ZXBT-1158项目简介

2016-12-14

适应症：


复发晚期B细胞淋巴瘤、中枢神经系统淋巴瘤、多发性硬化等自身免疫系统疾病



项目优势：


前期实验显示，ZXBT-1158比母体化合物ACP-196更安全有效；

多种适应症，对B细胞恶性肿瘤、实体肿瘤、自身免疫性疾病均有效；

抑制BTK选择性更好，避免或减少了与癌症治疗相关的某些不良反应；

临床上，可结合BTK含量水平，开展个体化治疗；

口服药，方便服用；


ZXBT-1158参考文献：

[1]  Rosenquist R, Beà S, Du MQ, Nadel B, Pan-Hammarström Q, Genetic landscape and deregulated pathways in B-cell lymphoid malignancies[J],Jama Intern Med.2017-11, 282(5): 371-394.

[2]  Seda V1, Mraz M, B-cell receptor signalling and its crosstalk with other pathways in normal and malignant cells[J], Eur J Haematol.2015-Mar, 94(3): 193-205.

[3]  Honigberg LA, Smith AM, Sirisawad M, Verner E, Loury D, Chang B, Shyr Li, Pan Z, Thamm DH, Miller RA, Buggy JJ. The Bruton tyrosine kinase inhibitor PCI-32765 blocks B-cell activation and is efficacious in models of autoimmune disease and B-cell malignancy[J]. Proc Natl Acad Sci USA 2010,107:13075–13080.

[4]  Advani RH, Buggy JH, Sharman JP, Smith SM, Boyd TE, Grant B,Kolibaba KS, Furman RR, Rodriguez S, Chang BY, Sukbunth-erng J, Izumi R, Hamdy A, Hedrick E, Fowler NH.Bruton tyrosine kinase inhibitor ibrutinib (PCI-32765) has significant activity in patients with relapsed/refractory B-cell malignancies[J].J Clin Oncol,2003, 31:88–94.

[5]  Parmar S, Patel K, Pinilla-Ibarz. Ibrutinib (Imbruvica): a novel targeted therapy for chronic lymphocytic leukemia[J]. Pharm Ther, 2014, 39:483–487.

[6]  John C. Byrd, M.D., Bonnie Harrington, D.V.M., Susan O’Brien, M.D., Jeffrey A. Jones, M.D., M.P.H., Anna Schuh, M.D., Ph.D., Steve Devereux, M.D., Jorge Chaves, M.D., William G. Wierda, M.D., Ph.D., Farrukh T. Awan, M.D., Jennifer R. Brown, M.D., Ph.D., Peter Hillmen, M.B., Ch.B., Ph.D., Deborah M. Stephens, D.O., etal. Acalabrutinib (ACP-196) in Relapsed Chronic Lymphocytic Leukemia[J]. N Engl J Med, 2016,374:323-332.



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