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Table 1 Overview of clinical drug–drug interaction studies with oral OCA in healthy, fasted subjects

From: Assessment of Pharmacokinetic Interactions Between Obeticholic Acid and Caffeine, Midazolam, Warfarin, Dextromethorphan, Omeprazole, Rosuvastatin, and Digoxin in Phase 1 Studies in Healthy Subjects

Study OCA administration Probe substrate administration CYP/transporter
Dose Days Probe substrate (oral dose) Days
I 10 and 25 mg QD Day 5 through day 23 Caffeine (200 mg)
Midazolam (2 mg)
Day 3 and day 21
Day 1 and day 19
CYP1A2
CYP3A
II 10 and 25 mg QD Day 8 through day 27 Warfarin (25 mg) Day 1, day 21 CYP2C9 (S-warfarin)
CYP1A2, CYP3A (R-warfarin)
III 10 and 25 mg QD Day 5 through day 28 Dextromethorphan (30 mg)
Omeprazole (20 mg)
Day 1, day 18
Day 4, day 21–28
CYP2D6
CYP2C19
IV 10 and 25 mg QD Day 6 through day 23 Rosuvastatin (20 mg) Day 1, day 19 BCRP/OATP1B1/OATP1B3
V 10 and 25 mg QD Day 6 through day 23 Digoxin (0.25 mg) Day 1, day 19 P-gp (MDR1)
  1. BCRP breast cancer resistance protein, CYP cytochrome P450, MDR1 multidrug resistance protein 1, OATP organic anion transporting polypeptide, QD once daily