Obeticholic Acid + Rosuvastatin = Unknown or no reaction

Effect on Concentration

Obeticholic Acid
Increase
Applies within class?
No
Rosuvastatin
Decrease
Applies within class?
No

Pharmacologic Effects

Obeticholic Acid
Effect
N/A
Applies within class?
No
Rosuvastatin
Effect
N/A
Applies within class?
No

Interaction History

N/A

Last Updated 20-Jul-2018

Summary

Sources

Obeticholic Acid Versus Rosuvastatin ^

Study Design

Obeticholic acid (OCA), a potent and selective farnesoid X receptor agonist, is indicated for the treatment of primary biliary cholangitis (PBC). We investigated the potential drug–drug interaction effect of OCA on metabolic CYP450 enzymes and drug transporters. Methods: Five phase 1 single-center, openlabel, fixed-sequence, inpatient studies were conducted in healthy adult subjects to evaluate the effect of oral daily doses of 10 or 25 mg OCA on single-dose plasma pharmacokinetics of specific probe substrates for enzymes CYP1A2 (caffeine, R-warfarin), CYP3A (midazolam, Rwarfarin), CYP2C9 (S-warfarin), CYP2D6 (dextromethorphan), CYP2C19 (omeprazole), and drug transporters, BCRP/OATP1B1/OATP1B3 (rosuvastatin), and P-gp (digoxin).

Study Results

Following multiple doses of OCA 10mg QD, AUC and Cmax increased by 22% and 27% respectively. Following multiple doses of OCA 25mg QD, AUC and Cmax of rosuvastatin decreased by 30% and 26% respectively.

Study Conclusions

Per the investigators, the changes in systemic exposures to rosuvastatin were small thus no dose adjustment is needed when co-administering with OCA.

References

Edwards JE, Eliot L, Parkinson A, Karan S, MacConell L. Assessment of pharmacokinetic interactions between obeticholic acid and caffeine, midazolam, warfarin, dextromethorphan, omeprazole, rosuvastatin, and digoxin in phase 1 studies in healthy subjects. Advances In Therapy. 2017; 9: 2120-2138.