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 It is likely to become outdated with time.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 Deuterated testosterone (AVA-291; AVA291; d3-testosterone; d3-T; testosterone-19-d3) – deuterated and highly aromatase-resistant testosterone analogue with little/no estrogenic activity 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 Masofaniten (EPI-7386) – N-terminal domain androgen receptor antagonist for prostate cancer 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
Estrogenics 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 Leflutrozole (BGS-649) – aromatase inhibitor (estrogen synthesis inhibitor) for male hypogonadism
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
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
GnRH/gonadotropins GnRH receptor antagonists Merigolix (HS-10518, NCE-403, SKI-2670, TU-2670) – small-molecule GnRH antagonist for endometriosis and uterine fibroids
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"
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
Androgen, estrogen, and progesterone receptor modulators Ethinylestradiol/drospirenone/prasterone – estrogen, progestogen, and dehydroepiandrosterone combination for female birth control
See also List of investigational drugs List of investigational PMS/PMDD drugs
References
External links AdisInsight - Springer 2011 Medicines in Development for Women - PhRMA