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¹³¹I-利妥昔单抗在一名CD20阳性非霍奇金淋巴瘤患者体内的药代动力学:放射性碘化对利妥昔单抗生物学特性影响的评估

The pharmacokinetics of ¹³¹I-rituximab in a patient with CD20 positive non-Hodgkin Lymphoma: evaluation of the effect of radioiodination on the biological properties of rituximab.

作者信息

Tran L, Baars J W, de Boer J P, Hoefnagel C A, Beijnen J H, Huitema A D R

机构信息

Department of Pharmacy and Pharmacology, The Netherlands Cancer Institute/Slotervaart Hospital, Amsterdam, The Netherlands.

出版信息

Hum Antibodies. 2011;20(1-2):37-40. doi: 10.3233/hab20110240.

Abstract

PURPOSE

To report the pharmacokinetics of ¹³¹I-rituximab a patient with a CD20 positive non-Hodgkin Lymphoma who has received ¹³¹I-rituximab as consolidation treatment after remission induction and to evaluate the effect of radioiodination on the biological properties of rituximab.

RESULTS

The patient was a 65-year-old male with a relapsed CD20 positive follicular non-Hodgkin Lymphoma. After induction therapy the patient was in partial remission. Following administration of a diagnostic dose of 185 MBq ¹³¹I-rituximab, remaining lesions were identified on the wholebody scans. The patient then received a therapeutic dose of 1000 MBq ¹³¹I-rituximab. The uptake by the tumor in the right axilla was 0.17-0.21% of the injected dose. The calculated biological half-life of ¹³¹I-rituximab was 684 hrs. This biological half-life corresponded well with the half-life of unlabeled rituximab which was approximately 720 hrs.

DISCUSSION AND CONCLUSION

Even though radioiodination of rituximab results in a reduced binding capacity, whole body scans demonstrated localization of ¹³¹I-rituximab in the tumor area. This observation supports the specific targeting of ¹³¹I-rituximab. The half-life of ¹³¹I-rituximab corresponded to the half-life of unlabeled rituximab. Hence, the pharmacokinetics of ¹³¹ I-rituximab was not relevantly affected by the radioiodination process.

摘要

目的

报告131I-利妥昔单抗在一名CD20阳性非霍奇金淋巴瘤患者中的药代动力学,该患者在缓解诱导后接受131I-利妥昔单抗作为巩固治疗,并评估放射性碘化对利妥昔单抗生物学特性的影响。

结果

该患者为65岁男性,患有复发性CD20阳性滤泡性非霍奇金淋巴瘤。诱导治疗后患者处于部分缓解状态。给予诊断剂量的185 MBq 131I-利妥昔单抗后,全身扫描发现了残留病灶。然后患者接受了1000 MBq 131I-利妥昔单抗的治疗剂量。右腋窝肿瘤的摄取量为注射剂量的0.17-0.21%。计算得出131I-利妥昔单抗的生物半衰期为684小时。这个生物半衰期与未标记利妥昔单抗的半衰期(约720小时)非常吻合。

讨论与结论

尽管利妥昔单抗的放射性碘化导致结合能力降低,但全身扫描显示131I-利妥昔单抗在肿瘤区域有定位。这一观察结果支持了131I-利妥昔单抗的特异性靶向作用。131I-利妥昔单抗的半衰期与未标记利妥昔单抗的半衰期相对应。因此,放射性碘化过程对131I-利妥昔单抗的药代动力学没有显著影响。

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