Ling Wang,1,2,* Guoquan Chen,2,* Wei Hu,3,* Jiale Chen,2 Yiling He1,2 

1School of Pharmaceutical Sciences, Zhejiang Chinese Medical University, Hangzhou, People’s Republic of China; 2Department of Pharmacy, Affiliated Jinhua Hospital, Medical College of Zhejiang University, Jinhua, People’s Republic of China; 3Department of Pharmacy, Second Affiliated Hospital, Zhejiang University School of Medicine, Hangzhou, People’s Republic of China

*These authors contributed equally to this work

Correspondence: Yiling He, Department of Pharmacy, Affiliated Jinhua Hospital, Medical College of Zhejiang University, Jinhua, People’s Republic of China, Email 1538583874@qq.com

Abstract: Rivaroxaban is a direct oral anticoagulant (DOAC) that directly inhibits coagulation factor Xa and exerts its anticoagulant effects. Although rivaroxaban generally exhibits predictable pharmacokinetic (PK) and pharmacodynamic (PD) profiles, significant interindividual variability in therapeutic responses exists. Research on the role of genetic factors in the clinical variability of rivaroxaban is relatively new and extensive. In this review, 12 pharmacogenetic studies on rivaroxaban were summarised, and 25 reported gene polymorphic sites were summarised, including ABCB1 (rs1045642, rs4148738, rs1128503, rs2032582, rs4728709, rs3789243 and rs3213619, ABCG2 (rs2231142, rs2231137, rs3114018, rs2622604 and rs1481012), CYP3A4 (rs35599367, rs2242480, rs4646437 and rs12333983), CYP3A5 (rs776746, rs15524, rs4646450), CYP2J2 (rs890293), CYP2J19 (rs4244285 and rs12248560), ABCA6 (rs7212506), AKR7A3 (rs1738023 and rs1738025). The review provided an overview of the current state of research on rivaroxaban gene polymorphisms. However, due to the significant heterogeneity of existing studies and the lack of consistency in results, the evidence to date has limited impact. Therefore, larger-scale, global, multi-centre clinical trials are needed in the future to validate potential gene loci for testing.

Keywords: rivaroxaban, pharmacogenomics, pharmacokinetics, bleeding events, polymorphism, variant