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. Author manuscript; available in PMC: 2021 Aug 17.
Published in final edited form as: AAPS J. 2020 Aug 17;22(5):111. doi: 10.1208/s12248-020-00469-6

Table I:

Substrate Specificities of Victim Drugs and Inhibitory Potential of Perpetrator Drugs for Metabolic Enzymes and Xenobiotic Transporters from Investigated Oral Drug-Drug Interactions

Victim Drug Dose BDDCS Class Substrate Specificity Perpetrator Drug Dose BDDCS Class Inhibitory Specificity Reference
Rosuvastatin (Single Dose) 20 mg PO 3 BCRP
OATP1B1
OATP1B3
Rifampin (Single Dose) 600 mg IV infusion 2 BCRP
OATP1B1
OATP1B3
CYP3A
(20,21)
Talinolol (Multiple Dose) 100 mg PO 7 Days 3 P-gp Rifampin (Multiple Dose) 600 mg PO q.d. 9 Days 2 (Inducer)
CYP3A
CYP2C9
P-gp
(22,54)
Triazolam (Single Dose) 0.25 mg PO 1 CYP3A Fluconazole (Multiple Dose) 100 mg PO q.d. 4 Days 3 CYP3A
CYP2C19
CYP2C9
(20,23)
Omeprazole (Multiple Dose) 40 mg PO 6 Days 1 CYP2C19
CYP3A (minor)
Clarithromycin (Multiple Dose) 500 mg PO t.i.d 5.33 Days 3 CYP3A
CYP2C19
P-gp
(20,24)
Apixaban (Single Dose) 10 mg PO 1 CYP3A
P-gp
Rifampin (Multiple Dose) 600 mg PO q.d. 11 Days 2 (Inducer)
CYP3A
P-gp
(25,54)

Intestinally expressed enzyme and transporters are highlighted in bold

Abbreviations: BCRP, Breast Cancer Resistance Protein; BDDCS, Biopharmaceutics Drug Disposition Classification System; CYP, Cytochrome P450; IV, Intravenous; OATP, Organic Anion-Transporting Protein; P-gp, P-glycoprotein