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Etacstil
Etacstil (developmental code names GW-5638, DPC974) is an orally active, nonsteroidal, combined selective estrogen receptor modulator (SERM) and selective estrogen receptor degrader (SERD) that was developed for the treatment of estrogen receptor-positive breast cancer. It was shown to overcome antiestrogen (tamoxifen, aromatase inhibitor, fulvestrant) resistance in breast cancer by altering the shape of the estrogen receptor, thus exhibiting SERD properties. Etacstil is a tamoxifen derivative and one of the first drugs to overcome tamoxifen-resistance. It is the predecessor of GW-7604, of which etacstil is a prodrug (GW-7604 being the 4-hydroxy metabolite of etacstil). This is analogous to the case of tamoxifen being a prodrug of afimoxifene (4-hydroxytamoxifen). Etacstil was developed in the early 1990s by Duke University, Glaxo Wellcome, and later, Dupont. In 2001, Bristol Myers-Squibb (BMS) acquired Dupont, and for non-scientific, corporate reasons, closed the trial and aba ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Timeline Of Cancer Treatment Development
This is a historical timeline of the development and progress of cancer treatments, which includes time of discovery, progress, and approval of the treatments. Ancient Era Cancer was traditionally treated with surgery, heat, or herbal (chemical) therapies. * 2600 BC Egyptian physician Imhotep recommended producing a localised infection to promote regression of tumours. According to the Ebers medical papyrus, this was done by placing a poultice near the tumour, followed by local incision. * BC Ancient Greeks, Romans, and Egyptians used heat to treat masses. Healers in ancient India used regional and whole-body hyperthermia as treatments. * 2 AD Ancient Greeks describe surgical treatment of cancer. Modern Era 1800s * 1820s British Dr. James Arnott, "the father of modern cryosurgery", starts to use cryotherapy to freeze tumours in the treatment of breast and uterine cancers * 1880s American Dr. William Stewart Halsted develops radical mastectomy for breast cancer * 1890s ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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 estrogen receptor (ER)-positive advanced breast cancer. Elacestrant has dose-dependent, tissue-selective estrogenic and antiestrogenic activities, with biphasic weak partial agonist activity at the ER at low doses and antagonist activity at higher doses. It shows agonistic activity on bone and antagonistic activity on breast and uterine tissues. Unlike the SERD fulvestrant, elacestrant is able to readily cross the blood-brain-barrier into the central nervous system, where it can target breast cancer metastases in the brain, and is orally bioavailable and does not require intramuscular injection. Menarini Group and Radius Health Announce Global License Agr ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Oral Administration
Oral administration is a route of administration where a substance is taken through the mouth. Per os abbreviated to P.O. is sometimes used as a direction for medication to be taken orally. Many medications are taken orally because they are intended to have a systemic effect, reaching different parts of the body via the bloodstream, for example. Oral administration can be easier and less painful than other routes, such as injection. However, the onset of action is relatively low, and the effectiveness is reduced if it is not absorbed properly in the digestive system, or if it is broken down by digestive enzymes before it can reach the bloodstream. Some medications may cause gastrointestinal side effects, such as nausea or vomiting, when taken orally. Oral administration can also only be applied to conscious patients, and patients willing and able to swallow. Terminology ''Per os'' (; ''P.O.'') is an adverbial phrase meaning literally from Latin "through the mouth" or "by ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Glaxo Wellcome
GSK plc, formerly GlaxoSmithKline plc, is a British multinational pharmaceutical and biotechnology company with global headquarters in London, England. Established in 2000 by a merger of Glaxo Wellcome and SmithKline Beecham. GSK is the tenth largest pharmaceutical company and #294 on the 2022 ''Fortune'' Global 500, ranked behind other pharmaceutical companies China Resources, Sinopharm, Johnson & Johnson, Pfizer, Roche, AbbVie, Novartis, Bayer, and Merck. The company has a primary listing on the London Stock Exchange and is a constituent of the FTSE 100 Index. , it had a market capitalisation of £70 billion, the eighth largest on the London Stock Exchange. It has a secondary listing on the New York Stock Exchange. The company developed the first malaria vaccine, RTS,S, which it said in 2014 it would make available for five percent above cost. Legacy products developed at GSK include several listed in the World Health Organization's List of Essential Medicines, such as ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Selective Estrogen Receptor Degraders
A selective estrogen receptor degrader or downregulator (SERD) is a type of drug which binds to the estrogen receptor (ER) and, in the process of doing so, causes the ER to be degraded and thus downregulated. They are used to treat estrogen receptor-sensitive or progesterone receptor-sensitive breast cancer, along with older classes of drugs like selective estrogen receptor modulators (SERMs) and aromatase inhibitors. As of 2016 the only marketed SERD was fulvestrant (brand name Faslodex). As of November 2016 other SERDs under development include brilanestrant and elacestrant. The clinical success of fulvestrant led to efforts to discover and develop a parallel drug class of selective androgen receptor degraders (SARDs). Investigational Fulvestrant requires large-volume and frequently painful intramuscular injections. In response, pharmaceutical companies are currently developing oral SERDs. Among products in development are: * Giredestrant: Roche * Amcenestrant (SAR ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Hormonal Antineoplastic Drugs
A hormone (from the Greek participle , "setting in motion") is a class of signaling molecules in multicellular organisms that are sent to distant organs by complex biological processes to regulate physiology and behavior. Hormones are required for the correct development of animals, plants and fungi. Due to the broad definition of a hormone (as a signaling molecule that exerts its effects far from its site of production), numerous kinds of molecules can be classified as hormones. Among the substances that can be considered hormones, are eicosanoids (e.g. prostaglandins and thromboxanes), steroids (e.g. oestrogen and brassinosteroid), amino acid derivatives (e.g. epinephrine and auxin), protein or peptides (e.g. insulin and CLE peptides), and gases (e.g. ethylene and nitric oxide). Hormones are used to communicate between organs and tissues. In vertebrates, hormones are responsible for regulating a variety of physiological processes and behavioral activities such as digestion, ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
GSK Plc Brands
GSK may refer to: *Galatasaray S.K. Galatasaray Spor Kulübü (, ''Galatasaray Sports Club'') is a Turkish sports club based on the European side of the city of Istanbul in Turkey. Most notable for its association football department, the club also consists of various other de ..., a Turkish sports club based in Istanbul * Glycogen synthase kinase * Golden State Killer, a California serial rapist and murderer * GSK plc, formerly GlaxoSmithKline, a multinational pharmaceutical corporation * GTK Scene Graph Kit, a rendering pipeline {{disambiguation ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Antiestrogens
Antiestrogens, also known as estrogen antagonists or estrogen blockers, are a class of drugs which prevent estrogens like estradiol from mediating their biological effects in the body. They act by blocking the estrogen receptor (ER) and/or inhibiting or suppressing estrogen production., Antiestrogens are one of three types of sex hormone antagonists, the others being antiandrogens and antiprogestogens. Antiestrogens are commonly used to stop steroid hormones, estrogen, from binding to the estrogen receptors leading to the decrease of estrogen levels. Decreased levels of estrogen can lead to complications in sexual development. Antiandrogens are sex hormone antagonists which are able to lower the production and the effects that testosterone can have on female bodies. Types and examples Antiestrogens include selective estrogen receptor modulators (SERMs) like tamoxifen, clomifene, and raloxifene, the ER silent antagonist and selective estrogen receptor degrader (SERD) f ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Bazedoxifene
Bazedoxifene, used as bazedoxifene acetate, is a medication for bone problems and possibly (pending more study) for cancer. It is a third-generation selective estrogen receptor modulator (SERM). Since late 2013 it has had U.S. FDA approval for bazedoxifene as part of the combination drug Duavee in the prevention (not treatment) of postmenopausal osteoporosis. It is also being studied for possible treatment of breast cancer and pancreatic cancer. Medical uses Bazedoxifene is used in the treatment of postmenopausal osteoporosis. Available forms Bazedoxifene is marketed both alone and in combination with conjugated estrogens. Pharmacology Pharmacodynamics Bazedoxifene is a selective estrogen receptor modulator (SERM), or a mixed agonist and antagonist of the estrogen receptor (ER) in different tissues. Chemistry The drug is a member of the 2-phenylindole group of SERMs, along with zindoxifene and pipendoxifene. History Development Bazedoxifene was developed by Pfizer fol ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Brilanestrant
Brilanestrant ( INN) (developmental code names GDC-0810, ARN-810, RG-6046, RO-7056118) is a nonsteroidal combined selective estrogen receptor modulator (SERM) and selective estrogen receptor degrader (SERD) that was discovered by Aragon Pharmaceuticals and was under development by Genentech for the treatment of locally advanced or metastatic estrogen receptor (ER)-positive breast cancer. Development of brilanestrant was discontinued by Roche in April 2017. It reached phase II clinical trials for the treatment of breast cancer prior to the discontinuation of its development. Mechanism of action Similarly to tamoxifen, a SERM, brilanestrant shows some capacity to activate the ER in certain contexts and possesses weak estrogenic activity in the rat uterus, and unlike fulvestrant, which is currently the only SERD to have been marketed, brilanestrant is not a steroid and is orally bioavailable and does not need to be administered by intramuscular injection. Brilanestrant has been ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Bristol Myers-Squibb
The Bristol Myers Squibb Company (BMS) is an American multinational pharmaceutical company. Headquartered in New York City, BMS is one of the world's largest pharmaceutical companies and consistently ranks on the ''Fortune'' 500 list of the largest U.S. corporations. For fiscal 2021, it had a total revenue of $46.4 billion. Bristol Myers Squibb manufactures prescription pharmaceuticals and biologics in several therapeutic areas, including cancer, HIV/AIDS, cardiovascular disease, diabetes, hepatitis, rheumatoid arthritis, and psychiatric disorders. BMS's primary research and development (R&D) sites are located in Lawrence, New Jersey (formerly Squibb, near Princeton), Summit, New Jersey, formerly HQ of Celgene, New Brunswick, New Jersey, Redwood City, California, and Seville in Spain, with other sites in Devens and Cambridge, Massachusetts, East Syracuse, New York, Braine-l'Alleud, Belgium, Tokyo, Japan, Bangalore, India, and Wirral, United Kingdom. BMS previously had an R ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
DuPont
DuPont de Nemours, Inc., commonly shortened to DuPont, is an American multinational chemical company first formed in 1802 by French-American chemist and industrialist Éleuthère Irénée du Pont de Nemours. The company played a major role in the development of Delaware and first arose as a major supplier of gunpowder. DuPont developed many polymers such as Vespel, neoprene, nylon, Corian, Teflon, Mylar, Kapton, Kevlar, Zemdrain, M5 fiber, Nomex, Tyvek, Sorona, Corfam and Lycra in the 20th century, and its scientists developed many chemicals, most notably Freon (chlorofluorocarbons), for the refrigerant industry. It also developed synthetic pigments and paints including ChromaFlair. In 2015, DuPont and the Dow Chemical Company agreed to a reorganization plan in which the two companies would merge and split into three. As a merged entity, DuPont simultaneously acquired Dow and renamed itself to DowDuPont on August 31, 2017, and after 18 months spin off the merged en ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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