Table 2.

Examples of in vitro and clinical studies that have investigated the effects of common drug transporter polymorphisms on drug transport

Drug transporter and polymorphism	Drug	In vitro effect on drug transport	Reference	Clinical effect on PK	Reference
ABCB1
3435C>T	Digoxin	No sign, change in digoxin transport in LLC-PK1 cells expressing SNP	[150]	Increased digoxin Cmax in T/T genotype Decreased digoxin AUC in T/T genotype	[93] [151]
ABCG2
421C>A	Topotecan	Increased topotecan accumulation in cells transfected with 421A	[121]	Increased AUCoral of topotecan in heterozygous C421A patients	[131]
	Imatinib	Increased imatinib accumulation in cells transfected with 421A	[131]	No significant differences in PK parameters of imatinib in heterozygous C421A patients (vs. wild-type)	[131]
OATP1B1
521T>C 388A>G	Simvastatin, Pravastatin, Atorvastatin, Cerivastatin	Decreased statin uptake in HEK293 cells transfected with OATPlBl*5 (521T>C), *15 (388A>G, 521T>C) and *15+C1007G	[152]	Increased pravastatin AUC in heterozygous OATPlBl*5 and *15 healthy volunteers compared to noncarriers of these variants	[153]
	Docetaxel	Decreased docetaxel uptake in Flp-In T-Rex293 cells transfected with OATPlBl*5 or *15	[38]	No significant association between docetaxel CL and 521T>C or 388G>A variants in cancer patients	[38]
OATP1B3
334T>G 699G>A IVS 12–5676A>G	Docetaxel	No in vitro studies regarding OATP1B3 genetic variants and docetaxel transport		In 334T>G, 699G>A, IVS 12–5676A>G variants no association with docetaxel CL was observed Homozygous IVS 12–5676A>G variant showed sign, higher ALTC and lower CL of docetaxel compared to AA +AG genotypes	[38] [132]

PK pharmacokinetics, C_max maximum plasma concentration, CL systemic clearance, AUC area under the concentration vs. time curve, SNP single-nucleotide polymorphism