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LU AF11167 + itraconazole
- Development stage
- Discontinued
- Lead developer
- Lundbeck
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
LU AF11167 + itraconazole is a **combination of an investigational small molecule** called LU AF11167 and **itraconazole**, a marketed azole antifungal. LU AF11167 is a selective, high-affinity inhibitor of **phosphodiesterase 10A (PDE10A)**, modulating dopamine D1 and D2 receptor-mediated signaling by inhibiting PDE10A, without direct binding to dopamine receptors. It was developed primarily for the treatment of schizophrenia with negative symptoms. Itraconazole inhibits fungal lanosterol 14α-demethylase (a cytochrome P450-dependent enzyme), disrupting ergosterol synthesis and thereby damaging fungal cell membrane integrity. This combination is not intended as a fixed-dose therapeutic; rather, it is used in clinical drug-drug interaction studies to investigate the effect of the strong CYP3A4/5 inhibitor itraconazole on the pharmacokinetics of LU AF11167[1][3][7].
- Other names
- itraconazoleLU AF11167
02
Targets
PDE10A (Phosphodiesterase 10A)CYP51A1 (Sterol 14α-demethylase)
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