Cytochrome P-450 CYP3A4 Inhibitors (weak)

DrugDrug NameDrug Indication
DB01254DasatinibFor the treatment of adults with chronic, accelerated, or myeloid or lymphoid blast phase chronic myeloid leukemia with resistance or intolerance to prior therapy. Also indicated for the treatment of adults with Philadelphia chromosome-positive acute lymphoblastic leukemia with resistance or intolerance to prior therapy.
DB01259LapatinibIndicated in combination with capecitabine for the treatment of patients with advanced or metastatic breast cancer whose tumors overexpress the human epidermal receptor type 2 (HER2) protein and who have received prior therapy including an anthracycline, a taxane, and trastuzuma.
DB00908QuinidineFor the treatment of ventricular pre-excitation and cardiac dysrhythmias
DB06589PazopanibTreatment of advanced renal cell cancer and advanced soft tissue sarcoma (in patients previously treated with chemotherapy)
DB00818PropofolUsed for induction and/or maintenance of anaesthesia and for management of refractory status epilepticus.
DB08820IvacaftorWhen used as monotherapy as the product Kalydeco, ivacaftor is indicated for the managmenet of CF in patients age 2 years and older who have a mutation in the CFTR gene that is responsive to ivacaftor potentiation. Ivacaftor received expanded approval in May 2017 for the following 33 CFTR mutations: E56K, P67L, R74W, D110E, D110H, R117C, R117H, G178R, E193K, L206W, R347H, R352Q, A455E, S549N, S549R, G551D, G551S, D579G, S945L, S977F, F1052V, K1060T, A1067T, G1069R, R1070Q, R1070W, F1074L, D1152H, G1244E, S1251N, S1255P, D1270N, and G1349D [L768, FDA Label]. When used in combination with the drug [DB09280] as the product Orkambi, ivacaftor is indicated for the management of CF patients age 6 years and older who are homozygous for the F508del mutation in the CFTR gene.
DB01764DalfopristinFor the treatment of bacterial infections (usually in combination with quinupristin).
DB01369QuinupristinFor the treatment of bacterial infections (usually in combination with dalfopristin).
DB08827LomitapideUsed in homozygous familial hypercholesterolemia (HoFH) patients to reduce low-density lipoprotein cholesterol (LDL-C), total cholesterol (TC), apolipoprotein B (apo B), and non-high-density lipoprotein cholesterol (non-HDL-C).
DB09073PalbociclibPalbociclib is indicated in combination with letrozole for the treatment of postmenopausal women with estrogen receptor (ER)-positive, human epidermal growth factor receptor 2 (HER2)-negative advanced breast cancer as initial endocrine-based therapy for their metastatic disease. This indication is approved under accelerated approval based on progression-free survival (PFS). Continued approval for this indication may be contingent upon verification and description of clinical benefit in a confirmatory trial.
DB06717FosaprepitantFor the prevention of nausea and vomiting associated with highly emetogenic cancer chemotherapy.
DB09238ManidipineFor the treatment of hypertension.
DB11767SarilumabIndicated for modere to severe reactive RA in adult patients who are irresponsive, respond inadequately or present intolerance to disease-modifying anti-rheumatic drugs (DMARDs) or tumor necrosis factor (TNF) antagonists. It is indicated to be used in combination with methotrexate (MTX) or as a monotherapy when there is intolerance to MTX or MTX administration is inappropriate.
DB13941PiperaquineFor the treatment of uncomplicated *Plasmodium falciparum* infection in adults, children, and infants aged 6 months and up weighing over 5 kg [FDA Label]. Used in combination with [DB11638].
DB12332RucaparibIndicated as monotherapy for the treatment of patients with deleterious BRCA mutation (germline and/or somatic) associated advanced ovarian cancer who have been treated with two or more chemotherapies. Select patients for therapy based on an FDA-approved companion diagnostic for rucaparib.
DB00501CimetidineFor the treatment and the management of acid-reflux disorders (GERD), peptic ulcer disease, heartburn, and acid indigestion.
DB00921BuprenorphineFor the treatment of moderate to severe pain, peri-operative analgesia, and opioid dependence.
DB01173OrphenadrineIndicated for the treatment of Parkinson's disease.
DB00188BortezomibFor treatment of multiple myeloma in patients who have not been successfully treated with at least two previous therapies.
DB00289AtomoxetineFor the treatment of Attention-Deficit/Hyperactivity Disorder (ADHD) alone or in combination with behavioral treatment, as an adjunct to psychological, educational, social, and other remedial measures.
DrugDrug NameTargetType
DB01254DasatinibTyrosine-protein kinase ABL1target
DB01254DasatinibAbelson tyrosine-protein kinase 2target
DB01254DasatinibProto-oncogene tyrosine-protein kinase Srctarget
DB01254DasatinibTyrosine-protein kinase Fyntarget
DB01254DasatinibTyrosine-protein kinase Lcktarget
DB01254DasatinibTyrosine-protein kinase Yestarget
DB01254DasatinibMast/stem cell growth factor receptor Kittarget
DB01254DasatinibPlatelet-derived growth factor receptor betatarget
DB01254DasatinibEphrin type-A receptor 2target
DB01254DasatinibSignal transducer and activator of transcription 5Btarget
DB01254DasatinibCytochrome P450 3A4enzyme
DB01254DasatinibMultidrug resistance protein 1transporter
DB01254DasatinibATP-binding cassette sub-family G member 2transporter
DB01254DasatinibCytochrome P450 1A1enzyme
DB01254DasatinibCytochrome P450 1A2enzyme
DB01254DasatinibCytochrome P450 1B1enzyme
DB01254DasatinibCytochrome P450 3A5enzyme
DB01254DasatinibDimethylaniline monooxygenase [N-oxide-forming] 3enzyme
DB01254DasatinibTyrosine-protein kinase BTKtarget
DB01254DasatinibNuclear receptor subfamily 4 group A member 3target
DB01254DasatinibBreakpoint cluster region proteintarget
DB01254DasatinibTyrosine-protein kinase CSKtarget
DB01254DasatinibEphrin type-A receptor 5target
DB01254DasatinibEphrin type-B receptor 4target
DB01254DasatinibTyrosine-protein kinase Fgrtarget
DB01254DasatinibTyrosine-protein kinase FRKtarget
DB01254DasatinibHeat shock cognate 71 kDa proteintarget
DB01254DasatinibTyrosine-protein kinase Lyntarget
DB01254DasatinibMitogen-activated protein kinase kinase kinase MLTtarget
DB01254DasatinibMitogen-activated protein kinase 14target
DB01254DasatinibAmidophosphoribosyltransferasetarget
DB01259LapatinibEpidermal growth factor receptortarget
DB01259LapatinibReceptor tyrosine-protein kinase erbB-2target
DB01259LapatinibCytochrome P450 3A4enzyme
DB01259LapatinibCytochrome P450 2C8enzyme
DB01259LapatinibMultidrug resistance protein 1transporter
DB01259LapatinibAntigen peptide transporter 1transporter
DB01259LapatinibCytochrome P450 3A5enzyme
DB01259LapatinibCytochrome P450 2C19enzyme
DB00908QuinidineSodium channel protein type 5 subunit alphatarget
DB00908QuinidineAlpha-1-acid glycoprotein 1carrier
DB00908QuinidinePotassium voltage-gated channel subfamily H member 2target
DB00908QuinidinePotassium channel subfamily K member 1target
DB00908QuinidinePotassium channel subfamily K member 6target
DB00908QuinidineCytochrome P450 1A2enzyme
DB00908QuinidineCytochrome P450 2E1enzyme
DB00908QuinidineCytochrome P450 1A1enzyme
DB00908QuinidineCytochrome P450 2D6enzyme
DB00908QuinidineCytochrome P450 3A4enzyme
DB00908QuinidineCytochrome P450 3A7enzyme
DB00908QuinidineSolute carrier family 22 member 2transporter
DB00908QuinidineSolute carrier family 22 member 1transporter
DB00908QuinidineSolute carrier family 22 member 5transporter
DB00908QuinidineMultidrug resistance protein 1transporter
DB00908QuinidineSolute carrier organic anion transporter family member 1A2transporter
DB00908QuinidineSolute carrier family 22 member 8transporter
DB00908QuinidineCanalicular multispecific organic anion transporter 1transporter
DB00908QuinidineSolute carrier family 22 member 4transporter
DB00908QuinidineSolute carrier organic anion transporter family member 1B1transporter
DB00908QuinidineCytochrome P450 2B6enzyme
DB00908QuinidineCytochrome P450 2C8enzyme
DB00908QuinidineCytochrome P450 2C9enzyme
DB00908QuinidineAlpha-1A adrenergic receptortarget
DB00908QuinidineAlpha-1B adrenergic receptortarget
DB00908QuinidineAlpha-1D adrenergic receptortarget
DB06589PazopanibVascular endothelial growth factor receptor 1target
DB06589PazopanibVascular endothelial growth factor receptor 2target
DB06589PazopanibVascular endothelial growth factor receptor 3target
DB06589PazopanibPlatelet-derived growth factor receptor alphatarget
DB06589PazopanibPlatelet-derived growth factor receptor betatarget
DB06589PazopanibMast/stem cell growth factor receptor Kittarget
DB06589PazopanibCytochrome P450 3A4enzyme
DB06589PazopanibCytochrome P450 2D6enzyme
DB06589PazopanibCytochrome P450 2C8enzyme
DB06589PazopanibCytochrome P450 1A2enzyme
DB06589PazopanibMultidrug resistance protein 1transporter
DB06589PazopanibATP-binding cassette sub-family G member 2transporter
DB06589PazopanibSolute carrier organic anion transporter family member 1B1transporter
DB06589PazopanibUDP-glucuronosyltransferase 1-1transporter
DB06589PazopanibFibroblast growth factor receptor 3target
DB06589PazopanibTyrosine-protein kinase ITK/TSKtarget
DB06589PazopanibFibroblast growth factor 1target
DB06589PazopanibSH2B adapter protein 3target
DB00818PropofolCytochrome P450 2B6enzyme
DB00818PropofolUDP-glucuronosyltransferase 1-1enzyme
DB00818PropofolUDP-glucuronosyltransferase 1-9enzyme
DB00818PropofolGamma-aminobutyric acid receptor subunit beta-2target
DB00818PropofolGamma-aminobutyric acid receptor subunit beta-3target
DB00818PropofolSerum albumincarrier
DB00818PropofolSodium channel protein type 4 subunit alphatarget
DB00818PropofolSodium channel protein type 2 subunit alphatarget
DB00818PropofolFatty-acid amide hydrolase 1enzyme
DB00818PropofolCytochrome P450 2C9enzyme
DB00818PropofolUDP-glucuronosyltransferase 1-8enzyme
DB00818PropofolCytochrome P450 2E1enzyme
DB00818PropofolCytochrome P450 1B1enzyme
DB00818PropofolCytochrome P450 1A1enzyme
DB00818PropofolCytochrome P450 1A2enzyme
DB00818PropofolCytochrome P450 2A6enzyme
DB00818PropofolCytochrome P450 2C18enzyme
DB00818PropofolCytochrome P450 2C19enzyme
DB00818PropofolCytochrome P450 2C8enzyme
DB00818PropofolCytochrome P450 2D6enzyme
DB00818PropofolCytochrome P450 3A4enzyme
DB00818PropofolUDP-glucuronosyltransferase 1-6enzyme
DB00818PropofolGABA-A receptor (anion channel)target
DB08820IvacaftorCystic fibrosis transmembrane conductance regulatortarget
DB08820IvacaftorCytochrome P450 3A4enzyme
DB08820IvacaftorSerum albumincarrier
DB08820IvacaftorAlpha-1-acid glycoprotein 1carrier
DB08820IvacaftorMultidrug resistance protein 1transporter
DB08820IvacaftorCytochrome P450 3A5enzyme
DB01764DalfopristinStreptogramin A acetyltransferasetarget
DB01764DalfopristinCytochrome P450 3A4enzyme
DB01369Quinupristin23S rRNAtarget
DB01369Quinupristin50S ribosomal protein L10target
DB01369Quinupristin50S ribosomal protein L22target
DB01369QuinupristinCytochrome P450 3A4enzyme
DB08827LomitapideMicrosomal triglyceride transfer protein large subunittarget
DB08827LomitapideCytochrome P450 3A4enzyme
DB08827LomitapideMultidrug resistance protein 1transporter
DB09073PalbociclibCyclin-dependent kinase 4target
DB09073PalbociclibCyclin-dependent kinase 6target
DB09073PalbociclibCytochrome P450 3A4enzyme
DB09073PalbociclibSulfotransferase 2A1enzyme
DB06717FosaprepitantCytochrome P450 3A4enzyme
DB09238ManidipineVoltage dependent L type calcium channeltarget
DB09238ManidipineVoltage-dependent T-type calcium channeltarget
DB09238ManidipineCytochrome P450 2C9enzyme
DB09238ManidipineCytochrome P450 2D6enzyme
DB09238ManidipineCytochrome P450 1A1enzyme
DB09238ManidipineCytochrome P450 1A2enzyme
DB09238ManidipineCytochrome P450 2B6enzyme
DB09238ManidipineCytochrome P450 2C19enzyme
DB09238ManidipineCytochrome P450 3A4enzyme
DB11767SarilumabAlanine aminotransferase 1enzyme
DB11767SarilumabAlanine aminotransferase 2enzyme
DB11767SarilumabAspartate aminotransferaseenzyme
DB11767SarilumabCytochrome P450 3A4enzyme
DB11767SarilumabInterleukin-6 receptor subunit alphatarget
DB11767SarilumabHigh affinity immunoglobulin gamma Fc receptor Itarget
DB11767SarilumabLow affinity immunoglobulin gamma Fc region receptor II-atarget
DB11767SarilumabLow affinity immunoglobulin gamma Fc region receptor II-btarget
DB11767SarilumabLow affinity immunoglobulin gamma Fc region receptor III-Atarget
DB11767SarilumabLow affinity immunoglobulin gamma Fc region receptor III-Btarget
DB13941PiperaquineCytochrome P450 3A4enzyme
DB13941PiperaquineCytochrome P450 2C19enzyme
DB13941PiperaquineCytochrome P450 2C9enzyme
DB13941PiperaquineCytochrome P450 2B6enzyme
DB13941PiperaquineCytochrome P450 2E1enzyme
DB12332RucaparibPoly [ADP-ribose] polymerase 1target
DB12332RucaparibPoly [ADP-ribose] polymerase 2target
DB12332RucaparibPoly [ADP-ribose] polymerase 3target
DB12332RucaparibCytochrome P450 2D6enzyme
DB12332RucaparibCytochrome P450 1A2enzyme
DB12332RucaparibCytochrome P450 3A4enzyme
DB12332RucaparibMultidrug resistance protein 1transporter
DB12332RucaparibATP-binding cassette sub-family G member 2transporter
DB12332RucaparibMultidrug and toxin extrusion protein 1transporter
DB12332RucaparibMultidrug and toxin extrusion protein 2transporter
DB12332RucaparibSolute carrier family 22 member 1transporter
DB12332RucaparibMultidrug resistance-associated protein 4transporter
DB12332RucaparibSolute carrier organic anion transporter family member 1B1transporter
DB12332RucaparibSolute carrier organic anion transporter family member 1B3transporter
DB12332RucaparibSolute carrier family 22 member 6transporter
DB12332RucaparibSolute carrier family 22 member 8transporter
DB12332RucaparibCytochrome P450 3A5enzyme
DB12332RucaparibCytochrome P450 3A7enzyme
DB12332RucaparibCytochrome P450 3A43enzyme
DB12332RucaparibCytochrome P450 2C19enzyme
DB12332RucaparibCytochrome P450 2C9enzyme
DB12332RucaparibCytochrome P450 2C8enzyme
DB12332RucaparibUDP-glucuronosyltransferase 1-1enzyme
DB00501CimetidineHistamine H2 receptortarget
DB00501CimetidineCytochrome P450 1A2enzyme
DB00501CimetidineCytochrome P450 2D6enzyme
DB00501CimetidineCytochrome P450 2C19enzyme
DB00501CimetidineCytochrome P450 3A4enzyme
DB00501CimetidineCytochrome P450 3A5enzyme
DB00501CimetidineCytochrome P450 3A7enzyme
DB00501CimetidineMultidrug resistance protein 1transporter
DB00501CimetidineSolute carrier family 22 member 2transporter
DB00501CimetidineSolute carrier family 22 member 1transporter
DB00501CimetidineSolute carrier family 22 member 3transporter
DB00501CimetidineSolute carrier family 22 member 5transporter
DB00501CimetidineSolute carrier family 22 member 6transporter
DB00501CimetidineSolute carrier family 22 member 8transporter
DB00501CimetidineMultidrug and toxin extrusion protein 1transporter
DB00501CimetidineSolute carrier family 22 member 4transporter
DB00501CimetidineSolute carrier family 22 member 11transporter
DB00501CimetidineSolute carrier family 22 member 7transporter
DB00501CimetidineCytochrome P450 11B1, mitochondrialenzyme
DB00501CimetidineCytochrome P450 2C8enzyme
DB00501CimetidineCytochrome P450 2C9enzyme
DB00501CimetidineCytochrome P450 2E1enzyme
DB00501CimetidineDimethylaniline monooxygenase [N-oxide-forming] 3enzyme
DB00501CimetidineDimethylaniline monooxygenase [N-oxide-forming] 1enzyme
DB00921BuprenorphineKappa-type opioid receptortarget
DB00921BuprenorphineMu-type opioid receptortarget
DB00921BuprenorphineCytochrome P450 3A4enzyme
DB00921BuprenorphineCytochrome P450 2D6enzyme
DB00921BuprenorphineMultidrug resistance protein 1transporter
DB00921BuprenorphineATP-binding cassette sub-family G member 2transporter
DB00921BuprenorphineCytochrome P450 2C9enzyme
DB00921BuprenorphineCytochrome P450 3A5enzyme
DB00921BuprenorphineCytochrome P450 2C8enzyme
DB00921BuprenorphineCytochrome P450 3A7enzyme
DB00921BuprenorphineUDP-glucuronosyltransferase 1-9enzyme
DB00921BuprenorphineDelta-type opioid receptortarget
DB00921BuprenorphineCytochrome P450 1A2enzyme
DB00921BuprenorphineCytochrome P450 2A6enzyme
DB00921BuprenorphineCytochrome P450 2C18enzyme
DB00921BuprenorphineCytochrome P450 2C19enzyme
DB00921BuprenorphineNociceptin receptortarget
DB00921BuprenorphineUDP-glucuronosyltransferase 1-1enzyme
DB01173OrphenadrineGlutamate receptor ionotropic, NMDA 1target
DB01173OrphenadrineGlutamate receptor ionotropic, NMDA 2Dtarget
DB01173OrphenadrineGlutamate receptor ionotropic, NMDA 3Btarget
DB01173OrphenadrineGlutamate receptor ionotropic, NMDA 3Atarget
DB01173OrphenadrineHistamine H1 receptortarget
DB01173OrphenadrineCytochrome P450 2B6enzyme
DB01173OrphenadrineCytochrome P450 2E1enzyme
DB01173OrphenadrineCytochrome P450 3A4enzyme
DB01173OrphenadrineSodium-dependent noradrenaline transportertarget
DB01173OrphenadrineSodium channel protein type 10 subunit alphatarget
DB01173OrphenadrineCytochrome P450 1A2enzyme
DB00188BortezomibCytochrome P450 3A4enzyme
DB00188BortezomibCytochrome P450 2C19enzyme
DB00188BortezomibCytochrome P450 1A2enzyme
DB00188BortezomibCytochrome P450 2D6enzyme
DB00188BortezomibCytochrome P450 2C9enzyme
DB00188BortezomibProteasome subunit beta type-5target
DB00188BortezomibProteasome subunit beta type-1target
DB00289AtomoxetineSodium-dependent noradrenaline transportertarget
DB00289AtomoxetineCytochrome P450 2D6enzyme
DB00289AtomoxetineSodium-dependent serotonin transportertarget
DB00289AtomoxetineCytochrome P450 2C19enzyme
DB00289AtomoxetineCytochrome P450 3A4enzyme
DB00289AtomoxetineSodium-dependent dopamine transportertarget
DB00289AtomoxetineNMDA receptortarget