Identification
- Summary
Ticagrelor is a P2Y12 platelet inhibitor used in patients with a history of myocardial infarction or with acute coronary syndrome (ACS) to prevent future myocardial infarction, stroke and cardiovascular death.
- Brand Names
- Brilinta, Brilique
- Generic Name
- Ticagrelor
- DrugBank Accession Number
- DB08816
- Background
Ticagrelor, or AZD6140, was first described in the literature in 2003.4,5 Ticagrelor is an ADP derivative developed for its P2Y12 receptor antagonism.5 Unlike clopidogrel, ticagrelor is not a prodrug.5 It is marketed by Astra Zeneca as Brilinta in the US6 and Brilique or Possia in the EU,7.
Ticagrelor was granted EMA approval on 3 December 2010.7 Ticagrelor was granted FDA approval on 20 July 2011.6
- Type
- Small Molecule
- Groups
- Approved
- Structure
Structure for Ticagrelor (DB08816)
- Weight
- Average: 522.568
Monoisotopic: 522.186080514 - Chemical Formula
- C23H28F2N6O4S
- Synonyms
- (1S,2S,3R,5S)-3-(7-((1R,2S)-2-(3,4-Difluorophenyl)cyclopropylamino)-5-(propylthio)-3H-(1,2,3)triazolo(4,5-d)pyrimidin-3-yl)-5-(2-hydroxyethoxy)cyclopentane-1,2-diol
- Ticagrelor
- External IDs
- AR-C126532XX
- AZD 6140
- AZD-6140
- AZD6140
Pharmacology
- Indication
Ticagrelor is indicated to reduce the risk of cardiovascular death, myocardial infarction, and stroke in patients with acute coronary syndrome or a history of myocardial infarction.6 Ticagrelor is also indicated to reduce the risk of a first myocardial infarction or stroke in high risk patients with coronary artery disease.6
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- Contraindications & Blackbox Warnings
Avoid life-threatening adverse drug eventsImprove clinical decision support with information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.Avoid life-threatening adverse drug events & improve clinical decision support.- Pharmacodynamics
Ticagrelor is a P2Y12 receptor antagonist that inhibits the formation of thromboses to reduce the risk of myocardial infarction and ischemic stroke.1,3 It has a moderate duration of action as it is given twice daily, and a wide therapeutic index as high single doses are well tolerated.6,7 Patients should be counselled regarding the risk of bleeding, dyspnea, and bradyarrhythmias.6
- Mechanism of action
Ticagrelor is a P2Y12 receptor antagonist.1
The P2Y12 receptor couples with Gαi2 and other Gi proteins which inhibit adenylyl cyclase.3 Gi mediated signalling also activates PI3K, Akt, Rap1b, and potassium channels.3 The downstream effects of these activities mediate hemostasis and lead to platelet aggregation.3
Antagonism of the P2Y12 receptor reduces development of occlusive thromboses, which can reduce the risk of myocardial infarction and ischemic stroke.3
Target Actions Organism AP2Y purinoceptor 12 inhibitorHumans - Absorption
Ticagrelor is 36% orally bioavailable.6 A single 200mg oral dose of ticagrelor reaches a Cmax of 923ng/mL, with a Tmax of 1.5 hours and an AUC of 6675ng*h/mL.1 The active metabolite of ticagrelor reaches a Cmax of 264ng/mL, with a Tmax of 3.0 hours and an AUC of 2538ng*h/mL.1
- Volume of distribution
The steady state volume of distribution of ticagrelor is 88 L.6
- Protein binding
Ticagrelor and its active metabolite ate >99% protein bound in plasma, particularly albumin.2,6
- Metabolism
The complete structure of all ticagrelor metabolites are not well defined.1 Ticagrelor can be dealkylated at postition 5 of the cyclopentane ring to form the active AR-C124910XX.1 AR-C124910XX's cyclopentane ring can be further glucuronidated or the alkyl chain attached to the sulfur can be hydroxylated.1 Ticagrelor can also be glucuronidated or hydroxylated.1 Ticagrelor can also be N-dealkylated to form AR-C133913XX, which is further glucuronidated or hydroxylated.1
Hover over products below to view reaction partners
- Route of elimination
A radiolabelled dose of ticagrelor is 57.8% recovered in feces and 26.5% recovered in urine.1,6 Less than 1% of the dose is recovered as the unmetabolized parent drug.6 The active metabolite AC-C124910XX makes up 21.7% of the recovery in the feces.1 The metabolite AR-C133913XX makes up 9.2% of the recovery in the urine and 2.7% of the recovery in the feces.1 Other minor metabolites are predominantly recovered in the urine.1
- Half-life
Ticagrelor has a plasma half life of approximately 8 hours, while the active metabolite has a plasma half life of approximately 12 hours.1
- Clearance
The renal clearance of ticagrelor is 0.00584L/h.1
- Adverse Effects
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Patients experiencing an overdose may present with bleeding, nausea, vomiting, diarrhea, and ventricular pauses.6 Overdose can be managed through symptomatic and supportive treatment, including ECG monitoring.6,7 Dialysis is not expected to remove ticagrelor from the blood due to it being highly protein bound.6
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs
- Not Available
Interactions
- Drug Interactions
- 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 Ticagrelor can be increased when it is combined with Abametapir. Abatacept The metabolism of Ticagrelor can be increased when combined with Abatacept. Abciximab The risk or severity of bleeding can be increased when Abciximab is combined with Ticagrelor. Abemaciclib The serum concentration of Abemaciclib can be increased when it is combined with Ticagrelor. Abrocitinib The risk or severity of bleeding and thrombocytopenia can be increased when Ticagrelor is combined with Abrocitinib. Acalabrutinib The metabolism of Acalabrutinib can be decreased when combined with Ticagrelor. Aceclofenac The risk or severity of bleeding and hemorrhage can be increased when Aceclofenac is combined with Ticagrelor. Acemetacin The risk or severity of bleeding and hemorrhage can be increased when Ticagrelor is combined with Acemetacin. Acenocoumarol The serum concentration of Acenocoumarol can be increased when it is combined with Ticagrelor. Acetohexamide The metabolism of Acetohexamide can be decreased when combined with Ticagrelor. 
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- Avoid grapefruit products. Grapefruit inhibits the CYP3A4 metabolism of ticagrelor, which may increase its serum concentration.
- Avoid herbs and supplements with anticoagulant/antiplatelet activity. Herbs with antiplatelet activity may increase the risk of bleeding. Examples include garlic, ginger, bilberry, danshen, piracetam, and ginkgo biloba.
- Avoid St. John's Wort. This herb induces the CYP3A4 metabolism of ticagrelor and may reduce its serum concentration.
- Take with or without food.
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 Images
- International/Other Brands
- Brilinta / Possia (AstraZeneca)
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Brilinta Tablet 60 mg Oral Astra Zeneca 2016-06-13 Not applicable Canada 
Brilinta Tablet 90 mg/1 Oral AstraZeneca Pharmaceuticals LP 2011-08-05 Not applicable US 
Brilinta Tablet 90 mg Oral Astra Zeneca 2011-06-01 Not applicable Canada Brilinta Tablet 90 mg/1 Oral bryant ranch prepack 2011-08-05 2016-04-30 US 
Brilinta Tablet 90 mg/1 Oral Cardinal Health 107, LLC 2011-08-05 Not applicable US 
Brilinta Tablet 60 mg/1 Oral AstraZeneca Pharmaceuticals LP 2015-09-04 Not applicable US Brilique Tablet, orally disintegrating 90 mg Oral Astra Zeneca Ab 2020-12-16 Not applicable EU 
Brilique Tablet, film coated 60 mg Oral Astra Zeneca Ab 2016-09-07 Not applicable EU Brilique Tablet, film coated 60 mg Oral Astra Zeneca Ab 2016-09-07 Not applicable EU Brilique Tablet, film coated 90 mg Oral Astra Zeneca Ab 2016-09-07 Not applicable EU - Generic Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Apo-ticagrelor Tablet 90 mg Oral Apotex Corporation 2022-12-14 Not applicable Canada Apo-ticagrelor Tablet 60 mg Oral Apotex Corporation 2022-12-22 Not applicable Canada Na Tablet 90 mg/1 Oral Sunshine Lake Pharma Co., Ltd. 2020-04-09 2020-04-10 US Na Tablet 60 mg/1 Oral Sunshine Lake Pharma Co., Ltd. 2020-04-09 2020-04-10 US Taro-ticagrelor Tablet 60 mg Oral Taro Pharmaceuticals, Inc. 2022-05-31 Not applicable Canada Taro-ticagrelor Tablet 90 mg Oral Taro Pharmaceuticals, Inc. 2022-04-29 Not applicable Canada Teva-ticagrelor Tablet 60 mg Oral TEVA Canada Limited Not applicable Not applicable Canada Teva-ticagrelor Tablet 90 mg Oral TEVA Canada Limited Not applicable Not applicable Canada Ticagrelor Tablet 90 mg/1 Oral Amneal Pharmaceuticals NY LLC 2019-01-23 Not applicable US
Categories
- ATC Codes
- B01AC24 — Ticagrelor
- Drug Categories
- Anticoagulants
- Antiplatelet agents
- Blood and Blood Forming Organs
- Carbohydrates
- Cytochrome P-450 CYP2B6 Inducers
- Cytochrome P-450 CYP2B6 Inducers (weak)
- Cytochrome P-450 CYP2C9 Inducers
- Cytochrome P-450 CYP2C9 Inducers (strength unknown)
- Cytochrome P-450 CYP2C9 Inducers (weak)
- Cytochrome P-450 CYP2C9 Inhibitors
- Cytochrome P-450 CYP2C9 Inhibitors (weak)
- Cytochrome P-450 CYP3A Inhibitors
- Cytochrome P-450 CYP3A Substrates
- Cytochrome P-450 CYP3A4 Inhibitors
- Cytochrome P-450 CYP3A4 Inhibitors (strength unknown)
- Cytochrome P-450 CYP3A4 Inhibitors (weak)
- Cytochrome P-450 CYP3A4 Substrates
- Cytochrome P-450 CYP3A5 Inhibitors
- Cytochrome P-450 CYP3A5 Substrates
- Cytochrome P-450 Enzyme Inducers
- Cytochrome P-450 Enzyme Inhibitors
- Cytochrome P-450 Substrates
- Decreased Platelet Aggregation
- Glycosides
- Hematologic Agents
- Heterocyclic Compounds, Fused-Ring
- Nucleic Acids, Nucleotides, and Nucleosides
- Nucleosides
- P-glycoprotein inhibitors
- P-glycoprotein substrates
- P2Y12 Platelet Inhibitor
- Phenylalanine Hydroxylase Activators
- Platelet Aggregation Inhibitors Excl. Heparin
- Purine Nucleosides
- Purinergic Agents
- Purinergic Antagonists
- Purinergic P2 Receptor Antagonists
- Purinergic P2Y Receptor Antagonists
- Purines
- Ribonucleosides
- Chemical TaxonomyProvided by Classyfire
- Description
- This compound belongs to the class of organic compounds known as triazolopyrimidines. These are polycyclic aromatic compounds containing triazole ring fused to a pyrimidine ring. Triazole is a five-membered ring consisting of two carbon atoms and three nitrogen atoms. Pyrimidine is a 6-membered ring consisting of four carbon atoms and two nitrogen centers at the 1- and 3- ring positions.
- Kingdom
- Organic compounds
- Super Class
- Organoheterocyclic compounds
- Class
- Triazolopyrimidines
- Sub Class
- Not Available
- Direct Parent
- Triazolopyrimidines
- Alternative Parents
- Alkylarylthioethers / Aminopyrimidines and derivatives / Secondary alkylarylamines / Fluorobenzenes / Aryl fluorides / Cyclitols and derivatives / Cyclopentanols / Imidolactams / Triazoles / Heteroaromatic compounds show 7 more
- Substituents
- 1,2,3-triazole / Alcohol / Alkylarylthioether / Amine / Aminopyrimidine / Aromatic heteropolycyclic compound / Aryl fluoride / Aryl halide / Aryl thioether / Azacycle show 30 more
- Molecular Framework
- Aromatic heteropolycyclic compounds
- External Descriptors
- organofluorine compound, aryl sulfide, secondary amino compound, triazolopyrimidines, hydroxyether (CHEBI:68558)
- Affected organisms
- Humans and other mammals
Chemical Identifiers
- UNII
- GLH0314RVC
- CAS number
- 274693-27-5
- InChI Key
- OEKWJQXRCDYSHL-FNOIDJSQSA-N
- InChI
- InChI=1S/C23H28F2N6O4S/c1-2-7-36-23-27-21(26-15-9-12(15)11-3-4-13(24)14(25)8-11)18-22(28-23)31(30-29-18)16-10-17(35-6-5-32)20(34)19(16)33/h3-4,8,12,15-17,19-20,32-34H,2,5-7,9-10H2,1H3,(H,26,27,28)/t12-,15+,16+,17-,19-,20+/m0/s1
- IUPAC Name
- (1S,2S,3R,5S)-3-(7-{[(1R,2S)-2-(3,4-difluorophenyl)cyclopropyl]amino}-5-(propylsulfanyl)-3H-[1,2,3]triazolo[4,5-d]pyrimidin-3-yl)-5-(2-hydroxyethoxy)cyclopentane-1,2-diol
- SMILES
- CCCSC1=NC2=C(N=NN2[C@@H]2C[C@H](OCCO)[C@@H](O)[C@H]2O)C(N[C@@H]2C[C@H]2C2=CC(F)=C(F)C=C2)=N1
References
- Synthesis Reference
Anil Shahaji Khile, "NOVEL PROCESSES FOR THE PREPARATION OF PHENYLCYCLOPROPYLAMINE DERIVATIVES AND USE THEREOF FOR PREPARING TICAGRELOR." U.S. Patent US20130165696, issued June 27, 2013.
US20130165696- General References
- Teng R, Oliver S, Hayes MA, Butler K: Absorption, distribution, metabolism, and excretion of ticagrelor in healthy subjects. Drug Metab Dispos. 2010 Sep;38(9):1514-21. doi: 10.1124/dmd.110.032250. Epub 2010 Jun 15. [Article]
- Angheloiu GO, Gugiu GB, Ruse C, Pandey R, Dasari RR, Whatling C: Ticagrelor Removal From Human Blood. JACC Basic Transl Sci. 2017 Apr 24;2(2):135-145. doi: 10.1016/j.jacbts.2017.01.007. eCollection 2017 Apr. [Article]
- Dorsam RT, Kunapuli SP: Central role of the P2Y12 receptor in platelet activation. J Clin Invest. 2004 Feb;113(3):340-5. doi: 10.1172/JCI20986. [Article]
- Jacobson KA, Costanzi S, Ohno M, Joshi BV, Besada P, Xu B, Tchilibon S: Molecular recognition at purine and pyrimidine nucleotide (P2) receptors. Curr Top Med Chem. 2004;4(8):805-19. doi: 10.2174/1568026043450961. [Article]
- Springthorpe B, Bailey A, Barton P, Birkinshaw TN, Bonnert RV, Brown RC, Chapman D, Dixon J, Guile SD, Humphries RG, Hunt SF, Ince F, Ingall AH, Kirk IP, Leeson PD, Leff P, Lewis RJ, Martin BP, McGinnity DF, Mortimore MP, Paine SW, Pairaudeau G, Patel A, Rigby AJ, Riley RJ, Teobald BJ, Tomlinson W, Webborn PJ, Willis PA: From ATP to AZD6140: the discovery of an orally active reversible P2Y12 receptor antagonist for the prevention of thrombosis. Bioorg Med Chem Lett. 2007 Nov 1;17(21):6013-8. Epub 2007 Aug 19. [Article]
- FDA Approved Drug Products: BRILINTA (ticagrelor) tablets, for oral use [Link]
- EMA Summary of Product Characteristics: Brilique Ticagrelor Oral Tablet [Link]
- External Links
- Human Metabolome Database
- HMDB0015702
- KEGG Drug
- D09017
- PubChem Compound
- 9871419
- PubChem Substance
- 175427101
- ChemSpider
- 8047109
- BindingDB
- 50397205
- 1116632
- ChEBI
- 68558
- ChEMBL
- CHEMBL398435
- ZINC
- ZINC000028957444
- PharmGKB
- PA165374673
- PDBe Ligand
- TIQ
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- Wikipedia
- Ticagrelor
- PDB Entries
- 5alb / 5alc
- FDA label
- Download (1.21 MB)
Clinical Trials
- Clinical Trials
Phase Status Purpose Conditions Count 4 Active Not Recruiting Prevention Acute Coronary Syndrome (ACS) 1 4 Active Not Recruiting Treatment Acute Coronary Syndrome (ACS) 1 4 Completed Basic Science Acute Coronary Syndrome (ACS) / Atrial Fibrillation 1 4 Completed Basic Science Coronary Artery Disease (CAD) 1 4 Completed Basic Science Coronary Artery Disease (CAD) / Endothelial Dysfunction / Myocardial Ischemia 1 4 Completed Basic Science Inflammation / Stenoses, Aortic / Thrombosis 1 4 Completed Basic Science Myocardial Infarction 1 4 Completed Basic Science Myocardial Infarction / Platelets Dysfunction / Thrombosis 1 4 Completed Other Acute Coronary Syndrome (ACS) 1 4 Completed Other Coronary Artery Disease (CAD) 1
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Tablet Oral 60 mg Tablet Oral 90 mg Tablet, film coated Oral Tablet, coated Oral 60 mg Tablet, orally disintegrating Oral 90 MG Tablet Oral 60 mg/1 Tablet Oral 90 mg/1 Tablet, film coated Oral 60 MG Tablet, film coated Oral 90 mg Tablet, coated Oral 90 mg - Prices
- Not Available
- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region CA2296665 No 2008-06-10 2018-07-15 Canada CA2351709 No 2010-04-06 2019-12-02 Canada CA2408596 No 2010-12-21 2021-05-31 Canada US7265124 No 2007-09-04 2021-07-09 US US6525060 No 2003-02-25 2019-12-02 US US7250419 No 2007-07-31 2019-12-02 US US6251910 No 2001-06-26 2018-07-15 US US8425934 Yes 2013-04-23 2030-10-17 US USRE46276 Yes 2017-01-17 2025-04-30 US US10300065 Yes 2019-05-28 2036-07-27 US
Properties
- State
- Solid
- Experimental Properties
Property Value Source water solubility 10 μg/mL FDA Label - Predicted Properties
Property Value Source Water Solubility 0.063 mg/mL ALOGPS logP 2.31 ALOGPS logP 2.28 Chemaxon logS -3.9 ALOGPS pKa (Strongest Acidic) 12.94 Chemaxon pKa (Strongest Basic) 1.11 Chemaxon Physiological Charge 0 Chemaxon Hydrogen Acceptor Count 9 Chemaxon Hydrogen Donor Count 4 Chemaxon Polar Surface Area 138.44 Å2 Chemaxon Rotatable Bond Count 10 Chemaxon Refractivity 142.13 m3·mol-1 Chemaxon Polarizability 51.31 Å3 Chemaxon Number of Rings 5 Chemaxon Bioavailability 1 Chemaxon Rule of Five No Chemaxon Ghose Filter No Chemaxon Veber's Rule No Chemaxon MDDR-like Rule Yes Chemaxon - Predicted ADMET Features
Property Value Probability Human Intestinal Absorption + 0.994 Blood Brain Barrier - 0.6719 Caco-2 permeable - 0.5989 P-glycoprotein substrate Substrate 0.7626 P-glycoprotein inhibitor I Non-inhibitor 0.5907 P-glycoprotein inhibitor II Non-inhibitor 0.9617 Renal organic cation transporter Non-inhibitor 0.8606 CYP450 2C9 substrate Non-substrate 0.7734 CYP450 2D6 substrate Non-substrate 0.8048 CYP450 3A4 substrate Substrate 0.5057 CYP450 1A2 substrate Non-inhibitor 0.5372 CYP450 2C9 inhibitor Non-inhibitor 0.5767 CYP450 2D6 inhibitor Non-inhibitor 0.8016 CYP450 2C19 inhibitor Non-inhibitor 0.6016 CYP450 3A4 inhibitor Inhibitor 0.8744 CYP450 inhibitory promiscuity High CYP Inhibitory Promiscuity 0.6243 Ames test Non AMES toxic 0.5075 Carcinogenicity Non-carcinogens 0.7777 Biodegradation Not ready biodegradable 1.0 Rat acute toxicity 2.6308 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.7742 hERG inhibition (predictor II) Non-inhibitor 0.5914
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
Spectrum Spectrum Type Splash Key Predicted GC-MS Spectrum - GC-MS Predicted GC-MS Not Available Predicted MS/MS Spectrum - 10V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 20V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 40V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 10V, Negative (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 20V, Negative (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 40V, Negative (Annotated) Predicted LC-MS/MS Not Available
Targets
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- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Inhibitor
- General Function
- Guanyl-nucleotide exchange factor activity
- Specific Function
- Receptor for ADP and ATP coupled to G-proteins that inhibit the adenylyl cyclase second messenger system. Not activated by UDP and UTP. Required for normal platelet aggregation and blood coagulation.
- Gene Name
- P2RY12
- Uniprot ID
- Q9H244
- Uniprot Name
- P2Y purinoceptor 12
- Molecular Weight
- 39438.355 Da
References
- Teng R: Ticagrelor: Pharmacokinetic, Pharmacodynamic and Pharmacogenetic Profile: An Update. Clin Pharmacokinet. 2015 Nov;54(11):1125-38. doi: 10.1007/s40262-015-0290-2. [Article]
- Bhatt DL, Pollack CV, Weitz JI, Jennings LK, Xu S, Arnold SE, Umstead BR, Mays MC, Lee JS: Antibody-Based Ticagrelor Reversal Agent in Healthy Volunteers. N Engl J Med. 2019 May 9;380(19):1825-1833. doi: 10.1056/NEJMoa1901778. Epub 2019 Mar 17. [Article]
Enzymes
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- SubstrateInhibitor
- 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
References
- Teng R, Oliver S, Hayes MA, Butler K: Absorption, distribution, metabolism, and excretion of ticagrelor in healthy subjects. Drug Metab Dispos. 2010 Sep;38(9):1514-21. doi: 10.1124/dmd.110.032250. Epub 2010 Jun 15. [Article]
- FDA Approved Drug Products: BRILINTA (ticagrelor) tablets, for oral use [Link]
- Flockhart Table of Drug Interactions [Link]
- FDA Drug Development and Drug Interactions: Table of Substrates, Inhibitors and Inducers [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- SubstrateActivator
- General Function
- Oxygen binding
- 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 oxidizes a variety of structurally un...
- Gene Name
- CYP3A5
- Uniprot ID
- P20815
- Uniprot Name
- Cytochrome P450 3A5
- Molecular Weight
- 57108.065 Da
References
- Adamski P, Buszko K, Sikora J, Niezgoda P, Baranska M, Ostrowska M, Paciorek P, Navarese EP, Gorog DA, Kubica J: Metabolism of ticagrelor in patients with acute coronary syndromes. Sci Rep. 2018 Aug 6;8(1):11746. doi: 10.1038/s41598-018-29619-9. [Article]
- Flockhart Table of Drug Interactions [Link]
- FDA Approved Drug Products: BRILINTA (ticagrelor) tablets, for oral use [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inducer
- General Function
- Steroid 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 oxidizes a variety of structurally un...
- Gene Name
- CYP2B6
- Uniprot ID
- P20813
- Uniprot Name
- Cytochrome P450 2B6
- Molecular Weight
- 56277.81 Da
References
- Zhou D, Andersson TB, Grimm SW: In vitro evaluation of potential drug-drug interactions with ticagrelor: cytochrome P450 reaction phenotyping, inhibition, induction, and differential kinetics. Drug Metab Dispos. 2011 Apr;39(4):703-10. doi: 10.1124/dmd.110.037143. Epub 2010 Dec 22. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- InhibitorInducer
- General Function
- Steroid 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 oxidizes a variety of structurally un...
- Gene Name
- CYP2C9
- Uniprot ID
- P11712
- Uniprot Name
- Cytochrome P450 2C9
- Molecular Weight
- 55627.365 Da
References
- Zhou D, Andersson TB, Grimm SW: In vitro evaluation of potential drug-drug interactions with ticagrelor: cytochrome P450 reaction phenotyping, inhibition, induction, and differential kinetics. Drug Metab Dispos. 2011 Apr;39(4):703-10. doi: 10.1124/dmd.110.037143. Epub 2010 Dec 22. [Article]
- Teng R: Ticagrelor: Pharmacokinetic, Pharmacodynamic and Pharmacogenetic Profile: An Update. Clin Pharmacokinet. 2015 Nov;54(11):1125-38. doi: 10.1007/s40262-015-0290-2. [Article]
Carriers
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Binder
- General Function
- Toxic substance binding
- Specific Function
- Serum albumin, the main protein of plasma, has a good binding capacity for water, Ca(2+), Na(+), K(+), fatty acids, hormones, bilirubin and drugs. Its main function is the regulation of the colloid...
- Gene Name
- ALB
- Uniprot ID
- P02768
- Uniprot Name
- Serum albumin
- Molecular Weight
- 69365.94 Da
References
- Angheloiu GO, Gugiu GB, Ruse C, Pandey R, Dasari RR, Whatling C: Ticagrelor Removal From Human Blood. JACC Basic Transl Sci. 2017 Apr 24;2(2):135-145. doi: 10.1016/j.jacbts.2017.01.007. eCollection 2017 Apr. [Article]
Transporters
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- SubstrateInhibitor
- 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
References
Drug created at August 01, 2011 21:32 / Updated at March 22, 2023 23:54