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.[2][3]
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| Other names | 17β-[2-[4-[(diethylamino)methyl]-2-methoxyphenoxy]ethyl]-7α-methylestra-1,3,5(10)-trien-3-ol; 17β-[2-[4-[(diethylamino)methyl]-2-methoxyphenoxy]ethyl]-7α-methylestradiol |
| Routes of administration | By mouth[1] |
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| Formula | C33H47NO3 |
| Molar mass | 505.743 g·mol−1 |
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Development
editMasato 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".[4] 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.[4]
The first of those, SR-16234, also inhibited the growth of blood vessels angiogenesis and accelerated the death of cancer cells apoptosis and thus was particularly well suited to be an anti-cancer drug.[4] As of August 2010, the drug had been through five Phase I and two Phase II studies,[5] and Phase III studies are being planned.[6]
See also
editReferences
edit- ^ Yamamoto Y, Shibata J, Yonekura K, Sato K, Hashimoto A, Aoyagi Y, et al. (January 2005). "TAS-108, a novel oral steroidal antiestrogenic agent, is a pure antagonist on estrogen receptor alpha and a partial agonist on estrogen receptor beta with low uterotrophic effect". Clinical Cancer Research. 11 (1): 315–322. doi:10.1158/1078-0432.315.11.1. PMID 15671561.
- ^ Yamamoto Y, Wada O, Takada I, Yogiashi Y, Shibata J, Yanagisawa J, et al. (December 2003). "Both N- and C-terminal transactivation functions of DNA-bound ERalpha are blocked by a novel synthetic estrogen ligand". Biochemical and Biophysical Research Communications. 312 (3): 656–662. doi:10.1016/j.bbrc.2003.10.178. PMID 14680815.
- ^ "Alumni Hall of Fame 2004: Masato Tanabe". SRI International. Retrieved 2013-02-10.
- ^ a b c Nielson D (2006). A Heritage of Innovation: SRI's First Half Century. Menlo Park, California: SRI International. pp. 10–15. ISBN 978-0-9745208-1-0.
- ^ "SRI International to Advance Clinical Development of TAS-108, a Late-Stage Breast Cancer Drug" (Press release). SRI International. Retrieved 2013-02-24.
- ^ Buzdar AU (January 2005). "TAS-108: a novel steroidal antiestrogen". Clinical Cancer Research. 11 (2 Pt 2): 906s–908s. doi:10.1158/1078-0432.906s.11.2. PMID 15701885.
External links
edit- SR-16234 (TAS-108) - AdisInsight
- TS 108 at the U.S. National Library of Medicine Medical Subject Headings (MeSH)