Name: Azetukalner (XEN1101) in Focal onset seizures: Effects of other drugs on Azetukalner
Published: 2026-09-21T21:41:53-04:00

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

Effects of other drugs on Azetukalner

4 evidence topics · 4 sources

CYP3A4 inhibition: itraconazole

“In healthy subjects, a single 400 mg oral dose of the CYP3A4 inhibitor itraconazole given after 10 days of treatment with azetukalner (20 mg q.d.) was associated with an approximately 10% increase in peak plasma azetukalner concentration and a < 30% increase in azetukalner exposure” (opens the source at this quote in a new tab)
“Longer treatment with itraconazole, however, would be required to adequately assess the effect of CYP3A4 inhibition on azetukalner pharmacokinetics.” (opens the source at this quote in a new tab)

Modelled effect of CYP3A4 inhibitors and inducers

“Modeling pharmacokinetic data from the phase 2b efficacy and safety study (see below) predicted a 32% increase in steady-state plasma azetukalner levels in the presence of CYP3A4 inhibitors. The same model predicted a 22% decrease in azetukalner exposure in the presence of concomitant treatment with a single CYP3A4 inducer, and a 39% decrease in the presence of two or more CYP3A4 inducers” (opens the source at this quote in a new tab)

Enzyme-inducing antiseizure medications and trial stratification

“Azetukalner is primarily metabolized by cytochrome P450 3A4 (CYP3A4), with minimal involvement from other cytochrome P450 enzymes, and plasma levels of azetukalner may decrease in the presence of CYP3A4 inducers.” (opens the source at this quote in a new tab)

Randomization stratified by enzyme-inducing background medication

“XEN1101 is primarily metabolized by cytochrome P450 3A4 isozyme (CYP3A4) without substantial involvement of other CYPs, and plasma levels of XEN1101 may decrease in the presence of CYP3A4 inducers. To ensure balanced distribution across groups, randomization was stratified by background use of CYP3A4 inducer medications (eg, carbamazepine, eslicarbazepine acetate, oxcarbazepine, phenytoin, topiramate, or phenobarbital).” (opens the source at this quote in a new tab)