List of investigational hormonal agents

Androgenics

• Clascoterone – androgen receptor antagonist for topical acne treatment
• Deuterated enzalutamide – androgen receptor antagonist for prostate cancer
• Dimethylcurcumin – androgen receptor degradation enhancer for topical acne treatment
• EC586 – oral prodrug of testosterone with improved pharmacokinetics
• EPI-7386 – N-terminal domain androgen receptor antagonist for prostate cancer
• Proxalutamide – androgen receptor antagonist for prostate cancer
• Seviteronel – CYP17A1 inhibitor for prostate cancer and breast cancer
• SHR-3680 – androgen receptor antagonist for prostate cancer

  Estrogenics

• Acolbifene – selective estrogen receptor modulator for breast cancer
• Acolbifene/prasterone – selective estrogen receptor modulator and supplement for vasomotor symptoms
• Afimoxifene – selective estrogen receptor modulator for breast cancer
• EC508 – oral prodrug of estradiol with improved pharmacokinetics
• Elacestrant – selective estrogen receptor modulator and selective estrogen receptor degrader for breast cancer
• Enclomifene – selective estrogen receptor modulator for male hypogonadism
• Endoxifen – selective estrogen receptor modulator for breast cancer
• Erteberel – selective ERβ agonist for schizophrenia
• Estetrol – estrogen for menopausal symptoms and other indications
• Estradiol sulfamate – estrogen and steroid sulfatase inhibitor for endometriosis
• Fulvestrant-3 boronic acid – estrogen receptor antagonist for breast cancer
• Leflutrozole – aromatase inhibitor for male hypogonadism

  Progestogenics

• Hydroxyprogesterone caproate – oral progesterone receptor agonist for prevention of preterm labor
• Onapristone – progesterone receptor antagonist for prostate cancer
• Telapristone – selective progesterone receptor modulator for breast cancer, endometriosis, and uterine fibroids
• Vilaprisan – selective progesterone receptor modulator for endometriosis and uterine fibroids
• VOLT-02 – water-soluble conjugate of progesterone for traumatic brain injury and gynecological disorders

  Glucocorticoidics

• IONIS-GCCR_Rx – glucocorticoid receptor antisense oligonucleotide for type 2 diabetes mellitus
• Levoketoconazole – glucocorticoid synthesis inhibitor for Cushing's syndrome
• Osilodrostat – 11β-hydroxylase inhibitor for Cushing's syndrome
• Relacorilant – glucocorticoid receptor antagonist for Cushing's syndrome

  Mineralocorticoidics

• Apararenone – mineralocorticoid receptor antagonist for diabetic nephropathy and non-alcoholic steatohepatitis
• Finerenone – mineralocorticoid receptor antagonist for chronic heart failure, diabetic nephropathy, and renal failure

  GnRH/gonadotropins

• Fezolinetant – small-molecule NK₃ receptor antagonist for hot flashes, polycystic ovary syndrome, and uterine fibroids
• Linzagolix – small-molecule GnRH receptor antagonist for uterine fibroids and endometriosis
• MVT-602 – small-molecule kisspeptin receptor agonist for female infertility and hypogonadism
• Relugolix – small-molecule GnRH antagonist for prostate cancer, uterine fibroids, and endometriosis

  Mixed

• 11β-Methyl-19-nortestosterone dodecylcarbonate – dual androgen/anabolic steroid and progestin for use as a male birth control pill
• Dimethandrolone undecanoate – dual androgen/anabolic steroid and progestin for use as a male birth control pill
• Estetrol/drospirenone – estrogen and progestogen combination for hormonal contraception
• Ethinylestradiol/drospirenone/prasterone – estrogen, progestogen, androgen, and neurosteroid combination for hormonal contraception
• 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