Cytochrome P450 3A4 Inducers

DrugDrug NameDrug Indication
DB08899EnzalutamideEnzalutamide is indicated for the treatment of patients with metastatic castration-resistant prostate cancer who have previously received docetaxel.
DB01609DeferasiroxFor the treatment of chronic iron overload due to blood transfusions (transfusional hemosiderosis) in patients 2 years of age and older.
DB08912DabrafenibTafinlar is a kinase inhibitor that was initially indicated as a single agent for the treatment of patients with unresectable or metastatic melanoma with BRAF V600E mutation as detected by an FDA-approved test [FDA label]. Tafinlar in combination with [DB08911] is indicated for the treatment of patients with unresectable or metastatic melanoma with BRAF V600E or V600K mutations as detected by an FDA-approved test. The use in combination is based on the demonstration of durable response rate. Improvement in disease-related symptoms or overall survival has not been demonstrated for Tafinlar in combination with trametinib [FDA label]. In May 2018, Tafinlar (dabrafenib) and Mekinist ([DB08911]) have been approved in combination to treat anaplastic thyroid cancer caused by an abnormal BRAF V600E gene [L2712].
DB00648MitotaneFor treatment of inoperable adrenocortical tumours; Cushing's syndrome
DB04911OritavancinInvestigated for use/treatment in bacterial infection and skin infections/disorders.
DB00701AmprenavirFor the treatment of HIV-1 infection in combination with other antiretroviral agents.
DB09330OsimertinibOsimertinib is indicated for the treatment of patients with metastatic epidermal growth factor receptor (EGFR) T790M mutation-positive non-small cell lung cancer (NSCLC), as detected by an FDA- approved test, who have progressed on or after EGFR-TKI therapy.
DB00673AprepitantFor the prevention of nausea and vomiting associated with highly emetogenic cancer chemotherapy, including high-dose cisplatin (in combination with other antiemetic agents).
DB00564CarbamazepineFor the treatment of epilepsy and pain associated with true trigeminal neuralgia.
DB00474MethohexitalMethohexital is indicated for use as an intravenous anaesthetic. It has also been commonly used to induce deep sedation.
DB00349ClobazamFor treatment and management of epilepsy and seizures associated with Lennox-Gastaut syndrome, a difficult-to-treat form of childhood epilepsy.
DrugDrug NameTargetType
DB08899EnzalutamideSerum albumincarrier
DB08899EnzalutamideCytochrome P450 2C8enzyme
DB08899EnzalutamideCytochrome P450 3A4enzyme
DB08899EnzalutamideAndrogen receptortarget
DB08899EnzalutamideCytochrome P450 2C9enzyme
DB08899EnzalutamideCytochrome P450 2C19enzyme
DB08899EnzalutamideCytochrome P450 2B6enzyme
DB08899EnzalutamideCytochrome P450 2D6enzyme
DB08899EnzalutamideCytochrome P450 3A5enzyme
DB08899EnzalutamideMultidrug resistance protein 1transporter
DB08899EnzalutamideThyroxine-binding globulincarrier
DB01609DeferasiroxIrontarget
DB01609DeferasiroxCytochrome P450 3A4enzyme
DB01609DeferasiroxUDP-glucuronosyltransferase 1-1enzyme
DB01609DeferasiroxUDP-glucuronosyltransferase 1-3enzyme
DB01609DeferasiroxUDP-glucuronosyltransferase 1-9enzyme
DB01609DeferasiroxCytochrome P450 2C8enzyme
DB01609DeferasiroxCytochrome P450 1A2enzyme
DB08912DabrafenibCytochrome P450 3A4enzyme
DB08912DabrafenibCytochrome P450 2C8enzyme
DB08912DabrafenibMultidrug resistance protein 1transporter
DB08912DabrafenibATP-binding cassette sub-family G member 2transporter
DB08912DabrafenibSolute carrier organic anion transporter family member 1B1transporter
DB08912DabrafenibSolute carrier organic anion transporter family member 1B3transporter
DB08912DabrafenibSolute carrier family 22 member 6transporter
DB08912DabrafenibSolute carrier family 22 member 8transporter
DB08912DabrafenibSerine/threonine-protein kinase B-raftarget
DB08912DabrafenibRAF proto-oncogene serine/threonine-protein kinasetarget
DB08912DabrafenibSerine/threonine-protein kinase SIK1target
DB08912DabrafenibSerine/threonine-protein kinase Nek11target
DB08912DabrafenibLIM domain kinase 1target
DB08912DabrafenibCytochrome P450 2B6enzyme
DB08912DabrafenibCytochrome P450 2C9enzyme
DB00648MitotaneCytochrome P450 11B1, mitochondrialtarget
DB00648MitotaneAdrenodoxin, mitochondrialtarget
DB00648MitotaneSex hormone-binding globulincarrier
DB00648MitotaneCorticosteroid-binding globulincarrier
DB00648MitotaneCytochrome P450 3A4enzyme
DB00648MitotaneEstrogen receptor alphatarget
DB00648MitotaneProgesterone receptortarget
DB00648MitotaneAndrogen receptortarget
DB00648MitotaneThyroxine-binding globulincarrier
DB04911OritavancinCytochrome P450 3A4enzyme
DB04911OritavancinCytochrome P450 2D6enzyme
DB04911OritavancinCytochrome P450 2C9enzyme
DB04911OritavancinCytochrome P450 2C19enzyme
DB00701AmprenavirHuman immunodeficiency virus type 1 proteasetarget
DB00701AmprenavirCytochrome P450 3A4enzyme
DB00701AmprenavirMultidrug resistance protein 1transporter
DB00701AmprenavirMultidrug resistance-associated protein 1transporter
DB00701AmprenavirCytochrome P450 2B6enzyme
DB00701AmprenavirCytochrome P450 2C19enzyme
DB00701AmprenavirCytochrome P450 2C8enzyme
DB00701AmprenavirCytochrome P450 2C9enzyme
DB00701AmprenavirCytochrome P450 2D6enzyme
DB00701AmprenavirCytochrome P450 3A5enzyme
DB00701AmprenavirSolute carrier organic anion transporter family member 1B1transporter
DB09330OsimertinibEpidermal growth factor receptortarget
DB09330OsimertinibMultidrug resistance protein 1transporter
DB09330OsimertinibATP-binding cassette sub-family G member 2transporter
DB09330OsimertinibCytochrome P450 3A4enzyme
DB09330OsimertinibCytochrome P450 1A2enzyme
DB00673AprepitantSubstance-P receptortarget
DB00673AprepitantCytochrome P450 3A4enzyme
DB00673AprepitantCytochrome P450 2C9enzyme
DB00673AprepitantCytochrome P450 3A5enzyme
DB00673AprepitantCytochrome P450 3A7enzyme
DB00673AprepitantCytochrome P450 2C19enzyme
DB00564CarbamazepineSodium channel protein type 5 subunit alphatarget
DB00564CarbamazepineCytochrome P450 2C8enzyme
DB00564CarbamazepineCytochrome P450 2B6enzyme
DB00564CarbamazepineCytochrome P450 3A4enzyme
DB00564CarbamazepineCytochrome P450 1A2enzyme
DB00564CarbamazepineCytochrome P450 2C19enzyme
DB00564CarbamazepineCytochrome P450 2C9enzyme
DB00564CarbamazepineMultidrug resistance protein 1transporter
DB00564CarbamazepineCytochrome P450 3A5enzyme
DB00564CarbamazepineCytochrome P450 3A7enzyme
DB00564CarbamazepineUDP-glucuronosyltransferase 2B7enzyme
DB00564CarbamazepineRalA-binding protein 1transporter
DB00564CarbamazepineCanalicular multispecific organic anion transporter 1transporter
DB00564CarbamazepineNeuronal acetylcholine receptor subunit alpha-4target
DB00564CarbamazepineNeuronal acetylcholine receptor subunit beta-2target
DB00564CarbamazepineNuclear receptor subfamily 1 group I member 2target
DB00564CarbamazepineUDP-glucuronosyltransferase 1-1enzyme
DB00564CarbamazepineThyroxine-binding globulincarrier
DB00474MethohexitalGamma-aminobutyric acid receptor subunit alpha-1target
DB00474MethohexitalCytochrome P450 2C19enzyme
DB00349ClobazamCytochrome P450 2C19enzyme
DB00349ClobazamCytochrome P450 3A4enzyme
DB00349ClobazamCytochrome P450 2B6enzyme
DB00349ClobazamCytochrome P450 2C18enzyme
DB00349ClobazamSodium- and chloride-dependent GABA transporter 1transporter
DB00349ClobazamSodium- and chloride-dependent GABA transporter 3transporter
DB00349ClobazamMultidrug resistance protein 1transporter
DB00349ClobazamGABA-A receptor (anion channel)target
DB00349ClobazamCytochrome P450 2D6enzyme