The first domestic research and development of a new generation of NTRK/ROS1 multi-kinase inhibitor project completed phase I clinical first subjects

The first domestic research and development of a new generation of NTRK/ROS1 multi-kinase inhibitor SIM1803-1A tablets in China on January 5, 2021 completed the first phase I clinical trial subjects of the first drug.
SIM1803-1A tablet is a new generation of selective multi-target tyrosine kinase inhibitors (TKI) developed by Syngenta Pharmaceuticals Ltd. for TRK A/B/C, ROS1 and ARK.
this clinical study is the first human study conducted by SIM1803-1A in solid tumor patients, the main purpose is to determine the safety and pharmacodynamic characteristics of SIM1803-1A, and the secondary purpose is to explore the efficacy of SIM1803-1A.
In recent years, pan-cancer treatment drugs based on specific biomarkers rather than the site of onset have opened a new chapter in cancer therapy drugs and accompanying diagnosis by not distinguishing between cancer species, unlimited tumor sites, and being able to overcome a variety of mutations and drug resistance.
, the FDA has approved a number of open-ended cancer drugs on the market, and there is no gene-based mutation, unlimited tumor site of the generic cancer target drug approved.
, the SIM1803-1A tablet under study by Synthesiothe Pharmaceuticals, is a new generation of precision therapy drugs developed based on this concept.
NTRK1/2/3, ROS1, and ARK gene fusion mutations are the driving genes of multiple solid tumors.
NTRK has low-frequency mutations (less than 1%) in a variety of common tumors, while ARK and ROS1 occur mainly in non-small cell lung cancer (incidence is about 7% and 1% respectively).
has approved a variety of ARK, ROS1 and NTRK selective inhibitors in the United States, as well as a variety of ARK and ROS1 inhibitors approved for listing in China, but no NTRK inhibitors approved for listing.
The drugs currently on the market for the above targets rarely achieve complete relief, generally in the treatment of 1-5 years will appear all kinds of drug-resistant mutations, including S, F. mutations, G.K. mutations and DFGx mutations, leading to disease progression, clinically urgent need for drug-resistant mutations effective next-generation TKI.
In preclinical trials, SIM1803-1A tablets were effective for TRK A/B/C, ROS1, and ARK-sensitive mutant tumors that had not been treated with a generation of TKI, and for TRK or ROS1-positive tumors that had been treated with a generation of TKI.
, SIM1803-1A shows greater activity and good safety in several preclinical models compared to similar products.
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