Raltitrexed药代动力学特性和临床应用

THE PHARMACOKINETICS AND CLINICAL USES OF RALTITREXED

altitrexed(ZD 1694 )是一种喹唑啉叶酸盐类似物 ,通过对胸苷合酶的专一抑制产生抗肿瘤作用。体外研究显示 ,raltitrexed主动运输进入细胞内很快被大量代谢成一系列聚合谷氨酸 ,这些代谢物比母药发挥更强的酶抑制作用 。

Raltitrexed(ZD 1694)is a quinazoline based folate analogue exerts its cytotoxic activity by specific inhibition of thymidylate synthase. In vitro studies show that raltitrexed is actively transported into cells and is then rapidly and extensively metabolized to a series of polyglutamates.These metabolites are significantly more potent inhibitors of thylmidylate synthase than the parent drug and are retained intracellularly,producing prolonged cytotoxic effects without the need for continuous drug exposure.