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.

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
 * Enobosarm (ostarine; GTx-024, MK-2866; S-22; VERU-024) – selective androgen receptor modulator for breast cancer
 * GSK-2881078 – selective androgen receptor modulator for cachexia
 * OPK-88004 (LY-2452473; OPK-88004; TT-701) – selective androgen receptor modulator for benign prostatic hyperplasia, erectile dysfunction, and prostate cancer
 * VK-5211 (LGD-4033; ligandrol) – selective androgen receptor modulator for hip fracture and muscle atrophy
 * Vosilasarm (EP-0062, RAD-140; testolone) – selective androgen receptor modulator for breast cancer

Androgen receptor antagonists

 * Bavdegalutamide (AVR-110) – androgen receptor antagonist for prostate cancer
 * Clascoterone (CB-03-01, Breezula, Winlevi) – androgen receptor antagonist for topical treatment of scalp hair loss
 * Deutenzalutamide (deuterated enzalutamide; HC-1119) – androgen receptor antagonist for prostate cancer
 * Pruxelutamide (GT-0918; proxalutamide) – androgen receptor antagonist for prostate cancer
 * 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

Atypical androgen receptor antagonists

 * Dimethylcurcumin (ASC-J9) – androgen receptor degradation enhancer for topical acne treatment
 * EPI-7386 – N-terminal domain androgen receptor antagonist for prostate cancer  [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

Estrogen receptor agonists

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

Selective estrogen receptor modulators

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

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
 * Leflutrozole (BGS-649) – aromatase inhibitor (estrogen synthesis inhibitor) for male hypogonadism

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

Selective progesterone receptor modulators

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

Progesterone receptor antagonists

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

Kisspeptin receptor agonists

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

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"

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

Androgen, estrogen, and progesterone receptor modulators

 * Ethinylestradiol/drospirenone/prasterone – estrogen, progestogen, and dehydroepiandrosterone combination for female birth control