gotop

Potent immune-regulatory multi-tyrosine kinase inhibitor

In the past 20 years, multiple tyrosine kinase inhibitors have been approved for the treatment of cancer and other indications. The GNTbm R&D team focuses on the development of multi-tyrosine kinase inhibitors with strong immune activation, for primary application in cancer immunotherapy. Therefore, the GNTbm R&D team has independently developed a novel immune-regulating multi-tyrosine kinase inhibitor, GNTbm-TKI.

GNTbm-TKI is a small molecule drug candidate that has been selected after years of R&D, displaying novel structure, advantage of oral administration, and excellent immunoregulation activity. Studies on enzyme, cell, and animal test platforms have shown that GNTbm-TKI possesses strong immunoregulatory activity, and when used in combination with specific HDAC inhibitors, it exhibits very superior TME modulation activity, capable of transforming cold tumors into hot tumors and significantly increasing tumor immune response rates. GNTbm-TKI can be used as a monotherapy for the treatment of advanced neuroendocrine tumors, or in combination with HDAC inhibitors, ICIs, and anti-PD-1/VEGF bispecific antibodies for cancer immunotherapy. GNTbm-TKI is a potent selective multiple tyrosine kinase inhibitor that effectively inhibits specific targets, including TYRO-3, AXL, c-MER, BTK, ROS-1, NTRK2, VEGFR2, and MET. GNTbm has completed patent applications in multiple countries worldwide. GNTbm-TKI is one of the key components of drug combinations in cancer immunotherapy, primarily functioning to effectively remodel the TME.

GNTbm-TKI has entered preclinical research and been expected to enter Phase I clinical trial around 2027. It is anticipated that Phase II clinical trial will be conducted in combination with GNTbm-38, which firstly will be applied for orphan drug designation. The strategy is to first obtain drug approval through a single-arm pivotal Phase II trial, and then expand into other new indications. GNTbm-TKI will be a multi-tyrosine kinase inhibitor with strong immunomodulatory effects, primarily applied in combination of 'GNTbm-TKI plus I' for indication expansion, where I represents HDAC inhibitor, ICI, or anti-PD-1/VEGF bispecific antibody, belonging to powerful cancer immunotherapy treatments that are expected to treat various advanced solid tumors.