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Ticagrelor

Generic Name
Ticagrelor
Brand Names
Brilinta, Brilique
Drug Type
Small Molecule
Chemical Formula
C23H28F2N6O4S
CAS Number
274693-27-5
Unique Ingredient Identifier
GLH0314RVC
Background

Ticagrelor, or AZD6140, was first described in the literature in 2003. Ticagrelor is an ADP derivative developed for its P2Y receptor antagonism. Unlike clopidogrel, ticagrelor is not a prodrug. It is marketed by Astra Zeneca as Brilinta in the US and Brilique or Possia in the EU,.

Ticagrelor was granted EMA approval on 3 December 2010.

Ticagrelor was granted FDA approval on 20 July 2011.

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. Ticagrelor is also indicated to reduce the risk of a first myocardial infarction or stroke in high risk patients with coronary artery disease.

Associated Conditions
Cardiovascular Mortality, Myocardial Infarction, Stroke, Thrombosis (Stent Thrombosis)

Alembic Pharmaceuticals Receives FDA Approval for Generic Ticagrelor Tablets to Reduce Cardiovascular Risks

• Alembic Pharmaceuticals has secured final FDA approval for Ticagrelor Tablets 90 mg and tentative approval for the 60 mg version, a generic equivalent to AstraZeneca's Brilinta. • The medication is indicated to reduce the risk of cardiovascular death, myocardial infarction, and stroke in patients with acute coronary syndrome or history of MI, with additional indications for stent thrombosis prevention. • The estimated market size for Ticagrelor Tablets is substantial, with the 90 mg version valued at $1.06 billion and the 60 mg version at $242 million for the twelve months ending March 2025.

2025 Pharmaceutical Pipeline: Major Patent Expirations Set to Transform Drug Market with Generics and Biosimilars

• The US pharmaceutical market is poised for significant change in 2025 as several blockbuster drugs including Xarelto, Entresto, and Stelara face patent expirations, opening the door to generic and biosimilar competition. • Multiple biosimilars for ustekinumab (Stelara) are entering the market in 2025, with Wezlana already launched in January as the first interchangeable biosimilar, while other major drugs like ticagrelor and denosumab will also face competition. • The pharmaceutical pipeline continues to expand with innovative therapies for cancer and neurological disorders, alongside the Medicare Drug Price Negotiation program which will further impact pricing dynamics for high-cost medications.

Bentracimab Shows Promising Results in Phase 3 Trial for Reversing Ticagrelor's Antiplatelet Effects

• The pivotal Phase 3 REVERSE-IT trial demonstrated that bentracimab rapidly restored platelet function within 5-10 minutes in patients on ticagrelor requiring urgent surgery or experiencing major bleeding. • The trial achieved its primary endpoint with 94.3% of eligible patients achieving effective hemostasis, including 100% of surgical patients and 83.1% of those with major bleeding, while maintaining a favorable safety profile. • Bentracimab, which received FDA Breakthrough Therapy Designation in 2019 and Orphan Drug Designation in March 2025, addresses a significant unmet need for patients on ticagrelor who face emergency situations.

AstraZeneca Discontinues Two Alexion Rare Disease Programs Amid Strong Q4 Performance

• AstraZeneca has terminated the development of two Alexion-acquired assets - vemircopan for rare liver and kidney conditions and ALXN1910 for bone metabolism disorders - due to insufficient efficacy data. • The company's rare disease portfolio showed robust growth with Q4 2024 revenue reaching $2.4 billion, driven by Ultomiris which generated nearly $1.1 billion, representing a 33% increase. • Despite the setbacks, AstraZeneca reported strong Q4 earnings of $14.90 billion, exceeding analyst expectations, with significant contributions from its oncology portfolio and rare disease treatments.

ACC.25 Highlights Novel Therapies and Strategies in Cardiovascular Care

• The SOUL trial demonstrated that oral semaglutide significantly reduces cardiovascular events in type 2 diabetes patients with atherosclerotic cardiovascular and/or chronic kidney disease. • The RIVAWAR trial investigated the efficacy of rivaroxaban versus warfarin in patients with acute left ventricular thrombus following myocardial infarction. • The FAIR-HF2 trial assessed the impact of ferric carboxymaltose on morbidity and mortality in patients with iron deficiency and chronic heart failure. • The ALPACA Phase 2 trial of Lepodisiran showed promising results for an extended duration small-interfering RNA targeting Lipoprotein(a).

Landmark Ticagrelor Trial Faces Renewed Scrutiny Over Data Integrity

• A _BMJ_ investigation raises concerns about the PLATO trial, which supported the approval of ticagrelor, citing issues in data reporting and accuracy. • The FDA approved ticagrelor despite internal objections regarding the reliability of PLATO trial data, particularly concerning outcomes in US patients. • Subsequent studies have struggled to replicate PLATO's positive results, leading to calls for a reappraisal of ticagrelor's role in clinical guidelines. • Discrepancies in death records and endpoint adjudication, along with potential conflicts of interest, further fuel the controversy surrounding the trial's validity.

CytoSorbents Seeks Approval for DrugSorb-ATR in Canada to Reduce Bleeding in Heart Surgery

• CytoSorbents has submitted a Medical Device License application to Health Canada for DrugSorb-ATR, targeting reduced bleeding during CABG surgery in patients on ticagrelor. • The application follows successful MDSAP certification, ensuring compliance with quality management system requirements in Canada and the U.S. • Regulatory decisions from Health Canada and the U.S. FDA are anticipated in 2025, potentially improving the standard of care for heart attack patients. • The STAR-T trial data supports the application, demonstrating DrugSorb-ATR's safety and efficacy in reducing perioperative bleeding complications.

CytoSorbents' DrugSorb-ATR Receives FDA Priority Review for Bleeding Reduction in Heart Surgery

• CytoSorbents has submitted a De Novo marketing application to the FDA for DrugSorb™-ATR, aimed at reducing perioperative bleeding in CABG surgery patients. • The FDA has granted DrugSorb-ATR a Breakthrough Device Designation, making it eligible for priority review and potentially accelerating the approval process. • Regulatory decisions from both the FDA and Health Canada regarding DrugSorb-ATR are anticipated in 2025, marking a crucial period for the device's market entry.

Exscientia Strengthens AI Drug Discovery Leadership with AstraZeneca Veteran as New CTO

• Former AstraZeneca head of hit discovery Dr. Garry Pairaudeau joins Exscientia as Chief Technology Officer, bringing 25 years of expertise in AI, machine learning, and drug discovery. • Pairaudeau's appointment comes as Exscientia advances its AI-driven drug discovery platform, which has already produced the first AI-designed drug molecule to enter clinical trials for OCD treatment. • The move reflects the growing importance of AI in pharmaceutical R&D, with the global AI healthcare market projected to grow from $2.1 billion in 2018 to $36 billion by 2025.
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