RA, Man W, et al. (March 2023). "Selective androgen receptor modulation for muscle weakness in chronic obstructive pulmonary disease: a randomised control trial". Thorax. 78 (3): 258–266. doi:10.1136/thorax-2021-218360. PMC 9985744. PMID 36283827.

External links

Androgen receptor modulators
Categories