List Of Investigational Hormonal Agents

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This is a list of investigational hormonal agents, or 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

  • Bavdegalutamide (AVR-110) – androgen receptor antagonist for prostate cancer[1][1]
  • Clascoterone (CB-03-01, Breezula, Winlevi) – androgen receptor antagonist for topical treatment of scalp hair loss [2]
  • Deuterated enzalutamide (HC-1119) – androgen receptor antagonist for prostate cancer [3] [4] [5]
  • Dimethylcurcumin (ASC-J9) – androgen receptor degradation enhancer for topical acne treatment [6]
  • EC586 – oral prodrug of testosterone with improved pharmacokinetics[2][3]
  • EPI-7386 – N-terminal domain androgen receptor antagonist for prostate cancer [7] [8] [9]
  • Proxalutamide (GT-0918) – androgen receptor antagonist for prostate cancer [10][4]
  • Rezvilutamide (SHR3680) – androgen receptor antagonist for prostate cancer [11]
  • Seviteronel (VT-464) – CYP17A1 inhibitor (androgen synthesis inhibitor) for prostate cancer and breast cancer [12]
  • Spironolactone (Aldactone) – androgen receptor antagonist for systemic acne treatment[13][5][14][6][15]

Estrogenics

  • Acolbifene (EM-652, SCH-57068) – selective estrogen receptor modulator for breast cancer [16]
  • Acolbifene/prasterone (Femivia) – selective estrogen receptor modulator and DHEA supplement for vasomotor symptoms [17]
  • Afimoxifene – selective estrogen receptor modulator for breast cancer [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]
  • EC508 – oral prodrug of estradiol with improved pharmacokinetics[2][7][3]
  • Elacestrant (RAD-1901, ER-306323) – selective estrogen receptor modulator and selective estrogen receptor degrader for breast cancer [21]
  • Endoxifen – selective estrogen receptor modulator for breast cancer [22]
  • Erteberel (LY-500307, SERBA-1) – selective ERβ agonist for schizophrenia [23]
  • Estetrol (Donesta) – estrogen for menopausal symptoms and other indications [24]
  • Estradiol sulfamate (E2MATE, J995, PGL-2, PGL-2001, ZK-190628) – estrogen and steroid sulfatase inhibitor (estrogen "activation" inhibitor) for endometriosis [25]
  • Fulvestrant-3 boronic acid (ZB716) – estrogen receptor antagonist for breast cancer[8][9]
  • Giredestrant (GDC-9545; RG-6171) – selective estrogen receptor modulator and selective estrogen receptor degrader for breast cancer[26]
  • Leflutrozole (BGS-649) – aromatase inhibitor (estrogen synthesis inhibitor) for male hypogonadism [27]
  • Rintodestrant (G1T-48) – selective estrogen receptor modulator and selective estrogen receptor degrader for breast cancer [28]

Progestogenics

  • Hydroxyprogesterone caproate (LPCN-1107) – oral progesterone receptor agonist for prevention of preterm labor[10]
  • Onapristone (AR-18, IVV-1001, ZK-299, ZK-98299) – progesterone receptor antagonist for prostate cancer [29]
  • Telapristone (CDB-4124, Proellex, Proellex-V, Progenta) – selective progesterone receptor modulator for breast cancer, endometriosis, and uterine fibroids [30]
  • Vilaprisan (BAY 1002670) – selective progesterone receptor modulator for endometriosis and uterine fibroids [31]
  • VOLT-02 – water-soluble conjugate of progesterone for traumatic brain injury and gynecological disorders [32]

Glucocorticoidics

  • IONIS-GCCRRx (ISIS-426115) – glucocorticoid receptor antisense oligonucleotide for type 2 diabetes mellitus [33]
  • Levoketoconazole (COR-003, NormoCort, Recorlev) – glucocorticoid synthesis inhibitor for Cushing's syndrome [34]
  • Relacorilant (CORT-125134) – glucocorticoid receptor antagonist for Cushing's syndrome [35]
  • Vamorolone (VB-15, VBP-15) – selective glucocorticoid receptor modulator [36]

Mineralocorticoidics

  • Apararenone (MT-3995) – mineralocorticoid receptor antagonist for diabetic nephropathy and non-alcoholic steatohepatitis [37]
  • Finerenone (BAY-94-8862) – mineralocorticoid receptor antagonist for chronic heart failure, diabetic nephropathy, and renal failure [38]

GnRH/gonadotropins

  • Elinzanetant (GSK1144814A) – NK1 receptor and NK3 receptor antagonist for schizophrenia [39]
  • Fezolinetant (ESN-364) – small-molecule NK3 receptor antagonist for hot flashes, polycystic ovary syndrome, and uterine fibroids [40]
  • Linzagolix (KLH-2109, OBE-2109) – small-molecule GnRH receptor antagonist for uterine fibroids and endometriosis [41]
  • MVT-602 (RVT-602, TAK-448) – small-molecule kisspeptin receptor agonist for female infertility and hypogonadism [42]

Mixed

  • 11β-Methyl-19-nortestosterone dodecylcarbonate (CDB-4754) – dual androgen/anabolic steroid and progestin for use as a male birth control pill[11]
  • Dimethandrolone undecanoate (CDB-4521) – dual androgen/anabolic steroid and progestin for use as a male birth control pill[12]
  • Ethinylestradiol/drospirenone/prasterone – estrogen, progestogen, androgen, and neurosteroid combination for hormonal contraception (pregnancy) [43]

See also

  • List of investigational drugs

References

  1. ↑ "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. 
  2. ↑ 2.0 2.1 http://www.evestra.com/index-Dateien/Page1242.htm
  3. ↑ 3.0 3.1 "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. 
  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. ↑ "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. 
  6. ↑ "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. 
  7. ↑ "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. 
  8. ↑ "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. 
  9. ↑ 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. 
  10. ↑ https://adisinsight.springer.com/drugs/800038483
  11. ↑ https://www.endocrine.org/news-room/2019/endo-2019---second-potential-male-birth-control-pill-passes-human-safety-tests
  12. ↑ https://www.endocrine.org/news-room/2018/dimethandrolone-undecanoate-shows-promise-as-a-male-birth-control-pill

External links

  • AdisInsight - Springer
  • 2011 Medicines in Development for Women - PhRMA




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Categories: [Experimental drugs]

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