On September 25, 2019 AnHeart Therapeutics (Hangzhou) Co., Ltd. reported that preclinical results of AB-106 (original R&D code: DS-6051b), an innovative anti-cancer drug made available exclusively from Daiichi Sankyo Company Limited, were published online by the peer-reviewed academic journal Nature Communications on August 9.[1] (Press release, AnHeart Therapeutics, SEP 25, 2019, View Source [SID1234555759])
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The research results reveal that (1) AB-106 can inhibit ROS1 tyrosine kinase and NTRK tyrosine kinase (NTRK1, NTRK2, and NTRK3) at low concentrations; (2) AB-106 has demonstrated tumor-reducing effects in the model cell lines harbouring ROS1 and NTRK fusion genes, patient-derived cancer cell lines, and tumor-bearing mice models with transplantation of these genes; (3) AB-106 also has inhibitory activity against the highly crizotinib-resistant ROS1-G2032R mutation and NTRK inhibitor-resistant variations.
ROS1 fusion gene is a potent oncogene found in approximately 1-2% of non-small cell lung cancer (NSCLC), and the first generation ROS1 inhibitor crizotinib has been approved for clinical use. However, in most cases, crizotinib-resistant tumors develop and the condition deteriorates again. The mechanism of resistance is often caused by a G2032R mutation in ROS1. However, no effective drugs against this resistance mutation have been developed. The emergence of AB-106 is expected to provide such patients with new treatment options.
AB-106, an oral and efficient ROS1/NTRK dual-target small molecule inhibitor, is a leading asset in AnHeart’s R&D pipeline. Two clinical trials of phase 1 on AB-106 have been conducted in Japan and the United States. The results showed that AB-106 was effective not only in patients with ROS1 positive lung cancer who had not been treated with ROS1 inhibitor but also in patients with ROS1 fusion gene-positive lung cancer who failed to be cured with ROS1 inhibitors such as clozotinib. At the same time, AB-106 has also demonstrated tumor-reducing effects on NTRK fusion gene-positive patients.
Dr. Wang Junyuan, co-founder and CEO of AnHeart, said "AB-106 is ready to start phase II clinical trials in China and the United States in the first quarter of 2020, as we pursue our goal of providing patients with effective, easy-to-take, low-cost and safer therapeutic drugs as soon as possible."
Dr. Yan Bing, co-founder and Chief Medical Officer at AnHeart, said: "our team has a wealth of clinical development experience, including successful drug approval experience in Asia, Europe and the United States, and maintains a good long-term cooperative relationship with a number of top external partners and opinion leaders in the industry. In the future, we will continue to explore innovative ways to maximize the potential of compounds in our tumor pipelines and provide sufficient resources to implement a rapid approval development strategy that achieves our mission of transforming scientific research results into value for cancer patients and bringing new treatments like this ROS1/NTRK inhibitor to patients as soon as possible."
Since its establishment in 2018, AnHeart has attracted professionals with many years of working experience in both multinational and innovative domestic pharmaceutical companies to create a senior management team with rich clinical development experience. AnHeartsecured round A financing of USD 15 million upon inception. At present, AnHeart aims to collaborate with large and medium-sized biopharma companies to strengthen its clinical product pipeline by obtaining and developing clinical assets that have shown good potential in animal experiments, before they enter clinical trials.
[1]Link to the original text:
The new-generation selective ROS1/NTRK inhibitor DS-6051b overcomes crizotinib resistant ROS1-G2032R mutation in preclinical models