GSK2881078 - Misplaced Pages

Chemical compound

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Pharmaceutical compound

GSK2881078
Legal status

Legal status	US: Investigational drug
Identifiers
IUPAC name 1--4-(trifluoromethyl)indole-5-carbonitrile
CAS Number	1539314-06-1
PubChem CID	86709174
ChemSpider	57621607
UNII	47M5ZXU844
Chemical and physical data
Formula	C₁₄H₁₃F₃N₂O₂S
Molar mass	330.33 g·mol
3D model (JSmol)	Interactive image
SMILES C(CS(=O)(=O)C)N1C=CC2=C1C=CC(=C2C(F)(F)F)C#N
InChI 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.

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

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.

ARTooltip Androgen receptor

Agonists

17α-Alkylated 5α-dihydro-19-nortestosterone derivatives: 5α-Dihydronorethandrolone
5α-Dihydronormethandrone

5α-Dihydro-17α-ethynyl-19-nortestosterone derivatives: 5α-Dihydrolevonorgestrel
5α-Dihydronorethisterone

SARMsTooltip Selective androgen receptor modulator

Antagonists

Agonists	Cations (incl. aluminium, calcium, gadolinium, magnesium, strontium, zinc) Dehydroandrosterone Dihydrotestosterone Estradiol L-α-Amino acids (incl. L-arginine, L-lysine, L-ornithine) Osteocalcin SHBGTooltip Sex hormone-binding globulin Testosterone

See also: Receptor/signaling modulators; Androgens and antiandrogens; Estrogen receptor modulators; Progesterone receptor modulators; List of androgens and anabolic steroids

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