SUBTYPE:Transporter Assays
APPLICATION & SPECIALITY USES:ADME-Toxicology Products and Services

Our OPTI-DDI Panel consists of transporters that are often implicated in clinically-significant drug-drug interactions (DDIs). Because drug transporters can determine systemic circulation and tissue exposure of substrate drugs, and drugs can impact the expression and function of transporters, it is critical to investigate potential DDI effects in the lead selection process. Our OPTI-DDI Panel research services can be customized from to assess the DDI liability of drug candidates.

Endogenous metabolites can be transporter substrates, and so have the potential to serve as biomarkers for transporter function in vivo in humans. Therefore, selecting appropriate clinical probe drugs and biomarkers is key to determining clinical risk for transporter inhibition. As part of our collaborative research programs, we provide advice on clinically-relevant probes and endogenous biomarkers to predict transporter-mediated DDIs.

In addition to transporter DDI studies for use in drug discovery we offer OPTI-REGULATORY Panel research services to provide data for IND submissions. Our IND-enabling studies are designed to comply with the published guidance from regulatory agencies.

The table below lists transporters that are associated with clinically-significant DDIs.

TransporterFDAEMAPMDAPharmacokinetic relevanceRepresentative substratesRepresentative inhibitors
BCRPIntestinal absorption, BBB penetration, hepatic and renal clearanceE17bG, CCK-8,
methothrexate, prazosin,
rosuvastatin, sulfasalazine, topotecan
Ko143, chrysin,
elacridar, cyclosporine, gefitinib, erlotinib
BSEPHepatic clearance and DILITaurocholate, glycocholate, lithocholate, bosentan, pravastatinRifampicin, cyclosporine, benzbromarone, troglitazone, clofazimine
MATE1LikelyRenal clearanceMetformin, creatinine, TEA, oxaliplatin, cimetidineCimetidine, ondansetrone, ritonavir, famotidine, imatinib
MATE2-KLikelyRenal clearanceMetformin, creatinine, TEA, oxaliplatin, cimetidineCimetidine, mitoxantrone, ondansetrone, nifekalant, imatinib
OAT1Renal clearancePAH, adefovir, cidofovir, tenofovir, olmesartanProbenecid, mefenamic acid, ketoprofen, indomethacin, olmesartan
OAT3Renal clearancePAH, E3S, methotrexate, acyclovir, peniciliin GProbenecid, diclofenic, furosemide, indomethacin, olmesartan
OATP1B1Hepatic clearanceE17bG, atorvastatin, rosuvastatin, pravastatin, bilirubinCyclosporine, rifampicin, gemfibrozil, ritonavir, lopinavir
OATP1B3Hepatic clearanceCCK8, rosuvastatin, pitavastatin, telmisartan, bilirubinCyclosporine, rifampicin, ritonavir, lopinavir, MK-571
OATP2B1Hepatic uptake; intestinal uptakeEstrone-3-sulfateBromosulfophthalein
OCT1ConsiderHepatic clearanceMetformin, MPP+, TEA, oxaliplatinCimetidine, quinidine, disopyramide, rosiglitazone, clonidine
OCT2Renal clearanceMetformin, creatinine, TEA, oxaliplatin, famotidineCimetidine, quinidine, dolutegravir, disopyramide, impramine
P-gpIntestinal absorption, BBB penetration, hepatic and renal clearanceDigoxin, quinidine, vinblastine, fexofenadine, atorvastatinElacridar, verapamil, ketoconazole, cyclosporine, ritonavir
THTR1Vitamin transportThiamineAmprolium
THTR2Vitamin transportThiamineAmprolium