ticagrelor
Trade name: brilinta
Approved
Jul 20, 2011
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%. — NCATS
Clinical trial activity
407 trials · 305 clinical orgs · 19 marketing orgs
Earliest trial started Oct 1, 2006 (NCT00391872)
Timeline
2000s
- Jan 1, 2006
AstraZeneca — Earliest Phase 3 Sponsor(trial)
- Jan 1, 2007
AstraZeneca — Earliest Phase 1 Sponsor(trial)
- Jan 1, 2007
AstraZeneca — Earliest Phase 2 Sponsor(trial)
2010s
- Jul 20, 2011
AstraZeneca — Earliest FDA Approval
- Jul 20, 2011
AstraZeneca — Marketing Organization
- Jul 20, 2011
AstraZeneca — NDA Organization
- Sep 4, 2018
Watson Pharmaceuticals — Marketing Organization
- Sep 4, 2018
Allergan PLC (2015) — Marketing Organization
- Nov 6, 2018
Prinston Inc — Marketing Organization
- Nov 9, 2018
Alkem Labs Ltd — Marketing Organization
- Jan 23, 2019
Amneal Pharmaceuticals — Marketing Organization
- Jan 23, 2019
Zhejiang Hisun Pharmaceutical Co. Ltd. — Marketing Organization
2020s
- Apr 6, 2020
Sunshine Lake Pharma Co., Ltd. — Marketing Organization
- Apr 7, 2020
Sigmapharm Laboratories — Marketing Organization
- Apr 7, 2020
MSN Laboratories — Marketing Organization
- Oct 29, 2020
Dr. Reddy's Laboratories — Marketing Organization
- Jul 9, 2021
Mylan — Marketing Organization
- Dec 12, 2022
Changzhou Jinyuan Pharmaceutical Manufacturing Co., Ltd. — Marketing Organization
- May 1, 2025
Apotex — Marketing Organization
- May 2, 2025
Alembic — Marketing Organization
- May 5, 2025
Invagen Pharms — Marketing Organization
- Oct 28, 2025
Macleods Pharmaceuticals, Ltd — Marketing Organization
- Oct 28, 2025
Sciegen Pharmaceticals — Marketing Organization
- Oct 28, 2025
Taro Pharmaceuticals — Marketing Organization
Indications
Studied for
- Acute Coronary Syndrome · Phase 4
- Acute Lung Injury · Phase 1
- Adenosine · Phase 2
- Anemia, Sickle Cell · Phase 3
- Aneurysm · Phase 4
- Angina Pectoris · Phase 4
- Angina, Stable · Phase 4
- Angina, Unstable · Phase 4
- Angioplasty · Phase 4
- Angioplasty, Balloon, Coronary · Phase 4
- Ankle Injuries · Phase 4
- Antithrombins · Phase 4
- Aortic Aneurysm, Abdominal · Phase 2
- Aortic Stenosis, Subvalvular · Phase 4
- Aortic Valve Stenosis · Phase 4
- Arterial Occlusive Diseases · Phase 3
- Arthritis, Rheumatoid · Phase 4
- Aspirin · Early Phase 1
- Atherosclerosis · Phase 4
- Atrial Fibrillation · Phase 4
- Biological Availability · Phase 1
- Blood · Phase 1
- Blood Platelet Disorders · Phase 4
- Blood Platelets · Phase 4
- Cardiovascular Diseases · Phase 4
- Carotid Stenosis · Phase 2
- Cerebral Infarction · Phase 3
- Chest Pain · Phase 4
- Chronic Limb-Threatening Ischemia · Phase 1/Phase 2
- Community-Acquired Infections · Phase 2
- Constriction, Pathologic · Phase 4
- Coronary Artery Bypass · Phase 4
- Coronary Artery Disease · Phase 4
- Coronary Disease · Phase 4
- Coronary Stenosis · Phase 4
- Critical Illness · Phase 2
- Diabetes Mellitus · Phase 4
- Diabetes Mellitus, Type 2 · Phase 4
- Drug-Eluting Stents · Phase 4
- Drug Interactions · Phase 4
- Drug-Related Side Effects and Adverse Reactions · Phase 3
- Drugs, Investigational · Phase 4
- Embolism · Phase 4
- Endomyocardial Fibrosis · Phase 4
- Endothelial Cells · Phase 4
- Endothelium · Phase 4
- Fibrinolysis · Phase 4
- Foramen Ovale, Patent · Phase 3
- Fractional Flow Reserve, Myocardial · Phase 4
- Gout · Phase 1
- Headache · Phase 4
- Healthcare-Associated Pneumonia · Phase 1
- Healthy Volunteers · Phase 4
- Heart · Phase 4
- Heart Arrest · Phase 4
- Heart Diseases · Phase 4
- Hemorrhage · Phase 4
- Hypertrophy, Left Ventricular · Phase 4
- Hypothermia, Induced · Phase 4
- Infarction · Phase 4
- Inflammation · Phase 4
- Intermittent Claudication · Phase 4
- Intracranial Aneurysm · Phase 4
- Intracranial Arteriosclerosis · Phase 2/Phase 3
- Ischemia · Phase 4
- Ischemic Attack, Transient · Phase 3
- Ischemic Stroke · Phase 3
- Kidney Diseases · Phase 4
- Kidney Failure, Chronic · Phase 4
- Liver Transplantation · Phase 3
- Lung Diseases · Phase 4
- Metabolism · Phase 3
- Microvascular Angina · Phase 4
- Migraine Disorders · Phase 4
- Myocardial Infarction · Phase 4
- Myocardial Ischemia · Phase 4
- Myocardial Stunning · Phase 4
- Myocardium · Phase 4
- Non-ST Elevated Myocardial Infarction · Phase 4
- No-Reflow Phenomenon · Phase 4
- Pediatrics · Phase 3
- Percutaneous Coronary Intervention · Phase 4
- Peripheral Arterial Disease · Phase 4
- Peripheral Vascular Diseases · Phase 4
- Pharmacokinetics · Phase 3
- Pharmacology · Phase 1
- Plaque, Atherosclerotic · Phase 4
- Platelet Aggregation · Phase 4
- Platelet Aggregation Inhibitors · Phase 4
- Pneumonia · Phase 1
- Post-Cardiac Arrest Syndrome · Phase 4
- Prostheses and Implants · Phase 4
- Pulmonary Disease, Chronic Obstructive · Phase 2
- Renal Insufficiency, Chronic · Phase 4
- RNA · Early Phase 1
- Shock, Cardiogenic · Phase 4
- Sleep Initiation and Maintenance Disorders · Phase 1
- ST Elevation Myocardial Infarction · Phase 4
- Stents · Phase 4
- Stroke · Phase 4
- Therapeutic Equivalency · Phase 1
- Thrombosis · Phase 4
- Ticagrelor · Phase 4
- Transcatheter Aortic Valve Replacement · Phase 4
- Vascular Access Devices · Phase 1/Phase 2
- Vascular Diseases · Phase 4
- Vascular Grafting · Phase 4
Mechanism of action
- Purinergic receptor P2Y12ANTAGONIST
P2RY12 antagonist
Approval history
- approvedJul 20, 2011
Chemistry & pharmacology
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- Mol. weight
- 522.568 g/mol
- Lipinski Ro5
- 2 violation(s)
- Rule of 3
- No
- Chirality
- Single Stereoisomer
- Inorganic
- No
- Polymer
- No
- Delivery
- Oral
- Availability
- Prescription Only
Oral
Yes
Parenteral
No
Topical
No
Sources
- WikipediaTicagrelor ↗
- NCATSGLH0314RVC ↗
- ChEMBLCHEMBL398435 ↗
Also known as
- (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
- (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
- 3-(7-((2-(3,4-difluorophenyl)cyclopropyl)amino)-5-(propylthio)-3h-(1-3)-triazolo(4,5-d)pyrimidin-3-yl)-5-(2-hydroxyethoxy)cyclopentane-1,2-diol
- ar-c126532xx
- ar-c126532xx
- azd6140
- azd6140
- azd6140
- azd 6140
- azd 6140
- azd-6140
- azd-6140
- azd-6140
- brilinta
- brilinta
- brilinta
- brilinta
- brilinta
- brilinta
- brilique
- brilique
- brilique
- brilique
- brilique
- possia
- tiacrelor
- ticagrelor
- ticagrelor
- ticagrelor
- ticagrelor
- ticagrelor
- ticagrelor
- ticagrelor
- ticagrelor
- ticagrelor
- ticagrelor
- ticagrelor
- ticagrelor
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT07257198 | Phase 3 | Mar 1, 2026 | University of Montreal |
| NCT07080684 | Phase 4 | Dec 1, 2025 | University of Messina |
| NCT06853535 | Phase 3 | Apr 1, 2025 | Fudan University, Sichuan University |
| NCT06981390 | N/A | Feb 1, 2025 | Jilin University |
| NCT06714526 | N/A | Jan 31, 2025 | University of Toronto |
| NCT06756945 | Phase 4 | Jan 31, 2025 | Capital Medical University |
| NCT06691191 | Phase 4 | Jan 1, 2025 | University of Florida |
| NCT06653348 | Phase 2/Phase 3 (Phase 3) | Dec 1, 2024 | Mazandaran University of Medical Sciences |
| NCT06588595 | Phase 4 | Nov 1, 2024 | University of Florida |
| NCT06613191 | Phase 4 | Oct 1, 2024 | Ochsner Health System |
| NCT06584812 | Phase 1 | Sep 9, 2024 | Government of China |
| NCT06561867 | Phase 3 | Aug 30, 2024 | Kafrelsheikh University |
| NCT06671470 | Phase 1 | Aug 22, 2024 | Shanghai Haiyan Pharmaceutical Technology Co., Ltd. |
| NCT06554821 | Phase 1 | Aug 5, 2024 | AstraZeneca, Parexel |
| NCT06509893 | Phase 4 | Aug 1, 2024 | Shiraz University |
| NCT06486363 | Phase 4 | Aug 1, 2024 | Nanjing University |
| NCT06451198 | Phase 4 | Jul 1, 2024 | Fudan University |
| NCT06233266 | Phase 1 | Jun 18, 2024 | Bio-innova Co., Ltd |
| NCT06316570 | Phase 3 | Apr 3, 2024 | Capital Medical University |
| NCT06228456 | Phase 4 | Apr 1, 2024 | University of Florida |
Organizations
Research & Development (305)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| AstraZeneca | For profit | 90 | 43 | 5 | 2006 |
| University of Florida | Academic/Hospital | 21 | 21 | 4 | 2012 |
| Capital Medical University | Academic/Hospital | 14 | 11 | 4 | 2013 |
| University of Patras | Academic/Hospital | 12 | 12 | 2 | 2011 |
| Harbin Medical University | Academic/Hospital | 11 | 11 | 2 | 2014 |
| Kafrelsheikh University | Academic/Hospital | 10 | 10 | 1 | 2019 |
| Nicolaus Copernicus University | Academic/Hospital | 10 | 9 | 2 | 2014 |
| Nanjing Medical University | Academic/Hospital | 9 | 9 | 3 | 2013 |
| People's Liberation Army of China | Government | 9 | 3 | 3 | 2013 |
| Dong-A University | Academic/Hospital | 7 | 7 | 3 | 2014 |
| Harvard University | Academic/Hospital | 7 | 2 | 3 | 2013 |
| Icahn School of Medicine at Mount Sinai | Academic/Hospital | 7 | 6 | 2 | 2012 |
| IQVIA | For profit | 7 | 0 | 3 | 2011 |
| University of Ottawa | Academic/Hospital | 7 | 5 | 2 | 2013 |
| China Medical University | Academic/Hospital | 6 | 4 | 3 | 2014 |
| Chinese Academy of Medical Sciences | Academic/Hospital | 6 | 4 | 2 | 2013 |
| Jiao Tong University | Academic/Hospital | 6 | 6 | 2 | 2014 |
| University of Ulsan | Academic/Hospital | 6 | 4 | 3 | 2013 |
| University of Vienna | Academic/Hospital | 6 | 5 | 3 | 2010 |
| Yonsei University | Academic/Hospital | 6 | 6 | 2 | 2013 |
Marketing (24)
| Organization | Org type | Relationship | Date |
|---|---|---|---|
| Alembic | For profit | MKTG | May 2, 2025 |
| Alkem Labs Ltd | For profit | MKTG | Nov 9, 2018 |
| Allergan PLC (2015) | For profit | MKTG | Sep 4, 2018 |
| Amneal Pharmaceuticals | For profit | MKTG | Jan 23, 2019 |
| Amneal Pharmaceuticals | For profit | SYN | Jan 23, 2019 |
| Apotex | For profit | MKTG | May 1, 2025 |
| AstraZeneca | For profit | MKTG | Jul 20, 2011 |
| AstraZeneca | For profit | NDA | Jul 20, 2011 |
| Changzhou Jinyuan Pharmaceutical Manufacturing Co., Ltd. | For profit | MKTG | Dec 12, 2022 |
| Dr. Reddy's Laboratories | For profit | SYN | Oct 29, 2024 |
| Dr. Reddy's Laboratories | For profit | MKTG | Oct 29, 2020 |
| Invagen Pharms | For profit | MKTG | May 5, 2025 |
| MSN Laboratories | For profit | MKTG | Apr 7, 2020 |
| Macleods Pharmaceuticals, Ltd | For profit | MKTG | Oct 28, 2025 |
| Mylan | For profit | MKTG | Jul 9, 2021 |
| Prinston Inc | For profit | MKTG | Nov 6, 2018 |
| Prinston Inc | For profit | SYN | Aug 16, 2024 |
| Sciegen Pharmaceticals | For profit | MKTG | Oct 28, 2025 |
| Sigmapharm Laboratories | For profit | MKTG | Apr 7, 2020 |
| Sunshine Lake Pharma Co., Ltd. | For profit | MKTG | Apr 6, 2020 |
| Sunshine Lake Pharma Co., Ltd. | For profit | MKTG | Apr 6, 2020 |
| Taro Pharmaceuticals | For profit | MKTG | Oct 28, 2025 |
| Watson Pharmaceuticals | For profit | MKTG | Sep 4, 2018 |
| Zhejiang Hisun Pharmaceutical Co. Ltd. | For profit | MKTG | Jan 23, 2019 |