On October 16, 2020, Centre for Drug Evaluation (CDE) of National Medical Products Administration (NMPA) accepted the clinical application of TGRX-326, a potent next-generation inhibitor developed by Shenzhen TargetRx Inc. (a leading company in targeted anticancer drugs) for the treatment of ALK-positive non-small cell lung cancer (NSCLC) (acceptance number: CXHL2000531 and CXHL2000532).

ALK (anaplastic lymphoma kinase) is a relatively common target for non-small cell lung cancer, accounting for about 3-8%. Because ALK+ targeted drugs can effectively inhibit tumors, ALK mutation is also called “diamond mutation”.

TGRX-326 is a potent third-generation ALK inhibitor targeting the EML4-ALK fusion gene, which is used to treat NSCLC with ALK gene mutations, especially NSCLC with ALK^G1202R mutation that confers resistance to the first- and second-generation inhibitors. At the same time, it has specific biological activity against ROS1 kinase, so it can be used to treat ROS1-positive NSCLC.

Dr. Yihan Wang, the founder of TargetRx, has more than 20 years of R&D experience in the field of targeted new drugs and is the core inventor of the second-generation ALK inhibitor brigatinib (Alunbrig) that has been marketed in the United States. In May 2021, brigatinib was officially approved by the U.S. FDA for the first-line treatment of ALK-positive metastatic NSCLC. Dr. Wang's experience in the field of targeted drugs for non-small cell lung cancer has helped the development of TGRX-326. Pre-clinical studies have shown that due to its novel and unique drug structure, TGRX-326 has excellent activity and high selectivity against wild-type and most mutant ALK kinases. It has the best-in-class potential and is at the international leading level.

Previously, on June 3, 2020, CDE cleared the clinical trial application of TGRX-678, a fourth-generation Bcr-Abl inhibitor with a novel mechanism of action for treatment of CML independently developed by TargetRx (see: "TargetRx's next-generation Bcr-Abl inhibitor used to treat CML has been cleared for clinical trial in China"）). The R&D of the company's other next-generation targeted drugs is actively advancing.