EC-70124: oral multi-kinase inhibitor targeting both tumor and cancer stem cells in acute leukaemias and solid tumors (FL3-PIM-SYK triple inhibitor for AML)
Discovery and Development of kinase inhibitors represents a major effort in R&D for pharmaceutical companies nowadays, as a result the number of publications on this topic is at an all-time high. The mainstream goal is to develop selective and potent inhibitors of kinases involved in signal transduction pathways related to a variety of diseases, especially those unlocking new drug targets.
EntreChem has focused its efforts in the Indolocarbazole chemical class, since several examples of natural and synthetic indolocarbazoles have reached clinical trials, indicating they are safe in humans. Our unique core technology allows combinatorial biosynthesis of genes from the naturally occurring Staurosporine and Rebeccamycin, providing a library of hybrid indolocarbazoles, whose Mechanism of Action is based on potent but more selective kinase inhibition as compared to the all-natural hit compounds. Since these analogs are much less promiscuous than Staurosporine, their toxicity in vivo enables further preclinical development.
EntreChem has selected EC-70124 from this library for development, since the biochemical in vitro profile, confirmed by cellular experiments, indicates that its mode of action impacts solid tumors dependent of pathways like NF-kB, Akt/mTOR, JAK/STAT, and Acute Leukemias dependent on FLT3, PIM and SYK. Therefore, EC-7014 is potentially useful both in solid and hematological tumors.