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BCR-ABL tyrosine kinase

Cell culture and mouse studies suggest the BCR-ABL tyrosine kinase inhibitor GZD824 could help treat imatinib-resistant cancer. In leukemia cell lines expressing a BCR-ABL tyrosine kinase with drug-resistant mutations, GZD824 blocked BCR-ABL tyrosine kinase activation and signaling and inhibited proliferation. In mouse models of leukemia with wild-type or mutant BCR-ABL, oral dosing of GZD824 decreased proliferation and tumor burden compared with oral dosing of vehicle. Next steps include manufacturing sufficient amounts of GZD824 under GMP conditions for clinical trials.
Novartis AG's BCR-ABL tyrosine kinase inhibitor Gleevec imatinib is marketed to treat multiple cancers. Novartis' BCR-ABL tyrosine kinase inhibitor Tasigna nilotinib is marketed to treat chronic myelogenous leukemia (CML).

SciBX 6(4); doi:10.1038/scibx.2013.84
Published online Jan. 31, 2013

Patent application filed; licensed to Guangzhou Shunjian Pharma Inc.

Ding, K. et al. J. Med. Chem.; published online Jan. 9, 2013;
Contact: Ke Ding, Chinese Academy of Sciences, Guangzhou, China