From Wikipedia, the free encyclopedia
Chemical compound
GSK2881078
Legal status
1-[(2R)-1-methylsulfonylpropan-2-yl]-4-(trifluoromethyl)indole-5-carbonitrile
CAS Number
PubChem
CID
ChemSpider
UNII
Formula C 14 H 13 F 3 N 2 O 2 S
Molar mass 330.33 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
^ 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 .
^ 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 .
^ 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 .
^ 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
AR Tooltip Androgen receptor
Agonists
SARMs Tooltip Selective androgen receptor modulator Antagonists
GPRC6A