Cytochrome P-450 CYP2C8 Inhibitors (weak)

DrugDrug NameDrug Indication
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.
DB06589PazopanibTreatment of advanced renal cell cancer and advanced soft tissue sarcoma (in patients previously treated with chemotherapy)
DB08875CabozantinibFor the treatment of metastatic medullary thyroid cancer and for the treatment of patients with advanced renal cell carcinoma (RCC) who have received prior anti-angiogenic therapy.
DB01072AtazanavirUsed in combination with other antiretroviral agents for the treatment of HIV-1 infection, as well as postexposure prophylaxis of HIV infection in individuals who have had occupational or nonoccupational exposure to potentially infectious body fluids of a person known to be infected with HIV when that exposure represents a substantial risk for HIV transmission.
DB00857TerbinafineFor the treatment of dermatophyte infections of the toenail or fingernail caused by susceptible fungi. Also for the treatment of tinea capitis (scalp ringworm) and tinea corporis (body ringworm) or tinea cruris (jock itch).
DB00533RofecoxibFor the treatment of osteoarthritis, rheumatoid arthritis, acute pain in adults, and primary dysmenorrhea, as well as acute treatment of migraine attacks with or without auras.
DB00908QuinidineFor the treatment of ventricular pre-excitation and cardiac dysrhythmias
DB01039FenofibrateFor use as adjunctive therapy to diet to reduce elevated LDL-C, Total-C,Triglycerides and Apo B, and to increase HDL-C in adult patients with primary hypercholesterolemia or mixed dyslipidemia (Fredrickson Types IIa and IIb)
DB01393BezafibrateFor the treatment of primary hyperlipidaemia types IIa, IIb, III, IV and V (Fredrickson classification) corresponding to groups I, II and III of the European Atherosclerosis Society guidelines - when diet alone or improvements in lifestyle such as increased exercise or weight reduction do not lead to an adequate response. Also for the treatment of secondary hyperlipidaemias, e.g. severe hypertriglyceridemias, when sufficient improvement does not occur after correction of the underlying disorder (e.g. diabetes mellitus).
DB00091CiclosporinCyclosporine is officially approved for different conditions listed below: * Prophylaxis of organ rejection in kidney, liver, and heart allogeneic transplants. For this indication, it can be used concomitantly with azathioprine and corticosteroids. * Treatment of patients with severe active, rheumatoid arthritis when the patient no longer responds to methotrexate. * Concomitantly with methotrexate for the treatment of patients with severe active rheumatoid arthritis when patients do not respond to methotrexate treatment alone. * Treatment of adult nonimmunocompromised patients with severe, recalcitrant, plaque psoriasis that have failed to respond to at least one systemic therapy or when systemic therapies are not tolerated or contraindicated.[FDA label] * Its ophthalmic solution is indicated to increase tear production in patients with keratoconjunctivitis sicca in patients from 4 years old.[L5158] * Prevention of graft rejection following bone marrow transplantation and in the treatment of graft-versus-host disease (GVHD). * Treatment of steroid dependent and steroid-resistant nephrotic syndrome due to glomerular diseases such as minimal change nephropathy, focal and segmental glomerulosclerosis or membranous glomerulonephritis in adults and children.[F3091] Away from all this approved and reviewed indications, cyclosporine is commonly used on dermatology for the treatment of various inflammatory skin conditions such as atopic dermatitis, blistering disorders, and connective tissue diseases.[A174085]
DB00501CimetidineFor the treatment and the management of acid-reflux disorders (GERD), peptic ulcer disease, heartburn, and acid indigestion.
DB01009KetoprofenFor symptomatic treatment of acute and chronic rheumatoid arthritis, osteoarthritis, ankylosing spondylitis, primary dysmenorrhea and mild to moderate pain associated with musculotendinous trauma (sprains and strains), postoperative (including dental surgery) or postpartum pain.
DB00205PyrimethamineFor the treatment of toxoplasmosis and acute malaria; For the prevention of malaria in areas non-resistant to pyrimethamine
DB00208TiclopidineUsed in patients, who have had a stroke or stroke precursors and who cannot take aspirin or aspirin has not worked, to try to prevent another thrombotic stroke.
DB13179TroleandomycinFor the treatment of bacterial infection.
DB09054IdelalisibIdelalisib is indicated in the treatment of chronic lymphocytic leukemia (CLL), relapsed follicular B-cell non-Hodgkin lymphoma (FL), and relapsed small lymphocytic lymphoma (SLL). For the treatment of relapsed CLL, it is currently indicated as a second-line agent in combination with rituximab in patients for whom rituximab alone would be considered appropriate therapy due to other co-morbidities, while in the treatment of FL and SLL it is intended to be used in patients who have received at least two prior systemic therapies.
DB05015BelinostatBelinostat is indicated for the treatment of patients with relapsed or refractory peripheral T-cell lymphoma (PTCL) with manageable safety profile. It is a potential alternative therapy for patients who did not experience adequate response to first-line drugs for PTCL. It can be used in patients with baseline thrombocytopenia [A19161].
DB13919CandesartanNot Available
DB11632OpicaponeOpicapone is approved as an adjunctive therapy in adults with Parkinson’s disease and end-of-dose motor fluctuations whose symptoms cannot be stabilized on levodopa/dopa decarboxylase inhibitor combinations [L2336].
DB01079TegaserodTegaserod is a serotonin-4 (5-HT4) receptor agonist indicated for the treatment of adult women less than 65 years of age with irritable bowel syndrome with constipation (IBS-C) [F4223, F4229]. The safety and effectiveness of tegaserod in men with IBS-C have not been established [F4223, F4229].
DrugDrug NameTargetType
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
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
DB08875CabozantinibCytochrome P450 3A4enzyme
DB08875CabozantinibCytochrome P450 2C9enzyme
DB08875CabozantinibHepatocyte growth factor receptortarget
DB08875CabozantinibVascular endothelial growth factor receptor 2target
DB08875CabozantinibProto-oncogene tyrosine-protein kinase receptor Rettarget
DB08875CabozantinibCytochrome P450 2C8enzyme
DB01072AtazanavirHuman immunodeficiency virus type 1 proteasetarget
DB01072AtazanavirCytochrome P450 3A4enzyme
DB01072AtazanavirCytochrome P450 2C9enzyme
DB01072AtazanavirMultidrug resistance protein 1transporter
DB01072AtazanavirMultidrug resistance-associated protein 1transporter
DB01072AtazanavirSerum albumincarrier
DB01072AtazanavirUDP-glucuronosyltransferase 1-1enzyme
DB01072AtazanavirSolute carrier organic anion transporter family member 1B1transporter
DB01072AtazanavirSolute carrier organic anion transporter family member 1B3transporter
DB01072AtazanavirCytochrome P450 2C8enzyme
DB01072AtazanavirBile salt export pumptransporter
DB00857TerbinafineSqualene monooxygenasetarget
DB00857TerbinafineCytochrome P450 2D6enzyme
DB00857TerbinafineCytochrome P450 2C9enzyme
DB00857TerbinafineCytochrome P450 1A2enzyme
DB00857TerbinafineCytochrome P450 3A4enzyme
DB00857TerbinafineCytochrome P450 2C8enzyme
DB00857TerbinafineCytochrome P450 2C19enzyme
DB00857TerbinafineProstaglandin G/H synthase 1enzyme
DB00857TerbinafineCholesterol side-chain cleavage enzyme, mitochondrialenzyme
DB00857TerbinafineCytochrome P450 19A1enzyme
DB00533RofecoxibProstaglandin G/H synthase 2target
DB00533RofecoxibElastintarget
DB00533RofecoxibCytochrome P450 3A4enzyme
DB00533RofecoxibCytochrome P450 1A2enzyme
DB00533RofecoxibMultidrug resistance-associated protein 4transporter
DB00533RofecoxibProstaglandin G/H synthase 1enzyme
DB00533RofecoxibCytochrome P450 2C8enzyme
DB00533RofecoxibCytochrome P450 2C9enzyme
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 2C9enzyme
DB00908QuinidineAlpha-1A adrenergic receptortarget
DB00908QuinidineAlpha-1B adrenergic receptortarget
DB00908QuinidineAlpha-1D adrenergic receptortarget
DB00908QuinidineBile salt export pumptransporter
DB00908QuinidineCytochrome P450 2C8enzyme
DB01039FenofibratePeroxisome proliferator-activated receptor alphatarget
DB01039FenofibrateMetalloproteinasetarget
DB01039FenofibrateCytochrome P450 2C8enzyme
DB01039FenofibrateCytochrome P450 2C9enzyme
DB01039FenofibrateCytochrome P450 3A4enzyme
DB01039FenofibratePeroxisome proliferator-activated receptor gammatarget
DB01039FenofibratePeroxisome proliferator-activated receptor deltatarget
DB01039FenofibrateNuclear receptor subfamily 1 group I member 2target
DB01039FenofibrateUDP-glucuronosyltransferase 1-1enzyme
DB01039FenofibrateBile salt export pumptransporter
DB01393BezafibratePeroxisome proliferator-activated receptor alphatarget
DB01393BezafibrateSolute carrier organic anion transporter family member 1B1transporter
DB01393BezafibratePeroxisome proliferator-activated receptor deltatarget
DB01393BezafibratePeroxisome proliferator-activated receptor gammatarget
DB01393BezafibrateCytochrome P450 1A1enzyme
DB01393BezafibrateCytochrome P450 2C8enzyme
DB01393BezafibrateCytochrome P450 3A4enzyme
DB01393BezafibrateNuclear receptor subfamily 1 group I member 2target
DB01393BezafibrateRetinoic acid receptor RXR-alphatarget
DB01393BezafibrateRetinoic acid receptor RXR-betatarget
DB01393BezafibrateRetinoic acid receptor RXR-gammatarget
DB00091CiclosporinCalcium signal-modulating cyclophilin ligandtarget
DB00091CiclosporinPeptidyl-prolyl cis-trans isomerase Atarget
DB00091CiclosporinCalcineurin subunit B type 2target
DB00091CiclosporinCytochrome P450 3A5enzyme
DB00091CiclosporinCytochrome P450 3A4enzyme
DB00091CiclosporinCytochrome P450 3A7enzyme
DB00091CiclosporinMultidrug resistance protein 1transporter
DB00091CiclosporinCanalicular multispecific organic anion transporter 2transporter
DB00091CiclosporinBile salt export pumptransporter
DB00091CiclosporinSolute carrier organic anion transporter family member 1A2transporter
DB00091CiclosporinIleal sodium/bile acid cotransportertransporter
DB00091CiclosporinSodium/bile acid cotransportertransporter
DB00091CiclosporinSolute carrier family 22 member 6transporter
DB00091CiclosporinMultidrug resistance-associated protein 7transporter
DB00091CiclosporinCanalicular multispecific organic anion transporter 1transporter
DB00091CiclosporinATP-binding cassette sub-family G member 2transporter
DB00091CiclosporinSolute carrier organic anion transporter family member 1B1transporter
DB00091CiclosporinCytochrome P450 2C19enzyme
DB00091CiclosporinCytochrome P450 2C8enzyme
DB00091CiclosporinCytochrome P450 2C9enzyme
DB00091CiclosporinCytochrome P450 2D6enzyme
DB00091CiclosporinPeptidyl-prolyl cis-trans isomerase F, mitochondrialtarget
DB00091CiclosporinSolute carrier organic anion transporter family member 1B3transporter
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
DB00501CimetidineBile salt export pumptransporter
DB00501CimetidineMultidrug and toxin extrusion protein 2transporter
DB01009KetoprofenProstaglandin G/H synthase 1target
DB01009KetoprofenProstaglandin G/H synthase 2target
DB01009KetoprofenC-X-C chemokine receptor type 1target
DB01009KetoprofenSerum albumincarrier
DB01009KetoprofenMultidrug resistance-associated protein 4transporter
DB01009KetoprofenSolute carrier organic anion transporter family member 1A2transporter
DB01009KetoprofenSolute carrier family 22 member 6transporter
DB01009KetoprofenSolute carrier family 22 member 8transporter
DB01009KetoprofenSolute carrier family 22 member 11transporter
DB01009KetoprofenSolute carrier family 22 member 7transporter
DB01009KetoprofenCytochrome P450 2C9enzyme
DB01009KetoprofenCytochrome P450 2C8enzyme
DB01009KetoprofenUDP-glucuronosyltransferase 1-1enzyme
DB00205PyrimethamineBifunctional dihydrofolate reductase-thymidylate synthasetarget
DB00205PyrimethamineDihydrofolate reductasetarget
DB00205PyrimethamineCytochrome P450 2C8enzyme
DB00205PyrimethamineBeta-hexosaminidase subunit betatarget
DB00205PyrimethamineMultidrug and toxin extrusion protein 1transporter
DB00205PyrimethamineMultidrug and toxin extrusion protein 2transporter
DB00208TiclopidineP2Y purinoceptor 12target
DB00208TiclopidineCytochrome P450 3A4enzyme
DB00208TiclopidineCytochrome P450 2C19enzyme
DB00208TiclopidineCytochrome P450 2B6enzyme
DB00208TiclopidineCytochrome P450 2C9enzyme
DB00208TiclopidineCytochrome P450 2D6enzyme
DB00208TiclopidineMyeloperoxidaseenzyme
DB00208TiclopidineCytochrome P450 1A1enzyme
DB00208TiclopidineCytochrome P450 1A2enzyme
DB00208TiclopidineCytochrome P450 2C8enzyme
DB00208TiclopidineCytochrome P450 2E1enzyme
DB13179TroleandomycinCytochrome P450 2C9enzyme
DB13179TroleandomycinCytochrome P450 3A5enzyme
DB13179TroleandomycinCytochrome P450 3A43enzyme
DB13179Troleandomycin50S ribosomal protein L4target
DB13179Troleandomycin50S ribosomal protein L32target
DB13179TroleandomycinMultidrug resistance protein 1transporter
DB13179TroleandomycinCytochrome P450 2C18enzyme
DB13179TroleandomycinCytochrome P450 2C8enzyme
DB13179TroleandomycinCytochrome P450 3A4enzyme
DB13179TroleandomycinNuclear receptor subfamily 1 group I member 2target
DB13179TroleandomycinCytochrome P450 3A7enzyme
DB09054IdelalisibPhosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit delta isoform (P110δ)target
DB09054IdelalisibATP-binding cassette sub-family G member 2transporter
DB09054IdelalisibMultidrug resistance protein 1transporter
DB09054IdelalisibAldehyde oxidaseenzyme
DB09054IdelalisibUDP-glucuronosyltransferase 1A4enzyme
DB09054IdelalisibUDP-glucuronosyltransferase 1A1enzyme
DB09054IdelalisibCytochrome P450 2C8enzyme
DB09054IdelalisibCytochrome P450 2C19enzyme
DB09054IdelalisibCytochrome P450 2B6enzyme
DB09054IdelalisibCytochrome P450 3A4enzyme
DB09054IdelalisibSolute carrier organic anion transporter family member 1B1transporter
DB09054IdelalisibSolute carrier organic anion transporter family member 1B3transporter
DB09054IdelalisibCytochrome P450 3A5enzyme
DB09054IdelalisibCytochrome P450 3A43enzyme
DB09054IdelalisibCytochrome P450 3A7enzyme
DB05015BelinostatHistone deacetylasetarget
DB05015BelinostatCytochrome P450 1A2enzyme
DB05015BelinostatUDP-glucuronosyltransferase 1A1enzyme
DB05015BelinostatCytochrome P450 2C8enzyme
DB05015BelinostatCytochrome P450 2C9enzyme
DB05015BelinostatMultidrug resistance protein 1transporter
DB13919CandesartanType-1 angiotensin II receptortarget
DB13919CandesartanCytochrome P450 2C8enzyme
DB13919CandesartanCytochrome P450 2C9enzyme
DB13919CandesartanMultidrug resistance protein 1transporter
DB13919CandesartanUDP-glucuronosyltransferase 1-3enzyme
DB13919CandesartanProstaglandin G/H synthase 1enzyme
DB13919CandesartanSolute carrier organic anion transporter family member 1B1transporter
DB11632OpicaponeCytochrome P450 2C19enzyme
DB11632OpicaponeCytochrome P450 2C8enzyme
DB11632OpicaponeCatechol O-methyltransferasetarget
DB01079Tegaserod5-hydroxytryptamine receptor 4target
DB01079Tegaserod5-hydroxytryptamine receptor 2Btarget
DB01079Tegaserod5-hydroxytryptamine receptor 2Ctarget
DB01079Tegaserod5-hydroxytryptamine receptor 2Atarget
DB01079TegaserodSodium-dependent serotonin transportertransporter
DB01079TegaserodCytochrome P450 1A2enzyme
DB01079TegaserodCytochrome P450 2C8enzyme
DB01079TegaserodCytochrome P450 2D6enzyme
DB01079TegaserodCytochrome P450 2E1enzyme
DB01079TegaserodATP-binding cassette sub-family G member 2transporter
DB01079TegaserodMultidrug resistance protein 1transporter