TaiwanJ’s dual target pipelines focuses on new chemical entities that afford concurrent HMG-CoA reductase (HMGR) and histone deacteylase (HDAC) inhibition. Both are molecular targets for new anti-cancer and anti-inflammation drugs. HDAC suppresses the expression of anti-oncogenes and promotes tumorigenesis, as well as inflammatory and immune-activation genes. HMGR is the rate-limiting enzyme for cholesterol synthesis, which is up stream of Ras family oncoproteins activation through protein prenylation, and in turn suppresses the inflammatory cascade. Furthermore, HMGR inhibition has been shown to promote the function of HDAC inhibitors.

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The dual target inhibitors show improved preclinical safety and stability profiles over existing HDAC inhibitors (HDACi), and is expected to increase therapeutic index and widen therapeutic window clinically. The anti-cancer efficacy of HDAC-HMGR dual inhibition has been shown in colorectal cancer and liver metastasis in proof-of concept preclinical studies.