Indacaterol
Identification
- Summary
Indacaterol is an inhaled long-acting beta-2 adrenergic agonist used to relax bronchial smooth muscle and improve symptoms and airflow obstruction caused by Chronic Obstructive Pulmonary Disease (COPD) and moderate to severe asthma.
- Brand Names
- Hirobriz, Onbrez, Ultibro
- Generic Name
- Indacaterol
- DrugBank Accession Number
- DB05039
- Background
Indacaterol is a novel, ultra-long-acting, rapid onset β(2)-adrenoceptor agonist developed for Novartis for the once-daily management of asthma and chronic obstructive pulmonary disease. It was approved by the European Medicines Agency (EMA) on 30 November 2009 and by the FDA on 1 July 2011. It is marketed in Europe as Onbrez and in America as Arcapta Neohaler. Indacaterol is provided as its maleate salt form. Indacaterol is also a chiral molecule but only the pure R-enantiomer is dispensed.
- Type
- Small Molecule
- Groups
- Approved
- Structure
- Weight
- Average: 392.4907
Monoisotopic: 392.209992772 - Chemical Formula
- C24H28N2O3
- Synonyms
- Indacaterol
- External IDs
- QAB 149
- QAB-149
- QAB149
- QVA-149 COMPONENT INDACATEROL
Pharmacology
- Indication
For the long term, once-daily-dosing maintenance of airflow obstruction in patients with chronic obstructive pulmonary disease (COPD), including chronic bronchitis and/or emphysema.
Reduce drug development failure ratesBuild, train, & validate machine-learning modelswith evidence-based and structured datasets.Build, train, & validate predictive machine-learning models with structured datasets.- Associated Conditions
Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Used in combination to manage Asthma Combination Product in combination with: Mometasone furoate (DB14512) •••••••••••• •••••••• •••••••••••• •••••••••• •••• ••••••• ••••••••••••••• ••••••• ••••••• Used in combination to treat Asthma Combination Product in combination with: Glycopyrronium (DB00986), Mometasone furoate (DB14512) •••••••••••• ••••••• ••••••• Used in combination to manage Chronic obstructive pulmonary disease Combination Product in combination with: Glycopyrronium (DB00986) •••••••••••• Management of Chronic obstructive pulmonary disease •••••••••••• - Associated Therapies
- Contraindications & Blackbox Warnings
- Prevent Adverse Drug Events TodayTap into our Clinical API for life-saving information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.Avoid life-threatening adverse drug events with our Clinical API
- Pharmacodynamics
Bronchodilator drugs are the foundation for the treatment of chronic obstructive pulmonary disease. The principal inhaled bronchodilator treatments used are β(2) -agonists and anticholinergics, either alone or in combination. Currently available β(2) -agonists are of either short duration and used multiple times/day, or of long duration, which requires twice-daily administration. Indacaterol is considered an ultra-long-acting β(2) -agonist and was recently approved for use in the United States. Its duration of action is approximately 24 hours, allowing for once-daily administration. Furthermore, this chiral compound it is given as the R-enantiomer and acts as a full agonist. Cough was the most commonly reported adverse effect with use of indacaterol. Compared to salmeterol, it has 35% more agonist activity. Cough usually occurred within 15 seconds of inhalation of the drug, lasted around 6 seconds, was not associated with bronchospasm, and did not cause discontinuation of the drug. Otherwise, the drug's safety profile was similar to that of other bronchodilators. [PMID: 22499359]
- Mechanism of action
Indacaterol works by stimulating adrenergic beta-2 receptors in the smooth muscle of the airways. This causes relaxation of the muscle, thereby increasing the diameter of the airways, which become constricted in asthma and COPD. It is also long acting due to its high affinity to the lipid raft domains in the airway membrane so it slowly dissociates from the receptors. Indacaterol also has a high intrinsic efficacy so it is also very rapid acting - onset of action occurs within 5 minutes.
The pharmacological effects of beta2-adrenoceptor agonist drugs, including indacaterol, are at least in part attributable to stimulation of intracellular adenyl cyclase, the enzyme that catalyzes the conversion of adenosine triphosphate (ATP) to cyclic-3’, 5’-adenosine monophosphate (cyclic monophosphate). Increased cyclic AMP levels cause relaxation of bronchial smooth muscle. In vitro studies have shown that indacaterol has more than 24-fold greater agonist activity at beta2-receptors compared to beta1-receptors and 20-fold greater agonist activity compared to beta3-receptors. This selectivity profile is similar to formoterol. The clinical significance of these findings is unknown.
Target Actions Organism ABeta-2 adrenergic receptor agonistHumans - Absorption
The median time to reach peak serum concentrations of indacaterol was approximately 15 minutes after single or repeated inhaled doses. Absolute bioavailability of indacaterol after an inhaled dose was on average 43-45%.
- Volume of distribution
After intravenous infusion the volume of distribution (Vz) of indacaterol was 2,361 L to 2,557 L indicating an extensive distribution.
- Protein binding
The in vitro human serum and plasma protein binding was 94.1-95.3% and 95.1-96.2%, respectively.
- Metabolism
After oral administration of radiolabeled indacaterol, unchanged indacaterol was the main component in serum, accounting for about one third of total drug-related AUC over 24 hours. The monohydroxylated derivative, glucuronide conjugate, and the 8-O-glucuronide were the most prominent metabolites in serum. Other metabolites identified include a diastereomer of the hydroxylated derivative, a N-glucuronide of indacaterol, and C- and N-dealkylated products.
In vitro investigations indicated that UGT1A1 was the only UGT isoform that metabolized indacaterol to the phenolic O-glucuronide. CYP3A4 is the predominant isoenzyme responsible for hydroxylation of indacaterol.
Hover over products below to view reaction partners
- Route of elimination
Renal clearance plays a minor role (about 2 to 6% of systemic clearance) in the elimination of systemically available indacaterol. In a human ADME study where indacaterol was given orally, the fecal route of excretion was dominant over the urinary route. Indacaterol was excreted into human feces primarily as unchanged parent drug (54% of the dose) and, to a lesser extent, hydroxylated indacaterol metabolites (23% of the dose).
- Half-life
Indacaterol serum concentrations declined in a multi-phasic manner with an average terminal half-life ranging from 45.5 to 126 hours. The effective half-life, calculated from the accumulation of indacaterol after repeated dosing with once daily doses between 75 mcg and 600 mcg ranged from 40 to 56 hours which is consistent with the observed time-to-steady state of approximately 12-15 days.
- Clearance
Renal clearance of indacaterol is, on average, between 0.46 and 1.2 L/h. Serum clearance of indacaterol is 18.8 L/h to 23.3 L/h.
- Adverse Effects
- Improve decision support & research outcomesWith structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates. View sample adverse effects data in our new Data Library!Improve decision support & research outcomes with our structured adverse effects data.
- Toxicity
The expected signs and symptoms associated with overdosage of indacaterol are those of excessive beta-adrenergic stimulation and occurrence or exaggeration of any of the signs and symptoms, e.g., angina, hypertension or hypotension, tachycardia, with rates up to 200 bpm, arrhythmias, nervousness, headache, tremor, dry mouth, palpitation, muscle cramps, nausea, dizziness, fatigue, malaise, hypokalemia, hyperglycemia, metabolic acidosis and insomnia. As with all inhaled sympathomimetic medications, cardiac arrest and even death may be associated with an overdose of indacaterol.
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs Browse all" title="About SNP Mediated Effects/ADRs" id="snp-actions-info" class="drug-info-popup" href="javascript:void(0);">
- Not Available
Interactions
- Drug Interactions Learn More" title="About Drug Interactions" id="structured-interactions-info" class="drug-info-popup" href="javascript:void(0);">
- This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Drug Interaction Integrate drug-drug
interactions in your softwareAbametapir The serum concentration of Indacaterol can be increased when it is combined with Abametapir. Abemaciclib The serum concentration of Abemaciclib can be increased when it is combined with Indacaterol. Abrocitinib The serum concentration of Indacaterol can be increased when it is combined with Abrocitinib. Acebutolol The therapeutic efficacy of Indacaterol can be decreased when used in combination with Acebutolol. Aceclofenac The risk or severity of hypertension can be increased when Indacaterol is combined with Aceclofenac. - Food Interactions
- No interactions found.
Products
- Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.
- Product Ingredients
Ingredient UNII CAS InChI Key Indacaterol acetate RYI4401DTM 1000160-96-2 HZHXFIDENGBQFQ-FTBISJDPSA-N Indacaterol maleate 2JEC1ITX7R 753498-25-8 IREJFXIHXRZFER-PCBAQXHCSA-N - International/Other Brands
- Arcapta (Novartis) / Hirobriz / Onbrez (Novartis) / Onbrize
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Arcapta Neohaler Capsule 75 ug/1 Oral; Respiratory (inhalation) Sunovion Pharmaceuticals Inc. 2011-07-01 2021-01-31 US Arcapta Neohaler Capsule 75 ug/1 Oral; Respiratory (inhalation) Novartis 2011-07-01 2018-08-31 US Hirobriz Breezhaler Capsule 300 μg Respiratory (inhalation) Novartis Europharm Limited 2016-09-07 Not applicable EU Hirobriz Breezhaler Capsule 300 μg Respiratory (inhalation) Novartis Europharm Limited 2016-09-07 Not applicable EU Hirobriz Breezhaler Capsule 150 μg Respiratory (inhalation) Novartis Europharm Limited 2016-09-07 Not applicable EU - Mixture Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image Atectura Breezhaler Indacaterol acetate (125 mcg) + Mometasone furoate (62.5 mcg) Capsule Respiratory (inhalation) Novartis Europharm Limited 2020-12-16 Not applicable EU Atectura Breezhaler Indacaterol acetate (125 mcg) + Mometasone furoate (127.5 mcg) Capsule Respiratory (inhalation) Novartis Europharm Limited 2023-02-08 Not applicable EU ATECTURA BREEZHALER Indacaterol acetate (125 MCG) + Mometasone furoate (127.5 MCG) Powder, metered Respiratory (inhalation) Novartis Europharm Limited 2020-09-10 Not applicable Italy Atectura Breezhaler Indacaterol acetate (125 mcg) + Mometasone furoate (260 mcg) Capsule Respiratory (inhalation) Novartis Europharm Limited 2020-12-16 Not applicable EU ATECTURA BREEZHALER Indacaterol acetate (125 MCG) + Mometasone furoate (62.5 MCG) Powder, metered Respiratory (inhalation) Novartis Europharm Limited 2020-09-10 Not applicable Italy
Categories
- ATC Codes
- R03AC18 — Indacaterol
- R03AC — Selective beta-2-adrenoreceptor agonists
- R03A — ADRENERGICS, INHALANTS
- R03 — DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES
- R — RESPIRATORY SYSTEM
- R03AL — Adrenergics in combination with anticholinergics incl. triple combinations with corticosteroids
- R03A — ADRENERGICS, INHALANTS
- R03 — DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES
- R — RESPIRATORY SYSTEM
- R03AL — Adrenergics in combination with anticholinergics incl. triple combinations with corticosteroids
- R03A — ADRENERGICS, INHALANTS
- R03 — DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES
- R — RESPIRATORY SYSTEM
- Drug Categories
- Adrenergic Agonists
- Adrenergic beta-2 Receptor Agonists
- Adrenergic beta-Agonists
- Adrenergics, Inhalants
- Agents producing tachycardia
- Agents that produce hypertension
- Agents to Treat Airway Disease
- Cytochrome P-450 CYP3A Substrates
- Cytochrome P-450 CYP3A4 Substrates
- Cytochrome P-450 Substrates
- Drugs for Obstructive Airway Diseases
- Heterocyclic Compounds, Fused-Ring
- Indenes
- Long-acting beta-adrenoceptor agonists
- P-glycoprotein substrates
- Potential QTc-Prolonging Agents
- QTc Prolonging Agents
- Quinolines
- Selective Beta 2-adrenergic Agonists
- UGT1A1 Substrates
- Chemical TaxonomyProvided by Classyfire
- Description
- This compound belongs to the class of organic compounds known as hydroxyquinolones. These are compounds containing a quinoline moiety bearing a hydroxyl group and a ketone. Quinoline or benzo[b]pyridine is a bicyclic compound that consists of benzene fused to a pyridine.
- Kingdom
- Organic compounds
- Super Class
- Organoheterocyclic compounds
- Class
- Quinolines and derivatives
- Sub Class
- Quinolones and derivatives
- Direct Parent
- Hydroxyquinolones
- Alternative Parents
- 8-hydroxyquinolines / Hydroxyquinolines / Hydroquinolones / Hydroquinolines / Indanes / 1-hydroxy-2-unsubstituted benzenoids / Pyridinones / Aralkylamines / Heteroaromatic compounds / 1,2-aminoalcohols show 8 more
- Substituents
- 1,2-aminoalcohol / 1-hydroxy-2-unsubstituted benzenoid / 8-hydroxyquinoline / Alcohol / Amine / Aralkylamine / Aromatic alcohol / Aromatic heteropolycyclic compound / Azacycle / Benzenoid show 19 more
- Molecular Framework
- Aromatic heteropolycyclic compounds
- External Descriptors
- secondary alcohol, secondary amino compound, indanes, quinolone, monohydroxyquinoline (CHEBI:68575)
- Affected organisms
- Humans and other mammals
Chemical Identifiers
- UNII
- 8OR09251MQ
- CAS number
- 312753-06-3
- InChI Key
- QZZUEBNBZAPZLX-QFIPXVFZSA-N
- 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
- IUPAC Name
- 5-[(1R)-2-[(5,6-diethyl-2,3-dihydro-1H-inden-2-yl)amino]-1-hydroxyethyl]-8-hydroxy-1,2-dihydroquinolin-2-one
- SMILES
- CCC1=C(CC)C=C2CC(CC2=C1)NC[C@H](O)C1=C2C=CC(=O)NC2=C(O)C=C1
References
- General References
- Naline E, Trifilieff A, Fairhurst RA, Advenier C, Molimard M: Effect of indacaterol, a novel long-acting beta2-agonist, on isolated human bronchi. Eur Respir J. 2007 Mar;29(3):575-81. Epub 2006 Nov 29. [Article]
- Kagan M, Dain J, Peng L, Reynolds C: Metabolism and pharmacokinetics of indacaterol in humans. Drug Metab Dispos. 2012 Sep;40(9):1712-22. doi: 10.1124/dmd.112.046151. Epub 2012 May 30. [Article]
- Reid DJ, Pham NT: Emerging Therapeutic Options for the Management of COPD. Clin Med Insights Circ Respir Pulm Med. 2013 Apr 9;7:7-15. doi: 10.4137/CCRPM.S8140. Print 2013. [Article]
- External Links
- Human Metabolome Database
- HMDB0015608
- KEGG Drug
- D09318
- PubChem Compound
- 6918554
- PubChem Substance
- 175426936
- ChemSpider
- 5293751
- BindingDB
- 50318159
- 1114326
- ChEBI
- 68575
- ChEMBL
- CHEMBL1095777
- ZINC
- ZINC000035801098
- PharmGKB
- PA165958348
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- Wikipedia
- Indacaterol
- FDA label
- Download (360 KB)
- MSDS
- Download (479 KB)
Clinical Trials
- Clinical Trials Learn More" title="About Clinical Trials" id="clinical-trials-info" class="drug-info-popup" href="javascript:void(0);">
Phase Status Purpose Conditions Count 4 Completed Basic Science Chronic Obstructive Pulmonary Disease (COPD) 1 4 Completed Basic Science Chronic Obstructive Pulmonary Disease (COPD) / Hyperinflation / Right Cardiac Failure 1 4 Completed Treatment Asthma 2 4 Completed Treatment Chronic Obstructive Pulmonary Disease (COPD) 17 4 Completed Treatment Chronic Obstructive Pulmonary Disease (COPD) / Dyspnea / Hypoxemia / Lung Disorder / Tachycardia 1
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Capsule Respiratory (inhalation) Capsule Oral; Respiratory (inhalation) 75 ug/1 Powder Buccal Powder, metered Respiratory (inhalation) 150 mcg Powder Buccal 0.050 mg Powder, metered Respiratory (inhalation) 300 MCG Capsule Respiratory (inhalation) 150 UG Capsule Respiratory (inhalation) 75 mcg Powder Respiratory (inhalation) Powder Respiratory (inhalation) 194 MCG Powder Respiratory (inhalation) 389 MCG Powder Respiratory (inhalation) 150 MCG Powder Respiratory (inhalation) 300 MCG Capsule Respiratory (inhalation) 300 UG Capsule Respiratory (inhalation) 0.150 mg Capsule Respiratory (inhalation) 0.300 mg Drug delivery system Buccal 389.000 mcg Powder Respiratory (inhalation) 0.15 mg Capsule Respiratory (inhalation) 150 μg Capsule Respiratory (inhalation) 300 μg Drug delivery system Buccal Powder Respiratory (inhalation) Capsule Buccal Capsule, coated Respiratory (inhalation) Capsule Respiratory (inhalation) Powder, metered Respiratory (inhalation) Powder, metered Respiratory (inhalation) Capsule Respiratory (inhalation) 150 mcg Capsule Respiratory (inhalation) 300 mcg - Prices
- Not Available
- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region US6878721 No 2005-04-12 2020-10-10 US US8067437 No 2011-11-29 2020-06-02 US US8658673 No 2014-02-25 2020-06-02 US US8796307 No 2014-08-05 2020-06-02 US US8479730 No 2013-07-09 2028-10-11 US US7229607 No 2007-06-12 2021-04-09 US US7820694 No 2010-10-26 2020-06-02 US US8029768 No 2011-10-04 2021-04-09 US US8283362 No 2012-10-09 2020-06-02 US US7736670 No 2010-06-15 2021-06-27 US US8435567 No 2013-05-07 2021-06-27 US US8303991 No 2012-11-06 2021-06-27 US US8956661 No 2015-02-17 2021-06-27 US US8580306 No 2013-11-12 2021-06-27 US US6582678 No 2003-06-24 2018-04-24 US US8182838 No 2012-05-22 2028-10-20 US US6521260 No 2003-02-18 2016-01-31 US US8048451 No 2011-11-01 2021-06-27 US US9931304 No 2018-04-03 2021-06-27 US US9962338 No 2018-05-08 2021-06-27 US
Properties
- State
- Solid
- Experimental Properties
Property Value Source melting point (°C) 195-202°C with decomposition Not Available - Predicted Properties
Property Value Source Water Solubility 0.00798 mg/mL ALOGPS logP 3.31 ALOGPS logP 3.26 Chemaxon logS -4.7 ALOGPS pKa (Strongest Acidic) 8.51 Chemaxon pKa (Strongest Basic) 9.71 Chemaxon Physiological Charge 1 Chemaxon Hydrogen Acceptor Count 4 Chemaxon Hydrogen Donor Count 4 Chemaxon Polar Surface Area 81.59 Å2 Chemaxon Rotatable Bond Count 6 Chemaxon Refractivity 118.1 m3·mol-1 Chemaxon Polarizability 44.96 Å3 Chemaxon Number of Rings 4 Chemaxon Bioavailability 1 Chemaxon Rule of Five Yes Chemaxon Ghose Filter Yes Chemaxon Veber's Rule No Chemaxon MDDR-like Rule Yes Chemaxon - Predicted ADMET Features
Property Value Probability Human Intestinal Absorption + 0.9963 Blood Brain Barrier + 0.5 Caco-2 permeable - 0.6288 P-glycoprotein substrate Substrate 0.6953 P-glycoprotein inhibitor I Non-inhibitor 0.9284 P-glycoprotein inhibitor II Non-inhibitor 0.9178 Renal organic cation transporter Non-inhibitor 0.8838 CYP450 2C9 substrate Non-substrate 0.8148 CYP450 2D6 substrate Non-substrate 0.6907 CYP450 3A4 substrate Substrate 0.5896 CYP450 1A2 substrate Inhibitor 0.553 CYP450 2C9 inhibitor Non-inhibitor 0.56 CYP450 2D6 inhibitor Non-inhibitor 0.8547 CYP450 2C19 inhibitor Non-inhibitor 0.5581 CYP450 3A4 inhibitor Non-inhibitor 0.6546 CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.5888 Ames test Non AMES toxic 0.7577 Carcinogenicity Non-carcinogens 0.8559 Biodegradation Not ready biodegradable 0.9856 Rat acute toxicity 2.6531 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.9657 hERG inhibition (predictor II) Inhibitor 0.6406
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
Spectrum Spectrum Type Splash Key Predicted GC-MS Spectrum - GC-MS Predicted GC-MS splash10-03fr-1954000000-ccc7de5fce46537c0912 Predicted MS/MS Spectrum - 10V, Positive (Annotated) Predicted LC-MS/MS splash10-0006-0009000000-cbec9d56059af437dfcf Predicted MS/MS Spectrum - 10V, Negative (Annotated) Predicted LC-MS/MS splash10-0fdo-0049000000-83925c1ad51999083331 Predicted MS/MS Spectrum - 20V, Negative (Annotated) Predicted LC-MS/MS splash10-0006-0109000000-3baffa3c79830348e4d6 Predicted MS/MS Spectrum - 20V, Positive (Annotated) Predicted LC-MS/MS splash10-0006-0319000000-53ca387c3442df4ccf77 Predicted MS/MS Spectrum - 40V, Negative (Annotated) Predicted LC-MS/MS splash10-06y6-3936000000-a8102b2e45be875dfb5d Predicted MS/MS Spectrum - 40V, Positive (Annotated) Predicted LC-MS/MS splash10-0w2l-0955000000-ec1a9baaec4529a79dbb Predicted 1H NMR Spectrum 1D NMR Not Applicable Predicted 13C NMR Spectrum 1D NMR Not Applicable - Chromatographic Properties
Collision Cross Sections (CCS)
Adduct CCS Value (Å2) Source type Source [M-H]- 221.3031722 predictedDarkChem Lite v0.1.0 [M-H]- 221.4978722 predictedDarkChem Lite v0.1.0 [M-H]- 192.33443 predictedDeepCCS 1.0 (2019) [M+H]+ 222.4347722 predictedDarkChem Lite v0.1.0 [M+H]+ 222.6830722 predictedDarkChem Lite v0.1.0 [M+H]+ 194.69243 predictedDeepCCS 1.0 (2019) [M+Na]+ 222.0900722 predictedDarkChem Lite v0.1.0 [M+Na]+ 222.1065722 predictedDarkChem Lite v0.1.0 [M+Na]+ 200.89961 predictedDeepCCS 1.0 (2019)
Targets
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Agonist
- General Function
- Protein homodimerization activity
- Specific Function
- Beta-adrenergic receptors mediate the catecholamine-induced activation of adenylate cyclase through the action of G proteins. The beta-2-adrenergic receptor binds epinephrine with an approximately ...
- Gene Name
- ADRB2
- Uniprot ID
- P07550
- Uniprot Name
- Beta-2 adrenergic receptor
- Molecular Weight
- 46458.32 Da
References
- Cazzola M, Matera MG, Lotvall J: Ultra long-acting beta 2-agonists in development for asthma and chronic obstructive pulmonary disease. Expert Opin Investig Drugs. 2005 Jul;14(7):775-83. [Article]
Enzymes
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Vitamin d3 25-hydroxylase activity
- Specific Function
- Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
- Gene Name
- CYP3A4
- Uniprot ID
- P08684
- Uniprot Name
- Cytochrome P450 3A4
- Molecular Weight
- 57342.67 Da
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Steroid binding
- Specific Function
- UDPGT is of major importance in the conjugation and subsequent elimination of potentially toxic xenobiotics and endogenous compounds. This isoform glucuronidates bilirubin IX-alpha to form both the...
- Gene Name
- UGT1A1
- Uniprot ID
- P22309
- Uniprot Name
- UDP-glucuronosyltransferase 1-1
- Molecular Weight
- 59590.91 Da
Transporters
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Xenobiotic-transporting atpase activity
- Specific Function
- Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
- Gene Name
- ABCB1
- Uniprot ID
- P08183
- Uniprot Name
- Multidrug resistance protein 1
- Molecular Weight
- 141477.255 Da
Drug created at October 21, 2007 22:23 / Updated at January 02, 2024 23:47