Drug intelligence / Profile preview

venetoclax + itraconazole

Development stage
Unknown
Lead developer
AbbVie
Modality
Small Molecules
Administration
Oral
01

Overview

This is a **combination therapy** consisting of **venetoclax**, a BCL-2 inhibitor, and **itraconazole**, a triazole antifungal and potent CYP3A4 inhibitor. Venetoclax induces apoptosis in malignant cells by inhibiting the anti-apoptotic protein BCL-2, and is primarily metabolized by CYP3A4. Itraconazole inhibits CYP3A4, increasing venetoclax plasma concentrations and thus allowing for lower venetoclax dosing. This combination has been investigated primarily in patients with newly diagnosed acute myeloid leukemia (AML), especially those considered unfit for intensive chemotherapy. The addition of itraconazole to venetoclax regimens not only provides antifungal prophylaxis but also serves as a pharmacokinetic booster, reducing venetoclax dosing requirements. Reported studies indicate this outpatient, low-dose regimen is feasible with acceptable safety and preliminary efficacy, though close monitoring for hematological and gastrointestinal toxicities is required[1][4][2].

02

Targets

CYP3A4 (Cytochrome P450 3A4)BCL-2 (BCL-2 family)

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