Müller H J, Löning L, Horn A, Schwabe D, Gunkel M, Schrappe M, von Schütz V, Henze G, Casimiro da Palma J, Ritter J, Pinheiro J P, Winkelhorst M, Boos J
Department of Paediatric Haematology/Oncology, University of Münster, Germany.
Br J Haematol. 2000 Aug;110(2):379-84. doi: 10.1046/j.1365-2141.2000.02187.x.
Hypersensitivity reactions are relevant adverse effects of asparaginase therapy. Therefore, children treated with native Escherichia coli asparaginase in induction therapy of acute lymphoblastic leukaemia (ALL) or non-Hodgkin's lymphoma (NHL) were switched to the pegylated enzyme for reinduction under drug monitoring. Seventy children, including four patients with allergic reactions during induction, were given one dose of Oncaspar 1,000 U/m2 intravenously. Activity was determined every third or fourth day until it dropped below the limit of quantification. In current reinduction protocols [ALL/NHL-Berlin-Frankfurt-Münster (BFM) 95 trials], four doses of 10,000 U/m2 E. coli asparaginase deplete asparagine for about 2-3 weeks, therefore activities of >/= 100 U/l up to day 14 and >/= 50 U/l up to day 21 were targeted. In 66 patients without an allergic reaction during induction, the mean activity was 606 +/- 313 U/l, 232 +/- 211 U/l and 44 +/- 50 U/l after 1, 2 and 3 weeks respectively. In 44/66 patients, activity was >/= 100 U/l after 14 d. A rapid decline in activity was seen in the remaining 22 patients, including 8/22 patients who showed no activity after 1 week. Toxicity was low and comparable to the native enzymes but, in contrast to about 30% of hypersensitivity reactions with conventional reinduction therapy, no allergic reaction was seen. Substituting 4 x 10,000 U/m2 asparaginase medac for one dose of 1,000 U/m2 Oncaspar was safe and well tolerated. Comparable pharmacokinetic treatment intensity was achieved in about two-thirds of patients.
超敏反应是天冬酰胺酶治疗的相关不良反应。因此,在急性淋巴细胞白血病(ALL)或非霍奇金淋巴瘤(NHL)诱导治疗中接受天然大肠杆菌天冬酰胺酶治疗的儿童,在药物监测下改用聚乙二醇化酶进行再诱导治疗。70名儿童,包括4名在诱导治疗期间出现过敏反应的患者,静脉注射一剂1000 U/m²的培门冬酶。每隔三天或四天测定一次活性,直至其降至定量限以下。在当前的再诱导方案[ALL/NHL-柏林-法兰克福-明斯特(BFM)95试验]中,四剂10000 U/m²的大肠杆菌天冬酰胺酶可使天冬酰胺消耗约2 - 3周,因此目标是在第14天活性≥100 U/L,在第21天活性≥50 U/L。在66名诱导治疗期间无过敏反应的患者中,1周、2周和3周后的平均活性分别为606±313 U/L、232±211 U/L和44±50 U/L。在44/66名患者中,14天后活性≥100 U/L。其余22名患者的活性迅速下降,其中8/22名患者在1周后无活性。毒性较低,与天然酶相当,但与传统再诱导治疗约30%的超敏反应不同,未观察到过敏反应。用一剂1000 U/m²的培门冬酶替代4×10000 U/m²天冬酰胺酶medac是安全且耐受性良好的。约三分之二的患者实现了相当的药代动力学治疗强度。