This systematic review and meta-analysis aimed to verify the association between the genetic variants of adenosine triphosphate (ATP)-binding cassette subfamily B member 1 (
ABCB1) and ATP-binding cassette subfamily G member 2 (
ABCG2) genes and the presence and severity of gefitinib-associated adverse reactions. We systematically searched PubMed, Virtual Health Library/Bireme, Scopus, Embase, and Web of Science databases for relevant studies published up to February 2024. In total, five studies were included in the review. Additionally, eight genetic variants related to
ABCB1 (rs1045642, rs1128503, rs2032582, and rs1025836) and
ABCG2 (rs2231142, rs2231137, rs2622604, and 15622C>T) genes were analyzed. Meta-analysis showed a significant association between the
ABCB1 gene rs1045642 TT genotype and presence of diarrhea (OR = 5.41, 95% CI: 1.38–21.14, I
2 = 0%), the
ABCB1 gene rs1128503 TT genotype and CT + TT group and the presence of skin rash (OR = 4.37, 95% CI: 1.51–12.61, I
2 = 0% and OR = 6.99, 95%CI: 1.61–30.30, I
2= 0%, respectively), and the
ABCG2 gene rs2231142 CC genotype and presence of diarrhea (OR = 3.87, 95% CI: 1.53–9.84, I
2 = 39%). No
ABCB1 or
ABCG2 genes were positively associated with the severity of adverse reactions associated with gefitinib. In conclusion, this study showed that
ABCB1 and
ABCG2 variants are likely to exhibit clinical implications in predicting the presence of adverse reactions to gefitinib.
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