Public Release:  Taiho Pharmaceutical unveils data on 8 novel anticancer compounds

Data will showcase potentially first- or best-in-class compounds

GCI Health

DUBLIN, November 6, 2012 - Taiho Pharmaceutical Co., Ltd. (HQ: Tokyo, President: Masayuki Kobayashi), the developer of the first orally available fluorouracil (FU) Chemotherapeutic treatment (TS-1/S-1), is presenting early stage data for eight novel oncology compounds, including potential first-in-class therapies. The data being presented during the 24th EORTC-NCI-AACR Symposium on Molecular Targets and Cancer Therapeutics from November 6 - 9, 2012 in Dublin, Ireland underscore Taiho's steadfast commitment to improving cornerstone anti-metabolic cancer agents and developing novel molecular targeted therapies that can be used alone or in combination worldwide.

"The data being presented demonstrate Taiho's ability to develop novel molecular targeted agents as well as next generation cytotoxic therapies, and underscore our continued commitment to developing investigational anticancer drugs that have the potential to improve treatment options available to cancer patients," said Masayuki Kobayashi, Taiho Pharmaceutical's president. "Our strategy surrounding innovative research and clinical development reinforces Taiho's pursuit of becoming a top-ten oncology company in the next decade."

Rapid Advancement

Taiho established a foundation of innovative product development 50 years ago, and the Company is committed to achieving efficiencies to effectively yield rapid results. This commitment is best demonstrated by the recent movement of the TAS-102 antitumor agent through preclinical and clinical development. Preclinical results being presented at the EORTC-NCI-AACR Symposium show that TAS-102 exhibited marked tumor growth delay after drug treatment due to FTD incorporation into DNA when evaluated using a well-recognized animal model for breast cancer, and a survival benefit in a colon cancer model.

A Phase II study of TAS-102, conducted in Japan, demonstrated an improvement in overall survival of patients with metastatic colorectal cancer. Taiho took the encouraging results from this Phase II study and completed the required western Phase I studies to initiate a global Phase III program within a 15 month period.

Exploring New Treatment Options - Alone and in Combination

Taiho has established a seamlessly connected research network, consisting of Tsukuba Research Center, Tokushima Research Center, the Taiho Clinical Development Center, and Taiho Pharma USA. The integrated network supports the discovery and development of numerous treatments. The Company's research achieves the highest standards of drug discovery by letting science guide its development path, and then applying modern technology and innovation to achieve that end. Investigational drugs stemming from this research are being examined as potential stand-alone products, or ones that can be used in combination with existing therapies to potentially enhance the safety and efficacy profile of current cancer options.

Highlights of the preclinical results of Taiho's investigational drugs being presented at the EORTC-NCI-AACR Symposium include:

  • TAS-114, a first-in-class dUTPase (deoxyuridine 5'-triphosphate nucleotidehydrolase) and DPD (dihydropyrimidine dehydrogenase) dual inhibitor, was evaluated in three preclinical data sets in combination with a capecitabine-based chemotherapy as well as with S-1, and showed an impact on key pathway regulation and improvements in cytotoxicity of FU in vitro. Phase I studies are underway to explore the use of TAS-114 in combination with capecitabine, and separate studies examining the compound in combination with S-1. TAS-114 is being developed for potential use in treating solid tumors.
  • TAS-115, a dual inhibitor of hepatocyte and vascular endothelial growth factor receptors, suppressed prostate cancer cell proliferation and osteoclast differentiation following bone resportion. Additionally, the combination of hepatocyte growth factor receptor gene expression signature and hepatocyte growth factor may represent a promising therapeutic biomarker for TAS-115. Taiho is developing TAS-115 as a potential treatment for solid tumors, and a Phase I study is underway.
  • TAS-116, a HSP90 inhibitor, showed a high tumor/retina concentration ratio that may be important in minimizing ocular toxicity, which is a known class effect of this class of agents.
  • TAS-117, an AKT inhibitor, in combination with taxanes, enhanced apoptosis induction and exhibited synergistic antitumor activity in in vitro and in vivo models.
  • TAS-2104, a highly selective Aurora A inhibitor, was found to enhance anti-proliferation activity by taxanes, suggesting that the compound is suitable to test clinically in combination with taxanes.
  • TAS-2913, a mutant-selective epidermal growth factor receptor inhibitor, was studied in vitro and findings suggest it may represent a new therapeutic option in the treatment of non-small cell lung cancer that is resistant to epidermal growth factor receptors and tyrosine kinase inhibitors.
  • TAS-2985, a small molecule inhibitor of fibroblast growth factor receptors (FGFRs), demonstrated strong tumor growth inhibition in animal xenograft models, and a pharmacodynamic assay suggested the compound inhibits FGFR activity selectively in a human tumor xenograft model. Additionally, in vitro, the molecule selectively inhibited growth of human cancer cell lines in a FGFR-dependent manner.


About Taiho Pharmaceutical Co., Ltd.

Taiho Pharmaceutical, a subsidiary of Otsuka Holdings Co., Ltd., is an R&D-driven specialty pharma focusing on the three fields of oncology, allergies and immunology, and urology. Its corporate philosophy takes the form of a pledge: "We strive to improve human health and contribute to a society enriched by smiles." In the field of oncology in particular, Taiho Pharmaceutical is known as a leading company in Japan and around the world for developing evidence-based medicines for the treatment of cancer. In areas other than oncology, as well, the company creates quality products that effectively treat medical conditions and can help improve people's quality of life. Always putting customers first, Taiho Pharmaceutical also aims to offer over-the-counter medicinal products that support people's efforts to lead fulfilling and rewarding lives.

For more information about Taiho Pharmaceutical, please visit

About Otsuka Holdings Co., Ltd.

The Otsuka Group is a diversified healthcare group operating globally under the corporate philosophy "Otsuka-people creating new products for better health worldwide." The Otsuka Group has business operations in 24 countries and regions around the world. For more information, please visit the company's website at

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