Drug name  Drug class  Summary  References
Abacavir  NRTI  P-gp substrate. Inhibits MRP-1, MRP-2 and MRP-3 in a concentration-dependent manner. BCRP substratea  Shaik et al. (2007), Giri et al. (2008), Weiss et al. (2007), Pan et al. (2007)
Zidovudine (AZT)  NRTI  P-gp substrate, MRP-4 and MRP-5 substrate, BCRP substrate.a Removed by a member of the OAT family. OAT1 and OAT3 likely to be responsible for its uptake. OCT possibly involved in uptake. Transported by ENT2. Transported by CNT1 and CNT3  Gollapudi and Gupta (1990), Eilers et al. (2008), Wang and Baba (2005), Wang et al. (2004), Pan et al. (2007), Takasawa et al. (1997), Gibbs and Thomas (2002), Strazielle et al. (2003), Minuesa et al. (2008), Baldwin et al. (2004), Yao et al. (2001), Strazielle et al. (2003)
Nevirapine  NNRTI  Strongly induces the expression and function of P-gp. Inhibits MRP-1, MRP-2 and MRP-3 in a concentration-dependent manner  Stormer et al. (2002), Weiss et al. (2007)
Efavirenz  NNRTI  Induces the expression and function of P-gp. Strongly inhibits MRP-1, MRP-2 and MRP-3 in a concentration-dependent manner  Stormer et al. (2002), Weiss et al. (2007)
Delaviridine  NNRTI  Induces the expression and function of P-gp. Strongly inhibits MRP-1, MRP-2 and MRP-3 in a concentration-dependent manner  Stormer et al. (2002), Weiss et al. (2007)
Ritonavir  PI  P-gp substrate. Increased P-gp activity and expression in a concentration dependent manner. MRP-1 and MRP-2 substrate. Induces the expression of MRP-1 in a concentration-dependent manner. BCRP inhibitor. Possible OCT1 and OCT2 inhibitor  Polli et al. (1999), Perloff et al. (2007), Park and Sinko (2005), Janneh et al. (2005, 2007), Eilers et al. (2008), Gimenez et al. (2004), Gupta et al. (2004), Jung et al. (2008)
Saquinavir  PI  P-gp substrate. MRP-1 and MRP-2 substrate. BCRP inhibitor. Possible OCT1 and OCT2 inhibitor  Kim et al. (1998), Polli et al. (1999), Park and Sinko (2005), Janneh et al. (2005, 2007), Eilers et al. (2008), Gupta et al. (2004), Jung et al. (2008)
Lopanivir  PI  MRP-1 and MRP-2 substrate  Park and Sinko (2005), Janneh et al. (2005, 2007), Eilers et al. (2008)
Emtricitabine  NRTI  Strongly inhibits MRP-1, MRP-2 and MRP-3 in a concentration-dependent manner  Weiss et al. (2007)
Lamivudine (3TC)  NRTI  Inhibits MRP-1, MRP-2 and MRP-3 in a concentration dependent manner. Oatp-2 like transporter has been implicated in its uptake. OCT possibly involved in uptake. OCT1 and OCT2 substrate  Weiss et al. (2007), Gibbs and Thomas (2002), Gibbs et al. (2003a,b), Minuesa et al. (2008), Jung et al. (2008)
Tenofovir (PMPA)  NtRTI  Inhibits MRP-1, MRP-2 and MRP-3 in a concentration dependent manner. OAT1 and OAT3 are high- and low-affinity transporters of PMPA, respectively  Weiss et al. (2007), Cihlar et al. (2001), Izzedine et al. (2005)
Nelfinavir  PI  P-gp substrate. BCRP inhibitor. Possible OCT1 and OCT2 inhibitor  Kim et al. (1998), Gupta et al. (2004), Jung et al. (2008)
Zalcitabine (ddC)  NRTI  OATP has been implicated in its removal. Removed by a member of the OAT family. OAT1 and OAT3 likely to be responsible for its uptake. OCT1 and OCT2 substrate. Transported by ENT2. Transported by CNT3  Gibbs and Thomas (2002), Takasawa et al. (1997), Gibbs and Thomas (2002), Strazielle et al. (2003), Jung et al. (2008), Baldwin et al. (2004), Minuesa et al. (2008)
Didanosine (ddI)  NRTI  Oatp-2 like transporter has been implicated in its uptake. Transported by ENT1 across guinea pig BBB. Transported by ENT2. Transported by CNT1.b Transported by CNT3  Gibbs and Thomas (2002), Gibbs et al. (2003a,b), Baldwin et al. (2004), Li et al. (2001), Minuesa et al. (2008)
Indinavir  PI  P-gp substrate. Possible OCT1 and OCT2 inhibitor.  Kim et al. (1998), Polli et al. (1999), Jung et al. (2008)
Stavudine (d4T)  NRTI  Transported by CNT1b  Minuesa et al. (2008)
Amprenavir  PI  P-gp substrate  Polli et al. (1999), Choo et al. (2000)