Cabometyx for GIST – pro
In the majority of gastrointestinal stromal tumors (GIST), oncogenic signaling is driven by KIT mutations. Advanced GIST is treated with tyrosine kinase inhibitors (TKI) such as imatinib. Cabometyx acts against this mutation.
However, clinical use of this drug is still premature and results of several trials are expected. In a Phase I trial cabozantinib administered 60 mg daily appeared to be well tolerated and antitumor activity was observed in heavily pretreated GIST patients with long-lasting SD as best response. A multicenter, multinational, open label, single arm Phase II study of single-agent cabozantinib was opened by the European Organisation for Research and Treatment of Cancer. The study will assess the safety and activity of cabozantinib in patients with metastatic GIST who have previously progressed on imatinib and sunitinib and have not been exposed yet to other KIT – or PDGFR-directed TKIs.
Zoltan Szucs, Khin Thway, Cyril Fisher, Ramesh Bulusu, Anastasia Constantinidou, Charlotte Benson, Winette TA van der Graaf & Robin L Jones, Promising novel therapeutic approaches in the management of gastrointestinal stromal tumors. FUTURE ONCOLOGYVOL. 13, NO. 2 REVIEW
Gebreyohannes YK et al, Cabozantinib Is Active against Human Gastrointestinal Stromal Tumor Xenografts Carrying Different KIT Mutations.Mol Cancer Ther. 2016 Dec;15(12):2845-2852.