Cytochrome P450 3A Inducers

DrugDrug NameDrug Indication
DB00625EfavirenzFor use in combination treatment of HIV infection (AIDS)
DB00252PhenytoinFor the control of generalized tonic-clonic (grand mal) and complex partial (psychomotor, temporal lobe) seizures and prevention and treatment of seizures occurring during or following neurosurgery.
DB11560LesinuradFor use, in combination with a xanthine oxidase inhibitor, for the treatment of hyperuricemia associated with gout in patients who have not achieved target serum uric acid levels with a xanthine oxidase inhibitor alone.
DB00503RitonavirIndicated in combination with other antiretroviral agents for the treatment of HIV-1 infection.
DB12267BrigatinibThe anaplastic lymphoma kinase positive, metastatic non-small cell lung cancer (ALK+ NSCLC), represents only 3-5% of the NSCLC cancer cases, but the ALK mutation, overexpression and presence in several oncogenic fusion proteins in solid and hematologic tumors have pointed out the importance as well as its potential as a cancer therapy target.[A31311] The ALK-related cases of NSCLC are associated with the presence of the fusion gene EML4-ALK which fused the ALK protein with the echinoderm microtubule-associated protein like-4 whose original function is the correct formation of microtubules.[A31313] The presence of the aberrant fusion protein results in abnormal signaling that provokes increased cell growth, proliferation and survival.[A31316] Crizotinib is indicated for the treatment of such cases but the presence of ALK kinase domain mutations confer resistance to the treatment. Thus, brigatinib is indicated for the treatment of patients with ALK+ NSCLC with intolerance to Crizotinib.[A31314]
DB00559BosentanUsed in the treatment of pulmonary arterial hypertension (PAH), to improve exercise ability and to decrease the rate of clinical worsening (in patients with WHO Class III or IV symptoms).
DB09280LumacaftorWhen given in combination with [DB08820] as the fixed dose combination product Orkambi, lumacaftor is indicated for the treatment of cystic fibrosis (CF) in patients age 6 years and older who are homozygous for the F508del mutation in the CFTR gene. [FDA Label]
DrugDrug NameTargetType
DB00625EfavirenzCytochrome P450 2B6enzyme
DB00625EfavirenzCytochrome P450 3A4enzyme
DB00625EfavirenzCytochrome P450 2C19enzyme
DB00625EfavirenzCytochrome P450 2C9enzyme
DB00625EfavirenzCytochrome P450 1A2enzyme
DB00625EfavirenzCytochrome P450 2D6enzyme
DB00625EfavirenzReverse transcriptase/RNaseHtarget
DB00625EfavirenzCytochrome P450 2C8enzyme
DB00625EfavirenzSerum albumincarrier
DB00625EfavirenzCytochrome P450 3A5enzyme
DB00625EfavirenzCytochrome P450 3A7enzyme
DB00625EfavirenzUDP-glucuronosyltransferase 1-1enzyme
DB00625EfavirenzBile salt export pumptransporter
DB00625EfavirenzSolute carrier family 22 member 1transporter
DB00252PhenytoinSodium channel protein type 5 subunit alphatarget
DB00252PhenytoinSodium channel protein type 1 subunit alphatarget
DB00252PhenytoinCytochrome P450 2C8enzyme
DB00252PhenytoinCytochrome P450 2C19enzyme
DB00252PhenytoinCytochrome P450 2C9enzyme
DB00252PhenytoinCytochrome P450 2B6enzyme
DB00252PhenytoinCytochrome P450 3A5enzyme
DB00252PhenytoinSerum albumincarrier
DB00252PhenytoinCytochrome P450 3A4enzyme
DB00252PhenytoinSolute carrier organic anion transporter family member 1C1transporter
DB00252PhenytoinP-glycoprotein 1transporter
DB00252PhenytoinCanalicular multispecific organic anion transporter 1transporter
DB00252PhenytoinCytochrome P450 11B1, mitochondrialenzyme
DB00252PhenytoinCytochrome P450 3A7enzyme
DB00252PhenytoinNuclear receptor subfamily 1 group I member 2target
DB00252PhenytoinSodium channel subunit beta-1target
DB00252PhenytoinSodium channel protein type 3 subunit alphatarget
DB00252PhenytoinUDP-glucuronosyltransferase 1-1enzyme
DB00252PhenytoinUDP-glucuronosyltransferase 1-6enzyme
DB00252PhenytoinUDP-glucuronosyltransferase 1-9enzyme
DB00252PhenytoinThyroxine-binding globulincarrier
DB11560LesinuradSolute carrier family 22 member 12target
DB11560LesinuradSolute carrier family 22 member 11target
DB11560LesinuradCytochrome P450 2C9enzyme
DB00503RitonavirHuman immunodeficiency virus type 1 proteasetarget
DB00503RitonavirCytochrome P450 2D6enzyme
DB00503RitonavirCytochrome P450 2C9enzyme
DB00503RitonavirCytochrome P450 2C19enzyme
DB00503RitonavirCytochrome P450 2B6enzyme
DB00503RitonavirCytochrome P450 2C8enzyme
DB00503RitonavirP-glycoprotein 1transporter
DB00503RitonavirMultidrug resistance-associated protein 1transporter
DB00503RitonavirCanalicular multispecific organic anion transporter 1transporter
DB00503RitonavirSolute carrier organic anion transporter family member 1A2transporter
DB00503RitonavirATP-binding cassette sub-family G member 2transporter
DB00503RitonavirSolute carrier organic anion transporter family member 1B1transporter
DB00503RitonavirCytochrome P450 1A2enzyme
DB00503RitonavirCytochrome P450 2E1enzyme
DB00503RitonavirNuclear receptor subfamily 1 group I member 2target
DB00503RitonavirSerum albumincarrier
DB00503RitonavirCytochrome P450 3A4enzyme
DB00503RitonavirCytochrome P450 3A5enzyme
DB00503RitonavirCytochrome P450 3A7enzyme
DB00503RitonavirCytochrome P450 3A43enzyme
DB00503RitonavirUDP-glucuronosyltransferase 1-1enzyme
DB00503RitonavirSolute carrier organic anion transporter family member 2B1transporter
DB00503RitonavirBile salt export pumptransporter
DB12267BrigatinibALK tyrosine kinase receptortarget
DB12267BrigatinibEpidermal growth factor receptortarget
DB12267BrigatinibTyrosine-protein kinase ABL1target
DB12267BrigatinibInsulin-like growth factor 1 receptortarget
DB12267BrigatinibReceptor-type tyrosine-protein kinase FLT3target
DB12267BrigatinibCytochrome P450 2C8enzyme
DB12267BrigatinibCytochrome P450 3A4enzyme
DB12267BrigatinibInsulin receptortarget
DB12267BrigatinibHepatocyte growth factor receptortarget
DB12267BrigatinibReceptor tyrosine-protein kinase erbB-4target
DB12267BrigatinibReceptor tyrosine-protein kinase erbB-2target
DB12267BrigatinibATP-binding cassette sub-family B member 5transporter
DB12267BrigatinibATP-binding cassette sub-family G member 2transporter
DB12267BrigatinibSolute carrier family 22 member 1transporter
DB12267BrigatinibMultidrug and toxin extrusion protein 1transporter
DB12267BrigatinibMultidrug and toxin extrusion protein 2transporter
DB00559BosentanEndothelin B receptortarget
DB00559BosentanEndothelin-1 receptortarget
DB00559BosentanCytochrome P450 3A4enzyme
DB00559BosentanCytochrome P450 2C9enzyme
DB00559BosentanBile salt export pumptransporter
DB09280LumacaftorCytochrome P450 2B6enzyme
DB09280LumacaftorCytochrome P450 2C8enzyme
DB09280LumacaftorCytochrome P450 2C9enzyme
DB09280LumacaftorCytochrome P450 2C19enzyme
DB09280LumacaftorSerum albumincarrier
DB09280LumacaftorCystic fibrosis transmembrane conductance regulatortarget
DB09280LumacaftorCytochrome P450 3A4enzyme
DB09280LumacaftorP-glycoprotein 1transporter