DDInter1008 DDInter1435
Ketoconazole is an imidazole antifungal agent used in the prevention and treatment of a variety of fungal infections.[FDA Label] It functions by preventing the synthesis of ergosterol, the fungal equivalent of cholesterol, thereby increasing membrane fluidity and preventing growth of the fungus.[A181802,T116] Ketoconazole was first approved in an oral formulation for systemic use by the FDA in 1981. At this time it was considered a significant improvement over previous antifungals, [miconazole] and [clotrimazole], due to its broad spectrum and good absorption. However, it was discovered that ketoconazole produces frequent gastrointestinal side effects and dose-related hepatitis.[A188054,A188057] These effects combined with waning efficacy led to its eventual replacement by triazole agents, [fluconazole], [itraconazole], [voriconazole], and [posaconazole]. Ketoconazole and its predecessor [clotrimazole] continue
Pexidartinib is a selective tyrosine kinase inhibitor that works by inhibiting the colony-stimulating factor (CSF1)/CSF1 receptor pathway. Pexidartinib was originally developed by Daiichi Sankyo, Inc. and it was approved by the FDA in August 2019 as the first systemic therapy for adult patients with symptomatic tenosynovial giant cell tumor. Tenosynovial giant cell tumor is a rare form of non-malignant tumor that causes the synovium and tendon sheaths to thicken and overgrow, leading to damage in surrounding joint tissue.[A182240,L7901] Debilitating symptoms often follow with tenosynovial giant cell tumors, along with a risk of significant functional limitations and a reduced quality of life in patients. While surgical resection is a current standard of care for tenosynovial giant cell tumor, there are tumor types where surgeries are deemed clinically ineffective with a high risk of lifetime recurrence. Pexidartinib works by blocking the immune responses that are activated in tenosynovial giant cell tumors. In clinical trials, pexidartinib was shown to promote improvements in patient symptoms and functional outcomes in TGCT. Pexidartinib is available in oral formulations and it is commonly marketed as Turalio.
Ketoconazole {u} (Compound) resembles {v} (Compound) Itraconazole
Ketoconazole {u} (Compound) resembles {v} (Compound) Posaconazole
Ketoconazole {u} (Compound) binds {v} (Gene) CYP3A4
Ketoconazole {u} (Compound) upregulates {v} (Gene) FDFT1
Ketoconazole {u} (Compound) is included by {v} (Pharmacologic Class) Cytochrome P450 3A5 Inhibitors
Ketoconazole {u} (Compound) downregulates {v} (Gene) PPP2R3C
Ketoconazole {u} (Compound) causes {v} (Side Effect) Hypersensitivity
Ketoconazole {u} (Compound) binds {v} (Gene) and {u} (Compound) upregulates {v} (Gene) CYP51A1
Ketoconazole (Compound) resembles Itraconazole (Compound)
Ketoconazole (Compound) resembles Posaconazole (Compound)
Ketoconazole (Compound) binds CYP3A4 (Gene)
Ketoconazole (Compound) upregulates FDFT1 (Gene)
Ketoconazole (Compound) is included by Cytochrome P450 3A5 Inhibitors (Pharmacologic Class)
Ketoconazole (Compound) downregulates PPP2R3C (Gene)
Ketoconazole (Compound) causes Hypersensitivity (Side Effect)
Ketoconazole (Compound) binds CYP51A1 (Gene) and Ketoconazole (Compound) upregulates CYP51A1 (Gene)