Antiretrovirals | CYP450s and UGTs Substrates | Membrane transporters of drugs | References | |||
---|---|---|---|---|---|---|
ABC | SLC | |||||
Substrates | Inhibitors | Substrates | Inhibitors | |||
NRTIs and NtRTI | ||||||
Abacavir | UGT1A1 | ABCB1 ABCC4 ABCG2 | OCT1 OCT2 | Pan et al., 2007; Shaik et al., 2007; Weiss et al., 2007a; Yuen et al., 2008; Minuesa et al., 2009 | ||
Didanosine | ABCG2 | Wang et al., 2003 | ||||
Emtricitabine | ABCC1 | ABCC2 | OCT1 OCT2 | Weiss et al., 2007b; Bousquet et al., 2008a; Minuesa et al., 2009 | ||
Lamivudine | ABCC4 ABCG2 | OCT1 OCT2 OCT3 | Leung and Bendayan, 2001; Wang et al., 2003; Anderson et al., 2006; Jung et al., 2008 | |||
Stavudine | ABCG2 | Wang et al., 2003 | ||||
Tenofovir/tenofovir DF | ABCB1 ABCC2 ABCC4 | OAT1 OAT3 OCT1 OCT2 | van Gelder et al., 2002; Mallants et al., 2005; Ray et al., 2006; Minuesa et al., 2009 | |||
Zalcitabine | OCT1 OCT2 | Schuetz et al., 1999; Jung et al., 2008 | ||||
Zidovudine | UGT2B7 | ABCC4 ABCG2 | OAT1 OAT2 OCT1 OCT2 | Barbier et al., 2000; Wang et al., 2003; Pan et al., 2007; Minuesa et al., 2009 | ||
NNRTIs | ||||||
Efavirenz | CYP2B6 UGT2B7 | ABCB1 ABCG2 ABCC1/2 | Mutlib et al., 1999; Ward et al., 2003; Desta et al., 2007; Storch et al., 2007; Weiss et al., 2007a,b; Bélanger et al., 2009; Bousquet et al., 2009 | |||
Etravirine | CYP2C19 CYP3A4/5 | ABCB1 | Seminari et al., 2008 | |||
Nevirapine | CYP2B6 CYP3A4/5 | Erickson et al., 1999; Weiss et al., 2007b; Mahungu et al., 2009a | ||||
Protease inhibitors | ||||||
Atazanavir | CYP3A4/5 | ABCB1 ABCC1 ABCC2 | ABCG2 | OATP2B1 | Le Tiec et al., 2005; Roucairol et al., 2007; Weiss et al., 2007a; Bousquet et al., 2008b; Zastre et al., 2009; Kis et al., 2010 | |
Darunavir | CYP3A4/5 | ABCB1 | OATP1A2 OATP1A3 OATP1B1 | Back et al., 2008; Brown et al., 2009; Fujimoto et al., 2009; Kwan et al., 2009; Hartkoorn et al., 2010; König et al., 2010 | ||
Indinavir | CYP3A4/5 | ABCB1 ABCC1 ABCC2 | OCT1 OATP2B1 | Chiba et al., 1997; Kim et al., 1998b; Koudriakova et al., 1998; Lee et al., 1998; Hugen et al., 2000; Zhang et al., 2000; Hochman et al., 2001; van der Sandt et al., 2001; Huisman et al., 2002; Campbell et al., 2004; Jorajuria et al., 2004; Hamidi, 2006; Jung et al., 2008; Annaert et al., 2010 | ||
Lopinavir | CYP3A4/5 | ABCB1 ABCC1 ABCC2 | ABCG2 | OATP1A2 OATP1A3 OATP1B1 | OATP2B1 | Kumar et al., 1999; Agarwal et al., 2007; Janneh et al., 2007; Weiss et al., 2007a; Hartkoorn et al., 2010; Kis et al., 2010; van Waterschoot et al., 2010 |
Nelfinavir | CYP3A4/5 CYP2C19 | ABCB1 ABCC1 | ABCG2 | OCT1 OCT2 OATP2B1 | Kim et al., 1998b; Choo et al., 2000; Zhang et al., 2000; Baede-van Dijk et al., 2001; Jones et al., 2001a; Jones et al., 2001b; Gupta et al., 2004; Hirani et al., 2004; Salama et al., 2005; Kaddoumi et al., 2007; Weiss et al., 2007a; Hirt et al., 2008; Jung et al., 2008; Kis et al., 2010 | |
Ritonavir | CYP3A4/5 | ABCB1 ABCC1 ABCC2 | ABCG2 | OCT1 OCT2 OATP2B1 | Kumar et al., 1996; Koudriakova et al., 1998; Lee et al., 1998; Zhang et al., 2000; Jones et al., 2001a; Jones et al., 2001b; van der Sandt et al., 2001; Huisman et al., 2002; Gupta et al., 2004; Jung et al., 2008; Zastre et al., 2009; Kis et al., 2010 | |
Saquinavir | CYP3A4/5 | ABCB1 ABCC1 ABCC2 | ABCG2 | OATP1A2 OATP1A3 OATP1B1 | OCT1 | Fitzsimmons and Collins, 1997; Kim et al., 1998a,b; Kupferschmidt et al., 1998; Lee et al., 1998; Srinivas et al., 1998; Eagling et al., 1999, 2002; Choo et al., 2000; Zhang et al., 2000; Jones et al., 2001a; Meaden et al., 2002; Williams et al., 2002; Campbell et al., 2004; Gupta et al., 2004; Maffeo et al., 2004; Su et al., 2004; Janneh et al., 2005; Park and Sinko, 2005; Weiss et al., 2007a; Jung et al., 2008; Hartkoorn et al., 2010 |
Tipranavir | CYP3A4/5 | ABCB1 | OATP2B1 | Yeni, 2003; Vourvahis and Kashuba, 2007; Langmann et al., 2008; Kis et al., 2010 | ||
CCR5 co-receptor inhibitor | ||||||
Maraviroc | CYP3A4/5 | ABCB1 | Walker et al., 2005; Emmelkamp and Rockstroh, 2007; Abel et al., 2008 | |||
Integrase inhibitor | ||||||
Raltegravir | UGT1A1 | ABCB1 | SLC22A6 | Kassahun et al., 2007; Moss et al., 2011 |