Ticagrelor

ATC code

B01AC24

Therapeutic class

P2Y12 platelet inhibitor · P2Y12 receptor antagonist

Forms

oral tablet

Brand names

Brilique (EU) · Brilinta (US) · Ticagrelor (US)

Overall confidence

high

Regulatory sources consulted

openfda-label-505b2d2b-bc2d-41dd-9384-a90d3d4d91ec
ema-epar-EMEA/H/C/001241
aemps-cima-110655009
ansm-bdpm-69133266
PubMed PMID:38839268 ↗
PubMed PMID:40888737 ↗
PubMed PMID:35094598 ↗
PubMed PMID:38599220 ↗
PubMed PMID:34870698 ↗
OpenFDA · B01AC24
RxNorm rxcui 1116632 ↗

Approved indications

To reduce the risk of cardiovascular (CV) death, myocardial infarction (MI), and stroke in patients with acute coronary syndrome (ACS) or a history of MI. For at least the first 12 months following ACS, it is superior to clopidogrel. It also reduces the risk of stent thrombosis in patients who have been stented for treatment of ACS.
To reduce the risk of a first MI or stroke in patients with coronary artery disease (CAD) at high risk for such events. Efficacy was established in a population with type 2 diabetes mellitus (T2DM).
To reduce the risk of stroke in patients with acute ischemic stroke (NIH Stroke Scale score ≤5) or high-risk transient ischemic attack (TIA).

Contraindications

Absolute

History of intracranial hemorrhage.
Active pathological bleeding (e.g., peptic ulcer, intracranial hemorrhage).
Hypersensitivity to ticagrelor or any component of the product.
Severe hepatic impairment.
Concomitant administration with strong CYP3A4 inhibitors (e.g., ketoconazole, clarithromycin, ritonavir).

Clinical warnings

Boxed warning · BLEEDING RISK: Ticagrelor can cause significant, sometimes fatal bleeding. Do not use in patients with active pathological bleeding or a history of intracranial hemorrhage. Do not start in patients undergoing urgent coronary artery bypass graft surgery (CABG). If possible, manage bleeding without discontinuing ticagrelor, as stopping it increases the risk of subsequent cardiovascular events. — FDA

Drug interactions

HighStrong CYP3A4 inhibitors (e.g. ketoconazole)J02AB02
Mechanism: Potent inhibition of CYP3A4, increasing ticagrelor AUC by 7.3-fold.
Recommendation: Concomitant use is contraindicated.
EMA SPCFDA label
HighStrong CYP3A4 inducers (e.g. rifampin)J04AB02
Mechanism: Potent induction of CYP3A4, decreasing ticagrelor AUC by 86%.
Recommendation: Avoid concomitant use.
EMA SPCFDA label
ModerateSimvastatinC10AA01
Mechanism: Ticagrelor is a weak CYP3A4 inhibitor, increasing simvastatin concentrations.
Recommendation: Avoid simvastatin doses greater than 40 mg per day.
FDA label
HighCyclosporineL04AD01
Mechanism: Inhibition of P-gp and CYP3A4, increasing ticagrelor AUC by 2.8-fold.
Recommendation: If the combination cannot be avoided, administer with caution and monitor.
EMA SPC

Adverse events

Common (≥1%)

bleeding · dyspnea

Rare but serious

major bleeding (incl. intracranial) · bradycardia · atrioventricular block · thrombotic thrombocytopenic purpura (TTP)

Pregnancy and lactation

Not recommended during pregnancy due to risk of maternal and fetal bleeding and animal reproductive toxicity data. Breastfeeding is not recommended.

Recent literature (PubMed)

Ticagrelor alone versus ticagrelor plus aspirin from month 1 to month 12 after percutaneous coronary intervention in patients with acute coronary syndromes (ULTIMATE-DAPT): a randomised, placebo-controlled, double-blind clinical trial.
Ge Z, et al. · Lancet · 2024 · Relevance 5/5
En pacientes con SCA post-ICP, la monoterapia con ticagrelor después de 1 mes de DAPT redujo significativamente el sangrado clínicamente relevante (BARC 2, 3 o 5) en comparación con la continuación de DAPT (ticagrelor + aspirina) durante 11 meses, sin aumentar los eventos adversos cardiovasculares y cerebrovasculares mayores (MACCE).
Ticagrelor and Aspirin or Aspirin Alone after Coronary Surgery for Acute Coronary Syndrome.
Jeppsson A, et al. · N Engl J Med · 2025 · Relevance 5/5
El ensayo TACSI encontró que en pacientes que se sometieron a CABG por un SCA, la adición de ticagrelor a la aspirina no redujo la incidencia del compuesto de muerte, IM, ACV o revascularización repetida a 1 año en comparación con la aspirina sola. Sin embargo, el grupo de ticagrelor tuvo una incidencia significativamente mayor de sangrado mayor.
Comparison of Ticagrelor vs Clopidogrel in Addition to Aspirin in Patients With Minor Ischemic Stroke and Transient Ischemic Attack: A Network Meta-analysis.
Lun R, et al. · JAMA Neurol · 2022 · Relevance 4/5
Este metaanálisis en red de 5 ECA (22,098 pacientes) no encontró diferencias estadísticamente significativas entre ticagrelor+aspirina y clopidogrel+aspirina para la prevención de ACV recurrente o muerte después de un ACV isquémico menor o AIT. Ambas terapias duales fueron superiores a la aspirina sola.
Antiplatelet Use in Ischemic Stroke.
Kamarova M, et al. · Ann Pharmacother · 2022 · Relevance 3/5
Revisión sobre el uso de agentes antiplaquetarios para la prevención primaria y secundaria del ACV. Se discute la evidencia para aspirina, clopidogrel y ticagrelor, destacando que la terapia dual a corto plazo (21 días) es más eficaz pero el uso a largo plazo aumenta el riesgo de hemorragia.