TAS-108
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TAS-108
TAS-108, also known as SR-16234, is a drug discovered by Masato Tanabe and under development by SRI International and Taiho Pharmaceutical. It is a steroid hormone that has shown signs of treating and preventing breast cancer, even in patients where tamoxifen has failed. Development Masato Tanabe's team at SRI has focused on the development of steroid hormones. A compound discovered in a previous SRI contract from the National Institutes of Health showed potential – it acted like "anti-estrogen" in the breasts and uterus but like normal estrogen elsewhere in the body, and was more "tissue-selective". A contract was proposed to Taiho Pharmaceutical in July 1996, and within six years and slightly under $3 million (an unusually short amount of time), two new drugs were discovered and tested on people (particularly people for which tamoxifen has failed): SR-16234 and SR-16287. The first of those, SR-16234, also inhibited the growth of blood vessels angiogenesis and accelerated th ...
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Masato Tanabe
Masato "Mas" Tanabe was a drug researcher at SRI International, where he spent 45 years studying steroid hormones, which are instrumental in combatting breast cancer and prostate cancer. Education Tanabe graduated from the University of San Francisco in 1947 with a degree in chemistry; his thesis was "Studies in the hydroaromatic series". Tanabe would go on to study under professor William G. Dauben at the University of California, Berkeley. Career Tanabe was program manager of Steroid Chemistry group, then director of SRI's Bio-Organic Chemistry Laboratory for much of his career, and later the director of SRI's Pharmaceutical Chemistry group. In 1967, he was on a team that discovered Eschenmoser-Tanabe fragmentation. Much of the work was sponsored by the National Institute of Health and Schering Plough, the latter of which has at least eight patents and 30 journal articles via work sponsored at SRI. Other notable accomplishments include the use of stable isotopes to study metabol ...
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Taiho Pharmaceutical
is a Japanese pharmaceutical company, and a subsidiary of Otsuka Holdings, which focuses on developing cancer treatments. Taiho, headquartered in Tokyo, Japan, is an R&D-driven specialty pharma focusing on the three fields of oncology, allergies and immunology, and urology. Being Japan's second-largest pharmaceutical company by prescription oral oncology sales, Taiho covers oncology related therapeutic areas including stomach cancer, colorectal cancer, pancreatic cancer, and breast cancer. Taiho also engages in research and development, manufacturing, and the marketing of pharmaceutical products. The company is principally active in the prescription market, but also develops over-the-counter medication, and is a full member of the Japan Pharmaceutical Manufacturers Association (JPMA). As of March 2013, Taiho had over 2,500 employees worldwide. The company achieved approximately US$1.3 billion in revenue during the 2012 fiscal year. History 1963 — Taiho Pharmaceutical Co. ...
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SRI International
SRI International (SRI) is an American nonprofit scientific research institute and organization headquartered in Menlo Park, California. The trustees of Stanford University established SRI in 1946 as a center of innovation to support economic development in the region. The organization was founded as the Stanford Research Institute. SRI formally separated from Stanford University in 1970 and became known as SRI International in 1977. SRI performs client-sponsored research and development for government agencies, commercial businesses, and private foundations. It also licenses its technologies, forms strategic partnerships, sells products, and creates spin-off companies. SRI's headquarters are located near the Stanford University campus. SRI's annual revenue in 2014 was approximately $540 million, which tripled from 1998 under the leadership of Curtis Carlson. In 1998, the organization was on the verge of bankruptcy when Carlson took over as CEO. Over the next sixteen years wit ...
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ICI-164384
ICI-164384, also known as ''N''-''n''-butyl-''N''-methyl-11-(3,17β-dihydroxyestra-1,3,5(10)-trien-7α-yl)undecanamide, is a steroidal antiestrogen and a synthetic derivative of estradiol which is closely related to fulvestrant and was never marketed. It is a silent antagonist of the estrogen receptor (ER) with no intrinsic estrogenic activity and hence is a pure antiestrogen, unlike selective estrogen receptor modulators (SERMs) like tamoxifen. The drug was under development by AstraZeneca for the treatment of breast cancer but was discontinued in favor of fulvestrant, which is very similar to ICI-164384 but is more potent in comparison. See also * Cytestrol acetate * Ethamoxytriphetol * TAS-108 TAS-108, also known as SR-16234, is a drug discovered by Masato Tanabe and under development by SRI International and Taiho Pharmaceutical. It is a steroid hormone that has shown signs of treating and preventing breast cancer, even in patients w ... References External links ICI-1 ...
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Steroid Hormone
A steroid hormone is a steroid that acts as a hormone. Steroid hormones can be grouped into two classes: corticosteroids (typically made in the adrenal cortex, hence ''cortico-'') and sex steroids (typically made in the gonads or placenta). Within those two classes are five types according to the receptors to which they bind: glucocorticoids and mineralocorticoids (both corticosteroids) and androgens, estrogens, and progestogens (sex steroids). Vitamin D derivatives are a sixth closely related hormone system with homologous receptors. They have some of the characteristics of true steroids as receptor ligands. Steroid hormones help control metabolism, inflammation, immune functions, salt and water balance, development of sexual characteristics, and the ability to withstand injury and illness. The term steroid describes both hormones produced by the body and artificially produced medications that duplicate the action for the naturally occurring steroids. Synthesis The nat ...
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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 these ...
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Tamoxifen
Tamoxifen, sold under the brand name Nolvadex among others, is a selective estrogen receptor modulator used to prevent breast cancer in women and treat breast cancer in women and men. It is also being studied for other types of cancer. It has been used for Albright syndrome. Tamoxifen is typically taken daily by mouth for five years for breast cancer. Serious side effects include a small increased risk of uterine cancer, stroke, vision problems, and pulmonary embolism. Common side effects include irregular periods, weight loss, and hot flashes. It may cause harm to the baby if taken during pregnancy or breastfeeding. It is a selective estrogen-receptor modulator (SERM) and works by decreasing the growth of breast cancer cells. It is a member of the triphenylethylene group of compounds. Tamoxifen was initially made in 1962, by chemist Dora Richardson. It is on the World Health Organization's List of Essential Medicines. Tamoxifen is available as a generic medication. In 202 ...
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National Institutes Of Health
The National Institutes of Health, commonly referred to as NIH (with each letter pronounced individually), is the primary agency of the United States government responsible for biomedical and public health research. It was founded in the late 1880s and is now part of the United States Department of Health and Human Services. The majority of NIH facilities are located in Bethesda, Maryland, and other nearby suburbs of the Washington metropolitan area, with other primary facilities in the Research Triangle Park in North Carolina and smaller satellite facilities located around the United States. The NIH conducts its own scientific research through the NIH Intramural Research Program (IRP) and provides major biomedical research funding to non-NIH research facilities through its Extramural Research Program. , the IRP had 1,200 principal investigators and more than 4,000 postdoctoral fellows in basic, translational, and clinical research, being the largest biomedical research instit ...
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Menlo Park, California
Menlo Park is a city at the eastern edge of San Mateo County within the San Francisco Bay Area of California in the United States. It is bordered by San Francisco Bay on the north and east; East Palo Alto, Palo Alto, and Stanford to the south; and Atherton, North Fair Oaks, and Redwood City to the west. It is one of the most educated cities in California and the United States; nearly 70% of residents over 25 have earned a bachelor's degree or higher. It had 33,780 residents at the 2020 United States Census. It is home to the corporate headquarters of Meta, and is where Google, Roblox Corporation and Round Table Pizza were founded. Its train station holds the record as the oldest continually operating train station in California. Toponym "Menlo" is derived from Menlo (the anglicized spelling of Irish Gaelic 'Mionloch', meaning 'small lake') in County Galway, Ireland. The name "Menlo Park" was given to a ranch purchased by Irish settlers in honor of their home village in Ire ...
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Angiogenesis
Angiogenesis is the physiological process through which new blood vessels form from pre-existing vessels, formed in the earlier stage of vasculogenesis. Angiogenesis continues the growth of the vasculature by processes of sprouting and splitting. Vasculogenesis is the embryonic formation of endothelial cells from mesoderm cell precursors, and from neovascularization, although discussions are not always precise (especially in older texts). The first vessels in the developing embryo form through vasculogenesis, after which angiogenesis is responsible for most, if not all, blood vessel growth during development and in disease. Angiogenesis is a normal and vital process in growth and development, as well as in wound healing and in the formation of granulation tissue. However, it is also a fundamental step in the transition of tumors from a benign state to a malignant one, leading to the use of angiogenesis inhibitors in the treatment of cancer. The essential role of angiogenesis in ...
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Apoptosis
Apoptosis (from grc, ἀπόπτωσις, apóptōsis, 'falling off') is a form of programmed cell death that occurs in multicellular organisms. Biochemical events lead to characteristic cell changes (morphology) and death. These changes include blebbing, cell shrinkage, nuclear fragmentation, chromatin condensation, DNA fragmentation, and mRNA decay. The average adult human loses between 50 and 70 billion cells each day due to apoptosis. For an average human child between eight and fourteen years old, approximately twenty to thirty billion cells die per day. In contrast to necrosis, which is a form of traumatic cell death that results from acute cellular injury, apoptosis is a highly regulated and controlled process that confers advantages during an organism's life cycle. For example, the separation of fingers and toes in a developing human embryo occurs because cells between the digits undergo apoptosis. Unlike necrosis, apoptosis produces cell fragments called apoptotic ...
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Cytestrol Acetate
Cytestrol acetate is a steroidal antiestrogen and a cytostatic antineoplastic agent (i.e., chemotherapeutic) which was developed for the treatment of breast cancer but was never marketed.Smirnova Z. S, (2003). xperimental Study of Hormonocytostatics for Treatment of Breast Cancer.Российский биотерапевтический журнал, 2(2).Смирнова, З. С., Ржезников, В. М., Толкачев, В. Н., Борисова, Л. М., Киселева, М. П., Семейкин, А. В., ... & Шимановский, Н. Л. (2014). Противоопухолевое и антипролиферативное действие стероидного антиэстрогена цитэстрола ацетата на моделях гормонозависимых опухолей. Экспериментальная и клиническая фармакология, 77(10), 31-35. It is an 11α-hydroxylated derivative of ethinylestradiol in which a bis( ...
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