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Most of the drug transporters can also be molecularly and mechanistically classified as a member of the ABC transporter family or the SLC transporter family (Table 1.1).

ABC (ATP‐binding cassette) transporters is a family of membrane transport proteins that require ATP hydrolysis for the transport of substrates across membranes. Therefore, ABC transporters are primary active transporters. The protein family derives its name from the ATP‐binding domain found on the protein. The best studied drug transporters, which are classified as ABC transporters, are multidrug resistance protein (MDR), multidrug resistance‐associated protein (MRP), and breast cancer resistance protein (BCRP).

Some of the SLC (Solute Carrier) transporters utilize an electrochemical potential difference of the transported substrate and are therefore classified as facilitated transporters; other SLC transporters utilize an ion gradient, such as sodium and proton gradients across the membrane produced by the primary active transporters, and transport substrates against an electrochemical difference. These transporters are classified as secondary active transporters. In contrast to ABC transporters, SLC transporters do not possess ATP‐binding sites. Most drug transporters belong to SLC transporters.

TABLE 1.1 Classifications of representative drug transporters

Transporters family	Family member	Gene name	Human chromosome locus	References
Organic cation transporter (OCT)	hOCT1	SLC22A1	6q26	[1]
	hOCT2	SLC22A2	6q26	[1]
	hOCT3	SLC22A3	6q26‐q27	[2]
Zwitterion transporters	OCTN1	SLC22A4	5q31.1	[3]
	OCTN2	SLC22A5	5q31	[4]
	OCTN3	SLC22A21	5q31	[5]
	FLIPT1	SLC22A15	1p13.1	[6]
	CT2 (OCT6)	SLC22A16	6q21‐q22.1	[7]
Organic anion transporter (OAT)	OAT1	SLC22A6	11q13.1‐q13.2	[8]
	OAT2	SLC22A7	6p21.2‐p21.1	[9]
	OAT3	SLC22A8	11q11.7	[10]
	OAT4	SLC22A11	11q13.1	[11]
	OAT7	SLC22A9	11q12.3	[12]
	OAT10	SLC22A13	3p22.2	[13]
	URAT1	SLC22A12	11q13.1	[11]
Organic anion transporter polypeptides (OATP)	OATP1C1	SLCO1C1	12p12.2	[14]
	OATP1B1	SLCO1B1	12p12.2	[15]
	OATP1A2	SLCO1A2	12p12	[14]
	OATP1B3	SLCO1B3	12p12	[16]
	OATP2A1	SLCO2A1	3q21	[17]
	OATP2B1	SLCO2B1	11q13	[18]
	OATP3A1	SLCO3A1	15q26	[19]
	OATP4A1	SLCO4A1	20q13.33	[19]
	OATP4C1	SLCO4C1	5q21.2	[20]
	OATP5A1	SLCO5A1	8q13.3	[21]
	OATP6A1	SLCO6A1	5q21.1	[22]
Peptide transporter (PEPT)	PEPT1	SLC15A1	13q33‐q34	[23]
	PEPT2	SLC15A2	3q21.1	[24]
	PHT1	SLC15A4	12q24.32	[25]
	PHT2	SLC15A3	11q12.2	[26]
Monocarboxylate transporters (MCT, sMCT)	MCT1	SLC16A1	1p12	[26]
	MCT2	SLC16A7	12q13	[27]
	MCT3	SLC16A8	22q12.3‐q13.2	[28]
	MCT4	SLC16A3	17q25	[29]
	SMCT1	SLC5A8	12q23.1	[30]
	SMCT2	SLC5A12	11p14.2	[31]
Nucleoside transporters (CNT, ENT)	CNT1	SLC28A1	15q25‐26	[32]
	CNT2	SLC28A2	15q15	[33]
	CNT3	SLC28A3	9q22.2	[34]
	ENT1	SLC29A1	6p21.1‐p21.2	[35]
	ENT2	SLC29A2	11q13	[36]
	ENT3	SLC29A3	10q22.1	[37]
	ENT4	SLC29A4	7p22.1	[38]
Bile acid transporters	NTCP	SLC10A1	14q24.1	[39]
	ASBT	SLC10A2	13q33	[40]
	BSEP	ABCB11	2q24	[41]
	OST‐alpha	SLC51A	3q29	[42]
	OST‐beta	SLC51B	15q22.31 (Mapview)	[42]
P‐glycoprotein	MDR1	ABCB1	7q21.1	[43]
	MDR3	ABCB4	7q21.12	[44]
Multidrug resistance protein (MRP)	MRP1	ABCC1	16p13.1	[45]
	MRP2	ABCC2	10q24	[46]
	MRP3	ABCC3	17q22	[47]
	MRP4	ABCC4	13q32	[48]
	MRP5	ABCC5	3q27	[49]
	MRP6	ABCC6	16p13.1	[50]
	MRP7	ABCC10	6p21.1	[51]
	MRP8	ABCC11	16q12.1	[52]
	MRP9	ABCC12	16q12.1	[52]
Breast cancer resistance protein	BCRP	ABCG2	4q22	[53]
Multidrug and toxin extrusion protein	MATE1	SLC47A1	17p11.2	[54]
	MATE2	SLC47A2	17p11.2	[54]
Monoamine transporters	SERT	SLC6A4	17q11.2	[55]
	NET	SLC6A2	16q12.2	[56]
Folate transporters	RFT1	SLC19A1	21q22.3	[57]
	PCFT	SLC46A1	17q11.2	[58]

References listed above are those where the human chromosome locus were reported.