tipifarnib + cetuximab

TipCAT is a combination therapy regimen comprising tipifarnib and cetuximab, specifically developed to target HRAS-mutant head and neck squamous cell carcinoma (HNSCC). Tipifarnib is a first-in-class, orally bioavailable farnesyltransferase inhibitor (FTI) that prevents the farnesylation of HRAS, a critical step for its localization to the cell membrane and subsequent activation of pro-proliferative signaling cascades. Cetuximab is a chimeric monoclonal antibody that binds to the epidermal growth factor receptor (EGFR), inhibiting its activation and downstream signaling. By simultaneously inhibiting the HRAS driver and the EGFR pathway, TipCAT aims to provide a more robust anti-tumor response and delay the emergence of resistance in patients whose tumors are driven by HRAS mutations. The regimen has been evaluated in clinical trials led by Kura Oncology and academic collaborators.

Other names

Tipifarnib and Cetuximab combination