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. 2016 Sep 19;56(4):317–337. doi: 10.1007/s40262-016-0450-z

Table 4.

Polymorphisms in drug transporter genes affecting pharmacokinetics of anticancer drugs

Drugs Gene Mutations dbSNP ID ESP MAF ExAC MAF PK parameters
African American European American
Docetaxel ABCB1 c.1236T>C rs1128203 0.22 0.43 0.54 CL [1]
c.3435T>C rs1045642 0.23 0.48 0.50 CL [192]
Paclitaxel ABCB1 c.1236T>C rs1128203 0.22 0.43 0.54 AUC [193]
c.2677T>A/G rs2032582 nr nr 0.54 AUC [193]
Etoposide ABCB1 c.3435T>C rs1045642 0.77 0.47 0.50 CL [194]
Doxorubicin ABCB1 c.1236T>C rs1128203 0.22 0.43 0.54 C max [106]
c.2677T>A/G rs2032582 nr nr 0.54 CL [106]
SLC22A16 c.146A>G rs714368 0.36 0.22 0.25 AUC [195]
c.312T>C rs6907567 0.36 0.22 0.25 AUC [195]
Irinotecan ABCB1 c.1236T>C rs1128203 0.22 0.43 0.54 AUC, CL [110]
Hap*2 CL [111]
Bicalutamide ABCG2 c.421C>A rs2231142 0.03 0.11 0.12 AUC, T max, C max, t 1/2, CL plasma concentrations [113]
Topotecan ABCG2 c.421C>A rs2231142 0.03 0.11 0.12 F [196]
Imatinib ABCB1 c.1236T>C rs1128203 0.22 0.43 0.54 C min, CL, F [116, 117]
c.2677T>A/G rs2032582 nr nr 0.54 CL, F [117]
c.3435T>C rs1045642 0.23 0.48 0.50 CL, F [117]
Hap*4 C min [116]
ABCG2 c.421C>A rs2231142 0.03 0.11 0.12 C min, CL [118, 119]
SLC22A1 c.480C>G rs683369 0.05 0.22 0.17 CL, C min [128]
Gefitinib ABCG2 c.421C>A rs2231142 0.03 0.11 0.12 C ss,min/C 1,min [123]
Sunitinib ABCB1 c.2677T>A/G rs2032582 nr nr 0.54 CL [31]

The drug accumulation at the steady-state was assessed as the ratio of C ss,min to C 1,min, where C ss,min was the average pretreatment concentration on days 8, 15, 22 and 28, and C 1,min was the pretreatment concentration before the second dose

AUC area under the curve, ExAc Exome Aggregation Consortium, ESP Exome Sequencing Project, CL clearance, C max maximum plasma concentration, C min trough plasma concentration, C ss,min /C 1,min, F oral bioavailability, MAF minor allele frequency, nr not reported, PK pharmacokinetic, T max time to maximum plasma concentration, t 1/2 elimination half-life