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 A prodrug is a medication or compound that, after intake, is metabolized (i.e., converted within the body) into a pharmacologically active drug. Instead of administering a drug directly, a corresponding prodrug can be used to improve how the dru ...

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 Anabolic steroids, also known more properly as anabolic–androgenic steroids (AAS), are steroidal androgens that include natural androgens like testosterone as well as synthetic androgens that are structurally related and have similar effects ...

) with improved

pharmacokinetics Pharmacokinetics (from Ancient Greek ''pharmakon'' "drug" and ''kinetikos'' "moving, putting in motion"; see chemical kinetics), sometimes abbreviated as PK, is a branch of pharmacology dedicated to determining the fate of substances administered ...

Androgen receptor antagonists

* Bavdegalutamide (AVR-110) –

androgen receptor antagonist Antiandrogens, also known as androgen antagonists or testosterone blockers, are a class of drugs that prevent androgens like testosterone and dihydrotestosterone (DHT) from mediating their biological effects in the body. They act by blocking th ...

for prostate cancer

ref name="pmid33160761">
*

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 loss Pattern hair loss (also known as androgenetic alopecia (AGA)) is a hair loss condition that primarily affects the top and front of the scalp. In male-pattern hair loss (MPHL), the hair loss typically presents itself as either a receding front ...

br>
* 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 re ...

(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 Systemic fundamental to a predominant social, economic, or political practice. This refers to: In medicine In medicine, ''systemic'' means affecting the whole body, or at least multiple organ systems. It is in contrast with ''topical'' or ''loc ...

treatment of acne

ref name="pmid34446504">
ref name="pmid32586344">

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 invest ...

(ASC-J9) –

androgen receptor degradation enhancer A selective androgen receptor degrader or downregulator (SARD) is a type of drug which interacts with the androgen receptor (AR) such that it causes the AR to be degraded and thus downregulated. They are under investigation for the treatment of ...

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 pre ...

–

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 inter ...

for prostate cance
Androgen_synthesis_inhibitors

*_Seviteronel
_(VT-464)_–_CYP17A1_inhibitor.html" ;"title="Seviteronel">Androgen synthesis inhibitors

* Seviteronel
(VT-464) – CYP17A1 inhibitor">Seviteronel">Androgen synthesis inhibitors

* 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.Nickis ...

– 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 (LY-500307, SERBA-1) – selective ERβ

agonist An agonist is a chemical that activates a receptor to produce a biological response. Receptors are cellular proteins whose activation causes the cell to modify what it is currently doing. In contrast, an antagonist blocks the action of the ag ...

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 w ...

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 d ...

s and other indication

Selective estrogen receptor modulators

Acolbifene Acolbifene () (developmental code names EM-652, SCH-57068) is a nonsteroidal selective estrogen receptor modulator (SERM) which, as of 2015, is in phase III clinical trials for the treatment of breast cancer Breast cancer is cancer that d ...

(EM-652, SCH-57068) –

selective estrogen receptor modulator Selective estrogen receptor modulators (SERMs), also known as estrogen receptor agonist/antagonists (ERAAs), are a class of drugs that act on the estrogen receptor (ER). A characteristic that distinguishes these substances from pure ER agonists ...

for breast cance

*

Afimoxifene Afimoxifene, also known as 4-hydroxytamoxifen (4-OHT) and by its tentative brand name TamoGel, is a selective estrogen receptor modulator (SERM) of the triphenylethylene group and an active metabolite of tamoxifen. The drug is under development u ...

(4-hydroxytamoxifen; 4-OHT; TamoGel) – selective estrogen receptor modulator for topical treatment of breast cancer and

hyperplasia Hyperplasia (from ancient Greek ὑπέρ ''huper'' 'over' + πλάσις ''plasis'' 'formation'), or hypergenesis, is an enlargement of an organ or tissue caused by an increase in the amount of organic tissue that results from cell proliferatio ...

br>
* 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 discovered ...

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

* Endoxifen (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 (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 Steroid sulfatase (STS), or steryl-sulfatase (EC 3.1.6.2), formerly known as arylsulfatase C, is a sulfatase enzyme involved in the metabolism of steroids. It is encoded by the ''STS'' gene. Reactions This enzyme catalyses the following chemi ...

inhibitor Inhibitor or inhibition may refer to: In biology * Enzyme inhibitor, a substance that binds to an enzyme and decreases the enzyme's activity * Reuptake inhibitor, a substance that increases neurotransmission by blocking the reuptake of a neurotra ...

(estrogen "activation" inhibitor) for

endometriosis Endometriosis is a disease of the female reproductive system in which cells similar to those in the endometrium, the layer of tissue that normally covers the inside of the uterus, grow outside the uterus. Most often this is on the ovaries, fa ...

br>
* 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) 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 The progesterone receptor (PR), also known as NR3C3 or nuclear receptor subfamily 3, group C, member 3, is a protein found inside cells. It is activated by the steroid hormone progesterone. In humans, PR is encoded by a single ''PGR'' gene resid ...

agonist (

progestogen Progestogens, also sometimes written progestagens or gestagens, are a class of natural or synthetic steroid hormones that bind to and activate the progesterone receptors (PR). Progesterone is the major and most important progestogen in the bod ...

progestin A progestogen, also referred to as a progestagen, gestagen, or gestogen, is a type of medication which produces effects similar to those of the natural female sex hormone progesterone in the body. A progestin is a ''synthetic'' progestogen. Pro ...

) 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 Neurosteroids, also known as neuroactive steroids, are endogenous or exogenous steroids that rapidly alter neuronal excitability through interaction with ligand-gated ion channels and other cell surface receptors. The term ''neurosteroid'' was co ...

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

Progesterone receptor antagonists

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

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 ...

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 and hypogonadis

Neurokinin/tachykinin receptor antagonists

Elinzanetant Elinzanetant (developmental code names BAY-3427080 GSK-1144814, NT-814) is an orally active small-molecule neurokinin/tachykinin NK1 receptor and NK3 receptor antagonist which is under development by Bayer, GlaxoSmithKline, and NeRRe Therapeu ...

(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, an ...

es and "sex hormone disorder

*

Fezolinetant Fezolinetant (; former developmental code name ESN-364) is a small-molecule, orally active, selective neurokinin-3 (NK3) receptor antagonist which is under development by Ogeda (formerly Euroscreen) for the treatment of sex hormone-related d ...

(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 tak ...

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

Androgen and estrogen receptor modulators

Acolbifene/prasterone Acolbifene/prasterone (tentative brand name Femivia) is a combination formulation of acolbifene, a selective estrogen receptor modulator, and prasterone (dehydroepiandrosterone; DHEA), an androgen, estrogen, and neurosteroid, which is under deve ...

(Femivia) – selective estrogen receptor modulator and dehydroepiandrosterone 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