Fouladi Maryam, Nicholson H Stacy, Zhou Tianni, Laningham Fred, Helton Kathleen J, Holmes Emi, Cohen Kenneth, Speights Rose Anne, Wright John, Pollack Ian F
Department of Hematology-Oncology, St. Jude Children's Research Hospital, Memphis, Tennessee 38105-2794, USA.
Cancer. 2007 Dec 1;110(11):2535-41. doi: 10.1002/cncr.23078.
An open-label Phase II study of tipifarnib was conducted to evaluate its safety and efficacy in children with recurrent or refractory medulloblastoma (MB)/primitive neuroectodermal tumor (PNET), high-grade glioma (HGG), and diffuse intrinsic brainstem glioma (BSG).
Between January 2004 and July 2005, patients were enrolled and stratified as follows: Stratum 1, recurrent or refractory MB/PNET; Stratum 2, recurrent or refractory HGG; and Stratum 3, recurrent or refractory BSG. Patients received tipifarnib 200 mg/m2 per dose twice daily for 21 days repeated every 28 days. Patients who received enzyme-inducing anticonvulsants and other CYP3A4/5 inducers or inhibitors were excluded. The primary objective was to estimate the sustained response rate in all strata.
Ninety-seven patients with a median age of 11.2 years (range, 3.2-21.9 years) were enrolled on the study, and 81 patients were evaluable for response. One of 35 patients with BSG and 1 of 31 patients with HGG had a sustained partial response. No responses were observed in 15 patients with MB/PNET. Eight patients (3 HGG, 1 MB, and 4 BSG) remained stable for >or=4 courses (range, 4-25 courses). The median number of courses received was 2 (range, 1-25 courses). The most frequent grade 3 and 4 toxicities included neutropenia (18.7%), thrombocytopenia (14.3%), and leukopenia (14.3%). The 6-month progression-free survival rate (+/-standard deviation) was 14%+/-6% for HGG, 6%+/-6% for MB/PNET and 3%+/-3% for BSG.
Tipifarnib tolerated well but had little activity as a single agent in children with recurrent central nervous system malignancies.
开展了一项关于替匹法尼的开放标签II期研究,以评估其在复发或难治性髓母细胞瘤(MB)/原始神经外胚层肿瘤(PNET)、高级别胶质瘤(HGG)和弥漫性脑桥内在胶质瘤(BSG)患儿中的安全性和疗效。
2004年1月至2005年7月期间,患者入组并分层如下:第1层,复发或难治性MB/PNET;第2层,复发或难治性HGG;第3层,复发或难治性BSG。患者接受替匹法尼200mg/m²,每剂每日两次,共21天,每28天重复一次。接受酶诱导抗惊厥药和其他CYP3A4/5诱导剂或抑制剂的患者被排除。主要目标是估计所有层的持续缓解率。
97例中位年龄为11.2岁(范围3.2 - 21.9岁)的患者入组本研究,81例患者可评估缓解情况。35例BSG患者中有1例、31例HGG患者中有1例获得持续部分缓解。15例MB/PNET患者未观察到缓解。8例患者(3例HGG、1例MB和4例BSG)病情稳定≥4个疗程(范围4 - 25个疗程)。接受疗程的中位数为2个(范围1 - 25个疗程)。最常见的3级和4级毒性包括中性粒细胞减少(18.7%)、血小板减少(14.3%)和白细胞减少(14.3%)。HGG的6个月无进展生存率(±标准差)为14%±6%,MB/PNET为6%±6%,BSG为3%±3%。
替匹法尼耐受性良好,但作为单一药物对复发中枢神经系统恶性肿瘤患儿几乎没有活性。