Drug intelligence / Profile preview

varegacestat + itraconazole

Development stage
Phase 1
Lead developer
Immunome
Modality
Small Molecules
Administration
Oral
01

Overview

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
02

Targets

CYP51A1 (Sterol 14α-demethylase)NOTCH (Neurogenic locus notch homolog protein 3)PIK3R1 (Phosphatidylinositol 4-phosphate 3-kinase regulatory subunit alpha)STAT3 (Signal Transducer and Activator of Transcription 3)VDAC1 (Hexokinase 2–voltage-dependent anion channel 1 complex)GSEC (Gamma-Secretase Complex)

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