PMC:2678986 / 52017-56266 JSONTXT

{"target":"http://pubannotation.org/docs/sourcedb/PMC/sourceid/2678986","sourcedb":"PMC","sourceid":"2678986","source_url":"https://www.ncbi.nlm.nih.gov/pmc/2678986","text":"Table 3 Summary of the current understanding of transporter involvement in anti-HIV drug distribution at blood–CNS interfaces.\nDrug name Drug class Summary References\nAbacavir 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)\nZidovudine (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)\nNevirapine 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)\nEfavirenz 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)\nDelaviridine 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)\nRitonavir 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)\nSaquinavir 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)\nLopanivir PI MRP-1 and MRP-2 substrate Park and Sinko (2005), Janneh et al. (2005, 2007), Eilers et al. (2008)\nEmtricitabine NRTI Strongly inhibits MRP-1, MRP-2 and MRP-3 in a concentration-dependent manner Weiss et al. (2007)\nLamivudine (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)\nTenofovir (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)\nNelfinavir PI P-gp substrate. BCRP inhibitor. Possible OCT1 and OCT2 inhibitor Kim et al. (1998), Gupta et al. (2004), Jung et al. (2008)\nZalcitabine (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)\nDidanosine (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)\nIndinavir PI P-gp substrate. Possible OCT1 and OCT2 inhibitor. Kim et al. (1998), Polli et al. (1999), Jung et al. (2008)\nStavudine (d4T) NRTI Transported by CNT1b Minuesa et al. (2008)\nAmprenavir PI P-gp substrate Polli et al. (1999), Choo et al. (2000)\na Contradictory evidence also exists; see Giri et al. (2008).\nb Contradicting evidence also exists; see Minuesa et al. (2008), Chishty et al. (2004), Chang et al. (2004), Cano-Soldado et al. 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