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NT219

Overview and Mechanism of Action

NT219 is a first-in-class, novel small molecule targeting both IRS1/2 and STAT3, important oncogenic drivers and major drug resistance pathways in many hard-to-treat cancers. In preclinical studies, NT219 demonstrated strong efficacy in preventing acquired resistance and reversing tumor resistance when administered as a monotherapy and in combination with various existing oncology therapies.

IRS1/2

  • Scaffold protens, mediating mitogenic signals from IGF1R, IR, IL4R and other oncogenes, overexpressed in multiple tumor types
  • Regulates major survival pathways such as the PI3K/AKT, MEK/ERK and Wnt/β-cetenin
  • Activated as feedback response to anti-cancer therapies

STAT3

  • Well-established transcription factor associated with the tumorigenic phenotype
  • Provides a crucial axis to support cell proliferation and survival
  • Active in tumor JAK/STAT3 and TGF beta resistance mechanisms

Clinical Studies

A Phase 1/2 first-in-human clinical trial in the U.S. is ongoing, in which NT219 is used both as a monotherapy and in combination with cetuximab (Erbitux™), with plans to expand the combination study to include patients with recurrent or metastatic SCCHN cancer in 2021.

Study Design

Study Design Diagram

Dose Escalation Design

Dose Escalation Design Diagram
NT219 - References (Download)
ClinicalTrials.gov NCT04474470 - A Study to Evaluate NT219 Alone and in Combination With ERBITUX® (Cetuximab) in Adults With Advanced Solid Tumors and Head and Neck Cancer
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