Drug intelligence / Profile preview

azd0780 + itraconazole

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

Overview

**azd0780 + itraconazole** is an investigational oral combination involving AZD0780, a small molecule inhibitor of proprotein convertase subtilisin/kexin type 9 (PCSK9), and itraconazole, a triazole antifungal agent with potent CYP3A4 inhibitory activity. AZD0780 is being developed for hypercholesterolemia and other lipid disorders due to its ability to significantly reduce LDL cholesterol by inhibiting PCSK9, thereby increasing low-density lipoprotein receptor (LDLR) expression and LDL clearance from plasma. Itraconazole is used in this context to evaluate drug-drug interactions as a strong CYP3A4 inhibitor, potentially affecting the metabolism of AZD0780. The combination is studied to determine pharmacokinetic interactions and to quantify any impact on the efficacy or safety of AZD0780 when coadministered with strong CYP3A inhibitors such as itraconazole[1][2][3][4][6][7].

Brand names
sporonox
Other names
itraconazole
02

Targets

CYP51A1 (Sterol 14α-demethylase)PCSK9 (Proprotein convertase subtilisin/kexin type 9)

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