子弹 发表于 2020-08-10 12:47
bozantinib的二期临床实验NCT00940225,从2011年2月至2012年4月,美国和英国的
144例前列腺癌骨转移患者被依次纳入100毫克(n = 93)和40毫克(n = 51)队列
*91名患者(63%)有骨转移,57%的患者在接受 Cabozantinib治疗后疼痛缓解可减少或者终止服用止痛药。
*骨转缓解分别是73%和45%。骨转以外的肿瘤缓解别为80%和79%。
*肿瘤标志物PSA(前列腺特异抗原),骨生物标志物BSAP(骨特异性碱性磷酸酶)明显下降改善。
*整个人群的中位总生存期为10.8个月(100mg组12.1月,40mg组9.1月) 100mg组PFS4.4月(0.8-16.4),40mg组PFS4.2月(0.8-16.4)
*最常见的3级或4级不良事件是疲劳(22%),和高血压(14%),贫血(13%)和肺栓塞(11%)。
*因为副作用不耐受尽管积极处理后仍需要减量,100mg组平均剂量为55mg,40mg组平均剂量为36mg。
参考文献
Yakes FM, Chen J, Tan J, et al. Cabozantinib (XL184), a novel MET and VEGFR2 inhibitor, simultaneously suppresses metastasis, angiogenesis, and tumor growth. Mol Cancer Ther. 2011;10:2298–2308.
Schimmoller F, Zayzafoon M, Chung LWK, et al. Cabozantinib (XL184), a dual MET-VEGFR2 inhibitor, blocks osteoblastic and osteolytic progression of human prostate cancer xenografts in mouse bone. Mol Cancer Ther. 2011;10(suppl 1):233. abstr A233.
Nguyen HM, Ruppender N, Zhang X, et al. Cabozantinib inhibits growth of androgen-sensitive and castration-resistant prostate cancer and affects bone remodeling. PLoS One. 2013;8:e78881.
Graham TJ, Box G, Tunariu N, et al. Preclinical evaluation of imaging biomarkers for prostate cancer bone metastasis and response to cabozantinib. J Natl Cancer Inst. 2014;106:dju033.
Smith DC, Smith MR, Sweeney C, et al. Cabozantinib in patients with advanced prostate cancer: Results of a phase II randomized discontinuation trial. J Clin Oncol. 2013;31:412–419.
Lee RJ, Saylor PJ, Michaelson MD, et al. A dose-ranging study of cabozantinib in men with castration-resistant prostate cancer and bone metastases. Clin Cancer Res. 2013;19:3088–3094.
Brown MS, Chu GH, Kim HJ, et al. Computer-aided quantitative bone scan assessment of prostate cancer treatment response. Nucl Med Commun. 2012;33:384–394.
已经在盲试184,不知多久能起点效果? |