List of investigational sex-hormonal agents
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
- Clascoterone (CB-03-01, Breezula, Winlevi) – androgen receptor antagonist for topical acne treatment [1]
- Deuterated enzalutamide (HC-1119) – androgen receptor antagonist for prostate cancer [2] [3] [4]
- Dimethylcurcumin (ASC-J9) – androgen receptor degradation enhancer for topical acne treatment [5]
- EC586 – oral prodrug of testosterone with improved pharmacokinetics[1][2]
- EPI-7386 – N-terminal domain androgen receptor antagonist for prostate cancer [6] [7] [8]
- Proxalutamide (GT-0918) – androgen receptor antagonist for prostate cancer [9][3]
- Seviteronel (VT-464) – CYP17A1 inhibitor (androgen synthesis inhibitor) for prostate cancer and breast cancer [10]
- SHR-3680 – androgen receptor antagonist for prostate cancer [11]
Estrogenics
- Acolbifene (EM-652, SCH-57068) – selective estrogen receptor modulator for breast cancer [12]
- Acolbifene/prasterone (Femivia) – selective estrogen receptor modulator and DHEA supplement for vasomotor symptoms [13]
- Afimoxifene – selective estrogen receptor modulator for breast cancer [14]
- EC508 – oral prodrug of estradiol with improved pharmacokinetics[1][4][2]
- Elacestrant (RAD-1901, ER-306323) – selective estrogen receptor modulator and selective estrogen receptor degrader for breast cancer [15]
- Enclomifene (Androxal) – selective estrogen receptor modulator for male hypogonadism [16]
- Endoxifen – selective estrogen receptor modulator for breast cancer [17]
- Erteberel (LY-500307, SERBA-1) – selective ERβ agonist for schizophrenia [18]
- Estetrol (Donesta) – estrogen for menopausal symptoms and other indications [19]
- Estradiol sulfamate (E2MATE, J995, PGL-2, PGL-2001, ZK-190628) – estrogen and steroid sulfatase inhibitor (estrogen "activation" inhibitor) for endometriosis [20]
- Fulvestrant-3 boronic acid (ZB716) – estrogen receptor antagonist for breast cancer[5][6]
- Leflutrozole (BGS-649) – aromatase inhibitor (estrogen synthesis inhibitor) for male hypogonadism [21]
Progestogenics
- Hydroxyprogesterone caproate (LPCN-1107) – oral progesterone receptor agonist for prevention of preterm labor[7]
- Onapristone (AR-18, IVV-1001, ZK-299, ZK-98299) – progesterone receptor antagonist for prostate cancer [22]
- Telapristone (CDB-4124, Proellex, Proellex-V, Progenta) – selective progesterone receptor modulator for breast cancer, endometriosis, and uterine fibroids [23]
- Vilaprisan (BAY 1002670) – selective progesterone receptor modulator for endometriosis and uterine fibroids [24]
- VOLT-02 – water-soluble conjugate of progesterone for traumatic brain injury and gynecological disorders [25]
Glucocorticoidics
- IONIS-GCCRRx (ISIS-426115) – glucocorticoid receptor antisense oligonucleotide for type 2 diabetes mellitus[26]
- Levoketoconazole (COR-003, NormoCort, Recorlev) – glucocorticoid synthesis inhibitor for Cushing's syndrome [27]
- Osilodrostat (LCI-699) – 11β-hydroxylase inhibitor (glucocorticoid synthesis inhibitor) for Cushing's syndrome [28]
- Relacorilant (CORT-125134) – glucocorticoid receptor antagonist for Cushing's syndrome [29]
Mineralocorticoidics
- Apararenone (MT-3995) – mineralocorticoid receptor antagonist for diabetic nephropathy and non-alcoholic steatohepatitis [30]
- Finerenone (BAY-94-8862) – mineralocorticoid receptor antagonist for chronic heart failure, diabetic nephropathy, and renal failure [31]
GnRH/gonadotropins
- Fezolinetant (ESN-364) – small-molecule NK3 receptor antagonist for hot flashes, polycystic ovary syndrome, and uterine fibroids [32]
- Linzagolix (KLH-2109, OBE-2109) – small-molecule GnRH receptor antagonist for uterine fibroids and endometriosis [33]
- MVT-602 (RVT-602, TAK-448) – small-molecule kisspeptin receptor agonist for female infertility and hypogonadism [34]
- Relugolix (Relumina; RVT-601, TAK-385) – small-molecule GnRH antagonist for prostate cancer, uterine fibroids, and endometriosis [35]
Mixed
- 11β-Methyl-19-nortestosterone dodecylcarbonate (CDB-4754) – dual androgen/anabolic steroid and progestin for use as a male birth control pill[8]
- Dimethandrolone undecanoate (CDB-4521) – dual androgen/anabolic steroid and progestin for use as a male birth control pill[9]
- Estetrol/drospirenone (Estelle) – estrogen and progestogen combination for hormonal contraception (pregnancy prevention) [36]
- Ethinylestradiol/drospirenone/prasterone – estrogen, progestogen, androgen, and neurosteroid combination for hormonal contraception (pregnancy) [37]
- Relugolix/estradiol/norethisterone acetate – GnRH antagonist and add-back low-dose estrogen and progestogen combination for heavy menstrual bleeding associated with uterine fibroids and for endometriosis-associated pain[10][11]
See also
References
- ^ a b http://www.evestra.com/index-Dateien/Page1242.htm
- ^ a b 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.
- ^ 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.
- ^ 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.
- ^ 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.
- ^ 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.
- ^ https://adisinsight.springer.com/drugs/800038483
- ^ https://www.endocrine.org/news-room/2019/endo-2019---second-potential-male-birth-control-pill-passes-human-safety-tests
- ^ https://www.endocrine.org/news-room/2018/dimethandrolone-undecanoate-shows-promise-as-a-male-birth-control-pill
- ^ https://www.myovant.com/our-science/relugolix/
- ^ https://investors.myovant.com/news-releases/news-release-details/myovant-sciences-announces-97-response-rate-positive-phase-3