DDInter1042 DDInter1008
Leuprolide is a synthetic 9-residue peptide analogue of gonadotropin-releasing hormone (GnRH). Unlike the endogenous decapeptide GnRH, leuprolide contains a single D-amino acid (D-leucyl) residue, which helps to increase its circulating half-life from three to four minutes to approximately three hours. As a GnRH mimic, leuprolide is capable of binding to the GnRH receptor (GnRHR) and inducing downstream modulation of both gonadotropin hormone and sex steroid levels. Prolonged activation of GnRHR results in significant downregulation of sex steroid levels, which is primarily responsible for the clinical efficacy of leuprolide in diverse conditions, including advanced prostate cancer, endometriosis, and central precocious puberty.[A203126, A203132] Leuprolide was first approved in 1985 as a daily subcutaneous injection under the tradename
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 to be used in topical formulations.
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)