Astellas announced on February 4, 2021 that the National Medical Products Administration (NMPA) of China has conditionally approved Segatan® (geritinib fumarate tablets, Xospata®,) to be marketed for therapeutic use Fully validated detection methods have detected relapsed (relapsed disease) or refractory (treatment resistant) acute myeloid leukemia (AML) adult patients with FMS-like tyrosine kinase 3 (FLT3) mutations.

　　It is worth mentioning that in July 2020, gerritinib obtained the priority review qualification of the NMPA Center for Drug Evaluation (CDE), and CDE released the third batch of clinically urgently needed overseas new drugs in November 2020. Gerritinib is included.

　　In the United States, the FDA has been on the market in 2018. It is an FLT3 inhibitor approved for the treatment of relapsed and refractory AML with FLT3 mutations. Since then, it has been approved in many countries including the European Union, Canada, South Korea, Brazil and Australia.

　　Now that geritinib is approved in China, it will also meet the clinical treatment needs of Chinese patients with acute myeloid leukemia.

　　About Acute Myeloid Leukemia

　　Acute myeloid leukemia (AML) is one of the types of leukemia commonly seen in adults. It is characterized by abnormal proliferation and differentiation of myeloid cells, which is more common in the elderly, and is accompanied by serious complications and high risk in death. According to estimates by epidemiologists, by 2029, the number of AML patients worldwide will increase to 90264 cases at an annual growth rate (AGR) of 2.51% per year. During the forecast period, the contribution rate of Chinese cities and towns is very high. The number of confirmed cases will increase from 29,535 in 2019 to 39,991 in 2029 (AGR of 3.54%). By 2029, among the population of eight major markets (the United States, France, Germany, Italy, Spain, Britain, Japan, and China), the five-year confirmed epidemic of AML cases is expected to increase from 99,624 to 1,240,65 [1] .

　　In the past ten years, the incidence of acute myeloid leukemia has been increasing, and the incidence of new acute myeloid leukemia has increased by an average of 1.5% per year. However, in the past 40 years, although a variety of treatment methods have been developed for acute myeloid leukemia, such as chemotherapy, radiotherapy, stem cell transplantation, immunotherapy and targeted therapy, the shortcomings of each existing method are also obvious. Generally, the overall long-term survival rate of acute myeloid leukemia is still not high, and the prognosis is poor, especially in refractory and elderly patients [2].

　　About targeting FLT3

　　Now, FLT3 has been confirmed to be a common carcinogenic mutation in AML, accounting for about 20%-30% of patients with acute myeloid leukemia [3]. The common types of FLT3 mutations mainly include internal tandemduplication (ITD) in the proximal membrane domain of the receptor and point mutations in the tyrosine kinase domain (TKD). The mutation probability is 25% and 5%, respectively [4] .

　　The prognosis of acute myeloid leukemia patients with FLT3 gene mutation is poor. The 3-year survival rate of FLT3 non-mutated patients receiving traditional chemotherapy is 45%-55%, while the 3-year survival rate of patients with ITD FLT3 mutation receiving the same treatment Less than 20% [5].

　　About Astellas' tumor strategic layout

　　Enzalutamide is an oncology drug previously marketed by Astellas in China for the treatment of castration-resistant prostate cancer. The study of metastatic hormone-sensitive prostate cancer is also in phase III clinical trials.

　　Giritinib's listing approval is of great significance to domestic AML patients and Astellas, and we look forward to bringing new medication options to patients with acute myeloid leukemia as soon as possible.

　　Reference materials

　　[1]GlobalData ：Acute Myeloid Leukemia-Epidemiology Forecast to 2029

　　[2] Cheng Hongji, Yang Yanli. Progress in targeted therapy of acute myeloid leukemia. Cancer Progress, vol18(1): 14-17

　　[3] Daniel R Reed, et al. Gilteritinib: An FMS-like tyrosine kinase 3/AXL tyrosine kinase inhibitor for the treatment of relapsed or refractory acute myeloid leukemia patients. J Oncol Pharm Practice 0(0) 1–13

　　[4] Gilliland DG, Griffin JD. The roles of FLT3 in hematopoiesis and leukemia. Blood2002; 100:1532–42

　　[5] Zhu Wenting, Bai Qiujiang. FLT3 I mutant acute myeloid leukemia targeted therapy drug Gilletinib. China Pharmaceuticals, 2020, 29(3): 74-77