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EC359 is a first-in-class, small-molecule antagonist of the leukemia inhibitory factor receptor (LIFR) developed by Evestra. It functions by directly binding to LIFR with high affinity (Kd of 10.2 nM), effectively blocking the interaction between the cytokine leukemia inhibitory factor (LIF) and its receptor. This inhibition attenuates the activation of downstream LIF/LIFR-driven signaling pathways, including STAT3, mTOR, and AKT, which are frequently implicated in tumor progression and therapy resistance. Preclinical studies have demonstrated that EC359 exhibits antiproliferative effects, reduces cancer cell invasiveness and stemness, and promotes apoptosis. While the molecule has shown oral bioavailability in research settings, Evestra's clinical pipeline specifically categorizes EC359 as an injectable formulation for the treatment of solid tumors such as triple-negative breast cancer (TNBC), ovarian cancer, and pancreatic cancer.
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