UCL Cancer Institute and University College Hospital, Department of Oncology, London, UK.
Expert Opin Biol Ther. 2010 Jan;10(1):105-11. doi: 10.1517/14712590903468677.
Glucarpidase (Carboxypeptidase G2 or Voraxaze) is a recombinant enzyme that belongs to the class of carboxypeptidases which are naturally occurring enzymes. Glucarpidase is able to cleave methotrexate (MTX) into non-cytotoxic metabolites that may help prevent or minimise subsequent toxicities such as renal failure. In this review, the authors outline the discovery of the carboxypeptidase class of enzymes and the pre-clinical data demonstrating that glucarpidase is highly effective in the rapid reduction of MTX levels. The authors summarise the compassionate use studies of glucarpidase for patients with nephrotoxicity following high dose MTX or with very high post-MTX levels and the current developmental status of the drug. In conclusion, glucarpidase has been shown to be very useful in emergency situations following administration of high-dose MTX. Glucarpidase has yet to receive marketing approval in the EU or USA, and we await further data from In conclusion, glucarpidase Phase I/II studies assessing routine prophylactic administration following high-dose methotrexate.
葡糖醛酸酶（羧肽酶 G2 或 Voraxaze）是一种重组酶，属于羧肽酶类，是天然存在的酶。葡糖醛酸酶能够将甲氨蝶呤（MTX）切割成非细胞毒性代谢物，这可能有助于预防或最小化随后的毒性，如肾衰竭。在这篇综述中，作者概述了羧肽酶类酶的发现以及临床前数据，证明葡糖醛酸酶在快速降低 MTX 水平方面非常有效。作者总结了葡糖醛酸酶在高剂量 MTX 治疗后发生肾毒性或 MTX 水平非常高的患者中的同情使用研究以及该药物的当前开发状况。总之，葡糖醛酸酶在高剂量 MTX 给药后出现紧急情况时非常有用。葡糖醛酸酶尚未在欧盟或美国获得上市批准，我们期待更多来自高剂量 MTX 后常规预防给药的葡糖醛酸酶 I/II 期研究的数据。
