NT-219 is a first-in-class small molecule targeting the novel cancer drug resistance pathways IRS1/2 and STAT3. Kitov is currently advancing NT-219 in combination with cetuximab, an EGFR antibody, as a second-line or third-line therapy for the treatment of recurrent and metastatic squamous cell carcinoma of the Head & Neck Cancer (SCCHN). NT-219 has the potential to prevent and overcome drug resistance in various cancer types when used in combination with existing agents. 

In preclinical models, NT-219 demonstrated outstanding efficacy in preventing acquired resistance and reversing tumor resistance for a variety of approved cancer therapies. These include EGFR antibodies (Erbitux®), small molecular inhibitors of MEK (Mekinist®), mutated BRAF (Zelboraf®), EGFR (Tagrisso®, Tarceva®), and mTOR (Afinitor®), as well as chemotherapy agents such as Gemcitabine, Oxaliplatin, and Docetaxel. Preliminary synergistic effects were also observed in combination with immune oncology agents such as Keytruda®. Preclinical data has also shown that short exposure of cancerous cells to NT-219 is sufficient to trigger an irreversible shutdown of cancer pathways, resulting in a long-term anti-cancer effect.

Kitov plans to initiate a phase 1/2 study in the second quarter of 2020.