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Wednesday, November 14, 2012

大鹏药品 Taiho Pharmaceutical: TS-1 + TAS-114 !!!


Taiho Pharmaceutical Unveils Data on Eight Novel Anticancer Compounds in Bid to Become a New Global Leader in Oncology BusinessWire · Nov. 6, 2012 | Last Updated: Nov. 6, 2012 3:00 AM ET 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.

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.

大鹏药品工业株式会社发布八种新型抗癌化合物数据 发布时间:2012-11-14 来源:药品资讯网信息中心大鹏药品工业株式会社(Taiho PHarmaceutical Co., Ltd.,总部:东京,总裁:小林将之)是首个口服给药的氟尿嘧啶(FU)化疗药(TS-1/S-1)的开发者,该公司正在呈报八种新型肿瘤科化合物的早期数据,包括可能是同类别中首个品种的药物。20121169日在爱尔兰都柏林召开的第24EORTC-NCI-AACR分子靶向和癌症治疗学研讨会期间呈报的数据凸显了大鹏在世界范围内的如下坚定承诺,即改善支持性抗代谢抗癌药以及开发用于单药治疗或联合治疗的新型分子靶向药物。 大鹏药品工业株式会社总裁小林将之说:"正在呈报的数据表明,大鹏有能力开发新型分子靶向药物以及下一代细胞毒药物,同时凸显了我们对开发有望改善癌症患者治疗选择的原研抗癌药的一贯承诺。我们围绕创新研究和临床开发的策略加强了本公司在今后十年跻身十大肿瘤产品公司的追求。" 快速进步 大鹏在50年前确立了创新产品开发的基础,该公司致力于高效、有效、快速产出成果。这一承诺的最佳体现就是抗肿瘤药物TAS-102近期通过了临床前和临床开发EORTC-NCI-AACR研讨会上呈报的临床前结果显示,在公认的乳腺癌动物模型中,TAS-102治疗后,FDT整合到DNA中,肿瘤生长因此显著延缓,而结肠癌模型中则显示有生存收益。 日本开展的TAS-102 II期研究显示,转移性结直肠癌患者的总生存出现改善。根据这项II期研究令人鼓舞的结果,大鹏完成了所需的西方I期研究,以便在15个月内启动一项全球III期研究。

探索新的治疗选择– 单药治疗和联合治疗 大鹏已确立了一个无缝连接的研究网络,包括筑波研究中心、德岛研究中心、大鹏临床开发中心和大鹏药品美国分公司。该整合网络为无数药物的发现和开发提供支持。通过科学引领开发道路,然后运用现代技术和创新来达成其目标,该公司的研究达到了药物发现的最高标准。根植于这种研究的原研药正在接受检验,以期成为有望用于单药治疗的产品,或成为与现有药物联合、从而有望提升现有抗癌药安全性和有效性的产品。 大鹏在EORTC-NCI-AACR研讨会上呈报的原研药临床前主要结果包括: ·TAS-114dUTPase(脱氧尿苷5'-三磷酸核苷酸水解酶)和DPD(二氢嘧啶脱氢酶)双重抑制剂这一类别药物中的首个品种,三项临床前数据集评估了该药与基于卡培他滨的化疗药以及与S-1的联合用药,结果显示该药能影响关键通路的调节、改善FU的体外细胞毒性。进行中的I期研究正在探索TAS-114与卡培他滨的联合用药,另有一些研究正在探寻该化合物与S-1联合用药。TAS-114正在开发用于治疗实体瘤。 ·TAS-115是肝细胞和血管内皮生长因子受体的双重抑制剂,可抑制前列腺癌细胞增生和骨吸收后的成骨细胞分化。此外,肝细胞生长因子受体基因表达标签与肝细胞生长因子的组合可能是TAS-115的一种有前景的治疗生物标记。大鹏正在开发TAS-115用于治疗实体瘤,一项I期研究正在进行中。 ·TAS-116是一种HSP90抑制剂,具有高肿瘤/视网膜浓度比,可能在减少眼毒性方面至关重要,眼毒性是此类药物已知的一种类别效应。 ·TAS-117是一种AKT抑制剂,在体外和体内模型中,与紫杉烷类联合用药时可提升凋亡诱导、显示协同的抗肿瘤活性。 ·TAS-2104是一种高度选择性的Aurora A抑制剂,可提升紫杉烷类的抗增生活性,这提示,该化合物适用于在临床测试中与紫杉烷类联合用药。 ·TAS-2913是一种突变子选择性表皮生长因子受体抑制剂,体外研究提示,它可能是表皮生长因子受体和酪氨酸激酶抑制剂难治的非小细胞肺癌的一种新的治疗选择。 ·TAS-2985是成纤维细胞生长因子受体(FGFR)的一种小分子抑制剂,在动物异体移植物模型中显示对肿瘤生长有强大的抑制作用,而人类肿瘤异体移植物模型中的药效动力学研究提示,该化合物可选择性抑制FGFR的活性。此外,在体外 ,该分子可通过依赖FGFR的方式选择性抑制人类癌细胞株的生长。

 

 

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