Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C23H28F2N6O4S |
Molecular Weight | 522.568 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 6 / 6 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CCCSC1=NC(N[C@@H]2C[C@H]2C3=CC(F)=C(F)C=C3)=C4N=NN([C@@H]5C[C@H](OCCO)[C@@H](O)[C@H]5O)C4=N1
InChI
InChIKey=OEKWJQXRCDYSHL-FNOIDJSQSA-N
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
Molecular Formula | C23H28F2N6O4S |
Molecular Weight | 522.568 |
Charge | 0 |
Count |
|
Stereochemistry | ABSOLUTE |
Additional Stereochemistry | No |
Defined Stereocenters | 6 / 6 |
E/Z Centers | 0 |
Optical Activity | UNSPECIFIED |
DescriptionCurator's Comment: description was created based on several sources, including http://www.ema.europa.eu/docs/en_GB/document_library/PIP_decision/WC500123240.pdf; http://www.ema.europa.eu/docs/en_GB/document_library/EPAR_-_Summary_for_the_public/human/002303/WC500100562.pdf; https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022433Orig1s000PharmR.pdf
Curator's Comment: description was created based on several sources, including http://www.ema.europa.eu/docs/en_GB/document_library/PIP_decision/WC500123240.pdf; http://www.ema.europa.eu/docs/en_GB/document_library/EPAR_-_Summary_for_the_public/human/002303/WC500100562.pdf; https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022433Orig1s000PharmR.pdf
Ticagrelor (known trade names Brilinta, Brilique and Possia) is a P2Y12 platelet inhibitor. Brilinta has been approved by the US Food and Drug administration (FDA) in 2011 and is indicated to reduce the rate of cardiovascular death, myocardial infarction, and stroke in patients with acute coronary syndrome (ACS) or a history of myocardial infarction. Brilinta also reduces the rate of stent thrombosis in patients who have been stented for treatment of ACS. Ticagrelor and its major metabolite reversibly interact with the platelet P2Y12 ADP-receptor to prevent signal transduction and platelet activation. Ticagrelor and its active metabolite are approximately equipotent. In vitro metabolism studies demonstrate that ticagrelor and its major active metabolite are weak inhibitors of CYP3A4, potential activators of CYP3A5 and inhibitors of the P-gp transporter. Most common adverse reactions are bleeding 12% and dyspnea 14%.
Originator
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL2001 |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Secondary | BRILINTA Approved UseIndicated to reduce the rate of cardiovascular death, myocardial infarction, and stroke in patients with acute coronary syndrome (ACS) or a history of myocardial infarction (MI). For at least the first 12 months following ACS, it is superior to clopidogrel. Reduces the rate of stent thrombosis in patients who have been stented for treatment of ACS. Launch Date2011 |
|||
Secondary | BRILINTA Approved UseIndicated to reduce the rate of cardiovascular death, myocardial infarction, and stroke in patients with acute coronary syndrome (ACS) or a history of myocardial infarction (MI). For at least the first 12 months following ACS, it is superior to clopidogrel. Reduces the rate of stent thrombosis in patients who have been stented for treatment of ACS. Launch Date2011 |
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
1208 ng/mL Clinical Trial https://clinicaltrials.gov/ct2/show/NCT01898442 |
270 mg single, oral dose: 270 mg route of administration: oral experiment type: single co-administered: |
TICAGRELOR plasma | Homo sapiens |
|
1208 ng/mL Clinical Trial https://clinicaltrials.gov/ct2/show/NCT01898442 |
360 mg single, oral dose: 360 mg route of administration: oral experiment type: single co-administered: |
TICAGRELOR plasma | Homo sapiens |
|
1583 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/20642549/ |
200 mg 2 times / day multiple, oral dose: 200 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
TICAGRELOR plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
AUC
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
12379 ng*h/mL Clinical Trial https://clinicaltrials.gov/ct2/show/NCT01898442 |
270 mg single, oral dose: 270 mg route of administration: oral experiment type: single co-administered: |
TICAGRELOR plasma | Homo sapiens |
|
12381 ng*h/mL Clinical Trial https://clinicaltrials.gov/ct2/show/NCT01898442 |
360 mg single, oral dose: 360 mg route of administration: oral experiment type: single co-administered: |
TICAGRELOR plasma | Homo sapiens |
|
10160 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/20642549/ |
200 mg 2 times / day multiple, oral dose: 200 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
TICAGRELOR plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
T1/2
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
7 h |
90 mg single, oral dose: 90 mg route of administration: Oral experiment type: SINGLE co-administered: |
TICAGRELOR plasma | Homo sapiens population: UNKNOWN age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
Funbound
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
1% |
90 mg single, oral dose: 90 mg route of administration: Oral experiment type: SINGLE co-administered: |
TICAGRELOR plasma | Homo sapiens population: UNKNOWN age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
Doses
Dose | Population | Adverse events |
---|---|---|
1260 mg single, oral Highest studied dose Dose: 1260 mg Route: oral Route: single Dose: 1260 mg Sources: |
healthy |
DLT: Gastrointestinal disorder NOS, Sinus arrest... Dose limiting toxicities: Gastrointestinal disorder NOS (50%) Sources: Sinus arrest (serious, 16.7%) High grade atrioventricular block (serious, 16.7%) Ventricular escape rhythm (serious, 16.7%) |
900 mg single, oral MTD |
healthy |
|
90 mg 2 times / day multiple, oral Recommended Dose: 90 mg, 2 times / day Route: oral Route: multiple Dose: 90 mg, 2 times / day Sources: |
unhealthy Health Status: unhealthy Sex: M+F Sources: |
Disc. AE: Dyspnea... AEs leading to discontinuation/dose reduction: Dyspnea (0.9%) Sources: |
90 mg 2 times / day multiple, oral Recommended Dose: 90 mg, 2 times / day Route: oral Route: multiple Dose: 90 mg, 2 times / day Sources: |
unhealthy Health Status: unhealthy Sources: |
Disc. AE: Bleeding... AEs leading to discontinuation/dose reduction: Bleeding (grade 3-5) Sources: |
AEs
AE | Significance | Dose | Population |
---|---|---|---|
Gastrointestinal disorder NOS | 50% DLT |
1260 mg single, oral Highest studied dose Dose: 1260 mg Route: oral Route: single Dose: 1260 mg Sources: |
healthy |
High grade atrioventricular block | serious, 16.7% DLT |
1260 mg single, oral Highest studied dose Dose: 1260 mg Route: oral Route: single Dose: 1260 mg Sources: |
healthy |
Sinus arrest | serious, 16.7% DLT |
1260 mg single, oral Highest studied dose Dose: 1260 mg Route: oral Route: single Dose: 1260 mg Sources: |
healthy |
Ventricular escape rhythm | serious, 16.7% DLT |
1260 mg single, oral Highest studied dose Dose: 1260 mg Route: oral Route: single Dose: 1260 mg Sources: |
healthy |
Dyspnea | 0.9% Disc. AE |
90 mg 2 times / day multiple, oral Recommended Dose: 90 mg, 2 times / day Route: oral Route: multiple Dose: 90 mg, 2 times / day Sources: |
unhealthy Health Status: unhealthy Sex: M+F Sources: |
Bleeding | grade 3-5 Disc. AE |
90 mg 2 times / day multiple, oral Recommended Dose: 90 mg, 2 times / day Route: oral Route: multiple Dose: 90 mg, 2 times / day Sources: |
unhealthy Health Status: unhealthy Sources: |
Overview
OverviewOther
Drug as perpetrator
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022433Orig1s000ClinPharmR.pdf#page=13 Page: 13.0 |
likely | |||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022433Orig1s000ClinPharmR.pdf#page=13 Page: 13.0 |
likely | |||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022433Orig1s000ClinPharmR.pdf#page=12 Page: 12-13 |
likely | |||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022433Orig1s000ClinPharmR.pdf#page=12 Page: 12-13 |
likely | |||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022433Orig1s000ClinPharmR.pdf#page=9, Page: 9-11 |
moderate [IC50 10.5 uM] | |||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022433Orig1s000ClinPharmR.pdf#page=9, Page: 9-11 |
moderate [IC50 11.7 uM] | |||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022433Orig1s000ClinPharmR.pdf#page=9, Page: 9-11 |
moderate [IC50 26.7 uM] | |||
moderate [IC50 33 uM] | ||||
moderate [IC50 43 uM] | ||||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022433Orig1s000ClinPharmR.pdf#page=9, Page: 9-11 |
moderate [IC50 6.9 uM] | no (co-administration study) Comment: Human liver microsomes, dicrofenac (substrate); Co-administration of ticagrelor (180 mg BID x 9 days) did not alter the systemic exposure of tolbutamide (500 mg QD on Day 5, CYP2C9 substrate) (GM ratio of AUCinf and Cmax were 103%, 110%, while 4-OH tolbutamide AUCinf GM ratio and Cmax GM ratio were 94% and 90%). Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022433Orig1s000ClinPharmR.pdf#page=9, Page: 9-11 |
||
moderate [IC50 7.6 uM] | ||||
Page: 9-12, 60-61, 66-67, (PMDA) 130 |
moderate [IC50 8.2 uM] | yes (co-administration study) Comment: Human liver microsomes, midazolam (4-hydroxylation, substrate), no time-dependent inhibition; Co-administration of ticagrelor (270 mg AM + 180 mg PM on Day1, 180 mg BID on Days 2-7) significantly increased simvastatin (80 mg on Day 5, CYP3A4/5 substrate) AUCinf by 56% and Cmax 81%, and simvastatin acid AUCinf by 52% and Cmax by 64%. Co-administration of ticagrelor (270 mg AM + 180 mg PM on Day1, 180 mg BID on Days 2-7) significantly reduced oral midazolam (7.5 mg AM on Days 1 & 7) AUCinf by 10%, and 4’-OH-midazolam by 42%. Co-administration of ticagrelor (270 mg AM + 180 mg PM on Day 1, 180 mg BID on Days 2-7) does not alter the systemic exposure of IV midazolam (2.5 mg IV over 2 min AM on Days 1 & 7) and significantly reduced 4’-OH- midazolam systemic exposure by ~ 23%. Page: 9-12, 60-61, 66-67, (PMDA) 130 |
||
no [IC50 40 uM] | ||||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022433Orig1s000ClinPharmR.pdf#page=9, Page: 9-11 |
no [IC50 >50 uM] | |||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022433Orig1s000ClinPharmR.pdf#page=9, Page: 9-11 |
no [IC50 >50 uM] | |||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022433Orig1s000ClinPharmR.pdf#page=9, Page: 9-11 |
no [IC50 >50 uM] | |||
no [IC50 >50 uM] | ||||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022433Orig1s000ClinPharmR.pdf#page=9, Page: 9-11 |
no [IC50 >50 uM] | |||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022433Orig1s000ClinPharmR.pdf#page=9, Page: 9-11 |
no [IC50 >50 uM] | |||
Page: 9-12, 62-63, 64-65, 66-67 (PMDA) 124-125, 130 |
no [IC50 >50 uM] | weak (co-administration study) Comment: Human liver microsomes, midazolam (1-hydroxylation, substrate), midazolam 1-hydroxylation was activated in the presence of Cyt-b5 by 144.9% (CYP3A4 (cDNA expressed enzyme):Cyp-b5 = 1: 3 + 5.56 mcM ticagrelor), no time-dependent inhibition; Inhibited testosterone intrinsic clearance (IC50 = 23 mcM, pooled human liver microsomes (33 male and female donors); Co-administration of ticagrelor (270 mg AM + 90 mg PM on Day 1, 90 mg BID on Days 2-7) significantly increased atorvastatin (80 mg QD on Day 5) AUCinf 36% and Cmax 23%, atorvastatin lactone AUCinf 32% and Cmax 39%, s 2-OH atorvastatin AUCinf 33% and Cmax 13%, and 4-OH atorvastatin AUCinf 67% and Cmax 55%. Co-administration of ticagrelor (90 mg BID x 21 days) significantly increased ethinyl estradiol AUCinf, Cmax, and Cmin by 20%, 30.6%, and 20.2%, respectively. Co-administration of ticagrelor does not alter the systemic exposure of levonorgestrel. Co-administration of ticagrelor (270 mg AM + 180 mg PM on Day1, 180 mg BID on Days 2-7) significantly reduced oral midazolam (7.5 mg AM on Days 1 & 7) AUCinf by 10%, but did not alter 1’-OH- midazolam AUC. Co-administration of ticagrelor (270 mg AM + 180 mg PM on Day 1, 180 mg BID on Days 2-7) did not alter the systemic exposure of IV midazolam (2.5 mg IV over 2 min AM on Days 1 & 7) and 1’-OH-midazolam. Page: 9-12, 62-63, 64-65, 66-67 (PMDA) 124-125, 130 |
||
no | ||||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022433Orig1s000ClinPharmR.pdf#page=12 Page: 12-13 |
no | |||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022433Orig1s000ClinPharmR.pdf#page=12 Page: 12-13 |
no | |||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022433Orig1s000ClinPharmR.pdf#page=12 Page: 12-13 |
no | |||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022433Orig1s000ClinPharmR.pdf#page=12 Page: 12-13 |
no | |||
no | ||||
Sources: https://www.pmda.go.jp/drugs/2016/P20161026001/670227000_22800AMX00680_I100_1.pdf#page=160 Page: (PMDA) 160-161 |
no | |||
Sources: https://www.pmda.go.jp/drugs/2016/P20161026001/670227000_22800AMX00680_I100_1.pdf#page=160 Page: (PMDA) 160-161 |
no | |||
Sources: https://www.pmda.go.jp/drugs/2016/P20161026001/670227000_22800AMX00680_I100_1.pdf#page=160 Page: (PMDA) 160-161 |
strong [Ki 13.4 uM] | |||
Sources: https://www.pmda.go.jp/drugs/2016/P20161026001/670227000_22800AMX00680_I100_1.pdf#page=160 Page: (PMDA) 160-161 |
strong [Ki 16.3 uM] | |||
Sources: https://www.pmda.go.jp/drugs/2016/P20161026001/670227000_22800AMX00680_I100_1.pdf#page=160 Page: (PMDA) 160-161 |
strong [Ki 4.9 uM] | |||
Sources: https://www.pmda.go.jp/drugs/2016/P20161026001/670227000_22800AMX00680_I100_1.pdf#page=160 Page: (PMDA) 160-161 |
strong | |||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022433Orig1s000PharmR.pdf#page=116 Page: 116.0 |
weak | |||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022433Orig1s000PharmR.pdf#page=116 Page: 116.0 |
weak | |||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022433Orig1s000PharmR.pdf#page=117 Page: 26, 117 |
yes [IC50 0.759 uM] | |||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022433Orig1s000PharmR.pdf#page=117 Page: 26, 117 |
yes [IC50 1 uM] | |||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022433Orig1s000PharmR.pdf#page=117 Page: 117.0 |
yes [IC50 10 uM] | |||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022433Orig1s000PharmR.pdf#page=117 Page: 117.0 |
yes [IC50 16.9 uM] | |||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022433Orig1s000PharmR.pdf#page=117 Page: 117.0 |
yes [IC50 19.2 uM] | |||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022433Orig1s000PharmR.pdf#page=117 Page: 117.0 |
yes [IC50 19.9 uM] | |||
Page: 4-5, 58-59 (PMDA) 157 |
yes [IC50 7.8 uM] | yes (co-administration study) Comment: MDR1-MDCK monolayer, H3-digoxin (5 mcM) as a substrate, Flux ratio = 19.5 (digoxin only), 3.1 (digoxin + 10 mcM Ticagrelor); Co-administration of ticagrelor (400 mg QD, Days 1-16) significantly increased digoxin (0.25 mg BID on Day 6, 0.25 mg QD on Days 7-14, P-gp substrate) AUC0-72, Css,max, and Css, min by 28%, 75% and 31%, respectively. Page: 4-5, 58-59 (PMDA) 157 |
||
yes [IC50 9.9 uM] |
Drug as victim
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
Page: 123, (ClinPharm) 5-6, 43-44, 45-47, 47-49 |
major [Km 11 uM] | yes (co-administration study) Comment: Human liver microsomes (determination of CYPs) and human cDNA expressed emzymes (Km for AR-C124910XX formation), Km (AR-C124910XX, human liver microsomes) = 27 mcM; Km (AR-C133913XX formation) = 41 mcM; Co-administration of ketoconazole (200 mg BID for 10 days, CYP3A4 inhibitor) significantly increased ticagrelor (90 mg QD on Day 4) AUCinf by 7.32 fold and Cmax by 2.35 fold, and decreased AR-C124910XX AUCinf by 56% and Cmax by 89%. Co-administration of diltiazem (240 mg QD x 14 days, moderate CYP3A4 inhibitor) significantly increased ticagrelor (90 mg QD on Day 8) AUCinf by 2.74 fold and Cmax by 1.69, and decreased AR-C124910XX AUCinf by 13% and Cmax by 38%. Co-administration of rifampin (600 mg QD Days 4-17, strong CYP3A4/P-gp inducer) significantly decreased ticagrelor (180 mg QD Days 1 & 15) AUCinf by 86% and Cmax by 73%, and decreased AR-C124910XX AUCinf by 46% and did not affect Cmax. Page: 123, (ClinPharm) 5-6, 43-44, 45-47, 47-49 |
||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
yes [Km 5.36 uM] | ||||
yes | ||||
yes |
Tox targets
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022433Orig1s000PharmR.pdf#page=117 Page: 117.0 |
||||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022433Orig1s000PharmR.pdf#page=117 Page: 117.0 |
||||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022433Orig1s000PharmR.pdf#page=117 Page: 117.0 |
||||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022433Orig1s000PharmR.pdf#page=117 Page: 117.0 |
||||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022433Orig1s000PharmR.pdf#page=119 Page: 119.0 |
PubMed
Title | Date | PubMed |
---|---|---|
Dyspnoea after AZD6140: safety first? | 2006 Jun |
|
P2Y12 receptor antagonists: a rapidly expanding group of antiplatelet agents. | 2006 May |
|
Aspirin and clopidogrel resistance: consideration and management. | 2006 Oct |
|
Platelet P2 receptors: old and new targets for antithrombotic drugs. | 2007 Jan |
|
Molecule of the month. Ticagrelor. | 2007 May |
|
Dyspnoea and antiplatelet agents: revisited. | 2007 Sep |
|
Optimizing platelet P2Y12 inhibition for patients undergoing PCI. | 2007 Summer |
|
Clinical overview of promising nonthienopyridine antiplatelet agents. | 2008 Aug |
|
Pharmacology of emerging novel platelet inhibitors. | 2008 Aug |
|
Platelet ADP-receptor antagonists for cardiovascular disease: past, present and future. | 2008 Dec |
|
Antiplatelet therapy in acute coronary syndromes. | 2008 Jul |
|
Gateways to clinical trials. | 2008 Mar |
|
Investigational antiplatelet drugs for the treatment and prevention of coronary artery disease. | 2008 Sep-Oct |
|
P2Y(12) inhibitors: differences in properties and mechanisms of action and potential consequences for clinical use. | 2009 Aug |
|
Oral antiplatelet therapy for acute and chronic management of NSTE ACS: residual ischemic risk and opportunities for improvement. | 2009 Dec |
|
Ticagrelor versus clopidogrel in acute coronary syndromes. | 2009 Dec 10 |
|
Ticagrelor versus clopidogrel in acute coronary syndromes. | 2009 Dec 10 |
|
Ticagrelor versus clopidogrel in acute coronary syndromes. | 2009 Dec 10 |
|
Ticagrelor versus clopidogrel in acute coronary syndromes. | 2009 Dec 10 |
|
ACP Journal Club. Ticagrelor was more effective than clopidogrel, with no increase in major bleeding in acute coronary syndromes. | 2009 Dec 15 |
|
Current problems, new opportunities and future directions of anti-platelet therapy - increasing role of novel antiplatelet agents in cardiovascular diseases. | 2009 Jan |
|
New P2Y12 blockers. | 2009 Jul |
|
Effect of blocking platelet activation with AZD6140 on development of abdominal aortic aneurysm in a rat aneurysmal model. | 2009 Mar |
|
Update on oral antiplatelet therapy: principles, problems and promises. | 2009 May |
|
HOTLINE I, PLATO favours ticagrelor over clopidogrel in ACS. | 2009 Nov |
|
P2Y12 inhibitors: thienopyridines and direct oral inhibitors. | 2009 Nov |
|
European Society of Cardiology--2009 annual congress. 31 August - 2 September 2009, Barcelona, Spain. | 2009 Nov |
|
Ticagrelor binds to human P2Y(12) independently from ADP but antagonizes ADP-induced receptor signaling and platelet aggregation. | 2009 Sep |
|
Ticagrelor--is there need for a new player in the antiplatelet-therapy field? | 2009 Sep 10 |
|
Novel antiplatelet agents in development: prasugrel, ticagrelor, and cangrelor and beyond. | 2009 Sep-Oct |
|
Ticagrelor: the first reversibly binding oral P2Y12 receptor antagonist. | 2009 Winter |
|
The PLATO trial: do you believe in magic? | 2010 Apr |
|
Balancing the benefits and risks of antiplatelet agents in patients with non-ST-segment elevated acute coronary syndromes and undergoing percutaneous coronary intervention. | 2010 Aug |
|
Limitations of current therapies to prevent thrombosis: a need for novel strategies. | 2010 Feb |
|
The TRITON versus PLATO trials: differences beyond platelet inhibition. | 2010 Feb |
|
Pharmacokinetic, pharmacodynamic and clinical profile of novel antiplatelet drugs targeting vascular diseases. | 2010 Feb 1 |
|
Recent advances in cardiology. | 2010 Jan |
|
Comparison of ticagrelor with clopidogrel in patients with a planned invasive strategy for acute coronary syndromes (PLATO): a randomised double-blind study. | 2010 Jan 23 |
|
PLATO study of ticagrelor versus clopidogrel in patients with high-risk acute coronary syndromes. | 2010 Jul |
|
The case for routine genotyping in dual-antiplatelet therapy. | 2010 Jul 6 |
|
The novel P2Y 12 antagonist AZD6140 rapidly and reversibly reduces platelet activation in diabetic rats. | 2010 Mar |
|
Advances in antiplatelet treatment for acute coronary syndromes. | 2010 May |
|
Forecasting drug utilization and expenditure in a metropolitan health region. | 2010 May 17 |
Patents
Sample Use Guides
Initiate treatment with 180 mg (two 90 mg tablets) oral loading dose. Continue treatment with 90 mg twice daily.
Route of Administration:
Oral
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/?term=21177984
In human liver microsomes, ticagrelor inhibited midazolam 4-hydroxylation with an IC50 of 8.2 uM. Evaluated in fresh human hepatocytes at concentration up to 20 uM, ticagrelor was not an inducer of CYP1A2 or CYP3A4.
Substance Class |
Chemical
Created
by
admin
on
Edited
Mon Mar 31 18:18:18 GMT 2025
by
admin
on
Mon Mar 31 18:18:18 GMT 2025
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Record UNII |
GLH0314RVC
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Record Status |
Validated (UNII)
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Record Version |
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Code | English | ||
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Brand Name | English | ||
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Classification Tree | Code System | Code | ||
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EMA ASSESSMENT REPORTS |
POSSIA (WITHDRAWN: PERIPHERAL VASCULAR DISEASES)
Created by
admin on Mon Mar 31 18:18:18 GMT 2025 , Edited by admin on Mon Mar 31 18:18:18 GMT 2025
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EMA ASSESSMENT REPORTS |
BRILIQUE (AUTHORIZED: PERIPHERAL VASCULAR DISEASES)
Created by
admin on Mon Mar 31 18:18:18 GMT 2025 , Edited by admin on Mon Mar 31 18:18:18 GMT 2025
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WHO-ATC |
B01AC24
Created by
admin on Mon Mar 31 18:18:18 GMT 2025 , Edited by admin on Mon Mar 31 18:18:18 GMT 2025
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EMA ASSESSMENT REPORTS |
POSSIA (WITHDRAWN: ACUTE CORONARY SYNDROME)
Created by
admin on Mon Mar 31 18:18:18 GMT 2025 , Edited by admin on Mon Mar 31 18:18:18 GMT 2025
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WHO-VATC |
QB01AC24
Created by
admin on Mon Mar 31 18:18:18 GMT 2025 , Edited by admin on Mon Mar 31 18:18:18 GMT 2025
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NCI_THESAURUS |
C80483
Created by
admin on Mon Mar 31 18:18:18 GMT 2025 , Edited by admin on Mon Mar 31 18:18:18 GMT 2025
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NDF-RT |
N0000182142
Created by
admin on Mon Mar 31 18:18:18 GMT 2025 , Edited by admin on Mon Mar 31 18:18:18 GMT 2025
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EMA ASSESSMENT REPORTS |
BRILIQUE (AUTHORIZED:ACUTE CORONARY SYNDROME)
Created by
admin on Mon Mar 31 18:18:18 GMT 2025 , Edited by admin on Mon Mar 31 18:18:18 GMT 2025
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LIVERTOX |
NBK548529
Created by
admin on Mon Mar 31 18:18:18 GMT 2025 , Edited by admin on Mon Mar 31 18:18:18 GMT 2025
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Code System | Code | Type | Description | ||
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m10853
Created by
admin on Mon Mar 31 18:18:18 GMT 2025 , Edited by admin on Mon Mar 31 18:18:18 GMT 2025
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PRIMARY | Merck Index | ||
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C76404
Created by
admin on Mon Mar 31 18:18:18 GMT 2025 , Edited by admin on Mon Mar 31 18:18:18 GMT 2025
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PRIMARY | |||
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1667177
Created by
admin on Mon Mar 31 18:18:18 GMT 2025 , Edited by admin on Mon Mar 31 18:18:18 GMT 2025
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PRIMARY | |||
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4184
Created by
admin on Mon Mar 31 18:18:18 GMT 2025 , Edited by admin on Mon Mar 31 18:18:18 GMT 2025
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PRIMARY | |||
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1116632
Created by
admin on Mon Mar 31 18:18:18 GMT 2025 , Edited by admin on Mon Mar 31 18:18:18 GMT 2025
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PRIMARY | RxNorm | ||
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C503700
Created by
admin on Mon Mar 31 18:18:18 GMT 2025 , Edited by admin on Mon Mar 31 18:18:18 GMT 2025
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PRIMARY | |||
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8772
Created by
admin on Mon Mar 31 18:18:18 GMT 2025 , Edited by admin on Mon Mar 31 18:18:18 GMT 2025
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PRIMARY | |||
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100000115464
Created by
admin on Mon Mar 31 18:18:18 GMT 2025 , Edited by admin on Mon Mar 31 18:18:18 GMT 2025
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PRIMARY | |||
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Ticagrelor
Created by
admin on Mon Mar 31 18:18:18 GMT 2025 , Edited by admin on Mon Mar 31 18:18:18 GMT 2025
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PRIMARY | |||
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274693-27-5
Created by
admin on Mon Mar 31 18:18:18 GMT 2025 , Edited by admin on Mon Mar 31 18:18:18 GMT 2025
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PRIMARY | |||
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N0000182141
Created by
admin on Mon Mar 31 18:18:18 GMT 2025 , Edited by admin on Mon Mar 31 18:18:18 GMT 2025
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PRIMARY | Cytochrome P450 3A4 Inhibitors [MoA] | ||
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DTXSID901009337
Created by
admin on Mon Mar 31 18:18:18 GMT 2025 , Edited by admin on Mon Mar 31 18:18:18 GMT 2025
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PRIMARY | |||
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CHEMBL398435
Created by
admin on Mon Mar 31 18:18:18 GMT 2025 , Edited by admin on Mon Mar 31 18:18:18 GMT 2025
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PRIMARY | |||
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N0000190482
Created by
admin on Mon Mar 31 18:18:18 GMT 2025 , Edited by admin on Mon Mar 31 18:18:18 GMT 2025
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PRIMARY | Phenylalanine Hydroxylase Activators [MoA] | ||
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9871419
Created by
admin on Mon Mar 31 18:18:18 GMT 2025 , Edited by admin on Mon Mar 31 18:18:18 GMT 2025
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PRIMARY | |||
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N0000185503
Created by
admin on Mon Mar 31 18:18:18 GMT 2025 , Edited by admin on Mon Mar 31 18:18:18 GMT 2025
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PRIMARY | P-Glycoprotein Inhibitors [MoA] | ||
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8306
Created by
admin on Mon Mar 31 18:18:18 GMT 2025 , Edited by admin on Mon Mar 31 18:18:18 GMT 2025
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PRIMARY | |||
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N0000182143
Created by
admin on Mon Mar 31 18:18:18 GMT 2025 , Edited by admin on Mon Mar 31 18:18:18 GMT 2025
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PRIMARY | P2Y12 Receptor Antagonists [MoA] | ||
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68558
Created by
admin on Mon Mar 31 18:18:18 GMT 2025 , Edited by admin on Mon Mar 31 18:18:18 GMT 2025
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PRIMARY | |||
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Ticagrelor
Created by
admin on Mon Mar 31 18:18:18 GMT 2025 , Edited by admin on Mon Mar 31 18:18:18 GMT 2025
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PRIMARY | |||
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DB08816
Created by
admin on Mon Mar 31 18:18:18 GMT 2025 , Edited by admin on Mon Mar 31 18:18:18 GMT 2025
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PRIMARY | |||
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TT-94
Created by
admin on Mon Mar 31 18:18:18 GMT 2025 , Edited by admin on Mon Mar 31 18:18:18 GMT 2025
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PRIMARY | |||
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SUB30898
Created by
admin on Mon Mar 31 18:18:18 GMT 2025 , Edited by admin on Mon Mar 31 18:18:18 GMT 2025
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PRIMARY | |||
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GLH0314RVC
Created by
admin on Mon Mar 31 18:18:18 GMT 2025 , Edited by admin on Mon Mar 31 18:18:18 GMT 2025
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PRIMARY | |||
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1765
Created by
admin on Mon Mar 31 18:18:18 GMT 2025 , Edited by admin on Mon Mar 31 18:18:18 GMT 2025
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PRIMARY | |||
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N0000190115
Created by
admin on Mon Mar 31 18:18:18 GMT 2025 , Edited by admin on Mon Mar 31 18:18:18 GMT 2025
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PRIMARY | Cytochrome P450 3A5 Inhibitors [MoA] | ||
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GLH0314RVC
Created by
admin on Mon Mar 31 18:18:18 GMT 2025 , Edited by admin on Mon Mar 31 18:18:18 GMT 2025
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PRIMARY |
Related Record | Type | Details | ||
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SALT/SOLVATE -> PARENT | |||
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METABOLIC ENZYME -> SUBSTRATE | |||
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INHIBITOR -> TARGET |
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METABOLIC ENZYME -> INHIBITOR |
WEAK
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BINDER->LIGAND |
BINDING
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SOLVATE->ANHYDROUS | |||
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TRANSPORTER -> INHIBITOR | |||
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TARGET -> INHIBITOR |
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TRANSPORTER -> SUBSTRATE |
Related Record | Type | Details | ||
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METABOLITE -> PARENT |
MAJOR
URINE
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Related Record | Type | Details | ||
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IMPURITY -> PARENT |
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Related Record | Type | Details | ||
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ACTIVE MOIETY |
Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
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Biological Half-life | PHARMACOKINETIC |
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Volume of Distribution | PHARMACOKINETIC |
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Tmax | PHARMACOKINETIC |
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