Cytochrome P-450 CYP1A2 Inhibitors (moderate)

DrugDrug NameDrug Indication
DB00188BortezomibFor treatment of multiple myeloma in patients who have not been successfully treated with at least two previous therapies.
DB00201CaffeineFor management of fatigue, orthostatic hypotension, and for the short term treatment of apnea of prematurity in infants.
DB00268RopiniroleFor the treatment of the signs and symptoms of idiopathic Parkinson's disease. Also used for the treatment of restless legs syndrome.
DB00277TheophyllineFor the treatment of the symptoms and reversible airflow obstruction associated with chronic asthma and other chronic lung diseases, such as emphysema and chronic bronchitis.
DB00281LidocaineFor production of local or regional anesthesia by infiltration techniques such as percutaneous injection and intravenous regional anesthesia by peripheral nerve block techniques such as brachial plexus and intercostal and by central neural techniques such as lumbar and caudal epidural blocks.
DB06290SimeprevirIndicated for the treatment of adults with chronic hepatitis C virus (HCV) infection: typically in combination with sofosbuvir in patients with HCV genotype 1 without cirrhosis or with compensated cirrhosis and in combination with peginterferon alfa (Peg-IFN-alfa) and ribavirin (RBV) in patients with HCV genotype 1 or 4 without cirrhosis or with compensated cirrhosis. Resistance: Reduced susceptibility to simeprevir was most commonly associated with the viral NS3 Q80K polymorphism. Amino acid substitutions at NS3 positions S122, R155 and/or D168 are also shown to reduce susceptibility to simeprevir in genotype 1a/b patients.
DB09120ZucapsaicinIndicated to be used in conjunction with oral COX-2 inhibitors or NSAIDs for the relief of severe pain in adult patients with osteoarthritis of the knee, not controlled with oral COX-2 inhibitors or NSAIDs alone, for a duration of no more than three months.
DB09198LobeglitazoneLobeglitazone was approved by the Ministry of Food and Drug Safety (South Korea) in 2013, and is being monitored by postmarketing surveillance until 2019. Lobeglitazone is not approved for use by either the Food and Drug Administration (USA), Health Canada, or by the European Medicines Agency for use in the management of diabetes.
DB11672CurcuminNo approved therapeutic indications.
DB00379MexiletineFor the treatment of ventricular tachycardia and symptomatic premature ventricular beats, and prevention of ventricular fibrillation.
DB09167DosulepinIndicated in the treatment of symptoms of depressive illness, especially where an anti-anxiety effect is required.
DB00969AlosetronOnly for the treatment of symptoms of severe diarrhea-predominant irritable bowel syndrome (IBS) in women with chronic symptoms (generally lasting greater than 6 months) who does not present with anatomic or biochemical GI abnormalities and have not responded to conventional therapy.
DB00458ImipramineFor the relief of symptoms of depression and as temporary adjunctive therapy in reducing enuresis in children aged 6 years and older [FDA Label]. May also be used off-label to manage panic disorders with or without agoraphobia, as a second line agent for ADHD in children and adolescents, to manage bulimia nervosa, for short-term management of acute depressive episodes in bipolar disorder and schizophrenia, for the treatment of acute stress disorder and posttraumatic stress disorder, and for symptomatic treatment of postherpetic neuralgia and painful diabetic neuropathy [L1349,L1348,A31900,L1351,L1352,L1353,A31904].
DB08881VemurafenibVemurafenib is approved since 2011 for the treatment of metastatic melanoma with a mutation on BRAF in the valine located in the exon 15 at codon 600, this mutation is denominated as V600E.[A31270] The V600E mutation, a substitution of glutamic acid for valine, accounts for 54% of the cases of cutaneous melanoma.[A31271] Vemurafenib approval was extended in 2017, for its use as a treatment of adult patients with Erdheim-Chester Disease whose cancer cells present BRAF V600 mutation.[L1013] Erdheim-Chester disease is an extremely rare histiocyte cell disorder that affects large bones, large vessels, central nervous system, as well as, skin and lungs. It is reported an association of Erdheim-Chester disease and V600E mutation.[A31272]
DB01044GatifloxacinFor the treatment of bronchitis, sinusitis, community-acquired pneumonia, and skin infections (abscesses, wounds) caused by S. pneumoniae, H. influenzae, S. aureus, M. pneumoniae, C. pneumoniae, L. pneumophila, S. pyogenes
DB00218MoxifloxacinFor the treatment of sinus and lung infections such as sinusitis, pneumonia, and secondary infections in chronic bronchitis. Also for the treatment of bacterial conjunctivitis (pinkeye).
DB11774PazufloxacinNot Available
DrugDrug NameTargetType
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
DB00201CaffeineAdenosine receptor A1target
DB00201CaffeinecAMP-specific 3',5'-cyclic phosphodiesterase 4Btarget
DB00201CaffeineAdenosine receptor A2atarget
DB00201CaffeineCytochrome P450 1A2enzyme
DB00201CaffeineRyanodine receptor 1target
DB00201CaffeineCytochrome P450 3A4enzyme
DB00201CaffeineCytochrome P450 3A5enzyme
DB00201CaffeineCytochrome P450 3A7enzyme
DB00201CaffeineMultidrug resistance protein 1transporter
DB00201CaffeineCytochrome P450 2E1enzyme
DB00201CaffeineCytochrome P450 2C8enzyme
DB00201CaffeineCytochrome P450 2C9enzyme
DB00201CaffeineCytochrome P450 1A1enzyme
DB00201CaffeineCytochrome P450 1B1enzyme
DB00201CaffeineCytochrome P450 2D6enzyme
DB00201CaffeineCyclic nucleotide phosphodiesterasetarget
DB00201CaffeineDNA-dependent protein kinase catalytic subunittarget
DB00201CaffeinePhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoformtarget
DB00201CaffeinePhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformtarget
DB00201CaffeinePhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoformtarget
DB00201CaffeineInositol 1,4,5-trisphosphate receptortarget
DB00201CaffeineSerine-protein kinase ATMtarget
DB00268RopiniroleD(2) dopamine receptortarget
DB00268RopiniroleD(3) dopamine receptortarget
DB00268RopiniroleD(4) dopamine receptortarget
DB00268RopiniroleCytochrome P450 1A2enzyme
DB00268Ropinirole5-hydroxytryptamine receptor 1Atarget
DB00268Ropinirole5-hydroxytryptamine receptor 1Dtarget
DB00268Ropinirole5-hydroxytryptamine receptor 2Btarget
DB00268Ropinirole5-hydroxytryptamine receptor 1Btarget
DB00268Ropinirole5-hydroxytryptamine receptor 2Atarget
DB00268Ropinirole5-hydroxytryptamine receptor 2Ctarget
DB00268RopiniroleAlpha-2A adrenergic receptortarget
DB00268RopiniroleAlpha-2B adrenergic receptortarget
DB00268RopiniroleAlpha-2C adrenergic receptortarget
DB00268RopiniroleD(1A) dopamine receptortarget
DB00268RopiniroleD(1B) dopamine receptortarget
DB00268RopiniroleCytochrome P450 2D6enzyme
DB00268RopiniroleCytochrome P450 3A4enzyme
DB00277TheophyllinecGMP-inhibited 3',5'-cyclic phosphodiesterase Atarget
DB00277TheophyllinecAMP-specific 3',5'-cyclic phosphodiesterase 4Btarget
DB00277TheophyllineAdenosine receptor A2btarget
DB00277TheophyllinecAMP-specific 3',5'-cyclic phosphodiesterase 4Atarget
DB00277TheophyllinecGMP-specific 3',5'-cyclic phosphodiesterasetarget
DB00277TheophyllineAdenosine receptor A1target
DB00277TheophyllineAdenosine receptor A2atarget
DB00277TheophyllineCytochrome P450 1A2enzyme
DB00277TheophyllineAdenosine deaminaseenzyme
DB00277TheophyllineCytochrome P450 2E1enzyme
DB00277TheophyllineCytochrome P450 3A4enzyme
DB00277TheophyllineSolute carrier family 22 member 7transporter
DB00277TheophyllineCytochrome P450 1A1enzyme
DB00277TheophyllineCytochrome P450 1B1enzyme
DB00277TheophyllineCytochrome P450 2C8enzyme
DB00277TheophyllineCytochrome P450 2C9enzyme
DB00277TheophyllineCytochrome P450 2D6enzyme
DB00277TheophyllineHistone deacetylase 2target
DB00277TheophyllineCopine-1target
DB00277TheophyllineMinor histocompatibility antigen H13target
DB00277TheophyllineNodal modulator 1target
DB00277TheophyllinePoly [ADP-ribose] polymerase 1target
DB00277TheophyllineProtein RIC-3target
DB00277TheophyllineTubulin monoglycylase TTLL3target
DB00281LidocaineSodium channel protein type 5 subunit alphatarget
DB00281LidocaineSodium channel protein type 10 subunit alphatarget
DB00281LidocaineEpidermal growth factor receptortarget
DB00281LidocaineSodium channel protein type 9 subunit alphatarget
DB00281LidocaineCytochrome P450 1A2enzyme
DB00281LidocaineCytochrome P450 2D6enzyme
DB00281LidocaineCytochrome P450 3A4enzyme
DB00281LidocaineCytochrome P450 3A5enzyme
DB00281LidocaineCytochrome P450 3A7enzyme
DB00281LidocaineSolute carrier family 22 member 5transporter
DB00281LidocaineMultidrug resistance protein 1transporter
DB00281LidocaineCytochrome P450 2A6enzyme
DB00281LidocaineCytochrome P450 2B6enzyme
DB00281LidocaineCytochrome P450 2C18enzyme
DB00281LidocaineCytochrome P450 2C8enzyme
DB00281LidocaineCytochrome P450 2C9enzyme
DB00281LidocaineSodium channel protein type 4 subunit alphatarget
DB00281LidocaineAlpha-1-acid glycoprotein 1target
DB00281LidocaineAlpha-1-acid glycoprotein 2target
DB06290SimeprevirNS3 proteasetarget
DB06290SimeprevirSerum albumincarrier
DB06290SimeprevirCytochrome P450 1A2enzyme
DB06290SimeprevirMultidrug resistance protein 1transporter
DB06290SimeprevirSolute carrier organic anion transporter family member 1B1transporter
DB06290SimeprevirSolute carrier organic anion transporter family member 1B3transporter
DB06290SimeprevirCYP3Aenzyme
DB06290SimeprevirCytochrome P450 3A4enzyme
DB06290SimeprevirCanalicular multispecific organic anion transporter 1transporter
DB06290SimeprevirATP-binding cassette sub-family G member 2transporter
DB06290SimeprevirSolute carrier organic anion transporter family member 2B1transporter
DB06290SimeprevirSodium/bile acid cotransportertransporter
DB06290SimeprevirBile salt export pumptransporter
DB09120ZucapsaicinTransient receptor potential cation channel subfamily V member 1target
DB09120ZucapsaicinCytochrome P450 1A2enzyme
DB09120ZucapsaicinCytochrome P450 2C19enzyme
DB09120ZucapsaicinCytochrome P450 2C9enzyme
DB09120ZucapsaicinCytochrome P450 2E1enzyme
DB09198LobeglitazoneSolute carrier organic anion transporter family member 1B1transporter
DB09198LobeglitazoneSolute carrier organic anion transporter family member 3A1transporter
DB09198LobeglitazoneMultidrug resistance protein 1transporter
DB09198LobeglitazoneCytochrome P450 1A2enzyme
DB09198LobeglitazoneCytochrome P450 2C9enzyme
DB09198LobeglitazoneCytochrome P450 2C19enzyme
DB09198LobeglitazonePeroxisome proliferator-activated receptor gammatarget
DB09198LobeglitazoneCytochrome P450 3A4enzyme
DB09198LobeglitazoneCytochrome P450 2C8enzyme
DB11672CurcuminPeroxisome proliferator-activated receptor gammatarget
DB11672CurcuminVitamin D3 receptortarget
DB11672CurcuminMultidrug resistance-associated protein 5target
DB11672CurcuminCarbonyl reductase [NADPH] 1target
DB11672CurcuminGlutathione S-transferase Ptarget
DB11672CurcuminCytochrome P450 2C9enzyme
DB11672CurcuminCytochrome P450 3A4enzyme
DB11672CurcuminCytochrome P450 2B6enzyme
DB11672CurcuminCytochrome P450 1A2enzyme
DB11672CurcuminCytochrome P450 2D6enzyme
DB11672CurcuminGlutathione S-transferase A1enzyme
DB11672CurcuminGlutathione S-transferase Mu 1enzyme
DB11672CurcuminGlutathione S-transferase Penzyme
DB11672CurcuminMultidrug resistance protein 1transporter
DB00379MexiletineSodium channel protein type 5 subunit alphatarget
DB00379MexiletineCytochrome P450 1A2enzyme
DB00379MexiletineCytochrome P450 2D6enzyme
DB00379MexiletineCytochrome P450 2B6enzyme
DB00379MexiletineCytochrome P450 2E1enzyme
DB00379MexiletineCytochrome P450 3A4enzyme
DB00379MexiletineAryl hydrocarbon receptortarget
DB09167Dosulepin5-hydroxytryptamine receptor 1Atarget
DB09167Dosulepin5-hydroxytryptamine receptor 2Atarget
DB09167DosulepinCytochrome P450 2D6enzyme
DB09167DosulepinCytochrome P450 1A2enzyme
DB09167DosulepinCytochrome P450 2C19enzyme
DB09167DosulepinCytochrome P450 2C9enzyme
DB09167DosulepinHistamine H1 receptortarget
DB09167DosulepinMuscarinic acetylcholine receptor M1target
DB09167DosulepinMuscarinic acetylcholine receptor M2target
DB09167DosulepinMuscarinic acetylcholine receptor M3target
DB09167DosulepinMuscarinic acetylcholine receptor M4target
DB09167DosulepinMuscarinic acetylcholine receptor M5target
DB09167DosulepinSodium-dependent noradrenaline transportertarget
DB09167DosulepinSodium-dependent serotonin transportertarget
DB09167DosulepinAlpha-1 adrenergic receptorstarget
DB09167DosulepinAlpha-2 adrenergic receptorstarget
DB00969Alosetron5-hydroxytryptamine receptor 3Atarget
DB00969AlosetronCytochrome P450 1A2enzyme
DB00969AlosetronCytochrome P450 2C9enzyme
DB00969AlosetronCytochrome P450 3A4enzyme
DB00969AlosetronCytochrome P450 2E1enzyme
DB00458ImipramineSodium-dependent noradrenaline transportertarget
DB00458ImipramineSodium-dependent serotonin transportertarget
DB00458ImipramineCytochrome P450 1A2enzyme
DB00458ImipramineCytochrome P450 2C19enzyme
DB00458ImipramineCytochrome P450 2D6enzyme
DB00458ImipramineHistamine H1 receptortarget
DB00458ImipramineAlpha-1A adrenergic receptortarget
DB00458Imipramine5-hydroxytryptamine receptor 2Atarget
DB00458ImipramineMuscarinic acetylcholine receptor M1target
DB00458ImipramineMuscarinic acetylcholine receptor M2target
DB00458ImipramineMuscarinic acetylcholine receptor M3target
DB00458ImipramineMuscarinic acetylcholine receptor M4target
DB00458ImipramineMuscarinic acetylcholine receptor M5target
DB00458ImipraminePotassium voltage-gated channel subfamily D member 2target
DB00458ImipraminePotassium voltage-gated channel subfamily D member 3target
DB00458ImipramineAlpha-1D adrenergic receptortarget
DB00458ImipramineAlpha-1-acid glycoprotein 1carrier
DB00458ImipramineSolute carrier family 22 member 2transporter
DB00458ImipramineSolute carrier family 22 member 1transporter
DB00458ImipramineSolute carrier family 22 member 3transporter
DB00458ImipramineMultidrug resistance protein 1transporter
DB00458ImipramineSolute carrier family 22 member 4transporter
DB00458ImipramineCytochrome P450 3A4enzyme
DB00458ImipramineCytochrome P450 2B6enzyme
DB00458ImipramineCytochrome P450 2C18enzyme
DB00458ImipramineCytochrome P450 2E1enzyme
DB00458ImipramineCytochrome P450 3A7enzyme
DB00458Imipramine5-hydroxytryptamine receptor 2Ctarget
DB00458ImipramineAlpha-1B adrenergic receptortarget
DB00458Imipramine5-hydroxytryptamine receptor 7target
DB00458ImipramineD(1) dopamine receptortarget
DB00458ImipramineD(2) dopamine receptortarget
DB00458ImipraminePotassium voltage-gated channel subfamily H member 2target
DB00458ImipramineSodium-dependent dopamine transportertarget
DB00458Imipramine5-hydroxytryptamine receptor 1Atarget
DB00458Imipramine5-hydroxytryptamine receptor 6target
DB00458ImipraminePotassium voltage-gated channel subfamily H member 1target
DB00458ImipramineSerum albumincarrier
DB00458ImipramineAlpha-1-acid glycoprotein 2target
DB08881VemurafenibSerum albumincarrier
DB08881VemurafenibAlpha-1-acid glycoprotein 1carrier
DB08881VemurafenibCytochrome P450 1A2enzyme
DB08881VemurafenibCytochrome P450 2D6enzyme
DB08881VemurafenibCytochrome P450 3A4enzyme
DB08881VemurafenibSerine/threonine-protein kinase B-raftarget
DB08881VemurafenibMultidrug resistance-associated protein 1transporter
DB08881VemurafenibATP-binding cassette sub-family G member 2transporter
DB08881VemurafenibCytochrome P450 2C9enzyme
DB01044GatifloxacinSerum albumincarrier
DB01044GatifloxacinDNA gyrase subunit Atarget
DB01044GatifloxacinDNA gyrase subunit Btarget
DB01044GatifloxacinDNA topoisomerase 4 subunit Atarget
DB01044GatifloxacinDNA topoisomerase 4 subunit Btarget
DB01044GatifloxacinCytochrome P450 1A2enzyme
DB00218MoxifloxacinDNA gyrase subunit Atarget
DB00218MoxifloxacinDNA topoisomerase 4 subunit Atarget
DB00218MoxifloxacinDNA topoisomerase 2-alphatarget
DB00218MoxifloxacinCytochrome P450 1A2enzyme
DB11774PazufloxacinCytochrome P450 1A2enzyme