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1.前言本文报道已经上市或尚在继续临床阶段的药物研究的新进展。 2.抗肿瘤剂 2.1.烷化剂亚硝基脲如洛莫司汀和卡莫司汀在六十年代已进入临床,两药对实体癌、急性白血病和淋巴瘤疗效很好,但是亲脂性很强。牛磺莫司汀(Tauromustin,1,TCNU)是天然氨基酸——牛磺酸的氯乙基亚硝基脲衍生物,它提供了一种新的水溶性化合物。1对各种体外培养的人体肿瘤(如BE和HT-29结肠癌)具有与洛莫司汀和卡莫司汀相似的活性。在体内试验中,1对Walker256肉瘤有效,其治疗指数比洛莫司汀和卡莫司
1. Introduction This article reports new advances in drug research that are either already on the market or are still in clinical phase. 2. Antitumor agents 2.1. Alkylation agents Nitrosoureas such as lomustine and carmustine have entered clinical practice in the 1960s and have shown efficacy in solid cancers, acute leukemias and lymphomas, but lipophilic Very strong. Tauromustin (1, TCNU) is a chloroethyl nitrosourea derivative of the natural amino acid taurine, which provides a new water-soluble compound. 1 has similar activity to lomustine and carmustine for various in vitro cultured human tumors such as BE and HT-29 colon cancer. In vivo tests, 1 pair of Walker256 sarcoma effective treatment index bilomustine and carmust