14-alpha Demethylase Inhibitors

Compounds that specifically inhibit STEROL 14-DEMETHYLASE. A variety of azole-derived ANTIFUNGAL AGENTS act through this mechanism.
DrugDrug NameDrug Indication
DB00196FluconazoleFor the treatment of fungal infections.
DB00257ClotrimazoleFor the local treatment of oropharyngeal candidiasis and vaginal yeast infections, also used in fungal infections of the skin such as ringworm, athlete's foot, and jock itch.
DB00582VoriconazoleFor the treatment of esophageal candidiasis, invasive pulmonary aspergillosis, and serious fungal infections caused by Scedosporium apiospermum and Fusarium spp.
DB01007TioconazoleFor the local treatment of vulvovaginal candidiasis (moniliasis).
DB01026KetoconazoleFor the treatment of the following systemic fungal infections: candidiasis, chronic mucocutaneous candidiasis, oral thrush, candiduria, blastomycosis, coccidioidomycosis, histoplasmosis, chromomycosis, and paracoccidioidomycosis.
DB01110MiconazoleFor topical application in the treatment of tinea pedis (athlete’s foot), tinea cruris, and tinea corporis caused by Trichophyton rubrum, Trichophyton mentagrophytes, and Epidermophyton floccosum, in the treatment of cutaneous candidiasis (moniliasis), and in the treatment of tinea versicolor.
DB01127EconazoleFor topical application in the treatment of tinea pedis, tinea cruris, and tinea corporis caused by Trichophyton rubrum, Trichophyton mentagrophytes, Trichophyton tonsurans, Microsporum canis, Microsporum audouini, Microsporum gypseum, and Epidermophyton floccosum, in the treatment of cutaneous candidiasis, and in the treatment of tinea versicolor.
DB01167ItraconazoleFor the treatment of the following fungal infections in immunocompromised and non-immunocompromised patients: pulmonary and extrapulmonary blastomycosis, histoplasmosis, aspergillosis, and onychomycosis.
DB01263PosaconazoleFor prophylaxis of invasive Aspergillus and Candida infections in patients, 13 years of age and older, who are at high risk of developing these infections due to being severely immunocompromised as a result of procedures such as hematopoietic stem cell transplant (HSCT) recipients with graft-versus-host disease (GVHD), or due to hematologic malignancies with prolonged neutropenia from chemotherapy. Also for the treatment of oropharyngeal candidiasis, including oropharyngeal candidiasis refractory to itraconazole and/or fluconazole. Posaconazole is used as an alternative treatment for invasive aspergillosis, Fusarium infections, and zygomycosis in patients who are intolerant of, or whose disease is refractory to, other antifungals.
DrugDrug NameTargetType
DB00196FluconazoleCytochrome P450 3A4enzyme
DB00196FluconazoleCytochrome P450 2C9enzyme
DB00196FluconazoleCytochrome P450 2C19enzyme
DB00196FluconazoleCytochrome P450 3A5enzyme
DB00196FluconazoleCytochrome P450 3A7enzyme
DB00196FluconazoleMultidrug resistance protein 1transporter
DB00196FluconazoleLanosterol 14-alpha demethylasetarget
DB00196FluconazoleCytochrome P450 11B1, mitochondrialenzyme
DB00196FluconazoleCytochrome P450 1A2enzyme
DB00257ClotrimazoleIntermediate conductance calcium-activated potassium channel protein 4target
DB00257ClotrimazoleCholesterol side-chain cleavage enzyme, mitochondrialenzyme
DB00257ClotrimazoleCytochrome P450 1A2enzyme
DB00257ClotrimazoleCytochrome P450 2D6enzyme
DB00257ClotrimazoleCytochrome P450 2C8enzyme
DB00257ClotrimazoleCytochrome P450 3A4enzyme
DB00257ClotrimazoleCytochrome P450 2B6enzyme
DB00257ClotrimazoleCanalicular multispecific organic anion transporter 2transporter
DB00257ClotrimazoleMultidrug resistance protein 1transporter
DB00257ClotrimazoleCanalicular multispecific organic anion transporter 1transporter
DB00257ClotrimazoleCytochrome P450 11B1, mitochondrialenzyme
DB00257ClotrimazoleCytochrome P450 19A1enzyme
DB00257ClotrimazoleCytochrome P450 2A6enzyme
DB00257ClotrimazoleCytochrome P450 2C19enzyme
DB00257ClotrimazoleCytochrome P450 2C9enzyme
DB00257ClotrimazoleCytochrome P450 2E1enzyme
DB00257ClotrimazoleCytochrome P450 3A7enzyme
DB00257ClotrimazoleLanosterol 14-alpha demethylasetarget
DB00257ClotrimazoleNuclear receptor subfamily 1 group I member 2target
DB00257ClotrimazoleNuclear receptor subfamily 1 group I member 3target
DB00582VoriconazoleCytochrome P450 2C19enzyme
DB00582VoriconazoleCytochrome P450 3A4enzyme
DB00582VoriconazoleCytochrome P450 2C9enzyme
DB00582VoriconazoleDimethylaniline monooxygenase [N-oxide-forming] 1enzyme
DB00582VoriconazoleDimethylaniline monooxygenase [N-oxide-forming] 3enzyme
DB00582VoriconazoleCytochrome P450 3A5enzyme
DB00582VoriconazoleCytochrome P450 3A7enzyme
DB00582VoriconazoleProstaglandin G/H synthase 1enzyme
DB00582VoriconazoleLanosterol 14-alpha demethylasetarget
DB01007TioconazoleLanosterol 14-alpha demethylasetarget
DB01007TioconazoleCytochrome P450 19A1enzyme
DB01007TioconazoleCytochrome P450 1A2enzyme
DB01007TioconazoleCytochrome P450 2C19enzyme
DB01007TioconazoleCytochrome P450 2C8enzyme
DB01007TioconazoleCytochrome P450 2C9enzyme
DB01007TioconazoleCytochrome P450 2E1enzyme
DB01007TioconazoleCytochrome P450 3A4enzyme
DB01007TioconazoleLanosterol 14-alpha demethylasetarget
DB01007TioconazoleCytochrome P450 2D6enzyme
DB01026KetoconazoleCytochrome P450 3A4enzyme
DB01026KetoconazoleCytochrome P450 2C9enzyme
DB01026KetoconazoleCytochrome P450 2C19enzyme
DB01026KetoconazoleCytochrome P450 3A5enzyme
DB01026KetoconazoleCytochrome P450 1A2enzyme
DB01026KetoconazoleCytochrome P450 2C8enzyme
DB01026KetoconazoleCytochrome P450 1A1enzyme
DB01026KetoconazoleCytochrome P450 2D6enzyme
DB01026KetoconazoleCytochrome P450 3A7enzyme
DB01026KetoconazoleBile salt export pumptransporter
DB01026KetoconazoleMultidrug resistance protein 1transporter
DB01026KetoconazoleSolute carrier organic anion transporter family member 1A2transporter
DB01026KetoconazoleCholesterol side-chain cleavage enzyme, mitochondrialenzyme
DB01026KetoconazoleCytochrome P450 11B1, mitochondrialenzyme
DB01026KetoconazoleCytochrome P450 1B1enzyme
DB01026KetoconazoleCytochrome P450 26A1enzyme
DB01026KetoconazoleCytochrome P450 2A6enzyme
DB01026KetoconazoleCytochrome P450 2B6enzyme
DB01026KetoconazoleLanosterol 14-alpha demethylaseenzyme
DB01026KetoconazoleLanosterol 14-alpha demethylasetarget
DB01026KetoconazoleAndrogen receptortarget
DB01026Ketoconazole17-hydroxylasetarget
DB01026KetoconazoleSteroid 21-hydroxylasetarget
DB01026Ketoconazole11-hydroxylasetarget
DB01026KetoconazoleCytochrome P450 19A1target
DB01026KetoconazolePotassium voltage-gated channel subfamily H member 2target
DB01026KetoconazoleNuclear receptor subfamily 1 group I member 2target
DB01026KetoconazoleNuclear receptor subfamily 1 group I member 3target
DB01110MiconazoleCytochrome P450 2C9enzyme
DB01110MiconazoleCytochrome P450 2D6enzyme
DB01110MiconazoleCytochrome P450 3A4enzyme
DB01110MiconazoleMultidrug resistance protein 1transporter
DB01110MiconazoleLanosterol 14-alpha demethylasetarget
DB01110MiconazoleNitric oxide synthase, endothelialtarget
DB01110MiconazoleNitric oxide synthase, inducibletarget
DB01110MiconazoleCalcium-activated potassium channel subunit alpha-1target
DB01110MiconazoleCalcium-activated potassium channel subunit beta-1target
DB01110MiconazoleCalcium-activated potassium channel subunit beta-2target
DB01110MiconazoleCalcium-activated potassium channel subunit beta-3target
DB01110MiconazoleCalcium-activated potassium channel subunit beta-4target
DB01110MiconazoleIntermediate conductance calcium-activated potassium channel protein 4target
DB01110MiconazoleSmall conductance calcium-activated potassium channel protein 1target
DB01110MiconazoleSmall conductance calcium-activated potassium channel protein 2target
DB01110MiconazoleSmall conductance calcium-activated potassium channel protein 3target
DB01110MiconazolePotassium voltage-gated channel subfamily H member 2target
DB01110MiconazolePotassium voltage-gated channel subfamily H member 6target
DB01110MiconazolePotassium voltage-gated channel subfamily H member 7target
DB01110MiconazoleCytochrome P450 11B1, mitochondrialenzyme
DB01110MiconazoleCytochrome P450 19A1enzyme
DB01110MiconazoleCytochrome P450 1A2enzyme
DB01110MiconazoleCytochrome P450 2A6enzyme
DB01110MiconazoleCytochrome P450 2B6enzyme
DB01110MiconazoleCytochrome P450 2C19enzyme
DB01110MiconazoleCytochrome P450 2E1enzyme
DB01110MiconazoleNuclear receptor subfamily 1 group I member 2target
DB01127EconazoleCytochrome P450 19A1enzyme
DB01127EconazoleCytochrome P450 2E1enzyme
DB01127EconazoleCytochrome P450 3A4enzyme
DB01127EconazoleLanosterol 14-alpha demethylasetarget
DB01127EconazoleNuclear receptor subfamily 1 group I member 2target
DB01167ItraconazoleLanosterol 14-alpha demethylasetarget
DB01167ItraconazoleLanosterol 14-alpha demethylasetarget
DB01167ItraconazoleCytochrome P450 3A4enzyme
DB01167ItraconazoleCytochrome P450 2D6enzyme
DB01167ItraconazoleCytochrome P450 3A5enzyme
DB01167ItraconazoleCytochrome P450 3A7enzyme
DB01167ItraconazoleCytochrome P450 2B6enzyme
DB01167ItraconazoleMultidrug resistance protein 1transporter
DB01167ItraconazoleCytochrome P450 1A1enzyme
DB01167ItraconazoleCytochrome P450 2E1enzyme
DB01263PosaconazoleCytochrome P450 3A4enzyme
DB01263PosaconazoleMultidrug resistance protein 1transporter
DB01263PosaconazoleLanosterol 14-alpha demethylasetarget