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Drug intelligence / Profile preview
rilapladib + itraconazole
- Development stage
- Unknown
- Lead developer
- GSK
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
**Rilapladib + itraconazole** is a combination of two small molecules: rilapladib, a potent and selective inhibitor of lipoprotein associated phospholipase A2 (Lp-PLA2), and itraconazole, a triazole antifungal agent that inhibits fungal cytochrome P450 enzyme lanosterol 14α-demethylase, thereby impairing ergosterol synthesis. This combination has been studied primarily to assess pharmacokinetic interactions between rilapladib and itraconazole[1]. Rilapladib was developed for atherosclerosis and investigated for Alzheimer's disease, while itraconazole is approved for various systemic fungal infections. The combination is not an approved therapy; clinical trials have evaluated their co-administration to measure the effect of itraconazole (a strong CYP3A4 inhibitor) on rilapladib metabolism[1].
- Other names
- rilapladib + itraconazole
02
Targets
CYP3A4 (Cytochrome P450 3A4)PLA2G7 (Platelet-activating factor acetylhydrolase)CYP51A1 (Sterol 14α-demethylase)
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