Flumatinib, the first second generation BCR ABL tyrosine kinase inhibitor in China, is on the market

Flumatinib (trade name: hausen Xinfu), a new anti-tumor class 1 drug independently developed by hausen, is intended to be used to treat Philadelphia chromosome positive chronic myeloid leukemia (Ph + CML), which was approved by nmpa on November 26, 2019 Figure 1 Chemical structure formula of flumatinib Flumatinib is a tyrosine kinase (TKI) inhibitor, which is the first second generation of BCR ABL TKI inhibitor in China From September 2009, the first application for chemical 1.1 clinical trial was submitted to CFDA, and now it has been successfully put on the market The R & D of the drug has lasted more than ten years, and the investment has reached up to 100 million yuan Chronic myeloid leukemia (CML) is a malignant tumor of clonal proliferation of bone marrow hematopoietic stem cells, accounting for 15% of adult leukemia, and the global incidence rate is 1.6~2/10 million CML patients in China are younger than those in western countries The epidemiological survey in many areas in China shows that the median age of CML patients is 45-50 years old, while in western countries it is 67 years old According to the drug delivery database, there are 7 BCR ABL tyrosine kinase inhibitors approved for CML, including Novartis imatinib, Bristol Myers Squibb dasatinib, Novartis nilotinib, South Korea Yiyang ladotinib, Pfizer bosudinib, ariad Pharm punatinib, Jiangsu Haosen flumatinib Figure 2 Sales volume of imatini, sadatini and nilotini in recent years (the data is compiled from the drug delivery database and the annual report of the company) There are 17 kinds of BCR ABL tyrosine kinase inhibitors (including drugs in the market and under development) for CML treatment worldwide In addition to the seven drugs approved for marketing, the drugs under research include asciminib (clinical phase III, Novartis), cmlvaxb2a2-25 (clinical phase II, University of Leipzig), pf-114 (clinical phase II, fusion Pharma), an-019 (clinical phase II, NATCO), sun-k706 (clinical phase II, sun Pharma advanced Research), Nike tinib (clinical phase II, Guangzhou Institute of biomedicine and health, Chinese Academy of Sciences, Guangzhou Shunjian biomedical technology), dasatinib nanoparticle formula (clinical phase I, xspreay Pharma), etc-206 (clinical phase I, experimental therapeutics Center), adaphosin (clinical phase I, mayoclinic, National Cancer Institute, meditinib (clinical phase I, Harbin Yuheng Pharmaceutical Co., Ltd.) Figure 3 Global BCR ABL tyrosine kinase inhibitor R & D pipeline (as of November 2019) Transaction & Investment and financing information of Jiangsu Haosen Pharmaceutical (as of November 2019): The approved flumatinib is the second generation of BCR abltki inhibitor independently developed by hausen medicine and approved for marketing in China It can improve the clinical treatment effect of some imatinib resistant patients, with good safety and tolerance The efficacy of wild-type and imatinib resistant patients is better than that of imatinib It is believed that hausen can easily compete in the domestic CML market with imatinib, a generic drug, and flumatini, an upgraded version Former title: Jiangsu Haosen's "flumatinib" - the first second generation of BCR ABL tyrosine kinase inhibitor in China Main references: