This is a list of investigational sex-hormonal agents, or

sex-hormonal agent __NOTOC__ A sex-hormonal agent, also known as a sex-hormone receptor modulator, is a type of hormonal agent which specifically modulates the effects of sex hormones and of their biological targets, the sex hormone receptors. The sex hormones inclu ...

s 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 The word oral may refer to: Relating to the mouth * Relating to the mouth, the first portion of the alimentary canal that primarily receives food and liquid **Oral administration of medicines ** Oral examination (also known as an oral exam or or ...

prodrug of

testosterone Testosterone is the primary sex hormone and anabolic steroid in males. In humans, testosterone plays a key role in the development of male reproductive tissues such as testes and prostate, as well as promoting secondary sexual characteristi ...

(

androgen An androgen (from Greek ''andr-'', the stem of the word meaning "man") is any natural or synthetic steroid hormone that regulates the development and maintenance of male characteristics in vertebrates by binding to androgen receptors. This in ...

/ anabolic steroid) with improved pharmacokinetics

Androgen receptor antagonists

* Bavdegalutamide (AVR-110) – androgen receptor antagonist for prostate cancer

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*

Clascoterone Clascoterone, sold under the brand name Winlevi, is an antiandrogen medication which is used topically in the treatment of acne. It is also under development in a higher concentration for the treatment of androgen-dependent scalp hair loss, und ...

(CB-03-01, Breezula, Winlevi) – androgen receptor antagonist for

topical A topical medication is a medication that is applied to a particular place on or in the body. Most often topical medication means application to body surfaces such as the skin or mucous membranes to treat ailments via a large range of classes ...

treatment of scalp hair lossbr>
* Deutenzalutamide (deuterated enzalutamide; HC-1119) – androgen receptor antagonist for prostate cance

* Pruxelutamide (GT-0918; proxalutamide) – androgen receptor antagonist for prostate cance

ref name="TongChen2014"> * Pyrilutamide (KX-826) – androgen receptor antagonist for

treatment of androgen-dependent scalp hair loss and

acne Acne, also known as ''acne vulgaris'', is a long-term skin condition that occurs when dead skin cells and oil from the skin clog hair follicles. Typical features of the condition include blackheads or whiteheads, pimples, oily skin, and ...

Rezvilutamide Rezvilutamide (), sold under the brand name Ariane, is a nonsteroidal antiandrogen which is approved for the treatment of prostate cancer in China and is or was under development for the treatment of breast cancer. It is a selective androgen ...

(SHR3680) – androgen receptor antagonist for prostate cance

*

Spironolactone Spironolactone, sold under the brand name Aldactone among others, is a medication that is primarily used to treat fluid build-up due to heart failure, liver scarring, or kidney disease. It is also used in the treatment of high blood press ...

(Aldactone) – androgen receptor antagonist for systemic treatment of acne

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Atypical androgen receptor antagonists

Dimethylcurcumin Dimethylcurcumin (development code ASC-J9) is a nonsteroidal antiandrogen and a synthetic curcuminoid which is under development by AndroScience Corporation as a topical medication for the treatment of acne vulgaris. It has also been under inve ...

(ASC-J9) – androgen receptor degradation enhancer for topical acne treatmen

*

EPI-7386 EPI-7386 is an ''N''-terminal domain antiandrogen, or antagonist of the ''N''-terminal domain (NTD) of the androgen receptor (AR), which is under development for the treatment of prostate cancer. The compound was developed as a successor of p ...

–

N-terminal domain androgen receptor antagonist ''N''-Terminal domain antiandrogens are a novel type of antiandrogen that bind to the ''N''-terminal domain of the androgen receptor (AR) instead of the ligand-binding domain (where all currently-available antiandrogens bind) and disrupt inte ...

for prostate cance
Androgen_synthesis_inhibitors

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* Seviteronel
(VT-464) – CYP17A1 inhibitor (androgen synthesis inhibitor) for prostate cancer and breast cancer]

Estrogenics

Estrogen receptor agonists

EC508 EC508, also known as estradiol 17β-(1-(4-(aminosulfonyl)benzoyl)--proline), is an estrogen which is under development by Evestra for use in menopausal hormone therapy and as a hormonal contraceptive for the prevention of pregnancy in women.Nicki ...

– oral prodrug of

estradiol Estradiol (E2), also spelled oestradiol, is an estrogen steroid hormone and the major female sex hormone. It is involved in the regulation of the estrous and menstrual female reproductive cycles. Estradiol is responsible for the development o ...

(

estrogen Estrogen or oestrogen is a category of sex hormone responsible for the development and regulation of the female reproductive system and secondary sex characteristics. There are three major endogenous estrogens that have estrogenic hormonal ac ...

) with improved pharmacokinetics *

Erteberel Erteberel (, ; former developmental code name LY-500307; also known as selective estrogen receptor beta agonist-1 or SERBA-1) is a synthetic, nonsteroidal estrogen which acts as a selective ERβ agonist and is under development by Eli Lilly for ...

(LY-500307, SERBA-1) – selective

ERβ Estrogen receptor beta (ERβ) also known as NR3A2 (nuclear receptor subfamily 3, group A, member 2) is one of two main types of estrogen receptor—a nuclear receptor which is activated by the sex hormone estrogen. In humans ERβ is encoded by ...

agonist for

schizophrenia Schizophrenia is a mental disorder characterized by continuous or relapsing episodes of psychosis. Major symptoms include hallucinations (typically hearing voices), delusions, and disorganized thinking. Other symptoms include social wit ...

br>
* Estetrol (medication), Estetrol (Donesta) – estrogen for

menopausal symptom Menopause, also known as the climacteric, is the time in women's lives when menstrual periods stop permanently, and they are no longer able to bear children. Menopause usually occurs between the age of 47 and 54. Medical professionals often ...

s and other indication

Selective estrogen receptor modulators

* Acolbifene (EM-652, SCH-57068) – selective estrogen receptor modulator for breast cance

* Afimoxifene (4-hydroxytamoxifen; 4-OHT; TamoGel) – selective estrogen receptor modulator for topical treatment of breast cancer and hyperplasiabr>
* Amcenestrant (SAR-439859; SERD '859) – selective estrogen receptor modulator and

selective estrogen receptor degrader A selective estrogen receptor degrader or downregulator (SERD) is a type of drug which binds to the estrogen receptor (ER) and, in the process of doing so, causes the ER to be degraded and thus downregulated. They are used to treat estrogen rece ...

for breast cance

* Camizestrant (AZ14066724, AZD-9833) – selective estrogen receptor modulator and selective estrogen receptor degrader for breast cance

*

Elacestrant Elacestrant (INN) (developmental code names RAD-1901, ER-306323) is a nonsteroidal combined selective estrogen receptor modulator (SERM) and selective estrogen receptor degrader (SERD) (described as a "SERM/SERD hybrid (SSH)") that was discovere ...

(RAD-1901, ER-306323) – selective estrogen receptor modulator and selective estrogen receptor degrader for breast cance

*

Endoxifen Endoxifen, also known as 4-hydroxy-''N''-desmethyltamoxifen, is a nonsteroidal selective estrogen receptor modulator (SERM) of the triphenylethylene group as well as a protein kinase C (PKC) inhibitor. It is under development for the treatment ...

(4-hydroxy-N-desmethyltamoxifen) – selective estrogen receptor modulator for breast cance

* Giredestrant (GDC-9545; RG-6171) – selective estrogen receptor modulator and selective estrogen receptor degrader for breast cance

*

Imlunestrant Imlunestrant is an experimental selective estrogen receptor degrader developed by Eli Lilly and Company for the treatment of some types of breast cancer. References

{{reflist Selective estrogen receptor degraders Drugs developed by Eli Lilly ...

(LY-3484356) – selective estrogen receptor modulator and selective estrogen receptor degrader for breast cancer and endometrial cance

* Rintodestrant (G1T-48) – selective estrogen receptor modulator and selective estrogen receptor degrader for breast cance

Estrogen receptor antagonists

* Fulvestrant-3 boronic acid (ZB716) – estrogen receptor antagonist (

antiestrogen Antiestrogens, also known as estrogen antagonists or estrogen blockers, are a class of drugs which prevent estrogens like estradiol from mediating their biological effects in the body. They act by blocking the estrogen receptor (ER) and/or ...

) for breast cancer

Estrogen synthesis inhibitors

Estradiol sulfamate Estradiol sulfamate (E2MATE; developmental code names J995, PGL-2, PGL-2001, ZK-190628, others), or estradiol-3-''O''-sulfamate, is a steroid sulfatase (STS) inhibitor which is under development for the treatment of endometriosis. It is the C3 su ...

(E2MATE, J995, PGL-2, PGL-2001, ZK-190628) – steroid sulfatase inhibitor (estrogen "activation" inhibitor) for endometriosisbr>
* Leflutrozole (BGS-649) –

aromatase inhibitor Aromatase inhibitors (AIs) are a class of drugs used in the treatment of breast cancer in postmenopausal women and in men, and gynecomastia in men. They may also be used off-label to reduce estrogen conversion when supplementing testosterone ex ...

(

estrogen synthesis inhibitor An estrogen synthesis inhibitor is a type of drug which inhibits the enzymatic synthesis of estrogens, such as estradiol. They include: * Aromatase inhibitors (CYP19A1 inhibitors): inhibit the synthesis of estrogens from androgens * CYP17A1 inhibi ...

) for male

hypogonadism Hypogonadism means diminished functional activity of the gonads—the testes or the ovaries—that may result in diminished production of sex hormones. Low androgen (e.g., testosterone) levels are referred to as hypoandrogenism and low estroge ...

br>

Progestogenics

Progesterone receptor agonists

Hydroxyprogesterone caproate Hydroxyprogesterone caproate (OHPC), sold under the brand names Proluton and Makena among others, is a progestin medication which is used to prevent preterm birth in pregnant women with a history of the condition and to treat gynecological diso ...

(LPCN-1107) –

progesterone receptor agonist ( progestogen/ progestin) for prevention of

preterm labor Preterm birth, also known as premature birth, is the birth of a baby at fewer than 37 weeks gestational age, as opposed to full-term delivery at approximately 40 weeks. Extreme preterm is less than 28 weeks, very early preterm birth is between ...

* VOLT-02 – water-soluble conjugate of progesterone and neurosteroid for

traumatic brain injury A traumatic brain injury (TBI), also known as an intracranial injury, is an injury to the brain caused by an external force. TBI can be classified based on severity (ranging from mild traumatic brain injury TBI/concussionto severe traumatic br ...

and

gynecological disorder Gynaecology or gynecology (see spelling differences) is the area of medicine that involves the treatment of women's diseases, especially those of the reproductive organs. It is often paired with the field of obstetrics, forming the combined area ...

Selective progesterone receptor modulators

Telapristone Telapristone (), as telapristone acetate (proposed brand names Proellex, Progenta; former code name CDB-4124), is a synthetic, steroidal selective progesterone receptor modulator (SPRM) related to mifepristone which is under development by Repros ...

(CDB-4124, Proellex, Proellex-V, Progenta) –

selective progesterone receptor modulator A selective progesterone receptor modulator (SPRM) is an agent that acts on the progesterone receptor (PR), the biological target of progestogens like progesterone. A characteristic that distinguishes such substances from full receptor agonists (e ...

for breast cancer, endometriosis, and

uterine fibroids Uterine fibroids, also known as uterine leiomyomas or fibroids, are benign smooth muscle tumors of the uterus. Most women with fibroids have no symptoms while others may have painful or heavy periods. If large enough, they may push on the bl ...

br>
*

Vilaprisan Vilaprisan (, ) (developmental code name BAY-1002670) is a synthetic and steroidal selective progesterone receptor modulator (SPRM) which is under development by Bayer HealthCare Pharmaceuticals for the treatment of endometriosis and uterine fibr ...

(BAY-1002670) – selective progesterone receptor modulator for endometriosis and uterine fibroid

Progesterone receptor antagonists

Onapristone Onapristone () (developmental code names ZK-89299, ZK-299) is a synthetic and steroidal antiprogestogen with additional antiglucocorticoid activity which was developed by Schering in and described in 1984 but was never marketed. in in It is a ...

(AR-18, IVV-1001, ZK-299, ZK-98299) –

progesterone receptor antagonist Antiprogestogens, or antiprogestins, also known as progesterone antagonists or progesterone blockers, are a class of drugs which prevent progestogens like progesterone from mediating their biological effects in the body. They act by blocking t ...

(

antiprogestogen Antiprogestogens, or antiprogestins, also known as progesterone antagonists or progesterone blockers, are a class of drugs which prevent progestogens like progesterone from mediating their biological effects in the body. They act by blocking the ...

) for prostate cance

GnRH/gonadotropins

Gonadotropin-releasing hormone receptor antagonists

Linzagolix Linzagolix, sold under the brand name Yselty, is a medication used in the treatment of uterine fibroids.https://www.ema.europa.eu/en/documents/product-information/yselty-epar-product-information_en.pdf Linzagolix is a small-molecule, non-peptid ...

(KLH-2109, OBE-2109) –

small-molecule Within the fields of molecular biology and pharmacology, a small molecule or micromolecule is a low molecular weight (≤ 1000 daltons) organic compound that may regulate a biological process, with a size on the order of 1 nm. Many drugs ar ...

GnRH receptor antagonist for uterine fibroids and endometriosi

Kisspeptin receptor agonists

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

female infertility Female infertility refers to infertility in women. It affects an estimated 48 million women, with the highest prevalence of infertility affecting women in South Asia, Sub-Saharan Africa, North Africa/Middle East, and Central/Eastern Europe and Cen ...

and hypogonadis

Neurokinin/tachykinin receptor antagonists

* Elinzanetant (BAY-3427080; GSK-1144814; NT-814) – small-molecule NK₁ receptor and NK₃ receptor antagonist for

hot flash Hot flashes (also known as hot flushes) are a form of flushing, often caused by the changing hormone levels that are characteristic of menopause. They are typically experienced as a feeling of intense heat with sweating and rapid heartbeat, and ...

es and "sex hormone disorder

* Fezolinetant (ESN-364) – small-molecule NK₃ receptor antagonist for hot flashes,

polycystic ovary syndrome Polycystic ovary syndrome, or PCOS, is the most common endocrine disorder in women of reproductive age. The syndrome is named after the characteristic cysts which may form on the ovaries, though it is important to note that this is a sign and no ...

, and uterine fibroid

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 Dimethandrolone undecanoate (DMAU), also known by its developmental code name CDB-4521, is an experimental androgen/ anabolic steroid (AAS) and progestogen medication which is under development as a potential birth control pill for men. It is t ...

(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 Dehydroepiandrosterone (DHEA), also known as androstenolone, is an endogenous steroid hormone precursor. It is one of the most abundant circulating steroids in humans. DHEA is produced in the adrenal glands, the gonads, and the brain. It fun ...

supplement for hot flashe

Androgen, estrogen, and progesterone receptor modulators

Ethinylestradiol/drospirenone/prasterone Ethinylestradiol/drospirenone/prasterone (EE/DRSP/DHEA), known under developmental code names like Androgen Restored Contraceptive (ARC), Female Balance Pill, Pill-Plus, and Triple Oral Contraceptive (Triple OC), is a combination of ethinylestrad ...

– estrogen, progestogen, and dehydroepiandrosterone combination for female birth controlbr>

References

External links

AdisInsight - Springer

2011 Medicines in Development for Women - PhRMA
{{Progesterone receptor modulators Sex-hormonal agents, investigational Experimental drugs Hormonal agents