Chemistry:GTx-027

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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][4][5] It is taken by mouth.[3]

Description

The drug is a nonsteroidal androgen receptor (AR) modulator with mixed agonistic (androgenic) and antagonistic (antiandrogenic) effects.[3][5] It has been found to reduce the growth of androgen receptor-expressing MDA-MB-231 breast cancer cells in vitro.[6][7] In addition, it has been found to increase pelvic floor muscle weight in ovariectomized female rodents.[3][8][4] The drug has been found to increase body weight, lean body mass, and muscle strength in animals as well.[9][10] In terms of chemical structure, GTx-027 is a nonsteroidal arylpropionamide SARM and is an analogue of enobosarm (ostarine; GTx-024).[3][4]

GTx-027 was first described in the scientific literature by 2013.[5][11] It is said to have either not passed preclinical research[3] or to have reached phase 1 clinical trials prior to the discontinuation of its development.[2] The drug was developed by GTx.[1][2]

References

  1. ↑ 1.0 1.1 "Research programme: selective androgen receptor modulators". AdisInsight. Springer Nature Switzerland AG. 16 April 2020. https://adisinsight.springer.com/drugs/800019102. 
  2. ↑ 2.0 2.1 2.2 "Delving into the Latest Updates on GTx-027 with Synapse". 13 October 2024. https://synapse.patsnap.com/drug/0ee7551b331241b9bf8980b35ba9d652. 
  3. ↑ 3.0 3.1 3.2 3.3 3.4 3.5 "Selective androgen receptor modulators: the future of androgen therapy?". Translational Andrology and Urology 9 (Suppl 2): S135–S148. March 2020. doi:10.21037/tau.2019.11.02. PMID 32257854. 
  4. ↑ 4.0 4.1 4.2 "Tissue Selective Androgen Receptor Modulators (SARMs) Increase Pelvic Floor Muscle Mass in Ovariectomized Mice". Journal of Cellular Biochemistry 118 (3): 640–646. March 2017. doi:10.1002/jcb.25751. PMID 27681158. 
  5. ↑ 5.0 5.1 5.2 "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): P5–09–21–P5–09–21. 15 December 2013. doi:10.1158/0008-5472.sabcs13-p5-09-21. ISSN 0008-5472. 
  6. ↑ "Androgen receptor: A promising therapeutic target in breast cancer". Critical Reviews in Clinical Laboratory Sciences 56 (3): 200–223. May 2019. doi:10.1080/10408363.2019.1575643. PMID 30821186. 
  7. ↑ "The Role of the Androgen Receptor Signaling in Breast Malignancies". Anticancer Research 37 (12): 6533–6540. December 2017. doi:10.21873/anticanres.12109. PMID 29187427. 
  8. ↑ "Pharmaceutical Options for Stress Urinary Incontinence". Current Bladder Dysfunction Reports (Springer Science and Business Media LLC) 14 (4): 357–364. 28 October 2019. doi:10.1007/s11884-019-00537-4. ISSN 1931-7212. 
  9. ↑ "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. doi:10.1093/hmg/ddx150. PMID 28453658. "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).". 
  10. ↑ "GTx, Inc. Announces Results From Preclinical Studies Of Sarms In Duchenne Muscular Dystrophy Models Published In Human Molecular Genetics". 3 May 2017. https://www.biospace.com/gtx-inc-announces-results-from-preclinical-studies-of-sarms-in-duchenne-muscular-dystrophy-models-published-in-i-b-human-molecular-genetics-b-i. "Other SARMs in the Company's portfolio, GTx-024 (enobosarm) and GTx-027, showed similar positive effects on muscle mass, function, and histological characteristics." 
  11. ↑ "Selective androgen receptor modulators (SARMs) negatively regulate triple-negative breast cancer growth and epithelial:mesenchymal stem cell signaling". PLOS ONE 9 (7). 2014. doi:10.1371/journal.pone.0103202. PMID 25072326. Bibcode: 2014PLoSO...9j3202N. 



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