Impact of interaction depends on dose of asunaprevir used along with concomitant drugs.
Asunaprevir versus Sertraline
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Study Design
In a drug-drug interaction study in healthy volunteers (n = 18), fasted men and women received sertraline (SER) 10 mg once daily on days 1-7 and 25-31, and asunaprevir (ASV) 100 mg twice daily on days 15-31.1 Blood samples for pharmacokinetic (PK) analyses were collected over 24 hours on days 7 and 31 for SER, and those for ASV were collected over 12 hours on days 24 and 31.
Study Results
The geometric mean ratios (GMRs; ASV + SER / SER) [90% CIs] of SER were 0.81 [0.67, 0.97] for Cmax and 0.79 [0.67, 0.94] for AUC, while GMRs (SER + ASV / ASV) [90% CIs] of ASV were 0.94 [0.70, 1.28] for Cmax and 0.88 [0.70, 1.11] for AUC.
Study Conclusions
. The investigators concluded that no dose adjustment is necessary when ASV 100mg and SER 50mg are co-administered. The concomitant use of the DCV-TRIO (DCV 30 mg, ASV 200 mg, BCV 75 mg twice daily) and SER 50 mg once daily resulted in significantly reduced exposure and plasma concentrations of SER.2 Therefore, monitoring for changes in depressive symptoms is warranted when this combination is utilized, and up-titration of SER should be considered if appropriate. **In this study DCV-TRIO was administered with additional BCV 75mg BID in order to achieve BCV exposures comparable to those seen in HCV-infected individuals.
References
Eley T, Garimella T, Li W, Bertz RJ. Asunaprevir: a review of preclinical and clinical pharmacokinetics and drug–drug interactions. Clinical Pharmacokinetics. 2015; 12: 1205-1222.
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