pharmacopeia
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/api/v1/drug/ticagrelor

Boxed warning

BLEEDING RISK • Ticagrelor, like other antiplatelet agents, can cause significant, sometimes fatal bleeding ( 5.1 , 6.1 ). • Do not use ticagrelor tablets in patients with active pathological bleeding or a history of intracranial hemorrhage (4.1 , 4.2 ). •Do not start ticagrelor tablets in patients undergoing urgent coronary artery bypass graft surgery (CABG) ( 5.1 , 6.1 ). • If possible, manage bleeding without discontinuing ticagrelor tablets. Stopping ticagrelor tablets increases the risk of subsequent cardiovascular events ( 5.2 ). WARNING: BLEEDING RISK See full prescribing information for complete boxed warning. • Ticagrelor, like other antiplatelet agents, can cause significant, sometimes fatal bleeding. ( 5.1 , 6.1 ) • Do not use ticagrelor tablets in patients with active pathological bleeding or a history of intracranial hemorrhage. ( 4.1 , 4.2 ) • Do not start ticagrelor tablets in patients undergoing urgent coronary artery bypass graft surgery(CABG). ( 5.1 , 6.1 ) • If possible, manage bleeding without discontinuing ticagrelor tablets. Stopping ticagrelor tablets increases the risk of subsequent cardiovascular events. ( 5.2 )

2D structure
(1S,2S,3R,5S)-3-[7-[[(1R,2S)-2-(3,4-difluorophenyl)cyclopropyl]amino]-5-propylsulfanyltriazolo[4,5-d]pyrimidin-3-yl]-5-(2-hydroxyethoxy)cyclopentane-1,2-diol
SMILES CCCSC1=NC(=C2C(=N1)N(N=N2)[C@@H]3C[C@@H]([C@H]([C@H]3O)O)OCCO)N[C@@H]4C[C@H]4C5=CC(=C(C=C5)F)F
InChIKey OEKWJQXRCDYSHL-FNOIDJSQSA-N

Mechanism of action

Sourced from openFDA

Ticagrelor and its major metabolite reversibly interact with the platelet P2Y 12 ADP-receptor to prevent signal transduction and platelet activation. Ticagrelor and its active metabolite are approximately equipotent.

Cytochrome P450 3A4P-GlycoproteinP2Y12 Receptor

Indications

Sourced from openFDA
  • Ticagrelor is a P2Y 12 platelet inhibitor indicated to reduce the risk of cardiovascular (CV) death, myocardial infarction (MI), 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.ICD-10: I21.9, I63.9

Contraindications

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  • • History of intracranial hemorrhage. ( 4.1 ) • Active pathological bleeding.contraindicated

Dosage & administration

Sourced from openFDA

ACS or History of MI Initiate treatment with 180 mg oral loading dose of ticagrelor tablets. Then administer 90 mg twice daily during the first year. After one year, administer 60 mg twice daily. ( 2.2 ) Patients with CAD and No Prior Stroke or MI Administer 60 mg ticagrelor tablets twice daily. ( 2.3 ) Acute Ischemic Stroke Initiate treatment with a 180 mg loading dose of ticagrelor tablets then continue with 90 mg twice daily for up to 30 days. ( 2.4 ) Use ticagrelor tablets with a daily maintenance dose of aspirin of 75 to 100 mg. ( 2 ) However, in patients who have undergone PCI, consider single antiplatelet therapy with ticagrelor tablets based on the evolving risk for thrombotic versusbleeding events. ( 2.2 ) 2.1 General Instructions Advise patients who miss a dose of ticagrelor tablets to take their next dose at its scheduled time. For patients who are unable to swallow tablets whole, ticagrelor tablets can be crushed, mixed with water, and drunk. The mixture can also be administered via a nasogastric tube (CH8 or greater) [see Clinical Pharmacology ( 12.3 )]. Do not administer ticagrelor tablets with another oral P2Y 12 platelet inhibitor. Avoid aspirin at doses higher than recommended [see Clinical Studies ( 14.1 )]. 2.2 Acute Coronary Syndrome or a History of Myocardial Infarction Initiate treatment with a 180 mg loading dose of ticagrelor tablets. Administer the first 90 mg maintenance dose of ticagrelor tablets, 6 to 12 hours after the loading dose. Administer 90 mg of ticagrelor tablets twice daily during the first year after an ACS event.

Warnings & precautions

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• Dyspnea was reported more frequently with ticagrelor than with control agents in clinical trials. Dyspnea from ticagrelor is self-limiting. ( 5.3 ) •Severe Hepatic Impairment: Likely increase in exposure to ticagrelor. ( 5.5 ) •Laboratory Test Interference: False negative platelet functional test results have been reported for Heparin Induced Thrombocytopenia (HIT). Ticagrelor is not expected to impact PF4 antibody testing for HIT. ( 5.7 ) 5.1 Risk of Bleeding Drugs that inhibit platelet function including ticagrelor increase the risk of bleeding [see Warnings and Precautions ( 5.2 ) and Adverse Reactions ( 6.1 )]. Patients treated for acute ischemic stroke or TIA Patients at NIHSS >5 and patients receiving thrombolysis were excluded from THALES and use of ticagrelor tablets in such patients is not recommended. 5.2 Discontinuation of Ticagrelor Tablets in Patients Treated for Coronary Artery Disease Discontinuation of ticagrelor tablets will increase the risk of myocardial infarction, stroke, and death in patients being treated for coronary artery disease. If ticagrelor tablets must be temporarily discontinued (e.g., to treat bleeding or for significant surgery), restart it as soon as possible. When possible, interrupt therapy with ticagrelor tablets for five days prior to surgery that has a major risk of bleeding. Resume ticagrelor tablets as soon as hemostasis is achieved. 5.3 Dyspnea In clinical trials, about 14% (PLATO and PEGASUS) to 21% (THEMIS) of patients treated with ticagrelor developed dyspnea.

Adverse reactions

Sourced from openFDA

The following adverse reactions are also discussed elsewhere in the labeling: •Bleeding [see Warnings and Precautions ( 5.1 )] •Dyspnea [see Warnings and Precautions ( 5.3 )] Most common adverse reactions (>5%) are bleeding and dyspnea. ( 5.1 , 5.3 , 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Dr. Reddy’s Laboratories Inc., at 1-888-375-3784 or FDA at 1-800-FDA-1088or www .fda.gov/medwatch. 6.1 Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice. Ticagrelor has been evaluated for safety in more than 58,000 patients. Bleeding in PLATO (Reduction in risk of thrombotic events in ACS) Figure 1 is a plot of time to the first non-CABG major bleeding event. Figure 1- Kaplan-Meier estimate of time to first non-CABG PLATO-defined major bleeding event (PLATO) Frequency of bleeding in PLATO is summarized in Tables 1 and 2. About half of the non-CABG major bleeding events were in the first 30 days. Table 1 - Non-CABG related bleeds (PLATO) Ticagrelor * N=9235 Clopidogrel N=9186 n (%) patients with event n (%) patients with event PLATO Major + Minor 713 (7.7) 567 (6.2) Major 362 (3.9) 306 (3.3) Fatal/Life-threatening 171 (1.9) 151 (1.6) Fatal 15 (0.2) 16 (0.2) Intracranial hemorrhage (Fatal/Life-threatening) 26 (0.3) 15 (0.2) PLATO Minor bleed: requires medical intervention to stop or treat bleeding.

Use in specific populations

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• Lactation: Breastfeeding not recommended ( 8.2 ) 8.1 Pregnancy Risk Summary Available data from case reports with ticagrelor use in pregnant women have not identified a drug-associated risk of major birth defects, miscarriage, or adverse maternal or fetal outcomes. Ticagrelor given to pregnant rats and pregnant rabbits during organogenesis caused structural abnormalities in the offspring at maternal doses about 5 to 7 times the maximum recommended human dose (MRHD) based on body surface area. When ticagrelor was given to rats during late gestation and lactation, pup death and effects on pup growth were seen at approximately 10 times the MRHD ( see Data ). The estimated background risk of major birth defects and miscarriage for the indicated population is unknown. All pregnancies have a background risk of birth defect, loss, or other adverse outcomes. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2 to 4% and 15 to 20%, respectively. Data Animal Data In reproductive toxicology studies, pregnant rats received ticagrelor during organogenesis at doses from 20 to 300 mg/kg/day. 20 mg/kg/day is approximately the same as the MRHD of 90 mg twice daily for a 60 kg human on a mg/m 2 basis.

Pharmacokinetics

Sourced from openFDA
Metabolism
Ticagrelor demonstrates dose proportional pharmacokinetics, which are similar in patients and healthy volunteers. Absorption Ticagrelor tablets can be taken with or without food.

Overdosage

Sourced from openFDA

There is currently no known treatment to reverse the effects of ticagrelor tablets, and ticagrelor is not dialyzable. Treatment of overdose should follow local standard medical practice. Bleeding is the expected pharmacologic effect of overdosing. If bleeding occurs, appropriate supportive measures should be taken. Platelet transfusion did not reverse the antiplatelet effect of ticagrelor tablets in healthy volunteers and is unlikely to be of clinical benefit in patients with bleeding. Other effects of overdose may include gastrointestinal effects (nausea, vomiting, diarrhea) or ventricular pauses. Monitor the ECG.

Approval history

Sourced from openFDA
  • Jul 20, 2011NDANDA022433Astrazeneca
  • Sep 4, 2018ANDAANDA208390Watson Labs Inc
  • Jan 23, 2019ANDAANDA208575Hisun Pharm Hangzhou
  • Apr 6, 2020ANDAANDA208508Sunshine
  • Apr 7, 2020ANDAANDA208596Msn
  • Jul 9, 2021ANDAANDA208597Mylan
  • Apr 21, 2023ANDAANDA208567Alkem Labs Ltd
  • Aug 16, 2024ANDAANDA208599Prinston Inc

FAERS reports

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Reference statistics only. FAERS reports are voluntarily submitted and are not incidence rates, safety signals, or causal evidence. Counts reflect reporting volume — how often a reaction was reported, not how often it occurs. For decision-grade use, consult openFDA and the FAERS Public Dashboard directly.
31,314 total reports matchedLatest report Share = reports listing the reaction ÷ total matched reports. Rows can sum to >100% because a single report often lists multiple reactions.
  1. 1Dyspnoea3,97713%
  2. 2Myocardial Infarction2,7608.8%
  3. 3Death1,7205.5%
  4. 4Fatigue1,5374.9%
  5. 5Off Label Use1,5144.8%
  6. 6Chest Pain1,4584.7%
  7. 7Dizziness1,2384.0%
  8. 8Contusion1,0853.5%
  9. 9Drug Interaction9473.0%
  10. 10Asthenia9132.9%
  11. 11Malaise8912.8%
  12. 12Haemorrhage8692.8%
  13. 13Nausea8492.7%
  14. 14Drug Ineffective8422.7%
  15. 15Chest Discomfort7632.4%

Literature

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Recent PubMed references pinned to Ticagrelor as a MeSH major topic. Citations link to pubmed.ncbi.nlm.nih.gov.

Clinical trials

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The 10 most recently updated of 615 ClinicalTrials.gov registrations naming Ticagrelor as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

Frequently asked questions

How does Ticagrelor work?
Ticagrelor and its major metabolite reversibly interact with the platelet P2Y 12 ADP-receptor to prevent signal transduction and platelet activation. Ticagrelor and its active metabolite are approximately equipotent.
What is Ticagrelor used for?
According to FDA labeling, Ticagrelor carries indications including: Ticagrelor is a P2Y 12 platelet inhibitor indicated to reduce the risk of cardiovascular (CV) death, myocardial infarction (MI), 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.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.
What class of drug is Ticagrelor?
Ticagrelor is classified as Platelet aggregation inhibitors excl. heparin, P2Y12 Platelet Inhibitor, Cytochrome P450 3A4 Inhibitors, P-Glycoprotein Inhibitors, P2Y12 Receptor Antagonists, Decreased Platelet Aggregation.
What are the brand names for Ticagrelor?
Ticagrelor is marketed under brand names including Brilinta.
What are the contraindications for Ticagrelor?
Ticagrelor labeling lists contraindications including: • History of intracranial hemorrhage. ( 4.1 ) • Active pathological bleeding.. Always consult the full prescribing information and a clinician.
Note. Data for ticagrelor is illustrative MVP content compiled from public sources. pharmacopeia is for educational and informational use only and is not a substitute for professional medical advice.

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