TAS-108

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 the death of cancer cells apoptosis and thus was particularly well suited to be an anti-cancer drug. As of August 2010, the drug had been through five Phase I and two Phase II studies, and Phase III studies are being planned.

References

References

1. (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.
2. (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.
3. "Alumni Hall of Fame 2004: Masato Tanabe". [[SRI International]].
4. (2006). "A Heritage of Innovation: SRI's First Half Century". SRI International.
5. "SRI International to Advance Clinical Development of TAS-108, a Late-Stage Breast Cancer Drug". [[SRI International]].
6. (January 2005). "TAS-108: a novel steroidal antiestrogen". Clinical Cancer Research.