パクリタキセル

解説パクリタキセル,針状晶．分解点213～216 ℃．[α]20D－49°(メタノール)．水に難溶性のため，ドラッグデリバリーに工夫がいる．細胞の微小管に結合し，その動的な構造変化を抑え，最終的に細胞分裂を阻害する．森北出版「化学辞典（第2版）

用途タキソイド系化合物です。β - チューブリンへ結合して微小管を安定化さ せ、微小管ダイナミクスを抑制することによ り有糸分裂阻害作用を示します。

用途パクリタキセルは肺がん、卵巣がん、乳がん、頭頸部がん、進行性カポジ肉腫患者の治療に用いられている。また再狭窄の予防にも用いられている。 パクリタキセルは微小管を安定化させることで微小管のダイナミクスを抑制し、その結果正常な細胞分裂の進行を妨げる。ドセタキセルと共に医薬品分類のタキサン類を構成する。フロリダ州立大学のロバート?ホルトンによって初めて全合成された。

説明Paclitaxel, a natural product isolated from the bark of the Pacific yew, is effective in treating refractory metastatic ovarian cancer. Unlike any other antineoplastic agents, paclitaxel appears to have several possible mechanisms of action, including an antimicrotubule action through the promotion of tubulin polymerization and stabilization of microtubules, thereby, halting mitosis and promoting cell death. The supply of paclitaxel is limited by its low natural abundance and currently it is being manufactured by a semi-synthetic route from deacetylbaccatin Ⅲ that is isolated from the needles of the yew tree. Recent completion of two total syntheses of taxol conquered the structural complexity of the title compound and may be useful in obtaining certain closely related analogs, some of which have been found to have antitumor activity. Paclitaxel has potential uses in the treatment of metastatic breast cancer, lung cancer, head and neck cancer, and malignant melanoma.

来歴Paclitaxel, initially named taxol, is a naturally occurring diterpenoid compound extracted from the Pacific yew tree, Taxus brevifolia. Paclitaxel was discovered by National Cancer Institute (NCI) in 1960s. Scientists were conducting screenings of plant extracts in search of potential anticancer agents when they discovered the distinctive cytotoxic properties of paclitaxel against cancer cells. In October of 1995, China became the second country with formal production of paclitaxel and its injection in the world.Paclitaxel/Taxol is on the World Health Organization’s Model List of Essential Medicines, and was at one point the best-selling cancer drug ever manufactured, with annual sales of $1.6 billion in 2000.

使用Paclitaxel is an antineoplastic that used to treat patients with lung, ovarian, breast cancer, head and neck cancer, and advanc ed forms of Kaposi's sarcoma. Paclitaxel is a mitotic inhibitor used in cancer chemotherapy. It is also used in the study of structure and function of microtubles into tubulin.

Paclitaxel (commercial name, Taxol) a complex diterpene alkaloid isnaturally obtained from Taxus species (family Taxaceae). Paclitaxel has been provedas highly effective in the treatment of various types of cancers, since it acts as amicrotubule-stabilizing agent to protect against disassembly. Paclitaxel was developed by the National Cancer Institute, USA, as a drug for cancer therapy andused for the treatment of refractory ovarian cancer, metastatic breast and lung cancer,and Kaposi’s sarcoma (Srivastava et al. 2005). The natural source of paclitaxelis the bark of several Taxus species; however, the cost of extraction is very highsince the concentration of paclitaxel accumulation is very low (0.02% of dry weight)and also entails the destruction of natural resources (Cusido et al. 2014). Eventhough, paclitaxel can be chemically synthesized, but this process is not commerciallyviable. Plant cell cultures have been developed for the production of paclitaxelby Phyton Biotech in 1995, and in 2004 the FDA has approved the use of plantculture supply of paclitaxel/Taxol (Leone and Roberts 2013).