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
- EC586 – oral prodrug of testosterone (androgen/anabolic steroid) with improved pharmacokinetics[1][2]
Androgen receptor antagonists
- Bavdegalutamide (AVR-110) – androgen receptor antagonist for prostate cancer[1][3][2]
- Clascoterone (CB-03-01, Breezula, Winlevi) – androgen receptor antagonist for topical treatment of scalp hair loss [3]
- Deutenzalutamide (deuterated enzalutamide; HC-1119) – androgen receptor antagonist for prostate cancer [4] [5] [6]
- Pruxelutamide (GT-0918; proxalutamide) – androgen receptor antagonist for prostate cancer [7][4]
- Pyrilutamide (KX-826) – androgen receptor antagonist for topical treatment of androgen-dependent scalp hair loss and acne[5]
- Spironolactone (Aldactone) – androgen receptor antagonist for systemic treatment of acne[8][6][9][7][10]
Atypical androgen receptor antagonists
- Dimethylcurcumin (ASC-J9) – androgen receptor degradation enhancer for topical acne treatment [11]
- EPI-7386 – N-terminal domain androgen receptor antagonist for prostate cancer [12] [13] [https://www.prnewswire.com/news-releases/essa-pharma-announces-nomination-of-epi-7386-as-lead-clinical-candidate-in-metastatic-castration-resistant-prostate-cancer-300820449.html
Androgen synthesis inhibitors
- Seviteronel (VT-464) – CYP17A1 inhibitor (androgen synthesis inhibitor) for prostate cancer and breast cancer [14]
Estrogenics
Estrogen receptor agonists
- EC508 – oral prodrug of estradiol (estrogen) with improved pharmacokinetics[1][8][2]
- Erteberel (LY-500307, SERBA-1) – selective ERβ agonist for schizophrenia [15]
- Estetrol (Donesta) – estrogen for menopausal symptoms and other indications [16]
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
- Estradiol sulfamate (E2MATE, J995, PGL-2, PGL-2001, ZK-190628) – steroid sulfatase inhibitor (estrogen "activation" inhibitor) for endometriosis [25]
- Leflutrozole (BGS-649) – aromatase inhibitor (estrogen synthesis inhibitor) for male hypogonadism [26]
Progestogenics
Progesterone receptor agonists
- Hydroxyprogesterone caproate (LPCN-1107) – oral progesterone receptor agonist (progestogen/progestin) for prevention of preterm labor[11]
- VOLT-02 – water-soluble conjugate of progesterone and neurosteroid for traumatic brain injury and gynecological disorders [27]
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
- Onapristone (AR-18, IVV-1001, ZK-299, ZK-98299) – progesterone receptor antagonist (antiprogestogen) for prostate cancer [30]
GnRH/gonadotropins
Kisspeptin receptor agonists
- MVT-602 (RVT-602, TAK-448) – small-molecule kisspeptin receptor agonist for female infertility and hypogonadism [31]
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
- 11β-Methyl-19-nortestosterone dodecylcarbonate (CDB-4754) – dual androgen/anabolic steroid and progestin for use as a male birth control pill[12]
- Dimethandrolone undecanoate (CDB-4521) – dual androgen/anabolic steroid and progestin for use as a male birth control pill[13]
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
- ↑ 1.0 1.1 "R&D Research". http://www.evestra.com/index-Dateien/Page1242.htm.
- ↑ 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.
- ↑ "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.
- ↑ 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.
- ↑ "Pyrilutamide - Suzhou Kintor Pharmaceuticals". AdisInsight. Springer Nature Switzerland AG. https://adisinsight.springer.com/drugs/800053879.
- ↑ "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.
- ↑ "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.
- ↑ "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.
- ↑ "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.
- ↑ 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.
- ↑ "Hydroxyprogesterone - Lipocine - AdisInsight". https://adisinsight.springer.com/drugs/800038483.
- ↑ "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.
- ↑ "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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