Product information and disease description Product description Product information Drug/Drug, drug/disease interactions

Effects of other drugs on bepirovirsen

5 evidence topics · 3 sources

Drug interaction studies and nucleos(t)ide analogue coadministration: prescribing information

“No formal clinical drug interaction studies have been conducted with HIBSAGO. In clinical trials, concomitant administration of HIBSAGO with a NrtI did not result in changes in bepirovirsen exposure.” (opens the prescribing information at this quote)
“Based on in vitro study results, HIBSAGO is not a substrate, inducer or inhibitor of major cytochrome P450 (CYP) enzymes, or drug transporters; therefore, clinically relevant pharmacokinetic interactions are not expected.” (opens the prescribing information at this quote)

Bepirovirsen exposure with and without entecavir or tenofovir: phase 2a study

Group and study day	AUC0-24 (µg•h/mL), mean (SD)	AUCtau (µg•h/mL), mean (SD)	Cmax (µg/mL), mean (SD)	tmax (hour), mean (SD)
Bepirovirsen 300 mg, day 1 (n = 12)	“134 (44.2)”View highlighted excerpt for this quote	Not applicable	“10.6 (3.4)”View highlighted excerpt for this quote	“4.0 (1.3)”View highlighted excerpt for this quote
Bepirovirsen 300 mg, day 22 (n = 12)	“117 (34.9)”View highlighted excerpt for this quote	“146 (34.7)”View highlighted excerpt for this quote	“9.5 (3.1)”View highlighted excerpt for this quote	“3.4 (0.9)”View highlighted excerpt for this quote
Bepirovirsen 300 mg plus entecavir or tenofovir, day 1 (n = 5)	“123 (33.1)”View highlighted excerpt for this quote	Not applicable	“9.7 (2.2)”View highlighted excerpt for this quote	“4.1 (0.4)”View highlighted excerpt for this quote
Bepirovirsen 300 mg plus entecavir or tenofovir, day 22 (n = 4)	“111 (54.3)”View highlighted excerpt for this quote	“147 (38.0)”View highlighted excerpt for this quote	“8.8 (4.7)”View highlighted excerpt for this quote	“4.2 (1.2)”View highlighted excerpt for this quote

No effect of nucleos(t)ide analogues on bepirovirsen pharmacokinetics

“Bepirovirsen plasma pharmacokinetic parameters and concentration–time profiles in patients with chronic HBV in the CS3 study (NCT02981602) were similar with or without ETV or TFV coadministration, indicating no effect of NA coadministration on bepirovirsen pharmacokinetics.” (opens the original PMC page at this quote in a new tab)View highlighted excerpt for this quote
“Bepirovirsen was not an in vitro substrate of MRP2, OATP1B1, OATP1B3, OAT1, OAT3, OCT1, OCT2, MATE1, or MATE2‐K.” (opens the original PMC page at this quote in a new tab)View highlighted excerpt for this quote
“Although reliable and meaningful efflux ratios could not be determined for P‐gp or BCRP, bepirovirsen is unlikely to be a substrate of P‐gp or BCRP efflux transporters.” (opens the original PMC page at this quote in a new tab)View highlighted excerpt for this quote
“ASOs are not typically metabolized by CYP enzymes but are instead primarily metabolized by endonucleases and exonucleases or have been chemically modified to resist degradation.” (opens the original PMC page at this quote in a new tab)View highlighted excerpt for this quote

Nucleos(t)ide analogue treatment status as a covariate in the population pharmacokinetic model

“Results of this PK analysis suggest that no dose adjustment should be recommended for bepirovirsen based on demographic or baseline characteristics, or according to nucleos(t)ide analogue treatment status.” (opens the original PMC page at this quote in a new tab)View highlighted excerpt for this quote

Limitations of the drug interaction assessment

“Second, only the most common NAs used to treat chronic HBV infection (ETV and TFV) 3 were evaluated as perpetrator and victim in this analysis.” (opens the original PMC page at this quote in a new tab)View highlighted excerpt for this quote
“Third, the small sample size did not allow for any statistical comparison.” (opens the original PMC page at this quote in a new tab)View highlighted excerpt for this quote