Beijing Avistone Biotechnology Co., Ltd (also referred to as “Avistone Biotechnology” or “Avistone”), an innovative biotechnology company focused on precision oncology therapeutics, has announced that the United States Food and Drug Administration (FDA) has cleared the investigational new drug (IND) application for ANS03, a next generation tyrosine kinase inhibitor (TKI) targeting both ROS proto-oncogene 1 (ROS1) and neurotrophic tropomyosin receptor kinase (NTRK).

To date, a number of ROS1/NTRK inhibitors (such as crizotinib, entrectinib, larotrectinib and repotrectinib) have been approved by the US Food and Drug Administration (FDA) and China’s National Medical Products Administration (NMPA) for the treatment of patients with metastatic NSCLC whose tumors are ROS1/NTRK-positive. Despite the clinical activity of ROS1/NTRK TKIs, resistance invariably develops, and nonclinical/clinical studies have identified ROS1/NTRK kinase domain point mutations that result in the resistance of ROS1/NTRK fusion-positive cancers to ROS1/NTRK TKIs. Therefore, there is an urgent clinical need for novel Type II ROS1/NTRK TKIs capable of overcoming acquired resistance mutations, particularly solvent front (SF) mutations like ROS1-G2032R and ROS1-D2033N and NTRK1-G595R, as well as ROS1 central beta sheet #6 (Cβ6) mutation L2086F and NTRK1 xDFG mutation G667C.

As a type II inhibitor, ANS03 possesses a broader spectrum of resistance mutation inhibition, occupying not only the ATP-bound pocket of the kinase with the “DFG-out” inactive conformation but also extending into the adjacent allosteric pocket, thereby conferring ANS03 a distinctive pharmacodynamic advantage.

ANS03 was specifically designed to provide patients afflicted with ROS1/NTRK fusion mutant cancers with a best-in-class, oral, small molecule therapy that can effectively overcome the acquired drug resistance problems caused by type I TKIs and also possesses a broader inhibitory range of ROS1/NTRK kinase activity, including wild-type ROS1/NTRK fusion and numerous acquired drug-resistant mutations. Enrollment of patients with locally advanced or metastatic tumors harboring a ROS1 or NTRK alteration is expected to begin in Q1 2025.

About Avistone Biotechnology

Beijing Avistone Biotechnology Co., Ltd. (also referred to as Avistone Biotechnology or Avistone) is an innovative biotechnology company focused on developing innovative therapies for patients with significant unmet medical needs globally. Avistone has an extensive portfolio and pipeline of targeted therapies in Non-Small Cell Lung Cancer (NSCLC) and in other solid tumors.

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