Details of the Drug

General Information of Drug (ID: DMQJHR7)

Drug Name
Indacaterol
Synonyms
312753-06-3; QAB149; Arcapta; Onbrez; QAB-149; QAB 149; UNII-8OR09251MQ; 753498-25-8; CHEMBL1095777; CHEBI:68575; 8OR09251MQ; (R)-5-(2-(5,6-diethyl-2,3-dihydro-1H-inden-2-ylamino)-1-hydroxyethyl)-8-hydroxyquinolin-2(1H)-one; 5-[(1R)-2-[(5,6-diethyl-2,3-dihydro-1H-inden-2-yl)amino]-1-hydroxyethyl]-8-hydroxy-1H-quinolin-2-one; Indacaterol Maleic Acid Salt; Indacaterol (USAN/INN); Indacaterol [USAN:INN:BAN]; 5-{(1R)-2-[(5,6-diethyl-2,3-dihydro-1H-inden-2-yl)amino]-1-hydroxyethyl}-8-hydroxyquinolin-2(1H)-one; QAB-149; 5-(2-(5,6-Diethylindan-2-ylamino)-1-hydroxyethyl)-8-hydroxy-1H-quinolin-2-one; Indacaterol/mometasone
Indication
Disease Entry ICD 11 Status REF
Chronic obstructive pulmonary disease CA22 Approved [1], [2]
Asthma CA23 Phase 4 [3]
Drug Type
Small molecular drug
Structure
3D MOL 2D MOL
#Ro5 Violations (Lipinski): 0 Molecular Weight (mw) 392.5
Topological Polar Surface Area (xlogp) 3.3
Rotatable Bond Count (rotbonds) 6
Hydrogen Bond Donor Count (hbonddonor) 4
Hydrogen Bond Acceptor Count (hbondacc) 4
ADMET Property
Clearance
The renal clearance of drug is 0.46-1.2 L/h [4]
Half-life
The concentration or amount of drug in body reduced by one-half in 45.5 - 126 hours [5]
Unbound Fraction
The unbound fraction of drug in plasma is 0.05% [5]
Vd
The volume of distribution (Vd) of drug is 2,361-2,557 L [4]
Chemical Identifiers
Formula
C24H28N2O3
IUPAC Name
5-[(1R)-2-[(5,6-diethyl-2,3-dihydro-1H-inden-2-yl)amino]-1-hydroxyethyl]-8-hydroxy-1H-quinolin-2-one
Canonical SMILES
CCC1=C(C=C2CC(CC2=C1)NC[C@@H](C3=C4C=CC(=O)NC4=C(C=C3)O)O)CC
InChI
InChI=1S/C24H28N2O3/c1-3-14-9-16-11-18(12-17(16)10-15(14)4-2)25-13-22(28)19-5-7-21(27)24-20(19)6-8-23(29)26-24/h5-10,18,22,25,27-28H,3-4,11-13H2,1-2H3,(H,26,29)/t22-/m0/s1
InChIKey
QZZUEBNBZAPZLX-QFIPXVFZSA-N
Cross-matching ID
PubChem CID
6918554
ChEBI ID
CHEBI:68575
CAS Number
312753-06-3
DrugBank ID
DB05039
TTD ID
D03DJL
VARIDT ID
DR00064
INTEDE ID
DR0867
ACDINA ID
D00326

Molecular Interaction Atlas of This Drug


Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Adrenergic receptor beta-2 (ADRB2) TT2CJVK ADRB2_HUMAN Agonist [6], [7]

Drug Transporter (DTP)
DTP Name DTP ID UniProt ID MOA REF
Organic cation transporter 1 (SLC22A1) DTT79CX S22A1_HUMAN Substrate [8]
P-glycoprotein 1 (ABCB1) DTUGYRD MDR1_HUMAN Substrate [9]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID MOA REF
Cytochrome P450 3A4 (CYP3A4)
Main DME 		DE4LYSA CP3A4_HUMAN Substrate [10]
UDP-glucuronosyltransferase 1A1 (UGT1A1)
Main DME 		DEYGVN4 UD11_HUMAN Substrate [10]
Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This Drug

Molecular Expression Atlas of This Drug

ICD Disease Classification 12 Disease of the respiratory system
Disease Class ICD-11: CA23 Asthma
The Studied Tissue Lung tissue
The Studied Disease Chronic obstructive pulmonary disease [ICD-11:CA23]
Molecule Name Molecule Type Gene Name p-value Fold-Change Z-score
Adrenergic receptor beta-2 (ADRB2) DTT ADRB2 4.88E-01 -0.05 -0.12
Adrenergic receptor beta-2 (ADRB2) DTT ADRB2 7.10E-01 0.06 0.09
P-glycoprotein 1 (ABCB1) DTP P-GP 1.24E-01 -4.12E-01 -4.68E-01
P-glycoprotein 1 (ABCB1) DTP P-GP 3.00E-02 -1.09E-02 -7.37E-02
Organic cation transporter 1 (SLC22A1) DTP SLC22A1 1.48E-01 6.33E-02 3.20E-01
Organic cation transporter 1 (SLC22A1) DTP SLC22A1 1.74E-02 1.21E-01 4.40E-01
UDP-glucuronosyltransferase 1A1 (UGT1A1) DME UGT1A1 8.29E-01 -5.44E-03 -2.25E-02
UDP-glucuronosyltransferase 1A1 (UGT1A1) DME UGT1A1 4.23E-03 9.31E-02 4.30E-01
Cytochrome P450 3A4 (CYP3A4) DME CYP3A4 2.13E-01 4.03E-02 2.50E-01
Cytochrome P450 3A4 (CYP3A4) DME CYP3A4 8.21E-02 8.17E-02 4.35E-01
Molecular Expression Atlas (MEA) Jump to Detail Molecular Expression Atlas of This Drug

Drug-Drug Interaction (DDI) Information of This Drug

Coadministration of a Drug Treating the Disease Different from Indacaterol (Comorbidity)
DDI Drug Name DDI Drug ID Severity Mechanism Comorbidity REF
Sarecycline DMLZNIQ Minor Decreased clearance of Indacaterol due to the transporter inhibition by Sarecycline . Acne vulgaris [ED80] [56]
Methylene blue DMJAPE7 Moderate Additive hypertensive effects by the combination of Indacaterol and Methylene blue. Acquired methaemoglobinaemia [3A93] [57]
Midostaurin DMI6E0R Moderate Increased risk of ventricular arrhythmias by the combination of Indacaterol and Midostaurin. Acute myeloid leukaemia [2A60] [58]
Arn-509 DMT81LZ Moderate Increased risk of prolong QT interval by the combination of Indacaterol and Arn-509. Acute myeloid leukaemia [2A60] [58]
Gilteritinib DMWQ4MZ Moderate Increased risk of prolong QT interval by the combination of Indacaterol and Gilteritinib. Acute myeloid leukaemia [2A60] [58]
Oliceridine DM6MDCF Moderate Increased risk of ventricular arrhythmias by the combination of Indacaterol and Oliceridine. Acute pain [MG31] [58]
Ivabradine DM0L594 Moderate Increased risk of prolong QT interval by the combination of Indacaterol and Ivabradine. Angina pectoris [BA40] [58]
Bedaquiline DM3906J Moderate Increased risk of ventricular arrhythmias by the combination of Indacaterol and Bedaquiline. Antimicrobial drug resistance [MG50-MG52] [58]
Droxidopa DM5YF4M Moderate Additive hypertensive effects by the combination of Indacaterol and Droxidopa. Autonomic nervous system disorder [8D87] [59]
Troleandomycin DMUZNIG Minor Decreased metabolism of Indacaterol caused by Troleandomycin mediated inhibition of CYP450 enzyme. Bacterial infection [1A00-1C4Z] [56]
Erdafitinib DMI782S Moderate Decreased clearance of Indacaterol due to the transporter inhibition by Erdafitinib. Bladder cancer [2C94] [60]
Pexidartinib DMS2J0Z Moderate Increased metabolism of Indacaterol caused by Pexidartinib mediated induction of CYP450 enzyme. Bone/articular cartilage neoplasm [2F7B] [61]
Eribulin DM1DX4Q Moderate Increased risk of ventricular arrhythmias by the combination of Indacaterol and Eribulin. Breast cancer [2C60-2C6Y] [58]
HKI-272 DM6QOVN Minor Decreased clearance of Indacaterol due to the transporter inhibition by HKI-272. Breast cancer [2C60-2C6Y] [56]
Tucatinib DMBESUA Minor Decreased clearance of Indacaterol due to the transporter inhibition by Tucatinib. Breast cancer [2C60-2C6Y] [56]
Palbociclib DMD7L94 Minor Decreased metabolism of Indacaterol caused by Palbociclib mediated inhibition of CYP450 enzyme. Breast cancer [2C60-2C6Y] [56]
Alpelisib DMEXMYK Minor Decreased clearance of Indacaterol due to the transporter inhibition by Alpelisib. Breast cancer [2C60-2C6Y] [56]
Bosutinib DMTI8YE Moderate Increased risk of prolong QT interval by the combination of Indacaterol and Bosutinib. Breast cancer [2C60-2C6Y] [58]
PF-04449913 DMSB068 Moderate Increased risk of ventricular arrhythmias by the combination of Indacaterol and PF-04449913. Chronic myelomonocytic leukaemia [2A40] [58]
Levomilnacipran DMV26S8 Moderate Additive hypertensive effects by the combination of Indacaterol and Levomilnacipran. Chronic pain [MG30] [62]
Ulipristal DMBNI20 Minor Decreased clearance of Indacaterol due to the transporter inhibition by Ulipristal. Contraceptive management [QA21] [56]
Pasireotide DMHM7JS Moderate Increased risk of ventricular arrhythmias by the combination of Indacaterol and Pasireotide. Cushing syndrome [5A70] [58]
Osilodrostat DMIJC9X Moderate Increased risk of prolong QT interval by the combination of Indacaterol and Osilodrostat. Cushing syndrome [5A70] [58]
Ivacaftor DMZC1HS Minor Decreased metabolism of Indacaterol caused by Ivacaftor mediated inhibition of CYP450 enzyme. Cystic fibrosis [CA25] [56]
MK-8228 DMOB58Q Minor Decreased clearance of Indacaterol due to the transporter inhibition by MK-8228. Cytomegaloviral disease [1D82] [56]
Desvenlafaxine DMHD4PE Moderate Increased risk of rapid heart rate by the combination of Indacaterol and Desvenlafaxine. Depression [6A70-6A7Z] [62]
Deutetrabenazine DMUPFLI Moderate Increased risk of ventricular arrhythmias by the combination of Indacaterol and Deutetrabenazine. Dystonic disorder [8A02] [58]
Stiripentol DMMSDOY Minor Decreased metabolism of Indacaterol caused by Stiripentol mediated inhibition of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [56]
Boceprevir DMBSHMF Minor Decreased metabolism of Indacaterol caused by Boceprevir mediated inhibition of CYP450 enzyme. Hepatitis virus infection [1E50-1E51] [56]
Telaprevir DMMRV29 Minor Decreased metabolism of Indacaterol caused by Telaprevir mediated inhibition of CYP450 enzyme. Hepatitis virus infection [1E50-1E51] [56]
Daclatasvir DMSFK9V Minor Decreased clearance of Indacaterol due to the transporter inhibition by Daclatasvir. Hepatitis virus infection [1E50-1E51] [56]
GS-5885 DMSL3DX Minor Decreased clearance of Indacaterol due to the transporter inhibition by GS-5885. Hepatitis virus infection [1E50-1E51] [56]
Fostemsavir DM50ILT Moderate Increased risk of ventricular arrhythmias by the combination of Indacaterol and Fostemsavir. Human immunodeficiency virus disease [1C60-1C62] [58]
Cobicistat DM6L4H2 Minor Decreased clearance of Indacaterol due to the transporter inhibition by Cobicistat. Human immunodeficiency virus disease [1C60-1C62] [56]
BMS-201038 DMQTAGO Minor Decreased metabolism of Indacaterol caused by BMS-201038 mediated inhibition of CYP450 enzyme. Hyper-lipoproteinaemia [5C80] [56]
Tolvaptan DMIWFRL Minor Decreased metabolism of Indacaterol caused by Tolvaptan mediated inhibition of CYP450 enzyme. Hypo-osmolality/hyponatraemia [5C72] [56]
Berotralstat DMWA2DZ Minor Decreased clearance of Indacaterol due to the transporter inhibition by Berotralstat. Innate/adaptive immunodeficiency [4A00] [56]
Suvorexant DM0E6S3 Minor Decreased clearance of Indacaterol due to the transporter inhibition by Suvorexant. Insomnia [7A00-7A0Z] [56]
Crizotinib DM4F29C Moderate Increased risk of ventricular arrhythmias by the combination of Indacaterol and Crizotinib. Lung cancer [2C25] [58]
Brigatinib DM7W94S Minor Decreased clearance of Indacaterol due to the transporter inhibition by Brigatinib. Lung cancer [2C25] [56]
Ceritinib DMB920Z Moderate Increased risk of prolong QT interval by the combination of Indacaterol and Ceritinib. Lung cancer [2C25] [58]
Osimertinib DMRJLAT Moderate Increased risk of prolong QT interval by the combination of Indacaterol and Osimertinib. Lung cancer [2C25] [58]
Capmatinib DMYCXKL Minor Decreased clearance of Indacaterol due to the transporter inhibition by Capmatinib. Lung cancer [2C25] [56]
Selpercatinib DMZR15V Moderate Increased risk of ventricular arrhythmias by the combination of Indacaterol and Selpercatinib. Lung cancer [2C25] [58]
Lumefantrine DM29GAD Moderate Increased risk of ventricular arrhythmias by the combination of Indacaterol and Lumefantrine. Malaria [1F40-1F45] [56]
Idelalisib DM602WT Minor Decreased metabolism of Indacaterol caused by Idelalisib mediated inhibition of CYP450 enzyme. Mature B-cell leukaemia [2A82] [56]
GDC-0199 DMH0QKA Minor Decreased clearance of Indacaterol due to the transporter inhibition by GDC-0199. Mature B-cell leukaemia [2A82] [56]
IPI-145 DMWA24P Minor Decreased metabolism of Indacaterol caused by IPI-145 mediated inhibition of CYP450 enzyme. Mature B-cell leukaemia [2A82] [56]
Ponatinib DMYGJQO Minor Decreased clearance of Indacaterol due to the transporter inhibition by Ponatinib. Mature B-cell lymphoma [2A85] [56]
Vemurafenib DM62UG5 Moderate Increased risk of prolong QT interval by the combination of Indacaterol and Vemurafenib. Melanoma [2C30] [58]
LGX818 DMNQXV8 Moderate Increased risk of ventricular arrhythmias by the combination of Indacaterol and LGX818. Melanoma [2C30] [58]
Lasmiditan DMXLVDT Moderate Decreased clearance of Indacaterol due to the transporter inhibition by Lasmiditan. Migraine [8A80] [63]
Panobinostat DM58WKG Moderate Increased risk of ventricular arrhythmias by the combination of Indacaterol and Panobinostat. Multiple myeloma [2A83] [58]
Siponimod DM2R86O Moderate Increased risk of ventricular arrhythmias by the combination of Indacaterol and Siponimod. Multiple sclerosis [8A40] [58]
Fingolimod DM5JVAN Moderate Increased risk of ventricular arrhythmias by the combination of Indacaterol and Fingolimod. Multiple sclerosis [8A40] [58]
Ozanimod DMT6AM2 Major Increased risk of ventricular arrhythmias by the combination of Indacaterol and Ozanimod. Multiple sclerosis [8A40] [64]
Romidepsin DMT5GNL Moderate Increased risk of prolong QT interval by the combination of Indacaterol and Romidepsin. Mycosis fungoides [2B01] [58]
Fedratinib DM4ZBK6 Minor Decreased metabolism of Indacaterol caused by Fedratinib mediated inhibition of CYP450 enzyme. Myeloproliferative neoplasm [2A20] [56]
Rolapitant DM8XP26 Minor Decreased clearance of Indacaterol due to the transporter inhibition by Rolapitant. Nausea/vomiting [MD90] [56]
Entrectinib DMMPTLH Moderate Increased risk of ventricular arrhythmias by the combination of Indacaterol and Entrectinib. Non-small cell lung cancer [2C25] [58]
Rucaparib DM9PVX8 Moderate Increased risk of ventricular arrhythmias by the combination of Indacaterol and Rucaparib. Ovarian cancer [2C73] [58]
Triclabendazole DMPWGBR Moderate Increased risk of ventricular arrhythmias by the combination of Indacaterol and Triclabendazole. Parasitic worm infestation [1F90] [58]
Safinamide DM0YWJC Moderate Additive hypertensive effects by the combination of Indacaterol and Safinamide. Parkinsonism [8A00] [57]
Istradefylline DM20VSK Minor Decreased metabolism of Indacaterol caused by Istradefylline mediated inhibition of CYP450 enzyme. Parkinsonism [8A00] [56]
Pimavanserin DMR7IVC Moderate Increased risk of ventricular arrhythmias by the combination of Indacaterol and Pimavanserin. Parkinsonism [8A00] [58]
Abametapir DM2RX0I Moderate Decreased metabolism of Indacaterol caused by Abametapir mediated inhibition of CYP450 enzyme. Pediculosis [1G00] [65]
Macimorelin DMQYJIR Major Increased risk of prolong QT interval by the combination of Indacaterol and Macimorelin. Pituitary gland disorder [5A60-5A61] [66]
Lefamulin DME6G97 Moderate Increased risk of ventricular arrhythmias by the combination of Indacaterol and Lefamulin. Pneumonia [CA40] [58]
Lonafarnib DMGM2Z6 Minor Decreased metabolism of Indacaterol caused by Lonafarnib mediated inhibition of CYP450 enzyme. Premature ageing appearance [LD2B] [56]
Degarelix DM3O8QY Moderate Increased risk of prolong QT interval by the combination of Indacaterol and Degarelix. Prostate cancer [2C82] [58]
ABIRATERONE DM8V75C Moderate Increased risk of ventricular arrhythmias by the combination of Indacaterol and ABIRATERONE. Prostate cancer [2C82] [58]
Enzalutamide DMGL19D Moderate Increased risk of ventricular arrhythmias by the combination of Indacaterol and Enzalutamide. Prostate cancer [2C82] [58]
Relugolix DMK7IWL Moderate Increased risk of ventricular arrhythmias by the combination of Indacaterol and Relugolix. Prostate cancer [2C82] [58]
Amisulpride DMSJVAM Moderate Increased risk of ventricular arrhythmias by the combination of Indacaterol and Amisulpride. Schizophrenia [6A20] [58]
Asenapine DMSQZE2 Moderate Increased risk of ventricular arrhythmias by the combination of Indacaterol and Asenapine. Schizophrenia [6A20] [58]
Voxelotor DMCS6M5 Minor Decreased clearance of Indacaterol due to the transporter inhibition by Voxelotor. Sickle-cell disorder [3A51] [56]
Larotrectinib DM26CQR Minor Decreased metabolism of Indacaterol caused by Larotrectinib mediated inhibition of CYP450 enzyme. Solid tumour/cancer [2A00-2F9Z] [56]
LEE011 DMMX75K Major Increased risk of prolong QT interval by the combination of Indacaterol and LEE011. Solid tumour/cancer [2A00-2F9Z] [67]
Vandetanib DMRICNP Moderate Increased risk of ventricular arrhythmias by the combination of Indacaterol and Vandetanib. Solid tumour/cancer [2A00-2F9Z] [58]
Triptorelin DMTK4LS Moderate Increased risk of ventricular arrhythmias by the combination of Indacaterol and Triptorelin. Solid tumour/cancer [2A00-2F9Z] [58]
Pitolisant DM8RFNJ Moderate Increased risk of ventricular arrhythmias by the combination of Indacaterol and Pitolisant. Somnolence [MG42] [58]
Telavancin DM58VQX Moderate Increased risk of ventricular arrhythmias by the combination of Indacaterol and Telavancin. Staphylococcal/streptococcal disease [1B5Y] [58]
Fostamatinib DM6AUHV Moderate Decreased clearance of Indacaterol due to the transporter inhibition by Fostamatinib. Thrombocytopenia [3B64] [68]
Lenvatinib DMB1IU4 Moderate Increased risk of ventricular arrhythmias by the combination of Indacaterol and Lenvatinib. Thyroid cancer [2D10] [58]
Cabozantinib DMIYDT4 Moderate Increased risk of ventricular arrhythmias by the combination of Indacaterol and Cabozantinib. Thyroid cancer [2D10] [58]
Elagolix DMB2C0E Minor Decreased clearance of Indacaterol due to the transporter inhibition by Elagolix. Uterine fibroid [2E86] [56]
Fluticasone DMGCSVF Minor Increased risk of hypokalemia by the combination of Indacaterol and Fluticasone. Vasomotor/allergic rhinitis [CA08] [69]
⏷ Show the Full List of 87 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
Lactose monohydrate E00393 104938 Binding agent; Diluent; Dry powder inhaler carrier; Lyophilization aid
Pharmaceutical Formulation
Formulation Name Drug Dosage Dosage Form Route
Indacaterol 0.075 mg powder 0.075 mg Inhalant Powder Oral
Indacaterol Maleate eq 75mcg base powder eq 75mcg base Powder Inhalation
Jump to Detail Pharmaceutical Formulation Page of This Drug

References

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56 Product Information. Arcapta Neohaler (indacaterol). Novartis Pharmaceuticals, East Hanover, NJ.
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59 Product Information. Northera (droxidopa). Chelsea Therapeutics Inc, Charlotte, NC.
60 Product Information. Balversa (erdafitinib). Janssen Products, LP, Horsham, PA.
61 Product Information. Turalio (pexidartinib). Daiichi Sankyo, Inc., Parsippany, NJ.
62 Product Information. Cymbalta (duloxetine). Lilly, Eli and Company, Indianapolis, IN.
63 Product Information. Reyvow (lasmiditan). Lilly, Eli and Company, Indianapolis, IN.
64 Product Information. Zeposia (ozanimod). Celgene Corporation, Summit, NJ.
65 Product Information. Xeglyze (abametapir topical). Dr. Reddy's Laboratories Inc, Upper Saddle River, NJ.
66 Product Information. Macrilen (macimorelin). Aeterna Zentaris, Charleston, SC.
67 Canadian Pharmacists Association.
68 Product Information. Tavalisse (fostamatinib). Rigel Pharmaceuticals, South San Francisco, CA.
69 Agencia Espaola de Medicamentos y Productos Sanitarios Healthcare "Centro de informacion online de medicamentos de la AEMPS - CIMA.".