Table 2.

Summary of the drug transporters that efflux or uptake ARVs.

Antiretroviral drug class	Antiretroviral drugs	BCS Class	ABC transporters	SLC transporters
Entry inhibitors (EIs)	Maraviroc†	3	P-gp	OATP1B1
Nucleoside/nucleotide reverse transcriptase inhibitor (NRTIs)	Lamivudine	3	BCRP	OCT1, OCT2, CNT1
	Emtricitabine†	3	MRP1
	Tenofovir DF†	3	P-gp
	Tenofovir†	3	MRP4, MRP7	OAT1, OAT3
	Abacavir	1	P-gp, BCRP, MRP4
	Zidovudine	1	BCRP, MRP4	OAT1, OAT2, OAT3, CNT1, CNT3, ENT2
	Didanosine	3	BCRP	CNT2, CNT3, ENT1, ENT2
	Stavudine	1	BCRP, MRP5	CNT1
Non-nucleoside reverse transcriptase inhibitors (NNRTIs)	Efavirenz	2
	Nevirapine	2	MRP7
	Delavirdine	1
	Etravirine	4
Protease inhibitors (PIs)	Atazanavir	2	P-gp, MRP1, MRP2
	Ritonavir	2	P-gp, MRP1, MRP2
	Fosamprenavir	2
	Amprenavir	2	P-gp
	Lopinavir	2	P-gp, MRP1, MRP2	OATP1A2, OATP1B1
	Saquinavir	2	P-gp, MRP1, MRP2	OATP1A2, OATP1B1
	Darunavir	2	P-gp	OATP1A2, OATP1B1
	Indinavir	2	P-gp, MRP1, MRP2
	Tipranavir	2	P-gp
	Nelfinavir	2	P-gp
Integrase inhibitors (IIs)	Raltegravir†	2	P-gp, BCRP*

The drug-transporter interactions listed in this table are adapted from a review by Kis et al [58].

^*Obtained from reference [173].

A number of these drugs are already undergoing clinical testing (denoted by ^†) toward the development of PrEP products, including MVC, emtricitabine, TFV, TDF, and raltegravir. The currently available transporter inhibitors of ARVs were reviewed previously by O. Kis et al [58].