Daiichi Sankyo Pharma Development, 399 Thornall Street, Edison, New Jersey 08837, USA.
J Neuroimmunol. 2012 May 15;246(1-2):100-7. doi: 10.1016/j.jneuroim.2012.03.007. Epub 2012 Mar 31.
CS-0777 is a selective sphingosine 1-phosphate receptor-1 modulator under investigation for treatment of multiple sclerosis (MS). We conducted an open-label, pilot study in 25 MS patients to assess the safety, pharmacokinetics, pharmacodynamics and exploratory efficacy of oral CS-0777 (0.1, 0.3 and 0.6 mg), administered once weekly or every other week for 12 weeks. CS-0777 resulted in a pronounced, dose-dependent decrease in lymphocytes and CD4 T cell subsets, which returned to baseline within 4 weeks after the last dose. Overall, CS-0777 was safe and well-tolerated. These results require confirmation in a double-blind, placebo-controlled and adequately powered phase 2 study in MS.
CS-0777 是一种鞘氨醇 1-磷酸受体-1 调节剂，正在研究用于治疗多发性硬化症 (MS)。我们对 25 例 MS 患者进行了一项开放性、先导性研究，以评估每周或每两周口服 CS-0777（0.1、0.3 和 0.6 mg）一次的安全性、药代动力学、药效学和探索性疗效，共 12 周。CS-0777 可显著、剂量依赖性地降低淋巴细胞和 CD4 T 细胞亚群，末次给药后 4 周内恢复至基线。总体而言，CS-0777 安全且耐受良好。这些结果需要在 MS 的双盲、安慰剂对照和充分效力的 2 期研究中得到证实。
