Compound | Estimated CYP3A5 Contribution (In Vitro) % | Clinical Impact of CYP3A5 Reported? | CYP3A5*1 Statusa | N | CL/F | Cmax | Cmin | References |
---|---|---|---|---|---|---|---|---|
% Change Compared with Nonexpressers (CYP3A5*3/*3) | ||||||||
Atazanavir | 82 | Yes | Expresser | 15 | +39b | −18 | −49b | Anderson et al., 2009 |
Yes | Expresser | 12 | +42b | Savic, et al., 2012 | ||||
Vincristine | 75 | Yes | Heterozygous | 11 | +∼100b,d | Egbelakin, et al., 2011 | ||
No | Heterozygous | 12 | +7 | Guilhaumou, et al., 2011 | ||||
Midazolam | 49 | No | Heterozygous | 22 | +12c | de Jonge et al., 2013 | ||
No | Heterozygous | 22 | +22 | −14 | de Jonge et al., 2013 | |||
No | Homozygous | 3 | +33c | Goh et al., 2002 | ||||
Yes | Heterozygous | 13 | +27b,c | Goh et al., 2002 | ||||
Yes | Expresser | 21 | +25b | Elens, et al., 2013 | ||||
No | Homozygous | 8 | −16 | Kharasch, et al., 2007 | ||||
No | Heterozygous | 28 | +3 | Kharasch, et al., 2007 | ||||
No | Homozygous | 6 | +1 | Tomalik-Scharte, et al., 2008 | ||||
No | Heterozygous | 17 | −4 | Tomalik-Scharte, et al., 2008 | ||||
No | Homozygous | 16 | −18c | Floyd, et al., 2003 | ||||
No | Heterozygous | 23 | −13c | Floyd, et al., 2003 | ||||
Vardenafil | 49 | Yes | Homozygous | 6 | +200b | −68b | Shon et al., 2011 | |
Yes | Heterozygous | 7 | +89b | −45b | Shon et al., 2011 | |||
Otenabant | 48 | Yes | Homozygous | 8 | +214b | Goosen et al., 2010 | ||
Yes | Expresser | 36 | +83b | Goosen et al., 2010 | ||||
Verapamil | 41 | Yes | Expresser | 13 | +90b,e | −86b,e | Jin, et al., 2007 | |
Tacrolimus | 41 | Yes | Heterozygous | 10 | +76b | −38b | −58b | de Jonge et al., 2012 |
Yes | Expresser | 12 | +55b | −25b | −50b | Zheng et al., 2012 | ||
Yes | Homozygous | 8 | — | −70b | Kim et al., 2012 | |||
Yes | Heterozygous | 44 | — | −54b | Kim et al., 2012 | |||
Yes | Heterozygous | 53 | — | −52b | Santoro et al., 2013 | |||
Rimonabant | 36 | Yes | Ethnicity Study | +75b | EMEA, 2009 | |||
Indinavir | 35 | Yes | Expresser | 11 | +44b | Anderson et al., 2006 | ||
No | Heterozygous | 6 | +45 | Solas et al., 2007 | ||||
Cilostazol | 24 | Yes | Homozygous | 4 | +49b | Yoo et al., 2009 | ||
Yes | Heterozygous | 20 | +34b | Yoo et al., 2009 | ||||
Simvastatin | 17 | No | Expresser | 10 | −12 | +22 | Zhou et al., 2013 | |
Yes | Homozygous | 4 | +256b | −44 | Kim et al., 2007 | |||
No | Heterozygous | 8 | +58 | −21 | Kim et al., 2007 | |||
Diltiazem | 14 | No | Expresser | 19 | −28 | +31 | Zheng et al., 2013 | |
No | Homozygous | 3 | −38 | +51 | Yamamoto et al., 2005 | |||
No | Heterozygous | 6 | −33 | +51 | Yamamoto et al., 2005 | |||
Nifedipine | 14 | Yes | Heterozygous | 3 | +171b | −46 | Haas et al., 2013 | |
Yes | Expresser | 5 | −50b | Haas et al., 2013 | ||||
No | Heterozygous | 8 | −30 | +4.5 | Fukuda et al., 2004 | |||
Saquinavir | 11 | No | Homozygous | 16 | +52 | −29 | Josephson et al., 2007 | |
Yes | Expresser | 6 | +90b | −68b | Mouly et al., 2005 | |||
Alprazolam | <10 | Nes | Homozygous | 5 | +40b | −31b | Park et al., 2006 | |
Nes | Heterozygous | 7 | +16 | −28b | Park et al., 2006 | |||
Quetiapine | <10 | No | Heterozygous | 4 | — | +10f | Nikisch et al., 2011 | |
Oxycodone | <10 | No | Expresser | 25 | — | −6.6 | Naito et al., 2011 | |
Erythromycin | <10 | No | Expresser | 5 | +6.3c | Elens et al., 2013 | ||
Everolimus | <10 | No | Heterozygous | 7 | +12 | −15 | −11 | Picard et al., 2011 |
↵a Homozygous = *1/*1; Heterozygous = one *1 allele and one other allele (i.e., *3, *6, or *7; Expresser = mixed genotype wherein each subject had at least one *1 allele.
↵b Denotes clinical findings that were claimed to be statistically significant.
↵c Denotes clearance determined from an intravenous dose. All other clearance values are CL/F.
↵d Vincristine demonstrated a two fold increase in metabolite/parent ratio in *1 carriers.
↵e CL/F and Cmax differences were averaged for individual values reported for R- and S-verapamil.
↵f Value reported is steady-state plasma concentration.