List of investigational sex-hormonal agents

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

Selective androgen receptor modulators

• DT-200 (G-100192, GLPG-0492) – selective androgen receptor modulator for Duchenne muscular dystrophy [1]
• Enobosarm (ostarine; GTx-024, MK-2866; S-22; VERU-024) – selective androgen receptor modulator for breast cancer [2]
• GSK-2881078 – selective androgen receptor modulator for cachexia [3]
• OPK-88004 (LY-2452473; OPK-88004; TT-701) – selective androgen receptor modulator for benign prostatic hyperplasia, erectile dysfunction, and prostate cancer [4]
• VK-5211 (LGD-4033; ligandrol) – selective androgen receptor modulator for hip fracture and muscle atrophy [5]
• Vosilasarm (EP-0062, RAD-140; testolone) – selective androgen receptor modulator for breast cancer [6]

Androgen receptor antagonists

• Bavdegalutamide (AVR-110) – androgen receptor antagonist for prostate cancer[7][8]
• Clascoterone (CB-03-01, Breezula, Winlevi) – androgen receptor antagonist for topical treatment of scalp hair loss [9]
• Deutenzalutamide (deuterated enzalutamide; HC-1119) – androgen receptor antagonist for prostate cancer [10] [11] [12]
• Pruxelutamide (GT-0918; proxalutamide) – androgen receptor antagonist for prostate cancer [13]
• Pyrilutamide (KX-826) – androgen receptor antagonist for topical treatment of androgen-dependent scalp hair loss and acne
• Spironolactone (Aldactone) – androgen receptor antagonist for systemic treatment of acne[14][15][16]

Atypical androgen receptor antagonists

• Dimethylcurcumin (ASC-J9) – androgen receptor degradation enhancer for topical acne treatment [17]
• EPI-7386 – N-terminal domain androgen receptor antagonist for prostate cancer [18] [19] [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 [20]

Estrogenics

Estrogen receptor agonists

• EC508 – oral prodrug of estradiol (estrogen) with improved pharmacokinetics
• Erteberel (LY-500307, SERBA-1) – selective ERβ agonist for schizophrenia [21]
• Estetrol (Donesta) – estrogen for menopausal symptoms and other indications [22]

Selective estrogen receptor modulators

• Acolbifene (EM-652, SCH-57068) – selective estrogen receptor modulator for breast cancer [23]
• Afimoxifene (4-hydroxytamoxifen; 4-OHT; TamoGel) – selective estrogen receptor modulator for topical treatment of breast cancer and hyperplasia [24]
• Amcenestrant (SAR-439859; SERD '859) – selective estrogen receptor modulator and selective estrogen receptor degrader for breast cancer [25]
• Camizestrant (AZ14066724, AZD-9833) – selective estrogen receptor modulator and selective estrogen receptor degrader for breast cancer [26]
• Endoxifen (4-hydroxy-N-desmethyltamoxifen) – selective estrogen receptor modulator for breast cancer [27]
• Giredestrant (GDC-9545; RG-6171) – selective estrogen receptor modulator and selective estrogen receptor degrader for breast cancer [28]
• Imlunestrant (LY-3484356) – selective estrogen receptor modulator and selective estrogen receptor degrader for breast cancer and endometrial cancer [29]
• Rintodestrant (G1T-48) – selective estrogen receptor modulator and selective estrogen receptor degrader for breast cancer [30]

Estrogen receptor antagonists

• Fulvestrant-3 boronic acid (ZB716) – estrogen receptor antagonist (antiestrogen) for breast cancer

Estrogen synthesis inhibitors

• Estradiol sulfamate (E2MATE, J995, PGL-2, PGL-2001, ZK-190628) – steroid sulfatase inhibitor (estrogen "activation" inhibitor) for endometriosis [31]
• Leflutrozole (BGS-649) – aromatase inhibitor (estrogen synthesis inhibitor) for male hypogonadism [32]

Progestogenics

Progesterone receptor agonists

• Hydroxyprogesterone caproate (LPCN-1107) – oral progesterone receptor agonist (progestogen/progestin) for prevention of preterm labor
• VOLT-02 – water-soluble conjugate of progesterone and neurosteroid for traumatic brain injury and gynecological disorders [33]

Selective progesterone receptor modulators

• Telapristone (CDB-4124, Proellex, Proellex-V, Progenta) – selective progesterone receptor modulator for breast cancer, endometriosis, and uterine fibroids [34]
• Vilaprisan (BAY-1002670) – selective progesterone receptor modulator for endometriosis and uterine fibroids [35]

Progesterone receptor antagonists

• Onapristone (AR-18, IVV-1001, ZK-299, ZK-98299) – progesterone receptor antagonist (antiprogestogen) for prostate cancer [36]

GnRH/gonadotropins

Kisspeptin receptor agonists

• MVT-602 (RVT-602, TAK-448) – small-molecule kisspeptin receptor agonist for female infertility and hypogonadism [37]

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"[38]

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
• Dimethandrolone undecanoate (CDB-4521) – dual androgen/anabolic steroid and progestin for use as a male birth control pill

Androgen and estrogen receptor modulators

• Acolbifene/prasterone (Femivia) – selective estrogen receptor modulator and dehydroepiandrosterone supplement for hot flashes [39]

Androgen, estrogen, and progesterone receptor modulators

• Ethinylestradiol/drospirenone/prasterone – estrogen, progestogen, and dehydroepiandrosterone combination for female birth control [40]

See also

• List of investigational drugs