Alimta (Premetrexed) PEG劑型開發 !!

博謙生技獲准進駐南部科學工業園區投資  2015-01-15 16:01:44　勁報記者羅蔚舟／台北報導  科技部於104年1月15日部召開科學工業園區審議委員會第10次會議，會中通過博謙生技股份有限公司申請進駐南部科學工業園區。據南部科學工業園區管理局指出，科學工業園區審議委員會第10次會議核准博謙生技股份有限公司投資新台幣0.6億元，該公司主要是研發聚乙二醇奈米複合微胞衍生之新藥及其相關針劑。據南部科學工業園區管理局指出，南部科學工業園區管理局轄下台南園區及高雄園區截至104年1月15日統計，核准進駐園區廠商已有368家，其中有197家有效核准廠商。此次通過南科管理局所提1件投資申請案博謙生技股份有限公司，投資金額新台幣0.6億元，申請在南部科學工業園區台南園區研發、設計、生產及銷售：聚乙二醇奈米複合微胞衍生之新藥及其相關針劑。據南部科學工業園區管理局指出，博謙生技擬設計開發之聚乙二醇奈米複合微胞衍生之新藥及其相關針劑等產品，初期擬發展之肺癌用藥(Premetrexed Disodium)相較原廠 (Eli Lilly)藥，可緩減此類抗癌藥物對於骨髓與胃腸之毒性及副作用，具較佳之治療指數，本本案產品之發展可強化國內生技產業自主研發的能力，提高國內生技醫療器材產業之國際競爭力，對帶動南科生技產業聚落之發展與成形當有具體貢獻。

Water-soluble poly(ethylene glycol) prodrug of pemetrexed: Synthesis, characterization, and preliminary cytotoxicity  Journal of Applied Polymer Science Volume 111, Issue 1, pages 444–451, 5 January 2009  Pemetrexed is a novel antifolate of antimetabolite with multiple enzyme targets involved in both pyrimidine and purine synthesis. It has entered the clinical usage due to favorable profiles especially in the cancer treatment of mesothelioma and non–small-cell lung carcinoma. But it presents numerous challenges associated with poor water solubility and unstability in its original form of glutamic acid. The aim of this study is to solubilize pemetrexed by designing and synthesizing its aqueous-soluble prodrug using high aqueous-soluble polymeric carrier poly(ethylene glycol) (PEG). A new type of soluble pemetrexed prodrug was synthesized with dihydroxyl PEG and a single amino acid linkage, and was extensively characterized using 1H-NMR, 13C-NMR, Fourier-transform infrared, and matrix-assisted laser desorption time of flight mass spectrometry. In addition, the prodrugs were evaluated for the drug loading capability, the aqueous solubility, and the preliminary in vitro cytotoxicity. The results indicate that the new PEGylated pemetrexed conjugates possess enhanced water solubility and stability, and provide another feasible choice of the pharmaceutical form of pemetrexed in the clinical application. © 2008 Wiley Periodicals, Inc. J Appl Polym Sci, 2009