Fiebrich-Westra H B, Visser O, Francken A B, Smolders E J
Department of Hematology and Medical Oncology, Isala Hospital, Zwolle, The Netherlands.
Department of Surgical Oncology, Isala Hospital, Zwolle, The Netherlands.
Cancer Chemother Pharmacol. 2025 Mar 20;95(1):45. doi: 10.1007/s00280-025-04766-9.
To explore the possibility of treating patients with alternative imatinib formulations.
Two patients were treated with different enteral en rectal imatinib formulations. During treatment plasma concentrations where measured to assure adequate exposure.
The first patient received imatinib suspension through the duodenum tube. With a dose of 400 mg BID the patient had an imatinib plasma concentration of 750 µg/L. After increasing the dose to 600 mg BID the imatinib plasma concentration was 1500 µg/L (target GIST treatment > 1100 µg/L). Rectal administration of the tablet did not lead to sufficient plasma concentrations. The second had adequate exposure of imatinib both when the suspension was taken orally and through the tube (target CML treatment are > 1000 µg/L).
For patients able to swallow liquids, we prefer the suspended imatinib tablets (comparable to drug label). If patients have a duodenum tube the use of a suspension base with pulverized tablets could be an alternative. Based on the extremely low exposure found in case 1, we do not recommend rectal administration of tablets. We recommend the monitor plasma concentrations when off label dosing forms are used.
探讨使用伊马替尼替代剂型治疗患者的可能性。
两名患者接受了不同的肠内和直肠伊马替尼剂型治疗。治疗期间测量血浆浓度以确保有足够的药物暴露。
第一名患者通过十二指肠管接受伊马替尼混悬液。剂量为400mg，每日两次时，患者的伊马替尼血浆浓度为750μg/L。将剂量增加至600mg，每日两次后，伊马替尼血浆浓度为1500μg/L（胃肠道间质瘤治疗目标浓度>1100μg/L）。直肠给药该片剂未导致足够的血浆浓度。第二名患者口服混悬液和通过导管给药时伊马替尼均有足够的药物暴露（慢性粒细胞白血病治疗目标浓度>1000μg/L）。
对于能够吞咽液体的患者，我们更倾向于使用伊马替尼混悬片（与药品标签相当）。如果患者有十二指肠管，使用粉碎片剂的混悬液基质可能是一种替代方法。基于病例1中发现的极低药物暴露，我们不建议直肠给药该片剂。我们建议在使用非标签剂型时监测血浆浓度。
