Drug intelligence / Profile preview

azd0780 + midazolam

Development stage
Phase 1
Lead developer
AstraZeneca
Modality
Small Molecules
Administration
Oral (AZD0780), Oral (midazolam; As Per Trial—used For Ddi Assessment)
01

Overview

**AZD0780 + midazolam** is an investigational combination used in clinical pharmacology studies, not as a therapeutic product. The combination is employed to evaluate potential drug-drug interactions between AZD0780, an oral small molecule proprotein convertase subtilisin/kexin type 9 (PCSK9) inhibitor developed for hypercholesterolemia and dyslipidemia, and midazolam, a sensitive CYP3A4 substrate frequently used to assess the impact of investigational drugs on CYP3A4 enzyme activity. AZD0780's mechanism of action involves inhibition of PCSK9, leading to reduced LDL receptor degradation and enhanced clearance of LDL cholesterol. Midazolam is a benzodiazepine used for sedation, anesthesia, and procedural comfort, acting primarily as a GABA-A receptor positive allosteric modulator. This combination is studied exclusively to characterize the pharmacokinetic and metabolic interaction profile of AZD0780 as a potential perpetrator or victim of CYP3A4-mediated drug-drug interactions, not for therapeutic co-use[1][3].

02

Targets

GABAA (Gamma-aminobutyric acid receptor)PCSK9 (Proprotein convertase subtilisin/kexin type 9)

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