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suciraslim + fluconazole
- Development stage
- Discontinued
- Lead developer
- Eli Lilly
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
Suciraslim (LY3154207) is a potent and selective small-molecule positive allosteric modulator (PAM) of the dopamine D1 receptor, originally developed by Eli Lilly for the treatment of cognitive impairment associated with Parkinson's disease and Dementia with Lewy Bodies. Fluconazole is a widely used triazole antifungal agent that acts by inhibiting the fungal enzyme lanosterol 14-alpha-demethylase. The combination of suciraslim and fluconazole has been investigated in Phase 1 clinical trials specifically to assess drug-drug interactions. Because suciraslim is a substrate for CYP3A4, fluconazole is utilized in these studies as a potent CYP3A4 inhibitor to determine the effect of metabolic inhibition on the systemic exposure, safety, and pharmacokinetics of suciraslim.
- Brand names
- Diflucan
- Other names
- LY3154207 + fluconazole
02
Targets
DRD1 (Dopamine D1 Receptor)CYP51A1 (Sterol 14α-demethylase)
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