ABCG2 and gastric carcinoma: For instance, ATP-binding cassette sub-family G member 2 (ABCG2) [breast cancer resistance protein (BCRP1)] was found to be significantly upregulated in NCI-N87 human gastric carcinoma cell line (N87) T-DXd-resistant cells compared with parental lines, and co-treatment with a potent and selective ABCG2 (BCRP) inhibitor (Ko143) or a small-molecule inhibitor of ABCG2 (BCRP) (KS176) successfully restored T-DXd sensitivity, providing early preclinical evidence for combination therapy[64].