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cabergoline + ketoconazole
- Development stage
- Unknown
- Lead developer
- Pfizer
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
Combination therapy of cabergoline and ketoconazole used as a second-line treatment for Cushing's disease when conventional treatments like transsphenoidal surgery have failed. This combination has shown effectiveness in normalizing urinary free cortisol (UFC) levels in patients with persistent hypercortisolism. Cabergoline is a dopamine receptor agonist that acts on D2 receptors, while ketoconazole inhibits cortisol synthesis. Studies show this combination can achieve UFC normalization in approximately 79% of patients with Cushing's disease, which is more effective than either medication used alone.
02
Targets
CYP2D6 (Cytochrome P450 2D6)CYP2C9 (Cytochrome P450 family 2 subfamily C member 9)CYP3A4 (Cytochrome P450 3A4)DRD2 (Dopamine D2 Receptor)CYP1A2 (Cytochrome P450 1A2)CYP2C19 (Cytochrome P450 2C19)
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