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List of investigational hormonal agents

Index List of investigational hormonal agents

This is a list of investigational hormonal agents, or hormonal agents that are currently under development for clinical use but are not yet approved. [1]

85 relations: Acne, Acolbifene, Acolbifene/prasterone, Afimoxifene, Agonist, Antiandrogen, Apararenone, Aromatase inhibitor, Breast cancer, Cortexolone 17α-propionate, Cushing's syndrome, CYP17A1 inhibitor, Darolutamide, Diabetes mellitus type 2, Diabetic nephropathy, Dimethylcurcumin, Elacestrant, Elagolix, EM-5854, Enclomifene, Endometrial hyperplasia, Endometriosis, Endoxifen, Enobosarm, Enzyme inhibitor, Erteberel, Esaxerenone, Estetrol, Estetrol/drospirenone, Estradiol sulfamate, Estradiol/progesterone, Estrogen, Estrogen receptor, Estrogen receptor beta, Fezolinetant, Finerenone, Glucocorticoid receptor, Gonadotropin-releasing hormone antagonist, GTx-758, Heart failure, Hormonal contraception, Hormone, Hot flash, Hyperaldosteronism, Hypertension, Hypogonadism, IONIS-GCCRRx, Kidney failure, Leflutrozole, Levoketoconazole, ..., Linzagolix, List of investigational drugs, Menopause, Mineralocorticoid receptor, Non-alcoholic fatty liver disease, Oligonucleotide, Onapristone, Osilodrostat, Ozarelix, Peptide, Polycystic ovary syndrome, Pregnancy, Progesterone receptor, Progestogen, Proxalutamide, Relacorilant, Relugolix, Schizophrenia, Selective androgen receptor degrader, Selective androgen receptor modulator, Selective estrogen receptor modulator, Selective progesterone receptor modulator, Seviteronel, Small molecule, Steroid 11β-hydroxylase, Steroid sulfatase, Stress incontinence, Symptom, Tachykinin receptor 3, TAS-108, Telapristone, Topical medication, Uterine fibroid, Vilaprisan, ZB716. Expand index (35 more) »

Acne

Acne, also known as acne vulgaris, is a long-term skin disease that occurs when hair follicles are clogged with dead skin cells and oil from the skin.

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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.

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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 development by Endoceutics for the treatment of vasomotor symptoms (hot flashes) in postmenopausal women.

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Afimoxifene

Afimoxifene, also known as 4-hydroxytamoxifen (4-OHT, 4-HT, OHTAM, others), is a selective estrogen receptor modulator (SERM) of the triphenylethylene group and the major active metabolite of tamoxifen.

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Agonist

An agonist is a chemical that binds to a receptor and activates the receptor to produce a biological response.

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Antiandrogen

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.

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Apararenone

Apararenone (INN) (developmental code name MT-3995) is a nonsteroidal antimineralocorticoid which is under development by Mitsubishi Tanabe Pharma for the treatment of diabetic nephropathies and non-alcoholic steatohepatitis.

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Aromatase inhibitor

Aromatase inhibitors (AIs) are a class of drugs used in the treatment of breast cancer in postmenopausal women and gynecomastia in men.

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Breast cancer

Breast cancer is cancer that develops from breast tissue.

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Cortexolone 17α-propionate

Cortexolone 17α-propionate (developmental code name CB-03-01; tentative brand names Breezula (for acne), Winlevi (for androgenic alopecia)), or 11-deoxycortisol 17α-propionate, is a synthetic steroidal antiandrogen – specifically, an androgen receptor antagonist – that is under development by Cassiopea and Intrepid Therapeutics for use as a topical medication in the treatment of androgen-dependent conditions including acne vulgaris and androgenic alopecia (male-pattern hair loss).

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Cushing's syndrome

Cushing's syndrome is a collection of signs and symptoms due to prolonged exposure to cortisol.

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CYP17A1 inhibitor

A CYP17A1 inhibitor is a type of drug which inhibits the enzyme CYP17A1.

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Darolutamide

Darolutamide (developmental code names ODM-201, BAY-1841788) is a nonsteroidal antiandrogen (NSAA) – specifically, a selective antagonist of the androgen receptor (AR) – which is under development by Orion and Bayer HealthCare for the treatment of advanced, castration-resistant prostate cancer (CRPC).

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Diabetes mellitus type 2

Diabetes mellitus type 2 (also known as type 2 diabetes) is a long-term metabolic disorder that is characterized by high blood sugar, insulin resistance, and relative lack of insulin.

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Diabetic nephropathy

Diabetic nephropathy (DN), also known as diabetic kidney disease, is the chronic loss of kidney function occurring in those with diabetes mellitus.

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Dimethylcurcumin

Dimethylcurcumin (developmental code name 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.

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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 by Eisai and is under development by Radius Health and Takeda for the treatment of menopausal vasomotor symptoms (hot flashes) and estrogen receptor (ER)-positive advanced breast cancer, as well as endometrial cancer and kidney cancer.

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Elagolix

Elagolix (former developmental code names NBI-56418, ABT-620) is a gonadotropin-releasing hormone antagonist (GnRH antagonist), developed for clinical use by Neurocrine Biosciences and AbbVie.

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EM-5854

EM-5854 is a steroidal antiandrogen which is or was under development by Endoceutics, Inc.

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Enclomifene

Enclomifene (tentative brand name Androxal), or enclomiphene, is a nonsteroidal selective estrogen receptor modulator (SERM) of the triphenylethylene group that is under development for the treatment of male hypogonadism.

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Endometrial hyperplasia

Endometrial hyperplasia is a condition of excessive proliferation of the cells of the endometrium, or inner lining of the uterus.

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Endometriosis

Endometriosis is a condition in which the endometrium, the layer of tissue that normally covers the inside of the uterus, grows outside of it.

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Endoxifen

Endoxifen, also known as N-desmethyl-4-hydroxytamoxifen, is an orally active nonsteroidal selective estrogen receptor modulator (SERM) of the triphenylethylene group that is or was under development for the treatment of estrogen receptor-positive breast cancer.

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Enobosarm

Enobosarm, also known as ostarine, is an investigational selective androgen receptor modulator (SARM) developed by GTX, Inc for the treatment of conditions such as muscle wasting and osteoporosis, formerly under development by Merck & Company.

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Enzyme inhibitor

4QI9) An enzyme inhibitor is a molecule that binds to an enzyme and decreases its activity.

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Erteberel

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

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Esaxerenone

Esaxerenone (INN) (developmental code names CS-3150, XL-550) is a nonsteroidal antimineralocorticoid which was discovered by Exelixis and is now under development by Daiichi Sankyo Company for the treatment of hypertension, essential hypertension, hyperaldosteronism, and diabetic nephropathies.

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Estetrol

Estetrol (E4), or oestetrol, is a weak estrogen steroid hormone which is found in detectable levels only during pregnancy.

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Estetrol/drospirenone

Estetrol/drospirenone (E4/DRSP; tentative brand name Estelle) is a combination of estetrol, an estrogen, and drospirenone, a progestin, which is under development by Estetra S.A. as a combined oral contraceptive for the prevention of pregnancy in women.

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Estradiol sulfamate

Estradiol sulfamate (E2MATE; developmental code names J995, PGL-2, PGL-2001, ZK-190628), or estradiol-3-O-sulfamate, is a synthetic estrogen and steroid sulfatase (STS) inhibitor which is under development for the treatment of endometriosis.http://adisinsight.springer.com/drugs/800026648 It is the 3-sulfamate ester of estradiol, and in terms of its estrogenic activity, acts as a prodrug of estradiol. The drug shows profoundly reduced susceptibility to first-pass metabolism relative to estradiol, and was the first "potent" estradiol prodrug to be discovered. As of 2017, E2MATE is in phase II clinical trials for endometriosis. The drug has also been clinically investigated for potential use in hormone replacement therapy. Unlike estradiol and other estradiol esters, due to its unique sulfamate ester, E2MATE is not hydrolyzed during first-pass metabolism, and is instead cleaved into estradiol systemically. E2MATE itself shows no affinity for the estrogen receptor or estrogenic activity in vitro, requiring hydrolysis into estradiol for its estrogenicity. In accordance, the systemic potency of oral E2MATE is increased approximately 100-fold relative to that of oral estradiol, whereas its hepatotropic activity is increased only marginally, by about 2- to 3-fold. As such, E2MATE has virtually absent effects on estrogen-modulated liver functions with oral administration at typical dosages equivalent to those of estradiol and behaves much like parenterally or transdermally administered estradiol, thereby combining the advantages of transdermal estradiol with the convenience of oral administration. Unfortunately, it has been found that E2MATE, without being hydrolyzed first, can be converted by 17β-hydroxysteroid dehydrogenase into estrone sulfamate (EMATE), analogously to conversion of estradiol into estrone. Moreover, EMATE is the dominant fraction found in circulation, and EMATE is hydrolyzed into estrone, which is a far less potent estrogen than estradiol. In relation to these findings, according to Elger et al., "In spite of high levels of and EMATE in the circulation, only insignificant levels and no estrogenic effects were generated in humans (W. Elger, unpublished data)." As such, E2MATE and EMATE are actually not clinically effective as estrogens, and the researchers have subsequently developed new 17-sulfonamide ester estradiol prodrugs, such as EC508, that are not STS inhibitors and that cannot be transformed into the corresponding estrone variants. In addition to its estrogenic activity, E2MATE has been found to act as a potent and irreversible inhibitor of STS. This enzyme is responsible for the transformation of hormonally inactive steroid sulfates into their hormonally active forms, for instance hydrolysis of estrone sulfate into estrone. Inhibition of STS appears to be the basis for E2MATE's clinical development for endometriosis, as STS is expressed in the endometrium and the severity of endometriosis has been found to correlate with STS expression. In a clinical study, E2MATE was found to inhibit endometrial STS activity by 91% in premenopausal women, while circulating levels of estradiol were not affected, implying potential tissue-selective antiestrogenic effects of E2MATE in the endometrium.

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Estradiol/progesterone

Estradiol/progesterone (developmental code name TX-001HR, formerly TX-12-001HR) is an oral combination of estradiol, an estrogen, and progesterone, a progestogen, which is under development in the United States by TherapeuticsMD for the treatment of menopausal symptoms and endometrial hyperplasia.

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Estrogen

Estrogen, or oestrogen, is the primary female sex hormone.

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Estrogen receptor

Estrogen receptors (ERs) are a group of proteins found inside cells.

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Estrogen receptor beta

Estrogen receptor beta (ER-β), 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.

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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 disorders.

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Finerenone

Finerenone (INN, USAN) (developmental code name BAY-94-8862) is a nonsteroidal antimineralocorticoid that is in phase III clinical trials for the treatment of chronic heart failure.

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Glucocorticoid receptor

The glucocorticoid receptor (GR, or GCR) also known as NR3C1 (nuclear receptor subfamily 3, group C, member 1) is the receptor to which cortisol and other glucocorticoids bind.

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Gonadotropin-releasing hormone antagonist

Gonadotropin-releasing hormone antagonists (GnRH antagonists) are a class of medications that antagonize the gonadotropin-releasing hormone receptor (GnRH receptor) and thus the action of gonadotropin-releasing hormone (GnRH).

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GTx-758

GTx-758 (tentative brand name Capesaris) is a synthetic nonsteroidal estrogen which is under development by GTx, Inc. for the treatment of advanced prostate cancer.

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Heart failure

Heart failure (HF), often referred to as congestive heart failure (CHF), is when the heart is unable to pump sufficiently to maintain blood flow to meet the body's needs.

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Hormonal contraception

Hormonal contraception refers to birth control methods that act on the endocrine system.

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Hormone

A hormone (from the Greek participle “ὁρμῶ”, "to set in motion, urge on") is any member of a class of signaling molecules produced by glands in multicellular organisms that are transported by the circulatory system to target distant organs to regulate physiology and behaviour.

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Hot flash

Hot flashes (American English) or hot flushes (British English) are a form of flushing due to reduced levels of estradiol.

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Hyperaldosteronism

Hyperaldosteronism, also aldosteronism, is a medical condition wherein too much aldosterone is produced by the adrenal glands, which can lead to lowered levels of potassium in the blood (hypokalemia) and increased hydrogen ion excretion (alkalosis).

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Hypertension

Hypertension (HTN or HT), also known as high blood pressure (HBP), is a long-term medical condition in which the blood pressure in the arteries is persistently elevated.

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Hypogonadism

Hypogonadism means diminished functional activity of the gonads—the testes or the ovaries —that may result in diminished sex hormone biosynthesis.

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IONIS-GCCRRx

IONIS-GCCRRx, also known as ISIS-426115, is an antiglucocorticoid which is under development by Ionis Pharmaceuticals (formerly Isis Pharmaceuticals) for the treatment of diabetes mellitus type 2.

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Kidney failure

Kidney failure, also known as end-stage kidney disease, is a medical condition in which the kidneys no longer work.

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Leflutrozole

Leflutrozole (developmental code names BGS-649, CGP-47645) is an aromatase inhibitor which is under development by Mereo BioPharma and Novartis for the treatment of hypogonadism in men.

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Levoketoconazole

Levoketoconazole (INN, USAN) (developmental code name COR-003; tentative brand name Recorlev, previously NormoCort), also known as (2S,4R)-ketoconazole, is a steroidogenesis inhibitor that is under development by Strongbridge Biopharma (formerly Cortendo AB) for the treatment of Cushing's syndrome.

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Linzagolix

Linzagolix (developmental code names KLH-2109, OBE-2109) is a small-molecule, non-peptide, orally active gonadotropin-releasing hormone antagonist (GnRH antagonist) which is under development by Kissei Pharmaceutical and ObsEva for the treatment of uterine leiomyoma and endometriosis.

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List of investigational drugs

List of investigational drugs may refer to.

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Menopause

Menopause, also known as the climacteric, is the time in most women's lives when menstrual periods stop permanently, and they are no longer able to bear children.

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Mineralocorticoid receptor

The mineralocorticoid receptor (or MR, MLR, MCR), also known as the aldosterone receptor or nuclear receptor subfamily 3, group C, member 2, (NR3C2) is a protein that in humans is encoded by the NR3C2 gene that is located on chromosome 4q31.1-31.2.

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Non-alcoholic fatty liver disease

Non-alcoholic fatty liver disease (NAFLD) is one of the types of fatty liver which occurs when fat is deposited (steatosis) in the liver due to causes other than excessive alcohol use.

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Oligonucleotide

Oligonucleotides are short DNA or RNA molecules, oligomers, that have a wide range of applications in genetic testing, research, and forensics.

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Onapristone

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

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Osilodrostat

Osilodrostat (INN, USAN) (developmental code name LCI-699) is an orally active, nonsteroidal corticosteroid biosynthesis inhibitor which is under development by Novartis for the treatment of Cushing's syndrome and adrenocorticotropic hormone hypersecretion (a specific subtype of Cushing's syndrome).

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Ozarelix

Ozarelix (developmental code names D-63153, SPI-153) is a peptide gonadotropin-releasing hormone antagonist (GnRH antagonist) which is under development by AEterna Zentaris Inc.

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Peptide

Peptides (from Gr.: πεπτός, peptós "digested"; derived from πέσσειν, péssein "to digest") are short chains of amino acid monomers linked by peptide (amide) bonds.

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Polycystic ovary syndrome

Polycystic ovary syndrome (PCOS) is a set of symptoms due to elevated androgens (male hormones) in females.

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Pregnancy

Pregnancy, also known as gestation, is the time during which one or more offspring develops inside a woman.

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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.

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Progestogen

Progestogens, also sometimes spelled progestagens or gestagens, are a class of steroid hormones that bind to and activate the progesterone receptor (PR).

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Proxalutamide

Proxalutamide (developmental code name GT-0918) is a nonsteroidal antiandrogen (NSAA) – specifically, a selective high-affinity silent antagonist of the androgen receptor (AR) – which is under development by Suzhou Kintor Pharmaceuticals for the treatment of prostate cancer.

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Relacorilant

Relacorilant (developmental code name CORT-125134) is an antiglucocorticoid which is under development by Corcept Therapeutics for the treatment of Cushing's syndrome.

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Relugolix

Relugolix (developmental code names RVT-601, TAK-385) is a non-peptide, orally active, selective antagonist of the gonadotropin-releasing hormone receptor (GnRHR) (.

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Schizophrenia

Schizophrenia is a mental disorder characterized by abnormal social behavior and failure to understand reality.

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Selective androgen receptor degrader

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.

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Selective androgen receptor modulator

Selective androgen receptor modulators or SARMs are a novel class of androgen receptor ligands.

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Selective estrogen receptor modulator

Selective estrogen receptor modulators (SERMs) are a class of drugs that act on the estrogen receptor (ER).

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Selective progesterone receptor modulator

A selective progesterone receptor modulator (SPRM) is an agent that acts on the progesterone receptor.

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Seviteronel

Seviteronel (developmental codes VT-464 and, formerly, INO-464) is an experimental cancer medication which is under development by Viamet Pharmaceuticals and Innocrin Pharmaceuticals for the treatment of prostate cancer and breast cancer.

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Small molecule

Within the fields of molecular biology and pharmacology, a small molecule is a low molecular weight (< 900 daltons) organic compound that may regulate a biological process, with a size on the order of 1 nm.

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Steroid 11β-hydroxylase

Steroid 11β-hydroxylase is a steroid hydroxylase found in the zona glomerulosa and zona fasciculata.

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Steroid sulfatase

Steroid sulfatase (STS), or steryl-sulfatase, formerly known as arylsulfatase C, is a sulfatase enzyme involved in the metabolism of steroids.

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Stress incontinence

Stress incontinence, also known as stress urinary incontinence (SUI) or effort incontinence is a form of urinary incontinence.

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Symptom

A symptom (from Greek σύμπτωμα, "accident, misfortune, that which befalls", from συμπίπτω, "I befall", from συν- "together, with" and πίπτω, "I fall") is a departure from normal function or feeling which is noticed by a patient, reflecting the presence of an unusual state, or of a disease.

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Tachykinin receptor 3

Tachykinin receptor 3, also known as TACR3, is a protein which in humans is encoded by the TACR3 gene.

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TAS-108

TAS-108, also known as SR-16234, is a drug discovered by Masato Tanabe and under development by SRI International and Taiho Pharmaceutical.

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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 Therapeutics for the treatment of breast cancer, endometriosis, and uterine fibroids.

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Topical medication

A topical medication is a medication that is applied to a particular place on or in the body.

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Uterine fibroid

Uterine fibroids, also known as uterine leiomyomas or fibroids, are benign smooth muscle tumors of the uterus.

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Vilaprisan

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

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ZB716

ZB716, also known as fulvestrant-3-boronic acid, is a synthetic, steroidal, orally active antiestrogen which is under development for the treatment of estrogen receptor (ER)-positive metastatic breast cancer.

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References

[1] https://en.wikipedia.org/wiki/List_of_investigational_hormonal_agents

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