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Dimebon + ketoconazole
- Development stage
- Phase 1
- Lead developer
- Pfizer
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
Dimebon + ketoconazole is a combination of two small molecule drugs studied together primarily to assess drug-drug interactions. Dimebon (also known as PF-01913539) is an investigational compound that was explored for neurodegenerative diseases such as Alzheimer's disease and Huntington's disease. Ketoconazole is an imidazole-class antifungal agent used to treat serious fungal infections by inhibiting the synthesis of ergosterol in fungal cell membranes. In clinical research settings, this combination has been used to evaluate how ketoconazole affects the pharmacokinetics of dimebon due to its potent inhibition of cytochrome P450 enzymes (notably CYP3A4), which can alter the metabolism and plasma levels of co-administered drugs[3][4][6]. The primary indication for this combination in trials has been pharmacokinetic interaction studies rather than therapeutic use.
- Other names
- dimebonPF-01913539PF01913539PF 01913539ketoconazole
02
Targets
CYP3A4 (Cytochrome P450 3A4)CYP51A1 (Sterol 14α-demethylase)
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