TABLE 5

Compounds considered as in vivo BCRP inhibitors, based on in vitro IC50 or Ki values <10 μM

IC50 and Ki values are presented as reported in the respective references.

PrecipitantTherapeutic ClassKiIC50Reference
μM
AfatinibKinase inhibitors0.75http://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/201292Orig1s000TOC.cfm
AripiprazoleAntipsychotics3.5Nagasaka et al., 2012
AxitinibKinase inhibitors4.4Reyner et al., 2013
CurcuminFood products1.6Kusuhara et al., 2012
CyclosporineImmunosuppressants6.713.4aXia et al., 2007
ElacridarDrug distribution modulators0.31Si et al., 2013
ErlotinibKinase inhibitors0.150.13Noguchi et al., 2009
FluvastatinHMG-CoA reductase inhibitors (statins)5.4310.86aHirano et al., 2005
Fumitremorgin CNone0.550.25Noguchi et al., 2009
GefitinibKinase inhibitors1.01Yanase et al., 2004
IvermectinAntiparasitics1.42.8aJani et al., 2011
Ko143Transporter modulators0.013Xia et al., 2007
LapatinibKinase inhibitors0.025Polli et al., 2008
NilotinibKinase inhibitors0.691.38aTiwari et al., 2009
NovobiocinAntibiotics0.063Elsby et al., 2011
PantoprazoleProton pump inhibitors5.5Suzuki et al., 2009
PitavastatinHMG-CoA reductase inhibitors (statins)2.925.84aHirano et al., 2005
PonatinibKinase inhibitors0.013http://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203469Orig1s000TOC.cfm
QuercetinFood products0.6Saito et al., 2006
Quizartinib (AC220)Kinase inhibitors0.5Bhullar et al., 2013
RabeprazoleProton pump inhibitors8.5Suzuki et al., 2009
RegorafenibKinase inhibitors0.0447http://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203085Orig1s000TOC.cfm
RilpivirineNonnucleoside reverse transcriptase inhibitors1.5Weiss and Haefeli, 2013
SulfasalazineNonsteroidal anti-inflammatory drugs0.46Elsby et al., 2011
SunitinibKinase inhibitors0.320.64aKawahara et al., 2010
TacrolimusImmunosuppressants6Saito et al., 2006
TeriflunomideOther immunomodulators0.146http://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/202992Orig1s000TOC.cfm
TrametinibKinase inhibitors1.1http://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/204114Orig1s000TOC.cfm
TrifluoperazineAntipsychotics7.56 Pan et al., 2013
VismodegibCancer treatments2.4http://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203388Orig1s000TOC.cfm
  • a IC50 value was calculated as 2 × Ki, assuming linearity.