晟科药业(江苏)有限公司 Shengke Pharmaceuticals

ETH-155008:Novel PIM3 and CDK4/6 Dual Inhibitor

  • Simultaneous inhibition of Pim1/3 and CDK4/6 pathways can act synergistically to arrest tumor cells in G1 phase and induces apoptosis.

  • Dual inhibition within the same modality could avoid DDI and increased toxicity caused by the combination of two single drugs and attenuates the drug resistance of CDK4/6 inhibitors

  • ETH-155008 also showed potent inhibition of FLT3

Emerging Data suggesting PIM3 as an excellent Co-targeting Target for Endodermal Solid Tumors

  • Pim-3 kinase is aberrantly expressed in malignant lesions, but not normal tissues,particularly those of endoderm-derived organs, including the liver, pancreas, colon, and stomach

  • A defificiency of the Pim-3 gene does not result in apparent changes in phenotype, suggesting that Pim-3 may be physiologically dispensable. Pim kinases are not localized downstream of the insulin receptor signaling pathway and therefore inhibition of the Pim kinases has few effects on normal metabolism

  • Inhibit Pim-3, with chemotherapeutic agents, can aid in decreasing chemoresistance in pancreatic cancer. Treatment of solid tumors having aberrant expression of Pim-3, with Pim-3 inhibitors either as single agents or in combination with traditional chemotherapy may help provide a safe and novel drug regimen

Pim-3 Kinases Expressed in many Solid Tumors

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