Chemistry:List of investigational sex-hormonal agents

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This is a list of investigational sex-hormonal agents, or sex-hormonal agents that are currently under development for clinical use but are not yet approved. Chemical/generic names are listed first, with developmental code names, synonyms, and brand names in parentheses.


Androgenics

Androgen receptor agonists

Androgen receptor antagonists

Atypical androgen receptor antagonists

Androgen synthesis inhibitors

Estrogenics

Estrogen receptor agonists

Selective estrogen receptor modulators

  • Acolbifene (EM-652, SCH-57068) – selective estrogen receptor modulator for breast cancer [17]
  • Afimoxifene (4-hydroxytamoxifen; 4-OHT; TamoGel) – selective estrogen receptor modulator for topical treatment of breast cancer and hyperplasia [18]
  • Amcenestrant (SAR-439859; SERD '859) – selective estrogen receptor modulator and selective estrogen receptor degrader for breast cancer [19]
  • Camizestrant (AZ14066724, AZD-9833) – selective estrogen receptor modulator and selective estrogen receptor degrader for breast cancer [20]
  • Endoxifen (4-hydroxy-N-desmethyltamoxifen) – selective estrogen receptor modulator for breast cancer [21]
  • Giredestrant (GDC-9545; RG-6171) – selective estrogen receptor modulator and selective estrogen receptor degrader for breast cancer [22]
  • Imlunestrant (LY-3484356) – selective estrogen receptor modulator and selective estrogen receptor degrader for breast cancer and endometrial cancer [23]
  • Rintodestrant (G1T-48) – selective estrogen receptor modulator and selective estrogen receptor degrader for breast cancer [24]

Estrogen receptor antagonists

  • Fulvestrant-3 boronic acid (ZB716) – estrogen receptor antagonist (antiestrogen) for breast cancer[9][10]

Estrogen synthesis inhibitors

Progestogenics

Progesterone receptor agonists

Selective progesterone receptor modulators

  • Telapristone (CDB-4124, Proellex, Proellex-V, Progenta) – selective progesterone receptor modulator for breast cancer, endometriosis, and uterine fibroids [28]
  • Vilaprisan (BAY-1002670) – selective progesterone receptor modulator for endometriosis and uterine fibroids [29]

Progesterone receptor antagonists

GnRH/gonadotropins

Kisspeptin receptor agonists

Neurokinin/tachykinin receptor antagonists

  • Elinzanetant (BAY-3427080; GSK-1144814; NT-814) – small-molecule NK1 receptor and NK3 receptor antagonist for hot flashes and "sex hormone disorders"[32]

Mixed/combinations

Androgen and progesterone receptor modulators

Androgen and estrogen receptor modulators

  • Acolbifene/prasterone (Femivia) – selective estrogen receptor modulator and dehydroepiandrosterone supplement for hot flashes [33]

Androgen, estrogen, and progesterone receptor modulators

  • Ethinylestradiol/drospirenone/prasterone – estrogen, progestogen, and dehydroepiandrosterone combination for female birth control [34]

See also

References

  1. 1.0 1.1 "R&D Research". http://www.evestra.com/index-Dateien/Page1242.htm. 
  2. 2.0 2.1 "A prodrug design for improved oral absorption and reduced hepatic interaction". Bioorg. Med. Chem. 25 (20): 5569–5575. October 2017. doi:10.1016/j.bmc.2017.08.027. PMID 28886996. 
  3. "Proteolysis targeting chimera (PROTAC) in drug discovery paradigm: Recent progress and future challenges". Eur J Med Chem 210: 112981. January 2021. doi:10.1016/j.ejmech.2020.112981. PMID 33160761. 
  4. Tong, Youzhi; Chen, Chunyun; Wu, Juan; Yang, Jiangtao; Zhang, Huihui; Wu, Xiaojun; Duan, Yanmei; Gao, Wei et al. (2014). "Abstract 614: Proxalutamide (GT0918), a potent androgen receptor pathway inhibitor". Cancer Research 74 (19 Supplement): 614. doi:10.1158/1538-7445.AM2014-614. ISSN 0008-5472. 
  5. "Pyrilutamide - Suzhou Kintor Pharmaceuticals". AdisInsight. Springer Nature Switzerland AG. https://adisinsight.springer.com/drugs/800053879. 
  6. "Spironolactone for adult female acne (SAFA): protocol for a double-blind, placebo-controlled, phase III randomised study of spironolactone as systemic therapy for acne in adult women". BMJ Open 11 (8): e053876. August 2021. doi:10.1136/bmjopen-2021-053876. PMID 34446504. 
  7. "FASCE, the benefit of spironolactone for treating acne in women: study protocol for a randomized double-blind trial". Trials 21 (1): 571. June 2020. doi:10.1186/s13063-020-04432-w. PMID 32586344. 
  8. "Estradiol prodrugs (EP) for efficient oral estrogen treatment and abolished effects on estrogen modulated liver functions". J. Steroid Biochem. Mol. Biol. 165 (Pt B): 305–311. January 2017. doi:10.1016/j.jsbmb.2016.07.008. PMID 27449818. 
  9. "Fulvestrant-3 Boronic Acid (ZB716): An Orally Bioavailable Selective Estrogen Receptor Downregulator (SERD)". J. Med. Chem. 59 (17): 8134–40. 2016. doi:10.1021/acs.jmedchem.6b00753. PMID 27529700. 
  10. Wang, G; Liu, J; Zheng, S; Miele, L; Wiese, T; Zhong, Q; Guo, S (2017). "Abstract P2-08-11: An orally bioavailable selective estrogen receptor downregulator". Cancer Research 77 (4 Supplement): P2-08-11–P2-08-11. doi:10.1158/1538-7445.SABCS16-P2-08-11. ISSN 0008-5472. 
  11. "Hydroxyprogesterone - Lipocine - AdisInsight". https://adisinsight.springer.com/drugs/800038483. 
  12. "Second potential male birth control pill passes human safety tests". https://www.endocrine.org/news-room/2019/endo-2019---second-potential-male-birth-control-pill-passes-human-safety-tests. 
  13. "Dimethandrolone undecanoate shows promise as a male birth control pill". https://www.endocrine.org/news-room/2018/dimethandrolone-undecanoate-shows-promise-as-a-male-birth-control-pill. 

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