Rivoceranib(a.k.a. Apatinib) is the first successful small-molecule tyrosine kinase inhibitor already approved to treat gastric cancer in China in December 2014. In US, Europe and South Korea, it has been granted orphan drug designation. The drug has been clinically tested with over 1,000 patients worldwide and has demonstrated its efficacy in numerous cancers including gastric cancer, colorectal cancer, hepatocellular carcinoma, non-small cell lung cancer, esophageal cancer, thyroid cancer, mesothelioma, and neuroendocrine tumors. Rivoceranib has also shown potential to significantly improve outcomes in combination treatment with chemotherapeutics and immunotherapy as well as for maintenance therapy.
Bruton’s tyrosine kinase (BTK) and Janus kinase 3 (JAK3) dual targeting presents a unique opportunity for the effective treatment of both hematologic and autoimmune disorders. BTK targeting has been clinically validated for the treatment of hematologic malignancies such as chronic lymphocytic leukemia (CLL) and mantle cell lymphoma (MCL), and for the treatment of autoimmune disorders such as rheumatoid arthritis. Similar to BTK, JAK3 is primarily expressed in lymphoid hematopoietic cells and has also been validated as clinical target in autoimmune diseases and has been implicated in a number of blood cancers. Dual targeting of both BTK and JAK3 has the potential to show synergistic effects in the treatment of such diseases.
Seclidemstat is a novel epigenetic oral small molecule for target therapy. It acts to normalize gene expression and suppress tumor growth via its highly selective and reversible inhibition of malfunctioned Lysine Specific Demethylase 1 (LSD 1) overexpressed in various solid tumors such as lung cancer, breast cancer, and prostate cancer.
Tegavivint is a potent and selective inhibitor of the Wnt/ß-catenin signaling pathway, implicated in cell proliferation, differentiation, and immune evasion. Tegavivint demonstrates pre-clinical in vivo efficacy in several cancer models including desmoid tumors, acute myeloid leukemia (AML), osteosarcoma, and a range of solid tumor types.