NT219

NT219 is a first-in-class small molecule drug developed to overcome tumor resistance to cancer therapies. It acts by promoting the degradation of insulin receptor substrate 1 (IRS1) and insulin receptor substrate 2 (IRS2) and inhibiting the phosphorylation of signal transducer and activator of transcription 3 (STAT3), both key oncogenic drivers involved in drug resistance pathways. By targeting these proteins, NT219 blocks major survival signals in cancer cells—including those mediated by IGF1R/IRS and STAT3—leading to apoptosis and inhibition of tumor proliferation. This mechanism resensitizes refractory tumors to immune checkpoint inhibitors (such as pembrolizumab), EGFR blockers (such as cetuximab), and chemotherapy. Preclinical studies have shown that NT219 can prevent acquired resistance as well as reverse existing resistance when used alone or in combination with other oncology drugs. The drug is currently being evaluated in Phase 2 clinical trials for recurrent/metastatic squamous cell carcinoma of the head and neck (SCCHN)[1][5][6][7][8].

Other names

2-propenethioamide, 3-(2-bromo-3,4-dihydroxyphenyl)-n-((3,4,5-trihydroxyphenyl)methyl)-UNII-K1WT1A1UP5UNII-K-1WT1A1UP5UNII-K 1WT1A1UP51198078-60-2