Cytochrome P-450 CYP2A6 Inhibitors

DrugDrug NameDrug Indication
DB01006LetrozoleFor the extended adjuvant treatment of early breast cancer in postmenopausal women who have received 5 years of adjuvant tamoxifen therapy. Also for first-line treatment of postmenopausal women with hormone receptor positive or hormone receptor unknown locally advanced or metastatic breast cancer. Also indicated for the treatment of advanced breast cancer in postmenopausal women with disease progression following antiestrogen therapy.
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.
DB01118AmiodaroneIntravenously, for initiation of treatment and prophylaxis of frequently recurring ventricular fibrillation and hemodynamically unstable ventricular tachycardia in patients refractory to other therapy. Orally, for the treatment of life-threatening recurrent ventricular arrhythmias such as recurrent ventricular fibrillation and recurrent hemodynamically unstable ventricular tachycardia.
DB00752TranylcypromineFor the treatment of major depressive episode without melancholia.
DB00313Valproic AcidFor treatment and management of seizure disorders, mania, and prophylactic treatment of migraine headache. In epileptics, valproic acid is used to control absence seizures, tonic-clonic seizures (grand mal), complex partial seizures, and the seizures associated with Lennox-Gastaut syndrome.
DB00860PrednisoloneFor the treatment of primary or secondary adrenocortical insufficiency, such as congenital adrenal hyperplasia, thyroiditis. Also used to treat psoriatic arthritis, rheumatoid arthritis, ankylosing spondylitis, bursitis, acute gouty arthritis and epicondylitis. Also indicated for treatment of systemic lupus erythematosus, pemphigus and acute rhematic carditis. Can be used in the treatment of leukemias, lymphomas, thrombocytopenia purpura and autoimmune hemolytic anemia. Can be used to treat celiac disease, insulin resistance, ulcerative colitis and liver disorders.
DB01026KetoconazoleFor the treatment of the following systemic fungal infections: candidiasis, chronic mucocutaneous candidiasis, oral thrush, candiduria, blastomycosis, coccidioidomycosis, histoplasmosis, chromomycosis, and paracoccidioidomycosis.
DB06712NilvadipineFor the management of vasospastic angina, chronic stable angina and hypertension.
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.
DrugDrug NameTargetType
DB01006LetrozoleCytochrome P450 19A1target
DB01006LetrozoleCytochrome P450 3A4enzyme
DB01006LetrozoleCytochrome P450 2A6enzyme
DB01006LetrozoleCytochrome P450 19A1enzyme
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 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
DB00257ClotrimazoleBile salt export pumptransporter
DB01118AmiodaroneBeta-1 adrenergic receptortarget
DB01118AmiodaronePotassium voltage-gated channel subfamily H member 2target
DB01118AmiodaroneCytochrome P450 2C8enzyme
DB01118AmiodaroneCytochrome P450 2C9enzyme
DB01118AmiodaroneCytochrome P450 2D6enzyme
DB01118AmiodaroneVoltage-dependent T-type calcium channel subunit alpha-1Htarget
DB01118AmiodaroneVoltage-dependent calcium channel subunit alpha-2/delta-2target
DB01118AmiodaroneCytochrome P450 3A4enzyme
DB01118AmiodaroneCytochrome P450 1A2enzyme
DB01118AmiodaroneCytochrome P450 3A5enzyme
DB01118AmiodaroneCytochrome P450 3A7enzyme
DB01118AmiodaroneCytochrome P450 1A1enzyme
DB01118AmiodaroneMultidrug resistance protein 1transporter
DB01118AmiodaroneCytochrome P450 2C19enzyme
DB01118AmiodaroneCytochrome P450 2A6enzyme
DB01118AmiodaroneThyroid hormone receptor alphatarget
DB01118AmiodaroneThyroid hormone receptor betatarget
DB01118AmiodaronePeroxisome proliferator-activated receptor gammatarget
DB01118AmiodaroneBile salt export pumptransporter
DB00752TranylcypromineAmine oxidase [flavin-containing] Btarget
DB00752TranylcypromineAmine oxidase [flavin-containing] Atarget
DB00752TranylcypromineCytochrome P450 2C19enzyme
DB00752TranylcypromineCytochrome P450 2A6enzyme
DB00752TranylcypromineCytochrome P450 2D6enzyme
DB00752TranylcypromineCytochrome P450 1A2enzyme
DB00752TranylcypromineCytochrome P450 2C9enzyme
DB00752TranylcypromineCytochrome P450 2E1enzyme
DB00752TranylcypromineCytochrome P450 3A4enzyme
DB00313Valproic Acid4-aminobutyrate aminotransferase, mitochondrialtarget
DB00313Valproic AcidHistone deacetylase 9target
DB00313Valproic AcidShort/branched chain specific acyl-CoA dehydrogenase, mitochondrialtarget
DB00313Valproic AcidCytochrome P450 2A6enzyme
DB00313Valproic AcidCytochrome P450 2B6enzyme
DB00313Valproic AcidCytochrome P450 2C9enzyme
DB00313Valproic AcidSolute carrier family 22 member 5transporter
DB00313Valproic AcidSolute carrier family 22 member 6transporter
DB00313Valproic AcidSolute carrier family 22 member 8transporter
DB00313Valproic AcidMonocarboxylate transporter 1transporter
DB00313Valproic AcidSolute carrier family 22 member 7transporter
DB00313Valproic AcidCytochrome P450 3A5enzyme
DB00313Valproic AcidUDP-glucuronosyltransferase 1-9enzyme
DB00313Valproic AcidProstaglandin G/H synthase 1enzyme
DB00313Valproic AcidCytochrome P450 1A2enzyme
DB00313Valproic AcidCytochrome P450 2C18enzyme
DB00313Valproic AcidCytochrome P450 2C19enzyme
DB00313Valproic AcidCytochrome P450 2C8enzyme
DB00313Valproic AcidCytochrome P450 3A4enzyme
DB00313Valproic AcidUDP-glucuronosyltransferase 1-4enzyme
DB00313Valproic AcidUDP-glucuronosyltransferase 1-8enzyme
DB00313Valproic AcidUDP-glucuronosyltransferase 1-10enzyme
DB00313Valproic AcidUDP-glucuronosyltransferase 1-6enzyme
DB00313Valproic AcidUDP-glucuronosyltransferase 1-3enzyme
DB00313Valproic AcidUDP-glucuronosyltransferase 2B7enzyme
DB00313Valproic AcidUDP-glucuronosyltransferase 2B15enzyme
DB00313Valproic Acid2-oxoglutarate dehydrogenase, mitochondrialtarget
DB00313Valproic AcidSuccinate-semialdehyde dehydrogenase, mitochondrialtarget
DB00313Valproic AcidSodium channel proteintarget
DB00313Valproic AcidHistone deacetylase 2target
DB00313Valproic AcidPeroxisome proliferator-activated receptor alphatarget
DB00313Valproic AcidPeroxisome proliferator-activated receptor deltatarget
DB00313Valproic AcidPeroxisome proliferator-activated receptor gammatarget
DB00313Valproic AcidSerum albumincarrier
DB00313Valproic AcidUDP-glucuronosyltransferase 1-1enzyme
DB00313Valproic AcidSolute carrier organic anion transporter family member 2B1transporter
DB00860PrednisoloneCorticosteroid-binding globulincarrier
DB00860PrednisoloneCytochrome P450 3A4enzyme
DB00860PrednisoloneGlucocorticoid receptortarget
DB00860PrednisoloneSolute carrier organic anion transporter family member 1A2transporter
DB00860PrednisoloneMultidrug resistance protein 1transporter
DB00860PrednisoloneCytochrome P450 2A6enzyme
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
DB01026KetoconazoleUDP-glucuronosyltransferase 1-1enzyme
DB01026KetoconazoleUDP-glucuronosyltransferase 2B7enzyme
DB01026KetoconazoleSolute carrier organic anion transporter family member 1B1transporter
DB01026KetoconazoleCytochrome P450 4F12enzyme
DB01026KetoconazoleLeukotriene-B(4) omega-hydroxylase 1enzyme
DB06712NilvadipineCytochrome P450 3A4enzyme
DB06712NilvadipineCytochrome P450 1A2enzyme
DB06712NilvadipineCytochrome P450 2A6enzyme
DB06712NilvadipineCytochrome P450 2C19enzyme
DB06712NilvadipineCytochrome P450 2C8enzyme
DB06712NilvadipineCytochrome P450 2C9enzyme
DB06712NilvadipineCytochrome P450 2E1enzyme
DB06712NilvadipineVoltage-dependent L-type calcium channel subunit alpha-1Ctarget
DB06712NilvadipineVoltage-dependent calcium channel subunit alpha-2/delta-1target
DB06712NilvadipineVoltage-dependent L-type calcium channel subunit beta-2target
DB06712NilvadipineVoltage-dependent L-type calcium channel subunit alpha-1Dtarget
DB06712NilvadipineVoltage-dependent L-type calcium channel subunit alpha-1Starget
DB06712NilvadipineVoltage-dependent calcium channel subunit alpha-2/delta-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 1A2enzyme
DB01110MiconazoleCytochrome P450 2A6enzyme
DB01110MiconazoleCytochrome P450 2B6enzyme
DB01110MiconazoleCytochrome P450 2C19enzyme
DB01110MiconazoleCytochrome P450 2E1enzyme
DB01110MiconazoleNuclear receptor subfamily 1 group I member 2target
DB01110MiconazoleLanosterol 14-alpha demethylaseenzyme
DB01110MiconazoleCytochrome P450 19A1enzyme