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List Of Investigational Sex-hormonal Agents
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.'' Androgenics Androgen receptor agonists * EC586 – oral prodrug of testosterone (androgen/anabolic steroid) with improved pharmacokinetics Androgen receptor antagonists * Bavdegalutamide (AVR-110) – androgen receptor antagonist for prostate cancer ref name="pmid33160761"> [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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 include androgens such as testosterone, estrogens such as estradiol, and progestogens such as progesterone. Sex-hormonal agents may be either steroidal or nonsteroidal in chemical structure and may serve to either enhance, inhibit, or have mixed effects on the function of the sex hormone systems. Sex-hormonal agents are used in medicine for a variety of purposes including hormone therapy (e.g., menopausal hormone therapy, androgen replacement therapy, transgender hormone therapy), antihormone therapy (e.g., androgen deprivation therapy, estrogen deprivation therapy), and hormonal contraception, among others. Types and examples Androgen receptor (AR) modulators * Androgens and anabolic steroids (AR agonists) ** Examples: testosterone, and ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Pattern 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 hairline, loss of hair on the crown (vertex) of the scalp, or a combination of both. Female-pattern hair loss (FPHL) typically presents as a diffuse thinning of the hair across the entire scalp. Male pattern hair loss seems to be due to a combination of oxidative stress, the microbiome of the scalp, genetics, and circulating androgens; particularly dihydrotestosterone (DHT). Men with early onset androgenic alopecia (before the age of 35) have been deemed as the male phenotypic equivalent for polycystic ovary syndrome (PCOS). As an early clinical expression of insulin resistance and metabolic syndrome, AGA is related to being an increased risk factor for cardiovascular diseases, glucose metabolism disorders, type 2 diabetes, and enlargeme ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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.Nickisch, K., Santhamma, B., Ahmed, G., Meece, F., Elger, W., Wyrwa, R., & Nair, H. (2017). ''U.S. Patent No. 9,745,338.'' Washington, DC: U.S. Patent and Trademark Office. https://patents.google.com/patent/US9745338B2/en It is an orally active estrogen ester – specifically, a C17β sulfonamide– proline ester of the natural and bioidentical estrogen estradiol – and acts as a prodrug of estradiol in the body. However, unlike oral estradiol and conventional oral estradiol esters such as estradiol valerate, EC508 undergoes little or no first-pass metabolism, has high oral bioavailability, and does not have disproportionate estrogenic effects in the liver. As such, it has a variety of desirable advantages over oral estradiol, similarly to ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Breast Cancer
Breast cancer is cancer that develops from breast tissue. Signs of breast cancer may include a lump in the breast, a change in breast shape, dimpling of the skin, milk rejection, fluid coming from the nipple, a newly inverted nipple, or a red or scaly patch of skin. In those with distant spread of the disease, there may be bone pain, swollen lymph nodes, shortness of breath, or yellow skin. Risk factors for developing breast cancer include obesity, a lack of physical exercise, alcoholism, hormone replacement therapy during menopause, ionizing radiation, an early age at first menstruation, having children late in life or not at all, older age, having a prior history of breast cancer, and a family history of breast cancer. About 5–10% of cases are the result of a genetic predisposition inherited from a person's parents, including BRCA1 and BRCA2 among others. Breast cancer most commonly develops in cells from the lining of milk ducts and the lobules that supply ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Androgen Synthesis Inhibitor
An androgen synthesis inhibitor is a type of drug which inhibits the enzymatic synthesis of androgens, such as testosterone and dihydrotestosterone (DHT). They include: * CYP17A1 inhibitors (17α-hydroxylase/17,20-lyase inhibitors): inhibit the synthesis of androgens from pregnanes * 3β-Hydroxysteroid dehydrogenase inhibitors (3β-HSD inhibitors): inhibit the conversion of weaker androgens such as dehydroepiandrosterone (DHEA) and androstenediol into more potent androgens like and testosterone * Cholesterol side-chain cleavage enzyme inhibitors (P450SCC/CYP11A1 inhibitors): inhibit the synthesis of pregnenolone from cholesterol, thereby inhibiting the synthesis of most steroid hormones (which are derived from pregnenolone) including androgens * 17β-Hydroxysteroid dehydrogenase inhibitors (17β-HSD inhibitors): inhibit the interconversion of androgens, including the synthesis of testosterone from the less-potent androstenedione * 5α-Reductase inhibitors (5α-RIs; SRD5A inhib ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
CYP17A1 Inhibitor
A CYP17A1 inhibitor is a type of drug which inhibits the enzyme CYP17A1. It may inhibit both of the functions of the enzyme, 17α-hydroxylase and 17,20-lyase, or may be selective for inhibition of one of these two functions (generally 17,20-lyase). These drugs prevent the conversion of pregnane steroids into androgens like testosterone and therefore are androgen biosynthesis inhibitors and functional antiandrogens. Examples of CYP17A1 inhibitors include the older drug ketoconazole and the newer drugs abiraterone acetate, orteronel, galeterone, and seviteronel. The CYP17A1 inhibitors that have been marketed, like abiraterone acetate, are used mainly in the treatment of prostate cancer. CYP17A1 inhibitors that are not selective for inhibition of 17,20-lyase must be combined with a glucocorticoid such as prednisone in order to avoid adrenal insufficiency and mineralocorticoid excess caused by prevention of cortisol production. See also * Steroidogenic enzyme * Steroidogenesis inhibit ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Seviteronel
__NOTOC__ 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. It is a nonsteroidal CYP17A1 inhibitor and works by inhibiting the production of androgens and estrogens in the body. As of July 2017, seviteronel is in phase II clinical trials for both prostate cancer and breast cancer. In January 2016, it was designated fast-track status by the United States Food and Drug Administration for prostate cancer. In April 2017, seviteronel received fast-track designation for breast cancer as well. __TOC__ Pharmacology Pharmacodynamics Seviteronel is a nonsteroidal antiandrogen, acting specifically as an androgen synthesis inhibitor via inhibition of the enzyme CYP17A1, for the treatment of castration-resistant prostate cancer. It has approximately 10-fold selectivity for the inhibition of 17,20-lyase ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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 interactions between the AR and its coregulatory binding partners, thereby blocking AR-mediated gene transcription Transcription is the process of copying a segment of DNA into RNA. The segments of DNA transcribed into RNA molecules that can encode proteins are said to produce messenger RNA (mRNA). Other segments of DNA are copied into RNA molecules called .... They are being investigated for the treatment of prostate cancer. See also * Androgen deprivation therapy * 5''N''-Bicalutamide References Antiandrogens {{Antineoplastic-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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 previous drugs in the EPI series such as EPI-001, ralaniten (EPI-002), and ralaniten acetate (EPI-506). EPI-7386 shows 20-fold higher antiandrogenic potency than ralaniten ''in vitro'' ( = 535 nM vs. 9,580 nM, respectively), as well as greater stability in human hepatocytes. It is planned to enter phase I clinical trial Clinical trials are prospective biomedical or behavioral research studies on human participants designed to answer specific questions about biomedical or behavioral interventions, including new treatments (such as novel vaccines, drugs, diet ...s in 2020. References Experimental cancer drugs Nonsteroidal antiandrogens {{genito-urinary-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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 prostate cancer and other androgen-dependent conditions. As of 2017, dimethylcurcumin (ASC-J9), a SARD, is under development for the treatment of acne vulgaris. See also * Androgen deprivation therapy Androgen deprivation therapy (ADT), also called androgen suppression therapy, is an antihormone therapy whose main use is in treating prostate cancer. Prostate cancer cells usually require androgen hormones, such as testosterone, to grow. ADT red ... References Antiandrogens Hormonal antineoplastic drugs {{Antineoplastic-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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 investigation for the treatment of male pattern hair loss, spinal muscular atrophy, and wounds, but no development has been reported for these indications. There has been interest in the drug for the potential treatment of prostate cancer as well. As of 2017, it is in phase II clinical trials for acne vulgaris. Dimethylcurcumin is an androgen receptor (AR) inhibitor and shows strong and specific antiandrogenic activity ''in vitro'' (e.g., against LNCaP cell growth) at sufficiently high concentrations. However, its mechanism of action and effects differ from those of conventional antiandrogens; it is not an antagonist of the AR and instead appears to act as a selective degradation enhancer (SARD) of certain subpopulations of the AR, fo ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Systemic Administration
Systemic administration is a route of administration of medication, nutrition or other substance into the circulatory system so that the entire body is affected. Administration can take place via enteral administration (absorption of the drug through the gastrointestinal tract) or parenteral administration (generally injection, infusion, or implantation). Contrast with 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 ... administration where the effect is generally local. References Routes of administration {{pharma-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
