General Information of Drug (ID: DMSQDLE)

Drug Name
Flecainide
Synonyms
flecainide; 54143-55-4; Flecaine; Tambocor; Flecainida; Flecainidum; (+-)-Flecainide; Flecainidum [INN-Latin]; Flecainida [INN-Spanish]; N-(piperidin-2-ylmethyl)-2,5-bis(2,2,2-trifluoroethoxy)benzamide; Flecainide [INN:BAN]; CCRIS 313; Benzamide, N-(2-piperidinylmethyl)-2,5-bis(2,2,2-trifluoroethoxy)-; C17H20F6N2O3; CHEMBL652; N-(2-Piperidinylmethyl)-2,5-bis(2,2,2-trifluoroethoxy)benzamide; CHEBI:75984; DJBNUMBKLMJRSA-UHFFFAOYSA-N; NCGC00015443-06; DSSTox_CID_3054; DSSTox_RID_76854; DSSTox_GSID_23054; (-)-Flecainide; Flecaine; Almarytm (TN); Apocard (TN); Ecrinal (TN); Flecainide (INN); Tambocor (TN); N-(piperidin-2-ylmethyl)-2,5-bis[(2,2,2-trifluoroethyl)oxy]benzamide; Ic Flecainide
Indication
Disease Entry ICD 11 Status REF
Tachyarrhythmias BC71 Approved [1], [2]
Paroxysmal atrial fibrillation BC81.30 Phase 1 [3]
Atrial fibrillation BC81.3 Investigative [4]
Therapeutic Class
Antiarrhythmic Agents
Drug Type
Small molecular drug
Structure
3D MOL 2D MOL
#Ro5 Violations (Lipinski): 0 Molecular Weight (mw) 414.34
Topological Polar Surface Area (xlogp) 3.8
Rotatable Bond Count (rotbonds) 7
Hydrogen Bond Donor Count (hbonddonor) 2
Hydrogen Bond Acceptor Count (hbondacc) 10
ADMET Property
Absorption Tmax
The time to maximum plasma concentration (Tmax) is 3-4 h [5]
BDDCS Class
Biopharmaceutics Drug Disposition Classification System (BDDCS) Class 1: high solubility and high permeability [6]
Bioavailability
The bioavailability of drug is 90% [5]
Clearance
The clearance of drug is 4.6-12.1 mL/min/kg [5]
Elimination
Approximately 86% of a single oral dose is eliminated in the urine, with 42% as unchanged flecainide and 14% as meta-O-dealkylated flecainide, a similar amount of the meta-O-dealkylated lactam of flecainide, approximately 3% as an unidentified acid metabolite, and <1% as 2 other unknown metabolites [5]
Half-life
The concentration or amount of drug in body reduced by one-half in 13 hours [5]
Metabolism
The drug is metabolized to meta-O-dealkylated flecainide or the meta-O-dealkylated lactam of flecainide [5]
MRTD
The Maximum Recommended Therapeutic Dose (MRTD) of drug that ensured maximising efficacy and moderate side effect is 12.06707 micromolar/kg/day [7]
Unbound Fraction
The unbound fraction of drug in plasma is 0.52% [8]
Vd
The volume of distribution (Vd) of drug is 5.0-13.4 L/kg [5]
Water Solubility
The ability of drug to dissolve in water is measured as 48.4 mg/mL [6]
Chemical Identifiers
Formula
C17H20F6N2O3
IUPAC Name
N-(piperidin-2-ylmethyl)-2,5-bis(2,2,2-trifluoroethoxy)benzamide
Canonical SMILES
C1CCNC(C1)CNC(=O)C2=C(C=CC(=C2)OCC(F)(F)F)OCC(F)(F)F
InChI
InChI=1S/C17H20F6N2O3/c18-16(19,20)9-27-12-4-5-14(28-10-17(21,22)23)13(7-12)15(26)25-8-11-3-1-2-6-24-11/h4-5,7,11,24H,1-3,6,8-10H2,(H,25,26)
InChIKey
DJBNUMBKLMJRSA-UHFFFAOYSA-N
Cross-matching ID
PubChem CID
3356
ChEBI ID
CHEBI:75984
CAS Number
54143-55-4
DrugBank ID
DB01195
TTD ID
D03DAP
VARIDT ID
DR00512
INTEDE ID
DR0700
ACDINA ID
D00278

Molecular Interaction Atlas of This Drug


Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
E3 ubiquitin-protein ligase COP1 (RFWD2) TT05DLS COP1_HUMAN Modulator [9]
Voltage-gated sodium channel alpha Nav1.9 (SCN11A) TTN9VTF SCNBA_HUMAN Blocker [4]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID MOA REF
Cytochrome P450 2D6 (CYP2D6)
Main DME
DECB0K3 CP2D6_HUMAN Substrate [10]
Cytochrome P450 1A2 (CYP1A2)
Main DME
DEJGDUW CP1A2_HUMAN Substrate [10]
Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This Drug

Drug-Drug Interaction (DDI) Information of This Drug

Coadministration of a Drug Treating the Disease Different from Flecainide (Comorbidity)
DDI Drug Name DDI Drug ID Severity Mechanism Comorbidity REF
Sodium bicarbonate DMMU6BJ Minor as urine pH determines the ionization state of weakly acidic or weakly alkaline drugs. Flecainide caused by Sodium bicarbonate mediated altered urine pH. Acidosis [5C73] [40]
Tromethamine DMOBLGK Minor as urine pH determines the ionization state of weakly acidic or weakly alkaline drugs. Flecainide caused by Tromethamine mediated altered urine pH. Acidosis [5C73] [40]
Ivosidenib DM8S6T7 Major Increased risk of prolong QT interval by the combination of Flecainide and Ivosidenib. Acute myeloid leukaemia [2A60] [41]
Midostaurin DMI6E0R Moderate Increased risk of prolong QT interval by the combination of Flecainide and Midostaurin. Acute myeloid leukaemia [2A60] [42]
Arn-509 DMT81LZ Moderate Increased risk of prolong QT interval by the combination of Flecainide and Arn-509. Acute myeloid leukaemia [2A60] [43]
Gilteritinib DMWQ4MZ Moderate Increased risk of prolong QT interval by the combination of Flecainide and Gilteritinib. Acute myeloid leukaemia [2A60] [44]
Oliceridine DM6MDCF Moderate Increased risk of prolong QT interval by the combination of Flecainide and Oliceridine. Acute pain [MG31] [42]
Emapalumab DMZG5WL Moderate Altered metabolism of Flecainide due to Emapalumab alters the formation of CYP450 enzymes. Adaptive immunity immunodeficiency [4A01] [43]
Siltuximab DMGEATB Moderate Altered metabolism of Flecainide due to Siltuximab alters the formation of CYP450 enzymes. Anemia [3A00-3A9Z] [43]
Ivabradine DM0L594 Major Increased risk of ventricular arrhythmias by the combination of Flecainide and Ivabradine. Angina pectoris [BA40] [43]
Bepridil DM0RKS4 Major Increased risk of prolong QT interval by the combination of Flecainide and Bepridil. Angina pectoris [BA40] [42]
Dronedarone DMA8FS5 Major Increased risk of prolong QT interval by the combination of Flecainide and Dronedarone. Angina pectoris [BA40] [42]
Bedaquiline DM3906J Major Increased risk of prolong QT interval by the combination of Flecainide and Bedaquiline. Antimicrobial drug resistance [MG50-MG52] [45]
Posaconazole DMUL5EW Moderate Increased risk of prolong QT interval by the combination of Flecainide and Posaconazole. Aspergillosis [1F20] [42]
Levalbuterol DM5YBO1 Moderate Increased risk of ventricular arrhythmias by the combination of Flecainide and Levalbuterol. Asthma [CA23] [46]
Pirbuterol DMI5678 Moderate Increased risk of prolong QT interval by the combination of Flecainide and Pirbuterol. Asthma [CA23] [47]
Lisdexamfetamine DM6W8V5 Moderate Increased risk of prolong QT interval by the combination of Flecainide and Lisdexamfetamine. Attention deficit hyperactivity disorder [6A05] [43]
Clarithromycin DM4M1SG Moderate Increased risk of prolong QT interval by the combination of Flecainide and Clarithromycin. Bacterial infection [1A00-1C4Z] [42]
Sparfloxacin DMB4HCT Major Increased risk of prolong QT interval by the combination of Flecainide and Sparfloxacin. Bacterial infection [1A00-1C4Z] [48]
Retigabine DMGNYIH Moderate Increased risk of prolong QT interval by the combination of Flecainide and Retigabine. Behcet disease [4A62] [42]
Eribulin DM1DX4Q Moderate Increased risk of prolong QT interval by the combination of Flecainide and Eribulin. Breast cancer [2C60-2C6Y] [42]
Lapatinib DM3BH1Y Moderate Increased risk of prolong QT interval by the combination of Flecainide and Lapatinib. Breast cancer [2C60-2C6Y] [42]
Bosutinib DMTI8YE Moderate Increased risk of prolong QT interval by the combination of Flecainide and Bosutinib. Breast cancer [2C60-2C6Y] [43]
PF-04449913 DMSB068 Moderate Increased risk of prolong QT interval by the combination of Flecainide and PF-04449913. Chronic myelomonocytic leukaemia [2A40] [49]
Olodaterol DM62B78 Moderate Increased risk of ventricular arrhythmias by the combination of Flecainide and Olodaterol. Chronic obstructive pulmonary disease [CA22] [47]
Vilanterol DMF5EK1 Moderate Increased risk of prolong QT interval by the combination of Flecainide and Vilanterol. Chronic obstructive pulmonary disease [CA22] [46]
Indacaterol DMQJHR7 Moderate Increased risk of prolong QT interval by the combination of Flecainide and Indacaterol. Chronic obstructive pulmonary disease [CA22] [47]
Arformoterol DMYM974 Moderate Increased risk of ventricular arrhythmias by the combination of Flecainide and Arformoterol. Chronic obstructive pulmonary disease [CA22] [47]
Sevoflurane DMC9O43 Moderate Increased risk of prolong QT interval by the combination of Flecainide and Sevoflurane. Corneal disease [9A76-9A78] [42]
Probucol DMVZQ2M Moderate Increased risk of prolong QT interval by the combination of Flecainide and Probucol. Coronary atherosclerosis [BA80] [42]
Pasireotide DMHM7JS Major Increased risk of prolong QT interval by the combination of Flecainide and Pasireotide. Cushing syndrome [5A70] [42]
Osilodrostat DMIJC9X Moderate Increased risk of prolong QT interval by the combination of Flecainide and Osilodrostat. Cushing syndrome [5A70] [43]
SODIUM CITRATE DMHPD2Y Minor as urine pH determines the ionization state of weakly acidic or weakly alkaline drugs. Flecainide caused by SODIUM CITRATE mediated altered urine pH. Discovery agent [N.A.] [40]
Tetrabenazine DMYWQ0O Moderate Increased risk of prolong QT interval by the combination of Flecainide and Tetrabenazine. Dissociative neurological symptom disorder [6B60] [42]
Deutetrabenazine DMUPFLI Moderate Increased risk of prolong QT interval by the combination of Flecainide and Deutetrabenazine. Dystonic disorder [8A02] [50]
Ingrezza DMVPLNC Moderate Additive CNS depression effects by the combination of Flecainide and Ingrezza. Dystonic disorder [8A02] [51]
Stiripentol DMMSDOY Moderate Decreased metabolism of Flecainide caused by Stiripentol mediated inhibition of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [52]
Solifenacin DMG592Q Moderate Increased risk of prolong QT interval by the combination of Flecainide and Solifenacin. Functional bladder disorder [GC50] [42]
Mirabegron DMS1GYT Moderate Decreased metabolism of Flecainide caused by Mirabegron mediated inhibition of CYP450 enzyme. Functional bladder disorder [GC50] [53]
Sunitinib DMCBJSR Moderate Increased risk of prolong QT interval by the combination of Flecainide and Sunitinib. Gastrointestinal stromal tumour [2B5B] [42]
Simeprevir DMLUA9D Moderate Decreased metabolism of Flecainide caused by Simeprevir mediated inhibition of CYP450 enzyme. Hepatitis virus infection [1E50-1E51] [54]
Fostemsavir DM50ILT Moderate Increased risk of prolong QT interval by the combination of Flecainide and Fostemsavir. Human immunodeficiency virus disease [1C60-1C62] [55]
Cobicistat DM6L4H2 Major Decreased metabolism of Flecainide caused by Cobicistat mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [56]
Saquinavir DMG814N Major Decreased metabolism of Flecainide caused by Saquinavir mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [57]
Etravirine DMGV8QU Moderate Increased metabolism of Flecainide caused by Etravirine mediated induction of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [58]
Rilpivirine DMJ0QOW Moderate Increased risk of prolong QT interval by the combination of Flecainide and Rilpivirine. Human immunodeficiency virus disease [1C60-1C62] [42]
Darunavir DMN3GCH Moderate Decreased metabolism of Flecainide caused by Darunavir mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [59]
Sodium acetate anhydrous DMH21E0 Minor as urine pH determines the ionization state of weakly acidic or weakly alkaline drugs. Flecainide caused by Sodium acetate anhydrous mediated altered urine pH. Hypo-osmolality/hyponatraemia [5C72] [40]
Givosiran DM5PFIJ Moderate Decreased metabolism of Flecainide caused by Givosiran mediated inhibition of CYP450 enzyme. Inborn porphyrin/heme metabolism error [5C58] [60]
Berotralstat DMWA2DZ Moderate Decreased metabolism of Flecainide caused by Berotralstat mediated inhibition of CYP450 enzyme. Innate/adaptive immunodeficiency [4A00] [61]
Polyethylene glycol DM4I1JP Moderate Increased risk of ventricular arrhythmias by the combination of Flecainide and Polyethylene glycol. Irritable bowel syndrome [DD91] [59]
Phenolphthalein DM5SICT Moderate Increased risk of ventricular arrhythmias by the combination of Flecainide and Phenolphthalein. Irritable bowel syndrome [DD91] [42]
Glycerol phenylbutyrate DMDGRQO Moderate Decreased metabolism of Flecainide caused by Glycerol phenylbutyrate mediated inhibition of CYP450 enzyme. Liver disease [DB90-DB9Z] [43]
Crizotinib DM4F29C Major Increased risk of prolong QT interval by the combination of Flecainide and Crizotinib. Lung cancer [2C25] [62]
Ceritinib DMB920Z Major Increased risk of prolong QT interval by the combination of Flecainide and Ceritinib. Lung cancer [2C25] [42]
Dacomitinib DMOH8VY Moderate Decreased metabolism of Flecainide caused by Dacomitinib mediated inhibition of CYP450 enzyme. Lung cancer [2C25] [63]
Osimertinib DMRJLAT Major Increased risk of prolong QT interval by the combination of Flecainide and Osimertinib. Lung cancer [2C25] [64]
Selpercatinib DMZR15V Major Increased risk of prolong QT interval by the combination of Flecainide and Selpercatinib. Lung cancer [2C25] [43]
Lumefantrine DM29GAD Major Increased risk of prolong QT interval by the combination of Flecainide and Lumefantrine. Malaria [1F40-1F45] [59]
Halofantrine DMOMK1V Major Increased risk of prolong QT interval by the combination of Flecainide and Halofantrine. Malaria [1F40-1F45] [65]
Hydroxychloroquine DMSIVND Major Increased risk of prolong QT interval by the combination of Flecainide and Hydroxychloroquine. Malaria [1F40-1F45] [66]
Inotuzumab ozogamicin DMAC130 Moderate Increased risk of prolong QT interval by the combination of Flecainide and Inotuzumab ozogamicin. Malignant haematopoietic neoplasm [2B33] [43]
Vemurafenib DM62UG5 Major Increased risk of prolong QT interval by the combination of Flecainide and Vemurafenib. Melanoma [2C30] [42]
Panobinostat DM58WKG Major Increased risk of prolong QT interval by the combination of Flecainide and Panobinostat. Multiple myeloma [2A83] [67]
Siponimod DM2R86O Major Increased risk of ventricular arrhythmias by the combination of Flecainide and Siponimod. Multiple sclerosis [8A40] [59]
Fingolimod DM5JVAN Major Increased risk of ventricular arrhythmias by the combination of Flecainide and Fingolimod. Multiple sclerosis [8A40] [42]
Ozanimod DMT6AM2 Major Increased risk of ventricular arrhythmias by the combination of Flecainide and Ozanimod. Multiple sclerosis [8A40] [68]
Romidepsin DMT5GNL Moderate Increased risk of prolong QT interval by the combination of Flecainide and Romidepsin. Mycosis fungoides [2B01] [42]
Fedratinib DM4ZBK6 Moderate Decreased metabolism of Flecainide caused by Fedratinib mediated inhibition of CYP450 enzyme. Myeloproliferative neoplasm [2A20] [43]
Nilotinib DM7HXWT Major Increased risk of prolong QT interval by the combination of Flecainide and Nilotinib. Myeloproliferative neoplasm [2A20] [42]
Dasatinib DMJV2EK Moderate Increased risk of prolong QT interval by the combination of Flecainide and Dasatinib. Myeloproliferative neoplasm [2A20] [69]
Rolapitant DM8XP26 Moderate Decreased metabolism of Flecainide caused by Rolapitant mediated inhibition of CYP450 enzyme. Nausea/vomiting [MD90] [70]
Entrectinib DMMPTLH Moderate Increased risk of prolong QT interval by the combination of Flecainide and Entrectinib. Non-small cell lung cancer [2C25] [59]
Lorcaserin DMG6OYJ Moderate Decreased metabolism of Flecainide caused by Lorcaserin mediated inhibition of CYP450 enzyme. Obesity [5B80-5B81] [71]
Levomethadyl Acetate DM06HG5 Major Increased risk of prolong QT interval by the combination of Flecainide and Levomethadyl Acetate. Opioid use disorder [6C43] [43]
Lofexidine DM1WXA6 Moderate Additive hypotensive effects by the combination of Flecainide and Lofexidine. Opioid use disorder [6C43] [42]
Rucaparib DM9PVX8 Moderate Increased risk of prolong QT interval by the combination of Flecainide and Rucaparib. Ovarian cancer [2C73] [42]
Triclabendazole DMPWGBR Moderate Increased risk of prolong QT interval by the combination of Flecainide and Triclabendazole. Parasitic worm infestation [1F90] [42]
Pimavanserin DMR7IVC Moderate Increased risk of prolong QT interval by the combination of Flecainide and Pimavanserin. Parkinsonism [8A00] [72]
Macimorelin DMQYJIR Major Increased risk of prolong QT interval by the combination of Flecainide and Macimorelin. Pituitary gland disorder [5A60-5A61] [73]
Lefamulin DME6G97 Major Increased risk of prolong QT interval by the combination of Flecainide and Lefamulin. Pneumonia [CA40] [74]
Degarelix DM3O8QY Moderate Increased risk of prolong QT interval by the combination of Flecainide and Degarelix. Prostate cancer [2C82] [43]
ABIRATERONE DM8V75C Moderate Decreased metabolism of Flecainide caused by ABIRATERONE mediated inhibition of CYP450 enzyme. Prostate cancer [2C82] [75]
Enzalutamide DMGL19D Moderate Increased risk of prolong QT interval by the combination of Flecainide and Enzalutamide. Prostate cancer [2C82] [43]
Relugolix DMK7IWL Moderate Increased risk of prolong QT interval by the combination of Flecainide and Relugolix. Prostate cancer [2C82] [43]
Ustekinumab DMHTYK3 Moderate Altered metabolism of Flecainide due to Ustekinumab alters the formation of CYP450 enzymes. Psoriasis [EA90] [43]
Ixekizumab DMXW92T Moderate Altered metabolism of Flecainide due to Ixekizumab alters the formation of CYP450 enzymes. Psoriasis [EA90] [43]
Levomepromazine DMIKFEL Moderate Increased risk of prolong QT interval by the combination of Flecainide and Levomepromazine. Psychotic disorder [6A20-6A25] [42]
Tocilizumab DM7J6OR Moderate Altered metabolism of Flecainide due to Tocilizumab alters the formation of CYP450 enzymes. Rheumatoid arthritis [FA20] [43]
Canakinumab DM8HLO5 Moderate Altered metabolism of Flecainide due to Canakinumab alters the formation of CYP450 enzymes. Rheumatoid arthritis [FA20] [43]
Rilonacept DMGLUQS Moderate Altered metabolism of Flecainide due to Rilonacept alters the formation of CYP450 enzymes. Rheumatoid arthritis [FA20] [43]
Golimumab DMHZV7X Moderate Altered metabolism of Flecainide due to Golimumab alters the formation of CYP450 enzymes. Rheumatoid arthritis [FA20] [43]
Sarilumab DMOGNXY Moderate Altered metabolism of Flecainide due to Sarilumab alters the formation of CYP450 enzymes. Rheumatoid arthritis [FA20] [43]
Quetiapine DM1N62C Moderate Increased risk of prolong QT interval by the combination of Flecainide and Quetiapine. Schizophrenia [6A20] [42]
Aripiprazole DM3NUMH Moderate Increased risk of prolong QT interval by the combination of Flecainide and Aripiprazole. Schizophrenia [6A20] [59]
Iloperidone DM6AUFY Major Increased risk of prolong QT interval by the combination of Flecainide and Iloperidone. Schizophrenia [6A20] [42]
Paliperidone DM7NPJS Moderate Increased risk of prolong QT interval by the combination of Flecainide and Paliperidone. Schizophrenia [6A20] [42]
Amisulpride DMSJVAM Major Increased risk of prolong QT interval by the combination of Flecainide and Amisulpride. Schizophrenia [6A20] [76]
Asenapine DMSQZE2 Moderate Increased risk of prolong QT interval by the combination of Flecainide and Asenapine. Schizophrenia [6A20] [42]
LEE011 DMMX75K Major Increased risk of prolong QT interval by the combination of Flecainide and LEE011. Solid tumour/cancer [2A00-2F9Z] [42]
Vandetanib DMRICNP Major Increased risk of prolong QT interval by the combination of Flecainide and Vandetanib. Solid tumour/cancer [2A00-2F9Z] [42]
Triptorelin DMTK4LS Moderate Increased risk of prolong QT interval by the combination of Flecainide and Triptorelin. Solid tumour/cancer [2A00-2F9Z] [43]
Pitolisant DM8RFNJ Moderate Increased risk of prolong QT interval by the combination of Flecainide and Pitolisant. Somnolence [MG42] [42]
Telavancin DM58VQX Moderate Increased risk of prolong QT interval by the combination of Flecainide and Telavancin. Staphylococcal/streptococcal disease [1B5Y] [42]
Lenvatinib DMB1IU4 Moderate Increased risk of prolong QT interval by the combination of Flecainide and Lenvatinib. Thyroid cancer [2D10] [42]
Cabozantinib DMIYDT4 Major Increased risk of prolong QT interval by the combination of Flecainide and Cabozantinib. Thyroid cancer [2D10] [43]
Trimeprazine DMEMV9D Moderate Increased risk of prolong QT interval by the combination of Flecainide and Trimeprazine. Vasomotor/allergic rhinitis [CA08] [77]
⏷ Show the Full List of 107 DDI Information of This Drug

Drug Inactive Ingredient(s) (DIG) and Formulation(s) of This Drug

DIG
DIG Name DIG ID PubChem CID Functional Classification
Sodium stearyl fumarate E00545 23665634 lubricant
Stearic acid E00079 5281 Emulsifying agent; Solubilizing agent; Viscosity-controlling agent; lubricant
Carmellose sodium E00625 Not Available Disintegrant
Magnesium stearate E00208 11177 lubricant
Silicon dioxide E00670 Not Available Anticaking agent; Opacifying agent; Viscosity-controlling agent
Pharmaceutical Formulation
Formulation Name Drug Dosage Dosage Form Route
Flecainide 100 mg tablet 100 mg Oral Tablet Oral
Flecainide 150 mg tablet 150 mg Oral Tablet Oral
Flecainide 50 mg tablet 50 mg Oral Tablet Oral
Jump to Detail Pharmaceutical Formulation Page of This Drug

References

1 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 2560).
2 FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 075442.
3 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
4 New antiarrhythmic agents for atrial fibrillation and atrial flutter. Expert Opin Emerg Drugs. 2005 May;10(2):311-22.
5 Metabolism of flecainide. Am J Cardiol. 1984 Feb 27;53(5):41B-51B. doi: 10.1016/0002-9149(84)90501-0.
6 BDDCS predictions, self-correcting aspects of BDDCS assignments, BDDCS assignment corrections, and classification for more than 175 additional drugs
7 Estimating the safe starting dose in phase I clinical trials and no observed effect level based on QSAR modeling of the human maximum recommended daily dose
8 Trend Analysis of a Database of Intravenous Pharmacokinetic Parameters in Humans for 1352 Drug Compounds
9 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
10 Flecainide: current status and perspectives in arrhythmia management. World J Cardiol. 2015 Feb 26;7(2):76-85.
11 Roles of cytochromes P450 1A2, 2A6, and 2C8 in 5-fluorouracil formation from tegafur, an anticancer prodrug, in human liver microsomes. Drug Metab Dispos. 2000 Dec;28(12):1457-63.
12 Effects of polyunsaturated fatty acids on prostaglandin synthesis and cyclooxygenase-mediated DNA adduct formation by heterocyclic aromatic amines in human adenocarcinoma colon cells. Mol Carcinog. 2004 Jul;40(3):180-8.
13 Endoxifen and other metabolites of tamoxifen inhibit human hydroxysteroid sulfotransferase 2A1 (hSULT2A1). Drug Metab Dispos. 2014 Nov;42(11):1843-50.
14 Cytochrome P450 1A2 (CYP1A2) activity and risk factors for breast cancer: a cross-sectional study. Breast Cancer Res. 2004;6(4):R352-65.
15 PharmGKB summary: pathways of acetaminophen metabolism at the therapeutic versus toxic doses. Pharmacogenet Genomics. 2015 Aug;25(8):416-26.
16 The effect of apigenin on pharmacokinetics of imatinib and its metabolite N-desmethyl imatinib in rats. Biomed Res Int. 2013;2013:789184.
17 Effects of morin on the pharmacokinetics of etoposide in rats. Biopharm Drug Dispos. 2007 Apr;28(3):151-6.
18 The influence of metabolic gene polymorphisms on urinary 1-hydroxypyrene concentrations in Chinese coke oven workers. Sci Total Environ. 2007 Aug 1;381(1-3):38-46.
19 Identification of P450 enzymes involved in metabolism of verapamil in humans. Naunyn Schmiedebergs Arch Pharmacol. 1993 Sep;348(3):332-7.
20 Metabolism and metabolic inhibition of xanthotoxol in human liver microsomes. Evid Based Complement Alternat Med. 2016;2016:5416509.
21 Inhibitory effects of anticancer drugs on dextromethorphan-O-demethylase activity in human liver microsomes. Cancer Chemother Pharmacol. 1993;32(6):491-5.
22 Effect of genetic polymorphism on the metabolism of endogenous neuroactive substances, progesterone and p-tyramine, catalyzed by CYP2D6. Brain Res Mol Brain Res. 2004 Oct 22;129(1-2):117-23.
23 CYP2D6 polymorphisms and tamoxifen metabolism: clinical relevance. Curr Oncol Rep. 2010 Jan;12(1):7-15.
24 Metabolic interactions between acetaminophen (paracetamol) and two flavonoids, luteolin and quercetin, through in-vitro inhibition studies. J Pharm Pharmacol. 2017 Dec;69(12):1762-1772.
25 Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675.
26 Inhibition of cytochrome P450 2D6: structure-activity studies using a series of quinidine and quinine analogues. Chem Res Toxicol. 2003 Apr;16(4):450-9.
27 Effects of propofol on human hepatic microsomal cytochrome P450 activities. Xenobiotica. 1998 Sep;28(9):845-53.
28 Pharmacogenetics of schizophrenia. Am J Med Genet. 2000 Spring;97(1):98-106.
29 Roles of CYP2A6 and CYP2B6 in nicotine C-oxidation by human liver microsomes. Arch Toxicol. 1999 Mar;73(2):65-70.
30 Structure-activity relationship for human cytochrome P450 substrates and inhibitors. Drug Metab Rev. 2002 Feb-May;34(1-2):69-82.
31 Barucainide, a novel class Ib antiarrhythmic agent with a slow kinetic property: electrophysiologic observations in isolated canine and rabbit cardiac muscle. Am Heart J. 1990 May;119(5):1050-60.
32 Mechanisms of analgesia of intravenous lidocaine. Rev Bras Anestesiol. 2008 May-Jun;58(3):280-6.
33 The effects of lamotrigine on the acquisition and expression of morphine-induced place preference in mice. Pak J Biol Sci. 2009 Jan 1;12(1):33-9.
34 Antibodies and venom peptides: new modalities for ion channels. Nat Rev Drug Discov. 2019 May;18(5):339-357.
35 Secondary injury mechanisms of spinal cord trauma: a novel therapeutic approach for the management of secondary pathophysiology with the sodium channel blocker riluzole. Prog Brain Res. 2002;137:177-90.
36 Tolperisone-type drugs inhibit spinal reflexes via blockade of voltage-gated sodium and calcium channels. J Pharmacol Exp Ther. 2005 Dec;315(3):1237-46.
37 Debate: Does genetic information in humans help us treat patients PRO--genetic information in humans helps us treat patients. CON--genetic information does not help at all. Epilepsia. 2008 Dec;49 Suppl 9:13-24.
38 Emerging drugs for spinal cord injury. Expert Opin Emerg Drugs. 2008 Mar;13(1):63-80.
39 Voltage-gated sodium channel blockers for the treatment of chronic pain. Curr Top Med Chem. 2009;9(4):362-76.
40 Hertrampf R, Gundert-Remy U, Beckmann J, et al "Elimination of flecainide as a function of urinary flow rate and pH." Eur J Clin Pharmacol 41 (1991): 61-3. [PMID: 1782979]
41 Product Information. Tibsovo (ivosidenib). Agios Pharmaceuticals, Cambridge, MA.
42 Canadian Pharmacists Association.
43 Cerner Multum, Inc. "UK Summary of Product Characteristics.".
44 Product Information. Xospata (gilteritinib). Astellas Pharma US, Inc, Deerfield, IL.
45 Product Information. Sirturo (bedaquiline). Janssen Pharmaceuticals, Titusville, NJ.
46 Product Information. Arcapta Neohaler (indacaterol). Novartis Pharmaceuticals, East Hanover, NJ.
47 Bengtsson B, Fagerstrom PO "Extrapulmonary effects of terbutaline during prolonged administration." Clin Pharmacol Ther 31 (1982): 726-32. [PMID: 7042176]
48 Ball P "Quinolone-induced QT interval prolongation: a not-so-unexpected class effect." J Antimicrob Chemother 45 (2000): 557-9. [PMID: 10797074]
49 Product Information. Daurismo (glasdegib). Pfizer U.S. Pharmaceuticals Group, New York, NY.
50 Product Information. Austedo (deutetrabenazine). Teva Pharmaceuticals USA, North Wales, PA.
51 Product Information. Ingrezza (valbenazine). Neurocrine Biosciences, Inc., San Diego, CA.
52 EMEA. European Medicines Agency "EPARs. European Union Public Assessment Reports.".
53 Product Information. Myrbetriq (mirabegron). Astellas Pharma US, Inc, Deerfield, IL.
54 Product Information. Olysio (simeprevir). Janssen Pharmaceuticals, Titusville, NJ.
55 Product Information. Rukobia (fostemsavir). ViiV Healthcare, Research Triangle Park, NC.
56 Product Information. Stribild (cobicistat/elvitegravir/emtricitabine/tenofov). Gilead Sciences, Foster City, CA.
57 Product Information. Fortovase (saquinavir) Roche Laboratories, Nutley, NJ.
58 Product Information. Intelence (etravirine). Ortho Biotech Inc, Bridgewater, NJ.
59 Cerner Multum, Inc. "Australian Product Information.".
60 Product Information. Givlaari (givosiran). Alnylam Pharmaceuticals, Cambridge, MA.
61 Product Information. Orladeyo (berotralstat). BioCryst Pharmaceuticals Inc, Durham, NC.
62 Product Information. Xalkori (crizotinib). Pfizer U.S. Pharmaceuticals Group, New York, NY.
63 Product Information. Vizimpro (dacomitinib). Pfizer U.S. Pharmaceuticals Group, New York, NY.
64 Product Information. Tagrisso (osimertinib). Astra-Zeneca Pharmaceuticals, Wilmington, DE.
65 Abernethy DR, Wesche DL, Barbey JT, et al. "Stereoselective halofantrine disposition and effect: concentration-related QTc prolongation." Br J Clin Pharmacol 51 (2001): 231-7. [PMID: 11298069]
66 Harper KM, Knapp DJ, Criswell HE, Breese GR "Vasopressin and alcohol: A multifaceted relationship." Psychopharmacology (Berl) 235 (2018): 3363-79. [PMID: 32936259]
67 Product Information. Farydak (panobinostat). Novartis Pharmaceuticals, East Hanover, NJ.
68 Product Information. Zeposia (ozanimod). Celgene Corporation, Summit, NJ.
69 Product Information. Sprycel (dasatinib). Bristol-Myers Squibb, Princeton, NJ.
70 Product Information. Varubi (rolapitant). Tesaro Inc., Waltham, MA.
71 Product Information. Belviq (lorcaserin). Eisai Inc, Teaneck, NJ.
72 Product Information. Nuplazid (pimavanserin). Accelis Pharma, East Windsor, NJ.
73 Product Information. Macrilen (macimorelin). Aeterna Zentaris, Charleston, SC.
74 Product Information. Xenleta (lefamulin). Nabriva Therapeutics US, Inc., King of Prussia, PA.
75 Product Information. Zytiga (abiraterone). Centocor Inc, Malvern, PA.
76 Product Information. Barhemsys (amisulpride). Acacia Pharma, Inc, Indianapolis, IN.
77 Iannini PB "Cardiotoxicity of macrolides, ketolides and fluoroquinolones that prolong the QTc interval." Expert Opin Drug Saf 1 (2002): 121-8. [PMID: 12904146]