Masitinib for gastrointestinal stromal tumors

Abstract

ABSTRACTIntroduction: Over the past decade, the development of tyrosine kinase inhibitors such as imatinib, targeting KIT and PDGFRα, has dramatically improved the prognosis of GIST patients. Masitinib, another TKI targeting KIT and PDGFRα, is currently in phase III development for patients with metastatic/unresectable GIST.Areas covered: A literature search using PubMed was conducted to include relevant preclinical and clinical studies using masitinib in GIST, and to describe GIST patients’ outcomes when treated with masitinib. Preclinical studies have demonstrated antitumor activity of masitinib. Phase I and II studies have established safety and efficacy of masitinib as first line therapy and after failure of imatinib. Commonly seen adverse events (AE) include gastrointestinal disorders and skin events but grade 3 AE were uncommon. Two phase III trials are currently recruiting, one comparing masitinib to sunitinib in patients with advanced imatinib-resistant GIST and the other comparing masitinib to imatinib as first line therapy for patients with advanced GIST. Another phase III trial, comparing masitinib to placebo in the adjuvant setting of GIST with high risk of recurrence is in preparation.Expert opinion: Based on its safety and efficacy profile, masitinib may represent a potentially useful addition to the current systemic therapies for advanced GIST.