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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 pare ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Estrogen (medication)
An estrogen (E) is a type of medication which is used most commonly in hormonal birth control and menopausal hormone therapy, and as part of feminizing hormone therapy for transgender women. They can also be used in the treatment of hormone-sensitive cancers like breast cancer and prostate cancer and for various other indications. Estrogens are used alone or in combination with progestogens. They are available in a wide variety of formulations and for use by many different routes of administration. Examples of estrogens include bioidentical estradiol, natural conjugated estrogens, synthetic steroidal estrogens like ethinylestradiol, and synthetic nonsteroidal estrogens like diethylstilbestrol. Estrogens are one of three types of sex hormone agonists, the others being androgens/ anabolic steroids like testosterone and progestogens like progesterone. Side effects of estrogens include breast tenderness, breast enlargement, headache, nausea, fluid retention, and e ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Bioavailability
In pharmacology, bioavailability is a subcategory of absorption and is the fraction (%) of an administered drug that reaches the systemic circulation. By definition, when a medication is administered intravenously, its bioavailability is 100%. However, when a medication is administered via routes other than intravenous, its bioavailability is generally lower than that of intravenous due to intestinal endothelium absorption and first-pass metabolism. Thereby, mathematically, bioavailability equals the ratio of comparing the area under the plasma drug concentration curve versus time (AUC) for the extravascular formulation to the AUC for the intravascular formulation. AUC is used because AUC is proportional to the dose that has entered the systemic circulation. Bioavailability of a drug is an average value; to take population variability into account, deviation range is shown as ±. To ensure that the drug taker who has poor absorption is dosed appropriately, the bottom value ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Estrogen Conjugate
An estrogen conjugate is a conjugate of an endogenous estrogen. They occur naturally in the body as metabolites of estrogens and can be reconverted back into estrogens. They serve as a circulating reservoir for estrogen, particularly in the case of orally administered pharmaceutical estradiol. Estrogen conjugates include sulfate and/or glucuronide conjugates of estradiol, estrone, and estriol: * Sulfated: ** Estrone 3-sulfate (E1S) ** Estradiol 3-sulfate (E2S, E2-3S) and estradiol 17β-sulfate (E2-17S) ** Estriol 3-sulfate (E3S) ** Estradiol 3,17β-disulfate (E2DS) * Glucuronidated: ** Estrone 3-glucuronide (E1-G) ** Estradiol 3-glucuronide (E2-3G) and estradiol 17β-glucuronide (E2-17G) ** Estriol 3-glucuronide (E3-3G), estriol 16α-glucuronide (E3-16G) * Mixed: ** Estradiol 3-glucuronide 17β-sulfate (E2-3G-17βS) ** Estradiol 3-sulfate 17β-glucuronide (E2-3S-17βG) ** Estriol 3-sulfate 16α-glucuronide (E3-3S-16G) Estrogen conjugates are conjugated at the C3, C ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Estrone (medication)
Estrone (E1), sold under the brand names Estragyn, Kestrin, and Theelin among many others, is an estrogen medication and naturally occurring steroid hormone which has been used in menopausal hormone therapy and for other indications. It has been provided as an aqueous suspension or oil solution given by injection into muscle and as a vaginal cream applied inside of the vagina. It can also be taken by mouth as estradiol/estrone/estriol (brand name Hormonin) and in the form of prodrugs like estropipate (estrone sulfate; brand name Ogen) and conjugated estrogens (mostly estrone sulfate; brand name Premarin). Side effects of estrogens like estrone include breast tenderness, breast enlargement, headache, nausea, fluid retention, and edema, among others. Estrone is a naturally occurring and bioidentical estrogen, or an agonist of the estrogen receptor, the biological target of estrogens like endogenous estradiol. It is a relatively weak estrogen, with much lower activity than ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Metabolism
Metabolism (, from el, μεταβολή ''metabolē'', "change") is the set of life-sustaining chemical reactions in organisms. The three main functions of metabolism are: the conversion of the energy in food to energy available to run cellular processes; the conversion of food to building blocks for proteins, lipids, nucleic acids, and some carbohydrates; and the elimination of metabolic wastes. These enzyme-catalyzed reactions allow organisms to grow and reproduce, maintain their structures, and respond to their environments. The word metabolism can also refer to the sum of all chemical reactions that occur in living organisms, including digestion and the transportation of substances into and between different cells, in which case the above described set of reactions within the cells is called intermediary (or intermediate) metabolism. Metabolic reactions may be categorized as '' catabolic'' – the ''breaking down'' of compounds (for example, of glucose to pyruvate ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Liver Protein Synthesis
The liver is a major organ only found in vertebrates which performs many essential biological functions such as detoxification of the organism, and the synthesis of proteins and biochemicals necessary for digestion and growth. In humans, it is located in the right upper quadrant of the abdomen, below the diaphragm. Its other roles in metabolism include the regulation of glycogen storage, decomposition of red blood cells, and the production of hormones. The liver is an accessory digestive organ that produces bile, an alkaline fluid containing cholesterol and bile acids, which helps the breakdown of fat. The gallbladder, a small pouch that sits just under the liver, stores bile produced by the liver which is later moved to the small intestine to complete digestion. The liver's highly specialized tissue, consisting mostly of hepatocytes, regulates a wide variety of high-volume biochemical reactions, including the synthesis and breakdown of small and complex molecules, many of ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Injection (medicine)
An injection (often and usually referred to as a "shot" in US English, a "jab" in UK English, or a "jag" in Scottish English and Scots) is the act of administering a liquid, especially a drug, into a person's body using a needle (usually a hypodermic needle) and a syringe. An injection is considered a form of parenteral drug administration; it does not involve absorption in the digestive tract. This allows the medication to be absorbed more rapidly and avoid the first pass effect. There are many types of injection, which are generally named after the body tissue the injection is administered into. This includes common injections such as subcutaneous, intramuscular, and intravenous injections, as well as less common injections such as intraperitoneal, intraosseous, intracardiac, intraarticular, and intracavernous injections. Injections are among the most common health care procedures, with at least 16 billion administered in developing and transitional countries each ye ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Transdermal Administration
Transdermal is a route of administration wherein active ingredients are delivered across the skin for systemic distribution. Examples include transdermal patches used for medicine delivery. The drug is administered in the form of a patch or ointment that delivers the drug into the circulation for systemic effect. Techniques Obstacles Although the skin is a large and logical target for drug delivery, its basic functions limit its utility for this purpose. The skin functions mainly to protect the body from external penetration (by e.g. harmful substances and microorganisms) and to contain all body fluids. There are two important layers to the human skin: (1) the Epidermis and (2) the Dermis. For transdermal delivery, drugs must pass through the two sublayers of the epidermis to reach the microcirculation of the dermis. The Stratum corneum is the top layer of the skin and varies in thickness from approximately ten to several hundred micrometres, depending on the region of the ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Vaginal Administration
Intravaginal administration is a route of administration where the substance is applied inside the vagina. Pharmacologically, it has the potential advantage to result in effects primarily in the vagina or nearby structures (such as the vaginal portion of cervix) with limited systemic adverse effects compared to other routes of administration. Formulation methods include vaginal tablets, vaginal cream, vaginal gel, vaginal suppository and vaginal ring. Medicines primarily delivered by intravaginal administration include vaginally administered estrogens and progestogens (a group of hormones including progesterone), and antibacterials and antifungals to treat bacterial vaginosis and yeast infections respectively. Medicines may also be administered intravaginally as an alternative to oral route in the case of nausea or other digestive problems. It is a potential means of artificial insemination Artificial insemination is the deliberate introduction of sperm into a female' ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Route Of Administration
A route of administration in pharmacology and toxicology is the way by which a drug, fluid, poison, or other substance is taken into the body. Routes of administration are generally classified by the location at which the substance is applied. Common examples include oral and intravenous administration. Routes can also be classified based on where the target of action is. Action may be topical (local), enteral (system-wide effect, but delivered through the gastrointestinal tract), or parenteral (systemic action, but delivered by routes other than the GI tract). Route of administration and dosage form are aspects of drug delivery. Classification Routes of administration are usually classified by application location (or exposition). The route or course the active substance takes from application location to the location where it has its target effect is usually rather a matter of pharmacokinetics (concerning the processes of uptake, distribution, and elimination of dru ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Oral Contraceptive
Oral contraceptives, abbreviated OCPs, also known as birth control pills, are medications taken by mouth for the purpose of birth control. Female Two types of female oral contraceptive pill, taken once per day, are widely available: * The combined oral contraceptive pill contains estrogen and a progestin. Colloquially known as "The Pill". * The progestogen-only pill, colloquially known as "minipill". * Ormeloxifene is a selective estrogen receptor modulator which offers the benefit of only having to be taken once a week. Emergency contraception pills ("morning after pills") are taken at the time of intercourse, or within a few days afterwards: * Levonorgestrel, sold under the brand name Plan B * Ulipristal acetate * Mifepristone Mifepristone, also known as RU-486, is a medication typically used in combination with misoprostol to bring about a medical abortion during pregnancy and manage early miscarriage. This combination is 97% effective during the first 63 days of .. ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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