GTx-027 explained

Routes Of Administration:Oral
Class:Selective androgen receptor modulator
Pubchem:23653581
Synonyms:GTx027
Iupac Name:(2S)-N-(3-chloro-4-cyanophenyl)-3-(4-cyanophenoxy)-2-hydroxy-2-methylpropanamide
C:18
H:14
Cl:1
N:3
O:3
Smiles:C[C@](COC1=CC=C(C=C1)C#N)(C(=O)NC2=CC(=C(C=C2)C#N)Cl)O
Stdinchi:1S/C18H14ClN3O3/c1-18(24,11-25-15-6-2-12(9-20)3-7-15)17(23)22-14-5-4-13(10-21)16(19)8-14/h2-8,24H,11H2,1H3,(H,22,23)/t18-/m0/s1
Stdinchikey:IEGVUEFEHAFTNS-SFHVURJKSA-N

GTx-027 is a selective androgen receptor modulator (SARM) which was under development for or of potential interest in the treatment of breast cancer and stress urinary incontinence (SUI) but was never marketed.[1] [2] [3] It is taken by mouth.

Description

The drug is a nonsteroidal androgen receptor (AR) modulator with mixed agonistic (androgenic) and antagonistic (antiandrogenic) effects. It has been found to reduce the growth of androgen receptor-expressing MDA-MB-231 breast cancer cells in vitro.[4] [5] In addition, it has been found to increase pelvic floor muscle weight in ovariectomized female rodents.[6] [7] The drug has been found to increase body weight, lean body mass, and muscle strength in animals as well.[8] [9] In terms of chemical structure, GTx-027 is a nonsteroidal arylpropionamide SARM and is an analogue of enobosarm (ostarine; GTx-024).

GTx-027 was first described in the scientific literature by 2013.[10] [11] It is said to have either not passed preclinical research or to have reached phase 1 clinical trials prior to the discontinuation of its development. The drug was developed by GTx.

Notes and References

  1. Web site: Research programme: selective androgen receptor modulators . AdisInsight . Springer Nature Switzerland AG . 16 April 2020 . 22 October 2024.
  2. Web site: Delving into the Latest Updates on GTx-027 with Synapse . Synapse . 13 October 2024 . 22 October 2024.
  3. Christiansen AR, Lipshultz LI, Hotaling JM, Pastuszak AW . Selective androgen receptor modulators: the future of androgen therapy? . Translational Andrology and Urology . 9 . Suppl 2 . S135–S148 . March 2020 . 32257854 . 7108998 . 10.21037/tau.2019.11.02 . free .
  4. Vasiliou SK, Diamandis EP . Androgen receptor: A promising therapeutic target in breast cancer . Critical Reviews in Clinical Laboratory Sciences . 56 . 3 . 200–223 . May 2019 . 30821186 . 10.1080/10408363.2019.1575643 .
  5. Christopoulos PF, Vlachogiannis NI, Vogkou CT, Koutsilieris M . The Role of the Androgen Receptor Signaling in Breast Malignancies . Anticancer Research . 37 . 12 . 6533–6540 . December 2017 . 29187427 . 10.21873/anticanres.12109 .
  6. Juneau AD, Gomelsky A . Pharmaceutical Options for Stress Urinary Incontinence . Current Bladder Dysfunction Reports . Springer Science and Business Media LLC . 14 . 4 . 28 October 2019 . 1931-7212 . 10.1007/s11884-019-00537-4 . 357–364.
  7. Ponnusamy S, Sullivan RD, Thiyagarajan T, Tillmann H, Getzenberg RH, Narayanan R . Tissue Selective Androgen Receptor Modulators (SARMs) Increase Pelvic Floor Muscle Mass in Ovariectomized Mice . Journal of Cellular Biochemistry . 118 . 3 . 640–646 . March 2017 . 27681158 . 10.1002/jcb.25751 . free .
  8. Ponnusamy S, Sullivan RD, You D, Zafar N, He Yang C, Thiyagarajan T, Johnson DL, Barrett ML, Koehler NJ, Star M, Stephenson EJ, Bridges D, Cormier SA, Pfeffer LM, Narayanan R . Androgen receptor agonists increase lean mass, improve cardiopulmonary functions and extend survival in preclinical models of Duchenne muscular dystrophy . Human Molecular Genetics . 26 . 13 . 2526–2540 . July 2017 . 28453658 . 6251687 . 10.1093/hmg/ddx150 . After 2 weeks, the body weights of the GTx-026-treated mice were greater than those of the vehicle-treated mice, with this difference increasing in magnitude throughout the duration of the study (62% in GTx-026-treated mice vs 31% in vehicle-treated mice; P < 0.001) (Fig. 2B). GTx-026 treatment also increased lean mass (20% vs 60%; P < 0.001) compared with vehicle treatment. Consistent with the increase in lean mass, grip strength also increased in the GTx-026-treated animals (Fig. 2B). These results were reproduced with the other two SARMs, GTx-024 and GTx-027, indicating that these effects are SARM-dependent (Supplementary Material, Fig. S1B). .
  9. Web site: GTx, Inc. Announces Results From Preclinical Studies Of Sarms In Duchenne Muscular Dystrophy Models Published In Human Molecular Genetics . BioSpace . 3 May 2017 . 22 October 2024 . Other SARMs in the Company’s portfolio, GTx-024 (enobosarm) and GTx-027, showed similar positive effects on muscle mass, function, and histological characteristics..
  10. Dalton JT, Narayanan R, Steiner MS . Abstract P5-09-21: Selective androgen receptor modulators (SARMs): Enobosarm as targeted therapy for the treatment of androgen receptor-positive breast cancer . Cancer Research . American Association for Cancer Research (AACR) . 73 . 24_Supplement . 15 December 2013 . 0008-5472 . 10.1158/0008-5472.sabcs13-p5-09-21 . P5–09–21–P5–09–21.
  11. Narayanan R, Ahn S, Cheney MD, Yepuru M, Miller DD, Steiner MS, Dalton JT . Selective androgen receptor modulators (SARMs) negatively regulate triple-negative breast cancer growth and epithelial:mesenchymal stem cell signaling . PLOS ONE . 9 . 7 . e103202 . 2014 . 25072326 . 4114483 . 10.1371/journal.pone.0103202 . free . 2014PLoSO...9j3202N .

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