Ticagrelor

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

3D
MOL SDF 3D-SDF PDB SMILES InChI

Similar Structures

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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Associated Conditions

Cardiovascular Mortality

Cerebrovascular Accident

Myocardial Infarction

Thrombosis (Stent Thrombosis)

Contraindications & Blackbox Warnings

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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 Gα_i2 and other G_i proteins which inhibit adenylyl cyclase.³ G_i 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
inhibitor
Humans

Absorption

Target	Actions	Organism
AP2Y purinoceptor 12	inhibitor	Humans

Ticagrelor is 36% orally bioavailable.⁶ A single 200mg oral dose of ticagrelor reaches a C_max of 923ng/mL, with a T_max of 1.5 hours and an AUC of 6675ng*h/mL.¹ The active metabolite of ticagrelor reaches a C_max of 264ng/mL, with a T_max 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
Ticagrelor

AR-C124910XX

AR-C133913XX

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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Toxicity

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
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Abametapir	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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Food Interactions

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

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Product Images

International/Other Brands

Brilinta / Possia (AstraZeneca)

Brand Name Prescription Products

Name	Dosage	Strength	Route	Labeller	Marketing Start	Marketing End
Brilinta	Tablet	60 mg/1	Oral	AstraZeneca Pharmaceuticals LP	2015-09-04	Not applicable
Brilinta	Tablet	60 mg	Oral	Astra Zeneca	2016-06-13	Not applicable
Brilinta	Tablet	90 mg/1	Oral	AstraZeneca Pharmaceuticals LP	2011-08-05	Not applicable
Brilinta	Tablet	90 mg	Oral	Astra Zeneca	2011-06-01	Not applicable
Brilinta	Tablet	90 mg/1	Oral	bryant ranch prepack	2011-08-05	2016-04-30
Brilinta	Tablet	90 mg/1	Oral	Cardinal Health 107, LLC	2011-08-05	Not applicable
Brilique	Tablet, film coated	90 mg	Oral	Astra Zeneca Ab	2016-09-07	Not applicable
Brilique	Tablet, film coated	90 mg	Oral	Astra Zeneca Ab	2016-09-07	Not applicable
Brilique	Tablet, orally disintegrating	90 mg	Oral	Astra Zeneca Ab	2020-12-16	Not applicable
Brilique	Tablet, film coated	60 mg	Oral	Astra Zeneca Ab	2016-09-07	Not applicable

Generic Prescription Products

Name	Dosage	Strength	Route	Labeller	Marketing Start	Marketing End
Apo-ticagrelor	Tablet	90 mg	Oral	Apotex Corporation	Not applicable	Not applicable
Apo-ticagrelor	Tablet	60 mg	Oral	Apotex Corporation	Not applicable	Not applicable
Na	Tablet	60 mg/1	Oral	Sunshine Lake Pharma Co., Ltd.	2020-04-09	2020-04-10
Na	Tablet	90 mg/1	Oral	Sunshine Lake Pharma Co., Ltd.	2020-04-09	2020-04-10
Taro-ticagrelor	Tablet	90 mg	Oral	Taro Pharmaceuticals, Inc.	Not applicable	Not applicable
Taro-ticagrelor	Tablet	60 mg	Oral	Taro Pharmaceuticals, Inc.	Not applicable	Not applicable
Teva-ticagrelor	Tablet	90 mg	Oral	TEVA Canada Limited	Not applicable	Not applicable
Teva-ticagrelor	Tablet	60 mg	Oral	TEVA Canada Limited	Not applicable	Not applicable
Ticagrelor	Tablet	90 mg/1	Oral	Amneal Pharmaceuticals NY LLC	2019-01-23	Not applicable

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
RxNav: 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	Diseased Saphenous Vein Grafts	1
4	Active Not Recruiting	Treatment	Acute Coronary Syndrome (ACS)	2
4	Active Not Recruiting	Treatment	Non ST Segment Elevation Myocardial Infarction (NSTEMI) / Non-STEMI Acute Coronary Syndrome / Unstable Angina Pectoris	1
4	Active Not Recruiting	Treatment	Percutaneous Coronary Intervention (PCI)	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	Myocardial Infarction	1
4	Completed	Other	Acute Coronary Syndrome (ACS)	1
4	Completed	Other	Healthy Subjects (HS)	1

Pharmacoeconomics

Manufacturers

Not Available

Packagers

Not Available

Dosage Forms

Form	Route	Strength
Tablet, film coated	Oral	60 mg
Tablet, film coated	Oral	90 mg
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, coated	Oral	90 mg

Prices

Not Available

Patents

Patent Number	Pediatric Extension	Approved	Expires (estimated)
CA2296665	No	2008-06-10	2018-07-15
CA2351709	No	2010-04-06	2019-12-02
CA2408596	No	2010-12-21	2021-05-31
US7265124	No	2007-09-04	2021-07-09
US6525060	No	2003-02-25	2019-12-02
US7250419	No	2007-07-31	2019-12-02
US6251910	No	2001-06-26	2018-07-15
US8425934	No	2013-04-23	2030-04-17
USRE46276	No	2017-01-17	2019-12-02
US10300065	No	2019-05-28	2036-01-27

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

ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

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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Details1. P2Y purinoceptor 12
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]

Property	Measurement	pH	Temperature (°C)	References
Ki (nM)	14	N/A	N/A	A31139

Enzymes

Details1. Cytochrome P450 3A4

Kind: Protein
Organism: Humans
Pharmacological action: Unknown
Actions: Substrate
Inhibitor

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]

Details2. Cytochrome P450 3A5

Kind: Protein
Organism: Humans
Pharmacological action: Unknown
Actions: Substrate
Activator

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]

Details3. Cytochrome P450 2B6

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]

Details4. Cytochrome P450 2C9

Kind: Protein
Organism: Humans
Pharmacological action: Unknown
Actions: Inhibitor
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: 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

Details1. Serum albumin

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

Details1. P-glycoprotein 1

Kind: Protein
Organism: Humans
Pharmacological action: Unknown
Actions: Substrate
Inhibitor

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

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]
FDA Approved Drug Products: BRILINTA (ticagrelor) tablets, for oral use [Link]

Drug created at August 01, 2011 21:32 / Updated at May 19, 2022 18:09

Ticagrelor

Identification

Structure for Ticagrelor (DB08816)

Pharmacology

Interactions

Products

Categories

Chemical Identifiers

References

Clinical Trials

Pharmacoeconomics

Properties

Spectra

Targets

References

Enzymes

References

References

References

References

Carriers

References

Transporters

References