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Inocoterone Acetate
Inocoterone acetate () (developmental code names RU-38882, RU-882) is a steroid-like nonsteroidal antiandrogen (NSAA) that was developed for topical administration to treat acne but was never marketed. It is the acetate ester of inocoterone, which is less potent in comparison. Inocoterone acetate is actually not a silent antagonist of the androgen receptor but rather a weak partial agonist, similarly to steroidal antiandrogens like cyproterone acetate. Inocoterone acetate was investigated for the treatment of acne but showed only modest (albeit statistically significant) efficacy in clinical trials. A reduction of 26% of lesions was observed in males treated with the drug after 16 weeks (~3.7 months). However, this is notably far less than that achieved with other agents such as benzoyl peroxide or antibiotics, which produce 50–75% reductions within 2 months. Similar poor results with the topical route have disappointingly been found for other antiandrogens such as cyproterone ...
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Nonsteroidal Antiandrogen
A nonsteroidal antiandrogen (NSAA) is an antiandrogen with a nonsteroidal chemical structure. They are typically selective and full or silent antagonists of the androgen receptor (AR) and act by directly blocking the effects of androgens like testosterone and dihydrotestosterone (DHT). NSAAs are used in the treatment of androgen-dependent conditions in men and women. They are the converse of steroidal antiandrogens (SAAs), which are antiandrogens that are steroids and are structurally related to testosterone. Medical uses NSAAs are used in clinical medicine for the following indications: * Prostate cancer in men * Androgen-dependent skin and hair conditions like acne, hirsutism, seborrhea, and pattern hair loss (androgenic alopecia) in women * Hyperandrogenism, such as due to polycystic ovary syndrome or congenital adrenal hyperplasia, in women * As a component of hormone therapy for transgender women * Precocious puberty in boys * Priapism in men Available forms Pharmacol ...
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Efficacy
Efficacy is the ability to perform a task to a satisfactory or expected degree. The word comes from the same roots as ''effectiveness'', and it has often been used synonymously, although in pharmacology a pragmatic clinical trial#Efficacy versus effectiveness, distinction is now often made between efficacy and effectiveness. The word ''efficacy'' is used in pharmacology and medicine to refer both to the maximum response achievable from a pharmaceutical drug in research settings, and to the capacity for sufficient therapeutic effect or beneficial change in clinical settings. Pharmacology In pharmacology, efficacy () is the maximum response achievable from an applied or dosed agent, for instance, a small molecule drug. Intrinsic activity is a relative term for a drug's efficacy relative to a drug with the highest observed efficacy. It is a purely descriptive term that has little or no mechanistic interpretation. In order for a drug to have an effect, it needs to bind to its t ...
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Anti-acne Preparations
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 possible scarring. It primarily affects skin with a relatively high number of oil glands, including the face, upper part of the chest, and back. The resulting appearance can lead to anxiety, reduced self-esteem, and, in extreme cases, depression or thoughts of suicide. Susceptibility to acne is primarily genetic in 80% of cases. The roles of diet and cigarette smoking in the condition are unclear, and neither cleanliness nor exposure to sunlight appear to play a part. In both sexes, hormones called androgens appear to be part of the underlying mechanism, by causing increased production of sebum. Another common factor is the excessive growth of the bacterium ''Cutibacterium acnes'', which is present on the skin. Treatments for acne are ...
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Acetate Esters
An acetate is a salt formed by the combination of acetic acid with a base (e.g. alkaline, earthy, metallic, nonmetallic or radical base). "Acetate" also describes the conjugate base or ion (specifically, the negatively charged ion called an anion) typically found in aqueous solution and written with the chemical formula . The neutral molecules formed by the combination of the acetate ion and a ''positive'' ion (called a cation) are also commonly called "acetates" (hence, ''acetate of lead'', ''acetate of aluminum'', etc.). The simplest of these is hydrogen acetate (called acetic acid) with corresponding salts, esters, and the polyatomic anion , or . Most of the approximately 5 billion kilograms of acetic acid produced annually in industry are used in the production of acetates, which usually take the form of polymers. In nature, acetate is the most common building block for biosynthesis. Nomenclature and common formula When part of a salt, the formula of the acetate ion ...
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List Of Steroidal Antiandrogens
This is a list of steroidal antiandrogens. Progesterone derivatives * 11α-Hydroxyprogesterone = 11α-hydroxyprogesterone * Chlormadinone acetate = 17α-acetoxy-6-chloro-δ6-progesterone * Clometerone (L-38000) = 6α-chloro-16α-methylprogesterone * Cyproterone (SH-80881) = 1,2α-methylene-6-chloro-δ6-17α-hydroxyprogesterone * Cyproterone acetate = 1,2α-methylene-6-chloro-δ6-17α-acetoxyprogesterone * Edogestrone (PH-218) = 17α-acetoxy-3,3-ethylenedioxy-6-methylpregn-5-en-20-one * Medrogestone = 6,17α-dimethyl-δ6-progesterone * Megestrol acetate = 17α-acetoxy-δ6-6-methylprogesterone * Nomegestrol acetate = 17α-acetoxy-δ6-6-methyl-19-norprogesterone * Osaterone acetate (TZP-4238) = 17α-acetoxy-6-chloro-2-oxa-δ6-progesterone Testosterone derivatives * Abiraterone (CB-7598) = 17-(3-pyridinyl)androsta-5,16-dien-3β-ol * Abiraterone acetate = 17-(3-pyridinyl)androsta-5,16-dien-3β-ol acetate * Benorterone (SKF-7690, FC-612) = 17α-methyl-''B''-nortestosterone * BO ...
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Steroidal Antiandrogen
A steroidal antiandrogen (SAA) is an antiandrogen with a steroidal chemical structure. They are typically antagonists of the androgen receptor (AR) and act both by blocking the effects of androgens like testosterone and dihydrotestosterone (DHT) and by suppressing gonadal androgen production. SAAs lower concentrations of testosterone through simulation of the negative feedback inhibition of the hypothalamus. SAAs are used in the treatment of androgen-dependent conditions in men and women, and are also used in veterinary medicine for the same purpose. They are the converse of nonsteroidal antiandrogens (NSAAs), which are antiandrogens that are not steroids and are structurally unrelated to testosterone. Medical uses SAAs are used in clinical medicine for the following indications: * Prostate cancer in men * Benign prostatic hyperplasia in men * Androgen-dependent skin and hair conditions like acne, hirsutism, seborrhea, and pattern hair loss (androgenic alopecia) in women * Hy ...
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Rosterolone
Rosterolone () (developmental code name SH-434), also known as 17α-propylmesterolone or 1α-methyl-17α-propyl-5α-androstan-17β-ol-3-one, is a steroidal antiandrogen which was first described in 1984 and was developed for topical administration but was never marketed. It has shown some efficacy in the treatment of acne, and lacks systemic effects with either topical or systemic administration. Rosterolone is a derivative of mesterolone, which, in contrast, is an androgen and anabolic steroid. See also * Steroidal antiandrogen -chemical * List of steroidal antiandrogens This is a list of steroidal antiandrogens. Progesterone derivatives * 11α-Hydroxyprogesterone = 11α-hydroxyprogesterone * Chlormadinone acetate = 17α-acetoxy-6-chloro-δ6-progesterone * Clometerone (L-38000) = 6α-chloro-16α-methylproge ... References Abandoned drugs Androstanes Anti-acne preparations Steroidal antiandrogens {{dermatologic-drug-stub ...
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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 pressure, low blood potassium that does not improve with supplementation, early puberty in boys, acne and excessive hair growth in women, and as a part of transgender hormone therapy in transfeminine people. Spironolactone is taken by mouth. Common side effects include electrolyte abnormalities, particularly high blood potassium, nausea, vomiting, headache, rashes, and a decreased desire for sex. In those with liver or kidney problems, extra care should be taken. Spironolactone has not been well studied in pregnancy and should not be used to treat high blood pressure of pregnancy. It is a steroid that blocks the effects of the hormones aldosterone and testosterone and has some estrogen-like effects. Spironolactone belongs to a class of medicati ...
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Antibiotic
An antibiotic is a type of antimicrobial substance active against bacteria. It is the most important type of antibacterial agent for fighting bacterial infections, and antibiotic medications are widely used in the treatment and prevention of such infections. They may either kill or inhibit the growth of bacteria. A limited number of antibiotics also possess antiprotozoal activity. Antibiotics are not effective against viruses such as the common cold or influenza; drugs which inhibit viruses are termed antiviral drugs or antivirals rather than antibiotics. Sometimes, the term ''antibiotic''—literally "opposing life", from the Greek roots ἀντι ''anti'', "against" and βίος ''bios'', "life"—is broadly used to refer to any substance used against microbes, but in the usual medical usage, antibiotics (such as penicillin) are those produced naturally (by one microorganism fighting another), whereas non-antibiotic antibacterials (such as sulfonamides and antiseptics) ...
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Benzoyl Peroxide
Benzoyl peroxide is a chemical compound (specifically, an organic peroxide) with structural formula , often abbreviated as (BzO)2. In terms of its structure, the molecule can be described as two benzoyl (, Bz) groups connected by a peroxide (). It is a white granular solid with a faint odour of benzaldehyde, poorly soluble in water but soluble in acetone, ethanol, and many other organic solvents. Benzoyl peroxide is an oxidizer, but it is principally used as in the production of polymers. Benzoyl peroxide is mainly used in production of plastics and for bleaching flour, hair, plastics and textiles. Synthesis, structure, and chemical reactivity The original 1858 synthesis by Liebig reacted benzoyl chloride with barium peroxide, a reaction described by the following idealized equation: : Benzoyl peroxide is usually prepared by treating hydrogen peroxide with benzoyl chloride under alkaline conditions. : As in many other peroxides, the C-O-O-C linkage has a dihedral angle ...
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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, dietary choices, dietary supplements, and medical devices) and known interventions that warrant further study and comparison. Clinical trials generate data on dosage, safety and efficacy. They are conducted only after they have received health authority/ethics committee approval in the country where approval of the therapy is sought. These authorities are responsible for vetting the risk/benefit ratio of the trial—their approval does not mean the therapy is 'safe' or effective, only that the trial may be conducted. Depending on product type and development stage, investigators initially enroll volunteers or patients into small pilot studies, and subsequently conduct progressively larger scale comparative studies. Clinical trials can vary i ...
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