DDInter1008 DDInter786
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
Fostemsavir is the phosphonooxymethyl prodrug of temsavir, a novel HIV-1 attachment inhibitor. It binds to and inhibits the activity of gp120, a subunit within the HIV-1 gp160 envelope glycoprotein that facilitates the attachment of HIV-1 to host cell CD4 receptors - in doing so, temsavir prevents the first step in the HIV-1 viral lifecycle. The discovery of gp120 as a potential target of interest in the treatment of HIV-1 infection is relatively recent, and was born out of a desire to find alternative target proteins (i.e. mechanistically orthogonal therapies) for the treatment of HIV-1 patients with resistant infections. Fostemavir is the first attachment inhibitor to receive FDA approval, granted in July 2020 for use in combination with other antiretrovirals in highly treatment-experienced patients with multidrug-resistant HIV-1 infection whom are failing their current therapy.[L14867,L14917] Targeting gp120 subunits is a new and novel therapeutic approach to HIV-1 infection, and the addition of attachment inhibitors, like temsavir, to the armament of therapies targeted against HIV-1 fills a necessary niche for therapeutic options in patients left with few, if any, viable treatments.
Ketoconazole {u} (Compound) binds {v} (Gene) CYP19A1
CYP19A1 {u} (Gene) is bound by {v} (Compound) Aminoglutethimide
Aminoglutethimide {u} may cause a minor interaction that can limit clinical effects when taken with {v} Fostemsavir
Ketoconazole {u} (Compound) binds {v} (Gene) CYP19A1
CYP19A1 {u} (Gene) is bound by {v} (Compound) Mefloquine
Mefloquine {u} may cause a moderate interaction that could exacerbate diseases when taken with {v} Fostemsavir
Ketoconazole {u} (Compound) causes {v} (Side Effect) Hypersensitivity
Hypersensitivity {u} (Side Effect) is caused by {v} (Compound) Aminoglutethimide
Aminoglutethimide {u} may cause a minor interaction that can limit clinical effects when taken with {v} Fostemsavir
Ketoconazole {u} (Compound) causes {v} (Side Effect) Hypersensitivity
Hypersensitivity {u} (Side Effect) is caused by {v} (Compound) Quinine
Quinine {u} may cause a moderate interaction that could exacerbate diseases when taken with {v} Fostemsavir
Ketoconazole {u} (Compound) binds {v} (Gene) CYP1A2
CYP1A2 {u} (Gene) is bound by {v} (Compound) Vemurafenib
Vemurafenib {u} may lead to a major life threatening interaction when taken with {v} Fostemsavir
Ketoconazole {u} (Compound) resembles {v} (Compound) Posaconazole
Posaconazole {u} may lead to a major life threatening interaction when taken with {v} Brigatinib
Brigatinib {u} may cause a minor interaction that can limit clinical effects when taken with {v} Fostemsavir
Ketoconazole {u} (Compound) causes {v} (Side Effect) Haemolytic anaemia
Haemolytic anaemia {u} (Side Effect) is caused by {v} (Compound) Halofantrine
Halofantrine {u} may lead to a major life threatening interaction when taken with {v} Fostemsavir
Ketoconazole {u} (Compound) resembles {v} (Compound) Posaconazole
Posaconazole {u} may cause a minor interaction that can limit clinical effects when taken with {v} Bexarotene
Bexarotene {u} may cause a minor interaction that can limit clinical effects when taken with {v} Fostemsavir
Ketoconazole {u} (Compound) resembles {v} (Compound) Posaconazole
Posaconazole {u} may cause a moderate interaction that could exacerbate diseases when taken with {v} Dexamethasone
Dexamethasone {u} may cause a minor interaction that can limit clinical effects when taken with {v} Fostemsavir
Ketoconazole {u} (Compound) resembles {v} (Compound) Posaconazole
Posaconazole {u} may cause a moderate interaction that could exacerbate diseases when taken with {v} Dabrafenib
Dabrafenib {u} may cause a minor interaction that can limit clinical effects when taken with {v} Fostemsavir
Ketoconazole (Compound) binds CYP19A1 (Gene) and CYP19A1 (Gene) is bound by Aminoglutethimide (Compound) and Aminoglutethimide may cause a minor interaction that can limit clinical effects when taken with Fostemsavir
Ketoconazole (Compound) binds CYP19A1 (Gene) and CYP19A1 (Gene) is bound by Mefloquine (Compound) and Mefloquine may cause a moderate interaction that could exacerbate diseases when taken with Fostemsavir
Ketoconazole (Compound) causes Hypersensitivity (Side Effect) and Hypersensitivity (Side Effect) is caused by Aminoglutethimide (Compound) and Aminoglutethimide may cause a minor interaction that can limit clinical effects when taken with Fostemsavir
Ketoconazole (Compound) causes Hypersensitivity (Side Effect) and Hypersensitivity (Side Effect) is caused by Quinine (Compound) and Quinine may cause a moderate interaction that could exacerbate diseases when taken with Fostemsavir
Ketoconazole (Compound) binds CYP1A2 (Gene) and CYP1A2 (Gene) is bound by Vemurafenib (Compound) and Vemurafenib may lead to a major life threatening interaction when taken with Fostemsavir
Ketoconazole (Compound) resembles Posaconazole (Compound) and Posaconazole may lead to a major life threatening interaction when taken with Brigatinib and Brigatinib may cause a minor interaction that can limit clinical effects when taken with Fostemsavir
Ketoconazole (Compound) causes Haemolytic anaemia (Side Effect) and Haemolytic anaemia (Side Effect) is caused by Halofantrine (Compound) and Halofantrine may lead to a major life threatening interaction when taken with Fostemsavir
Ketoconazole (Compound) resembles Posaconazole (Compound) and Posaconazole may cause a minor interaction that can limit clinical effects when taken with Bexarotene and Bexarotene may cause a minor interaction that can limit clinical effects when taken with Fostemsavir
Ketoconazole (Compound) resembles Posaconazole (Compound) and Posaconazole may cause a moderate interaction that could exacerbate diseases when taken with Dexamethasone and Dexamethasone may cause a minor interaction that can limit clinical effects when taken with Fostemsavir
Ketoconazole (Compound) resembles Posaconazole (Compound) and Posaconazole may cause a moderate interaction that could exacerbate diseases when taken with Dabrafenib and Dabrafenib may cause a minor interaction that can limit clinical effects when taken with Fostemsavir