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List of investigational sex-hormonal agents

Last updated

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.

Contents

This list was last comprehensively updated sometime between May 2017 and September 2021. It is likely to become outdated with time.

Androgenics

Androgen receptor agonists

Selective androgen receptor modulators

Androgen receptor antagonists

Atypical androgen receptor antagonists

Androgen synthesis inhibitors

Estrogenics

Estrogen receptor agonists

Selective estrogen receptor modulators

Estrogen receptor antagonists

Estrogen synthesis inhibitors

Progestogenics

Progesterone receptor agonists

Selective progesterone receptor modulators

Progesterone receptor antagonists

GnRH/gonadotropins

GnRH receptor antagonists

Kisspeptin receptor agonists

Neurokinin/tachykinin receptor antagonists

Mixed/combinations

Androgen and progesterone receptor modulators

Androgen and estrogen receptor modulators

Androgen, estrogen, and progesterone receptor modulators

See also

References

  1. 1 2 "Deuterated testosterone". AdisInsight. 28 December 2025. Retrieved 27 January 2026.
  2. ↑ "AVA 291". AdisInsight. 1 August 2025. Retrieved 27 January 2026.
  3. ↑ "Delving into the Latest Updates on d-Testosterone with Synapse". Synapse. 16 May 2025. Retrieved 27 January 2026.
  4. ↑ Clarke, Hannah (27 January 2026). "FDA provides guidance on development pathway for testosterone therapy for women". Urology Times. Retrieved 27 January 2026.
  5. ↑ Stemmerich, Karsten; Sewell, Adrian C; Arndt, Torsten (2022). "Weighty times ahead for the lab?" (PDF). TIAFT Bulletin. 52 (4). Retrieved 27 January 2026.
  6. ↑ "Lennham discloses deuterated testosterone compound". BioWorld. 11 November 2021. Retrieved 27 January 2026.
  7. ↑ Tarantino, Paul M; Boice, Judith A; Dudley, Robert Earle; Sippy, Bradford C (22 October 2025). "MON-261 Characterization of d3-Testosterone, A Novel, Non-Aromatizing Androgen". Journal of the Endocrine Society. 9 (Supplement_1) bvaf149.1839. doi: 10.1210/jendso/bvaf149.1839 . ISSN   2472-1972.
  8. ↑ "Deuterated forms of testosterone and methods of use". Google Patents. 23 March 2021. Retrieved 27 January 2026.
  9. 1 2 "R&D Research". www.evestra.com. Archived from the original on 2017-09-29.
  10. 1 2 Ahmed G, Elger W, Meece F, Nair HB, Schneider B, Wyrwa R, Nickisch K (October 2017). "A prodrug design for improved oral absorption and reduced hepatic interaction". Bioorg. Med. Chem. 25 (20): 5569–5575. doi:10.1016/j.bmc.2017.08.027. PMID   28886996.
  11. ↑ "DT 200 - AdisInsight".
  12. ↑ "Enobosarm - Veru Healthcare - AdisInsight".
  13. ↑ "GSK 2881078 - AdisInsight".
  14. ↑ "OPK 88004 - AdisInsight".
  15. ↑ "VK 5211 - AdisInsight".
  16. ↑ "Vosilasarm - Ellipses Pharma - AdisInsight".
  17. ↑ "Bavdegalutamide - Arvinas - AdisInsight".
  18. ↑ Zeng S, Huang W, Zheng X, Liyan C, Zhang Z, Wang J, Shen Z (January 2021). "Proteolysis targeting chimera (PROTAC) in drug discovery paradigm: Recent progress and future challenges". Eur J Med Chem. 210 112981. doi:10.1016/j.ejmech.2020.112981. PMID   33160761. S2CID   226287993.
  19. ↑ https://cdn.who.int/media/docs/default-source/international-nonproprietary-names-(inn)/pl125.pdf?sfvrsn=af269747_5&download=true
  20. ↑ "Clascoterone - Cosmo Pharmaceuticals - AdisInsight".
  21. ↑ "Deutenzalutamide - Hinova Pharmaceuticals - AdisInsight".
  22. ↑ Jiang, Jinfang; Pang, Xuehai; Dai, Xiaojian; Diao, Xingxing; Chen, Xiaoyan; Zhong, Dafang; Chen, Yuanwei; Li, Liang; Wang, Yingwei (2016). "Effect of N-methyl deuteration on metabolism and pharmacokinetics of enzalutamide". Drug Design, Development and Therapy. 10: 2181–2191. doi: 10.2147/DDDT.S111352 . PMID   27462143.
  23. ↑ Pang, Xuehai; Peng, Lingling; Chen, Yuanwei (2017). "Effect of N -methyl deuteration on pharmacokinetics and pharmacodynamics of enzalutamide". Journal of Labelled Compounds and Radiopharmaceuticals. 60 (9): 401–409. doi:10.1002/jlcr.3516. PMID   28432800.
  24. ↑ "Pruxelutamide - Suzhou Kintor Pharmaceuticals - AdisInsight".
  25. ↑ Tong, Youzhi; Chen, Chunyun; Wu, Juan; Yang, Jiangtao; Zhang, Huihui; Wu, Xiaojun; Duan, Yanmei; Gao, Wei; Qian, Weidong; Niu, Xiaoxia; Mi, Lili; Guo, Chuangxing (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.
  26. ↑ "Pyrilutamide - Suzhou Kintor Pharmaceuticals". AdisInsight. Springer Nature Switzerland AG.
  27. ↑ "ISRCTN".
  28. ↑ Renz S, Chinnery F, Stuart B, Day L, Muller I, Soulsby I, Nuttall J, Thomas K, Thomas KS, Sach T, Stanton L, Ridd MJ, Francis N, Little P, Eminton Z, Griffiths G, Layton AM, Santer M (August 2021). "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. doi: 10.1136/bmjopen-2021-053876 . PMC   8395279 . PMID   34446504.
  29. ↑ "Randomized Double-blind Study on the Benefit of Spironolactone for Treating Acne of Adult Woman". 17 July 2023.
  30. ↑ Poinas A, Lemoigne M, Le Naour S, Nguyen JM, Schirr-Bonnans S, Riche VP, Vrignaud F, Machet L, Claudel JP, Leccia MT, Hainaut E, Beneton N, Dert C, Boisrobert A, Flet L, Chiffoleau A, Corvec S, Khammari A, Dréno B (June 2020). "FASCE, the benefit of spironolactone for treating acne in women: study protocol for a randomized double-blind trial". Trials. 21 (1) 571. doi: 10.1186/s13063-020-04432-w . PMC   7318446 . PMID   32586344.
  31. ↑ "A Randomized, Double-Blind, Multi-Center Comparative Effectiveness Study of Spironolactone Versus Doxycycline Hyclate for the Treatment of Acne in Women". 20 October 2025.
  32. ↑ "ASCJ 9 - AdisInsight".
  33. ↑ "Research programme: Androgen receptor antagonists - ESSA Pharma - AdisInsight".
  34. ↑ https://www.essapharma.com/wp-content/uploads/2019/02/Final-Poster-Next-Gen_201902014_Website.pdf [ bare URL PDF ]
  35. ↑ "ESSA Pharma Announces Nomination of EPI-7386 as Lead Clinical Candidate in Metastatic Castration-Resistant Prostate Cancer" (Press release).
  36. ↑ "Seviteronel - Innocrin Pharmaceuticals - AdisInsight".
  37. ↑ Elger W, Wyrwa R, Ahmed G, Meece F, Nair HB, Santhamma B, Killeen Z, Schneider B, Meister R, Schubert H, Nickisch K (January 2017). "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. doi:10.1016/j.jsbmb.2016.07.008. PMID   27449818. S2CID   26650319.
  38. ↑ "Erteberel - Eli Lilly and Company - AdisInsight".
  39. ↑ "Estetrol - Mithra Pharmaceuticals/Pantarhei Bioscience - AdisInsight".
  40. ↑ "Acolbifene - Endoceutics - AdisInsight".
  41. ↑ "Afimoxifene - BHR Pharma - AdisInsight".
  42. ↑ "Amcenestrant - Sanofi - AdisInsight".
  43. ↑ "Camizestrant - AstraZeneca - AdisInsight".
  44. ↑ "Endoxifen - Intas Pharmaceuticals/Jina pharmaceuticals - AdisInsight".
  45. ↑ "Giredestrant - Genentech - AdisInsight".
  46. ↑ "Imlunestrant - Eli Lilly and Company/Loxo-Oncology - AdisInsight".
  47. ↑ "Rintodestrant - G1 Therapeutics - AdisInsight".
  48. ↑ Liu J, Zheng S, Akerstrom VL, Yuan C, Ma Y, Zhong Q, Zhang C, Zhang Q, Guo S, Ma P, Skripnikova EV, Bratton MR, Pannuti A, Miele L, Wiese TE, Wang G (2016). "Fulvestrant-3 Boronic Acid (ZB716): An Orally Bioavailable Selective Estrogen Receptor Downregulator (SERD)". J. Med. Chem. 59 (17): 8134–40. doi:10.1021/acs.jmedchem.6b00753. PMC   5499704 . PMID   27529700.
  49. ↑ 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.
  50. ↑ "PGL 2 - AdisInsight".
  51. ↑ "Leflutrozole - ReproNovo - AdisInsight".
  52. ↑ "Progesterone conjugate - Levolta Pharmaceuticals - AdisInsight".
  53. ↑ "Telapristone - Repros Therapeutics - AdisInsight".
  54. ↑ "Vilaprisan - Bayer HealthCare Pharmaceuticals - AdisInsight".
  55. ↑ "Onapristone - Context Therapeutics - AdisInsight".
  56. ↑ "Merigolix - TiumBio - AdisInsight".
  57. ↑ "MVT 602 - AdisInsight".
  58. ↑ "Elinzanetant - Bayer - AdisInsight".
  59. ↑ "Second potential male birth control pill passes human safety tests".
  60. ↑ "Dimethandrolone undecanoate shows promise as a male birth control pill".
  61. ↑ "Acolbifene/Prasterone - Endoceutics - AdisInsight".
  62. ↑ "Drospirenone/Estradiol/Prasterone - ANI Pharmaceuticals/Pantarhei Bioscience - AdisInsight".
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