This preclinical study aimed to investigate the putative antitumoral efficacy of gabexate mesilate, alone and in combination with the anti-EGFR monoclonal antibody cetuximab, in a panel of human CRC cell lines harbouring a different expression pattern of wild-type/mutated KRAS, BRAF and PIK3CA genes. Here, PIK3CA is linked to colorectal carcinoma.