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Estradiol 17β-(1-(4-(aminosulfonyl)benzoyl)-L-proline)
EC508, also known as estradiol 17β-(1-(4-(aminosulfonyl)benzoyl)--proline), is an estrogen (medication), 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. It is an oral administration, orally active estrogen ester – specifically, a C17β sulfonamide–proline ester of the natural product, natural and bioidentical estrogen estradiol (medication), 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 parenteral estradiol, but with the convenience of oral administration. EC508 is a candidate with the potential to replace not only oral estra ... [...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, and edema among ... [...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 lower due to intestinal epithelium 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 of the deviation range is employed ... [...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 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 tha ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Metabolism
Metabolism (, from ''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 of 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#Biological, 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 by c ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Liver Protein Synthesis
The liver is a major metabolic organ (anatomy), organ exclusively found in vertebrates, which performs many essential biological Function (biology), functions such as detoxification of the organism, and the Protein biosynthesis, synthesis of various proteins and various other Biochemistry, biochemicals necessary for digestion and growth. In humans, it is located in the quadrants and regions of abdomen, right upper quadrant of the abdomen, below the thoracic diaphragm, diaphragm and mostly shielded by the lower right rib cage. Its other metabolic roles include carbohydrate metabolism, the production of a number of hormones, conversion and storage of nutrients such as glucose and glycogen, and the decomposition of red blood cells. Anatomical and medical terminology often use the prefix List of medical roots, suffixes and prefixes#H, ''hepat-'' from ἡπατο-, from the Greek language, Greek word for liver, such as hepatology, and hepatitis The liver is also an accessory digestive ... [...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 epidural, 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 ... [...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. It is used as an administration method for issues related to women's health, such as contraception. 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 ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Route Of Administration
In pharmacology and toxicology, a route of administration is the way by which a medication, 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 administration, oral and intravenous therapy, intravenous administration. Routes can also be classified based on where the target of action is. Action may be topical medication, topical (local), enteral administration, enteral (system-wide effect, but delivered through the gastrointestinal tract), or #Parenteral, parenteral (systemic action, but is 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 rat ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Investigational New Drug
The United States Food and Drug Administration's Investigational New Drug (IND) program is the means by which a pharmaceutical industry, pharmaceutical company obtains permission to start human clinical trials and to ship an experimental drug interstate commerce, across state lines (usually to clinical investigators) before a marketing application for the drug has been approved. Regulations are primarily at . Similar procedures are followed in the European Union, Japan, and Canada due to regulatory harmonization efforts by the International Council for Harmonisation of Technical Requirements for Pharmaceuticals for Human Use, International Council for Harmonisation. Types * Research or investigator INDs are non-commercial INDs filed by researchers to study an unapproved drug or to study an approved drug for a new indication or in a new patient population. * Expanded access, Emergency Use INDs, also called compassionate use or single-patient INDs, are filed for emergency use of a ... [...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. The introduction of the birth control pill ("the Pill") in 1960 revolutionized the options for contraception, sparking vibrant discussion in the scientific and social science literature and in the media. Much attention focused on issues of women's rights, including ethics and personal choice. But these medications also introduced new questions about risk. 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". For perfect use it is 99% effective and typical use is 91% effective. Side effects of the pill include headache, dizziness, nausea, sore breasts, spotting, mood changes, acne, bloating, etc. One pill offers the benefit of only havi ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
