Table 2.
Rifampin-induced changes in gene expression of clinically relevant drug transporters.
| Common name | Gene name | Fold change | p-value | FDR | Example of substrates* |
|---|---|---|---|---|---|
| OSTbeta | SLC51B | 12.67 | 1.20E-113 | 4.90E-111 | Bile acids, conjugated steroids |
| MRP2 | ABCC2 | 1.85 | 3.56E-23 | 2.92E-21 | Chemotherapy, statin, antepileptics, tamoxifen, DMARDs, antidepressants, clopidogrel, anti-retroviral |
| MDR1 | ABCB1 | 1.72 | 6.63E-18 | 3.02E-16 | Chemotherapy, statin, antepileptics, tamoxifen, DMARDs, antidepressants, clopidogrel, anti-retroviral |
| OATP2B1 | SLCO2B1 | 1.73 | 2.34E-16 | 8.73E-15 | Fexofenadine, montelukast, grapefruit, orange juice, apple juice, endogenous steroids |
| MRP6 | ABCC6 | 1.65 | 5.82E-14 | 1.84E-12 | Thalidomide, docetaxel |
| OATP1B3 | SLCO1B3 | −1.57 | 2.15E-11 | 5.18E-10 | Irinotecan, docetaxe, myophenolate, statin, methotrexate |
| OATP4C1 | SLCO4C1 | 1.46 | 2.84E-07 | 3.88E-06 | Estrone 3-sulfate |
| MATE1 | SLC47A1 | 1.37 | 2.64E-06 | 2.84E-05 | Meformin, trimethoprim |
| ENT1 | SLC29A1 | 1.38 | 4.68E-06 | 4.80E-05 | Gemcitabine, paclitaxe, gemcitabine, peginterferon, ribavirin |
| OAT7 | SLC22A9 | −1.34 | 9.76E-05 | 0.0007 | Methotrexate |
| PEPT1 | SLC15A1 | −1.27 | 5.01E-04 | 0.0031 | Statin, oseltamivir |
| MRP3 | ABCC3 | 1.18 | 0.0098 | 0.038 | Cisplatin, MTX, doxorbuicn, cyclophosphamide, clopidogrel, codiene, morphine, etoposide |
| OSTalpha | SLC51A | 1.21 | 0.014 | 0.050 | Bile acids, conjugated steroids |
| BCRP | ABCG2 | 1.18 | 0.015 | 0.054 | Antiepileptics, MTX, statin, anti-retrovirals, tecans, anti-neoplastics (irinotecan, platinum, anthracycline, taxane) acetaminophen, uric acid |
| OCT1 | SLC22A1 | −1.16 | 0.019 | 0.060 | Morphine, metformin, tramadol, antiemetics, dopamine agonist, antiretrovirals, sorafinib |
| OAT2 | SLC22A7 | −1.15 | 0.040 | 0.11 | Fluoropyrimidine, zidovudine |
| MRP5 | ABCC5 | 1.17 | 0.066 | 0.16 | Antiepileptics, irinotecan |
| MRP4 | ABCC4 | 1.17 | 0.090 | 0.21 | cisplatin, antiretroviral, bisphosphonates, MTX, acetaminophen, azathioprine, mercaptopurine |
| NTCP | SLC10A1 | −1.08 | 0.21 | 0.39 | Bile acids |
| OCTN2 | SLC22A5 | −1.08 | 0.30 | 0.51 | Imatinib, oxaliplatin |
| BSEP | ABCB11 | −1.07 | 0.32 | 0.55 | Statin |
| OATP1B1 | SLCO1B1 | 1.04 | 0.57 | 0.74 | Simvastatin, statin, rifampin, irinotecan, methotrexate, thyroid, estrone sulfate, angiotensin receptor blocker, MTX, caspofungin, ace inhibitor |
| MCT1 | SLC16A1 | 1.03 | 0.61 | 0.78 | Lactate |
| ENT2 | SLC29A2 | −1.03 | 0.89 | 0.94 | Gemcitabine, thiopurine |
Primary human hepatocytes were treated with 10 μM Rifampin or vehicle for 24 h. Fold-change is the ratio of gene expression treatment/control. A fold-change equal 1 is defined as no change, and a fold change of 2 is defined as 2x the expression. FDR, False Discovery Rate.
*
Cited from PharmGKB.org.