List of investigational sex-hormonal agents#GnRH/gonadotropins

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.

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 It is likely to become outdated with time.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=

EC586 – oral prodrug of testosterone (androgen/anabolic steroid) with improved pharmacokinetics

=Selective androgen receptor modulators=

DT-200 (G-100192, GLPG-0492) – selective androgen receptor modulator for Duchenne muscular dystrophy [https://adisinsight.springer.com/drugs/800018432]
Enobosarm (ostarine; GTx-024, MK-2866; S-22; VERU-024) – selective androgen receptor modulator for breast cancer [https://adisinsight.springer.com/drugs/800022562]
GSK-2881078 – selective androgen receptor modulator for cachexia [https://adisinsight.springer.com/drugs/800039743]
OPK-88004 (LY-2452473; OPK-88004; TT-701) – selective androgen receptor modulator for benign prostatic hyperplasia, erectile dysfunction, and prostate cancer [https://adisinsight.springer.com/drugs/800033580]
VK-5211 (LGD-4033; ligandrol) – selective androgen receptor modulator for hip fracture and muscle atrophy [https://adisinsight.springer.com/drugs/800030373]
Vosilasarm (EP-0062, RAD-140; testolone) – selective androgen receptor modulator for breast cancer [https://adisinsight.springer.com/drugs/800028398]

=Androgen receptor antagonists=

Bavdegalutamide (AVR-110) – androgen receptor antagonist for prostate cancer[https://adisinsight.springer.com/drugs/800054393]{{cite journal | vauthors = Zeng S, Huang W, Zheng X, Liyan C, Zhang Z, Wang J, Shen Z | title = Proteolysis targeting chimera (PROTAC) in drug discovery paradigm: Recent progress and future challenges | journal = Eur J Med Chem | volume = 210 | issue = | pages = 112981 | date = January 2021 | pmid = 33160761 | doi = 10.1016/j.ejmech.2020.112981 | s2cid = 226287993 | url = }}[https://cdn.who.int/media/docs/default-source/international-nonproprietary-names-(inn)/pl125.pdf?sfvrsn=af269747_5&download=true]
Clascoterone (CB-03-01, Breezula, Winlevi) – androgen receptor antagonist for topical treatment of scalp hair loss [http://adisinsight.springer.com/drugs/800026561]
Deutenzalutamide (deuterated enzalutamide; HC-1119) – androgen receptor antagonist for prostate cancer [https://adisinsight.springer.com/drugs/800052304] [https://www.dovepress.com/effect-of-n-methyl-deuteration-on-metabolism-and-pharmacokinetics-of-e-peer-reviewed-article-DDDT] [https://onlinelibrary.wiley.com/doi/abs/10.1002/jlcr.3516]
Pruxelutamide (GT-0918; proxalutamide) – androgen receptor antagonist for prostate cancer [http://adisinsight.springer.com/drugs/800046361]{{cite journal|last1=Tong|first1=Youzhi|last2=Chen|first2=Chunyun|last3=Wu|first3=Juan|last4=Yang|first4=Jiangtao|last5=Zhang|first5=Huihui|last6=Wu|first6=Xiaojun|last7=Duan|first7=Yanmei|last8=Gao|first8=Wei|last9=Qian|first9=Weidong|last10=Niu|first10=Xiaoxia|last11=Mi|first11=Lili|last12=Guo|first12=Chuangxing|title=Abstract 614: Proxalutamide (GT0918), a potent androgen receptor pathway inhibitor|journal=Cancer Research|volume=74|issue=19 Supplement|year=2014|pages=614|issn=0008-5472|doi=10.1158/1538-7445.AM2014-614}}
Pyrilutamide (KX-826) – androgen receptor antagonist for topical treatment of androgen-dependent scalp hair loss and acne{{cite web | title = Pyrilutamide - Suzhou Kintor Pharmaceuticals | url = https://adisinsight.springer.com/drugs/800053879 | work = AdisInsight | publisher = Springer Nature Switzerland AG}}
Spironolactone (Aldactone) – androgen receptor antagonist for systemic treatment of acne[https://www.isrctn.com/ISRCTN12892056]{{cite journal | vauthors = 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 | title = 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 | journal = BMJ Open | volume = 11 | issue = 8 | pages = e053876 | date = August 2021 | pmid = 34446504 | doi = 10.1136/bmjopen-2021-053876 | pmc = 8395279 | url = }}[https://www.clinicaltrials.gov/ct2/show/NCT03334682]{{cite journal | vauthors = 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 | title = FASCE, the benefit of spironolactone for treating acne in women: study protocol for a randomized double-blind trial | journal = Trials | volume = 21 | issue = 1 | pages = 571 | date = June 2020 | pmid = 32586344 | pmc = 7318446 | doi = 10.1186/s13063-020-04432-w | url = | doi-access = free }}[https://www.clinicaltrials.gov/ct2/show/NCT04582383]

==Atypical androgen receptor antagonists==

Dimethylcurcumin (ASC-J9) – androgen receptor degradation enhancer for topical acne treatment [http://adisinsight.springer.com/drugs/800028542]
EPI-7386 – N-terminal domain androgen receptor antagonist for prostate cancer [https://adisinsight.springer.com/drugs/800037973] [https://www.essapharma.com/wp-content/uploads/2019/02/Final-Poster-Next-Gen_201902014_Website.pdf] [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]
Rosolutamide (ASC-JM17, JM17, ALZ-003) – androgen receptor degradation enhancer

=Androgen synthesis inhibitors=

Seviteronel (VT-464) – CYP17A1 inhibitor (androgen synthesis inhibitor) for prostate cancer and breast cancer [http://adisinsight.springer.com/drugs/800035241]

Estrogenics

=Estrogen receptor agonists=

EC508 – oral prodrug of estradiol (estrogen) with improved pharmacokinetics{{cite web |url=http://www.evestra.com/index-Dateien/Page1242.htm |title=R&D Research |website=www.evestra.com |url-status=dead |archive-url=https://web.archive.org/web/20170929164030/http://www.evestra.com/index-Dateien/Page1242.htm |archive-date=2017-09-29}}{{cite journal | vauthors = Elger W, Wyrwa R, Ahmed G, Meece F, Nair HB, Santhamma B, Killeen Z, Schneider B, Meister R, Schubert H, Nickisch K | title = Estradiol prodrugs (EP) for efficient oral estrogen treatment and abolished effects on estrogen modulated liver functions | journal = J. Steroid Biochem. Mol. Biol. | volume = 165 | issue = Pt B | pages = 305–311 | date = January 2017 | pmid = 27449818 | doi = 10.1016/j.jsbmb.2016.07.008 | s2cid = 26650319 }}{{cite journal | vauthors = Ahmed G, Elger W, Meece F, Nair HB, Schneider B, Wyrwa R, Nickisch K | title = A prodrug design for improved oral absorption and reduced hepatic interaction | journal = Bioorg. Med. Chem. | volume = 25 | issue = 20 | pages = 5569–5575 | date = October 2017 | pmid = 28886996 | doi = 10.1016/j.bmc.2017.08.027 }}
Erteberel (LY-500307, SERBA-1) – selective ERβ agonist for schizophrenia [http://adisinsight.springer.com/drugs/800031986]
Estetrol (Donesta) – estrogen for menopausal symptoms and other indications [http://adisinsight.springer.com/drugs/800044874]

=Selective estrogen receptor modulators=

Acolbifene (EM-652, SCH-57068) – selective estrogen receptor modulator for breast cancer [http://adisinsight.springer.com/drugs/800013630]
Afimoxifene (4-hydroxytamoxifen; 4-OHT; TamoGel) – selective estrogen receptor modulator for topical treatment of breast cancer and hyperplasia [http://adisinsight.springer.com/drugs/800019175]
Amcenestrant (SAR-439859; SERD '859) – selective estrogen receptor modulator and selective estrogen receptor degrader for breast cancer [https://adisinsight.springer.com/drugs/800048980]
Camizestrant (AZ14066724, AZD-9833) – selective estrogen receptor modulator and selective estrogen receptor degrader for breast cancer [https://adisinsight.springer.com/drugs/800052720]
Endoxifen (4-hydroxy-N-desmethyltamoxifen) – selective estrogen receptor modulator for breast cancer [http://adisinsight.springer.com/drugs/800036114]
Giredestrant (GDC-9545; RG-6171) – selective estrogen receptor modulator and selective estrogen receptor degrader for breast cancer [https://adisinsight.springer.com/drugs/800050643]
Imlunestrant (LY-3484356) – selective estrogen receptor modulator and selective estrogen receptor degrader for breast cancer and endometrial cancer [https://adisinsight.springer.com/drugs/800056808]
Rintodestrant (G1T-48) – selective estrogen receptor modulator and selective estrogen receptor degrader for breast cancer [https://adisinsight.springer.com/drugs/800052167]

=Estrogen receptor antagonists=

Fulvestrant-3 boronic acid (ZB716) – estrogen receptor antagonist (antiestrogen) for breast cancer{{cite journal | vauthors = 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 | title = Fulvestrant-3 Boronic Acid (ZB716): An Orally Bioavailable Selective Estrogen Receptor Downregulator (SERD) | journal = J. Med. Chem. | volume = 59 | issue = 17 | pages = 8134–40 | year = 2016 | pmid = 27529700 | doi = 10.1021/acs.jmedchem.6b00753 | pmc = 5499704 }}{{cite journal|last1=Wang|first1=G|last2=Liu|first2=J|last3=Zheng|first3=S|last4=Miele|first4=L|last5=Wiese|first5=T|last6=Zhong|first6=Q|last7=Guo|first7=S|title=Abstract P2-08-11: An orally bioavailable selective estrogen receptor downregulator|journal=Cancer Research|volume=77|issue=4 Supplement|year=2017|pages=P2-08-11–P2-08-11|issn=0008-5472|doi=10.1158/1538-7445.SABCS16-P2-08-11}}

=Estrogen synthesis inhibitors=

Estradiol sulfamate (E2MATE, J995, PGL-2, PGL-2001, ZK-190628) – steroid sulfatase inhibitor (estrogen "activation" inhibitor) for endometriosis [http://adisinsight.springer.com/drugs/800026648]
Leflutrozole (BGS-649) – aromatase inhibitor (estrogen synthesis inhibitor) for male hypogonadism [http://adisinsight.springer.com/drugs/800032111]

Progestogenics

=Progesterone receptor agonists=

Hydroxyprogesterone caproate (LPCN-1107) – oral progesterone receptor agonist (progestogen/progestin) for prevention of preterm labor{{cite web | url=https://adisinsight.springer.com/drugs/800038483 | title=Hydroxyprogesterone - Lipocine - AdisInsight }}
VOLT-02 – water-soluble conjugate of progesterone and neurosteroid for traumatic brain injury and gynecological disorders [https://adisinsight.springer.com/drugs/800041522]

=Selective progesterone receptor modulators=

Telapristone (CDB-4124, Proellex, Proellex-V, Progenta) – selective progesterone receptor modulator for breast cancer, endometriosis, and uterine fibroids [http://adisinsight.springer.com/drugs/800014404]
Vilaprisan (BAY-1002670) – selective progesterone receptor modulator for endometriosis and uterine fibroids [http://adisinsight.springer.com/drugs/800033040]

=Progesterone receptor antagonists=

Onapristone (AR-18, IVV-1001, ZK-299, ZK-98299) – progesterone receptor antagonist (antiprogestogen) for prostate cancer [http://adisinsight.springer.com/drugs/800000877]

GnRH/gonadotropins

=GnRH receptor antagonists=

Merigolix (HS-10518, NCE-403, SKI-2670, TU-2670) – small-molecule GnRH antagonist for endometriosis and uterine fibroids [https://adisinsight.springer.com/drugs/800065270]

=Kisspeptin receptor agonists=

MVT-602 (RVT-602, TAK-448) – small-molecule kisspeptin receptor agonist for female infertility and hypogonadism [https://adisinsight.springer.com/drugs/800029425]

=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"[https://adisinsight.springer.com/drugs/800044912]

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{{cite web | url=https://www.endocrine.org/news-room/2019/endo-2019---second-potential-male-birth-control-pill-passes-human-safety-tests | title=Second potential male birth control pill passes human safety tests }}
Dimethandrolone undecanoate (CDB-4521) – dual androgen/anabolic steroid and progestin for use as a male birth control pill{{cite web | url=https://www.endocrine.org/news-room/2018/dimethandrolone-undecanoate-shows-promise-as-a-male-birth-control-pill | title=Dimethandrolone undecanoate shows promise as a male birth control pill }}

=Androgen and estrogen receptor modulators=

Acolbifene/prasterone (Femivia) – selective estrogen receptor modulator and dehydroepiandrosterone supplement for hot flashes [http://adisinsight.springer.com/drugs/800043933]

=Androgen, estrogen, and progesterone receptor modulators=

Ethinylestradiol/drospirenone/prasterone – estrogen, progestogen, and dehydroepiandrosterone combination for female birth control [https://adisinsight.springer.com/drugs/800026485]

References

External links

[http://adisinsight.springer.com/ AdisInsight - Springer]
[http://phrma-docs.phrma.org/files/dmfile/medicinesindevelopmentforwomen20113.pdf 2011 Medicines in Development for Women - PhRMA]

Sex-hormonal agents, investigational

Category:Dynamic lists

Category:Experimental sex-hormone agents

Category:Hormonal agents