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PTK787/ZK 222584是一种血管内皮生长因子(VEGF)的小分子酪氨酸激酶受体抑制剂,在伴有髓样化生的骨髓纤维化中具有适度活性。

PTK787/ZK 222584, a small molecule tyrosine kinase receptor inhibitor of vascular endothelial growth factor (VEGF), has modest activity in myelofibrosis with myeloid metaplasia.

作者信息

Giles Francis J, List Alan F, Carroll Michael, Cortes Jorge E, Valickas Joyce, Chen Bee-Lian, Masson Eric, Jacques Christian, Laurent Dirk, Albitar Maher, Feldman Eric J, Roboz Gail J

机构信息

The University of Texas, M.D. Anderson Cancer Center, 1515 Holcombe Boulevard, Box 428, Houston, TX 77030, USA.

出版信息

Leuk Res. 2007 Jul;31(7):891-7. doi: 10.1016/j.leukres.2006.12.001.

DOI:10.1016/j.leukres.2006.12.001
PMID:17560285
Abstract

Angiogenesis is part of the pathophysiology of myelofibrosis with myeloid metaplasia (MMM). PTK787/ZK 222584 (PTK/ZK) is a novel inhibitor of vascular endothelial growth factor receptors. Twenty-nine patients with MMM received a continuous dosing schedule of PTK/ZK doses of 500 or 750 mg twice daily (BID). Transient potentially PTK/ZK related mild nausea, vomiting, dizziness, fatigue, thrombocytopenia, or anorexia occurred in 15% of patients. Dose limiting toxicities of dyspepsia, proteinurea, and/or mucositis were observed in patients treated with 750 mg BID. One (3%) and five (17%) patients achieved complete remission and clinical improvement, respectively. PTK/ZK has modest activity in patients with MMM.

摘要

血管生成是伴有髓外化生的骨髓纤维化(MMM)病理生理学的一部分。PTK787/ZK 222584(PTK/ZK)是一种新型血管内皮生长因子受体抑制剂。29例MMM患者接受了PTK/ZK每日两次(BID)、剂量为500或750 mg的持续给药方案。15%的患者出现了短暂的、可能与PTK/ZK相关的轻度恶心、呕吐、头晕、疲劳、血小板减少或厌食。接受每日两次750 mg治疗的患者出现了消化不良、蛋白尿和/或粘膜炎等剂量限制性毒性。分别有1例(3%)和5例(17%)患者实现了完全缓解和临床改善。PTK/ZK在MMM患者中具有适度的活性。

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PTK787/ZK 222584, a small molecule tyrosine kinase receptor inhibitor of vascular endothelial growth factor (VEGF), has modest activity in myelofibrosis with myeloid metaplasia.PTK787/ZK 222584是一种血管内皮生长因子(VEGF)的小分子酪氨酸激酶受体抑制剂,在伴有髓样化生的骨髓纤维化中具有适度活性。
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