varegacestat + itraconazole

Combination of **varegacestat (AL102)**, an oral small molecule **gamma-secretase inhibitor** in clinical development primarily for desmoid tumors, and **itraconazole**, an oral triazole antifungal agent. The combination is being studied to assess the effect of itraconazole (a potent CYP3A4 inhibitor) on the pharmacokinetics, safety, and tolerability of a single dose of varegacestat in healthy volunteers. Varegacestat exerts its action by inhibiting the gamma-secretase complex, which is involved in Notch signaling implicated in tumorigenesis, while itraconazole itself is not expected to have antitumor activity in this context, but is used as an interacting drug for drug-drug interaction studies[1][2][5].

Other names

varegacestat + itraconazole