What Is Selatogrel?
Selatogrel is an investigational medication currently being studied in clinical trials. It is a reversible P2Y12 receptor antagonist designed for subcutaneous administration. P2Y12 receptors are found on platelets, which are small blood cells that help form clots to stop bleeding. By blocking these receptors, selatogrel helps prevent platelets from clumping together, which can reduce the risk of harmful blood clots. This mechanism of action suggests its potential use in situations where rapid and effective prevention of blood clot formation is crucial.
Selatogrel is being investigated for its potential to treat conditions related to cardiovascular health, specifically those involving acute blood clot formation. Clinical trials are exploring its use in patients experiencing symptoms suggestive of an acute event, such as an acute myocardial infarction. The drug is often administered as a single dose, typically via an autoinjector, making it a potentially convenient option for rapid intervention outside of a hospital setting. Its development focuses on providing a quick-acting antiplatelet effect.
Uses and Conditions Under Study
Selatogrel is currently being studied in clinical trials for several conditions, primarily focusing on cardiovascular health and safety assessments.
- Cardiovascular Conditions: Selatogrel is being investigated for its potential use in treating acute cardiovascular events. Two trials are studying its effect in Acute Myocardial Infarction, commonly known as a heart attack. This condition occurs when blood flow to a part of the heart is blocked, often by a blood clot. As a P2Y12 receptor antagonist, selatogrel aims to prevent or reduce the formation of these clots, potentially limiting heart damage. One trial also explores its use in Stable Coronary Artery Disease, a long-term condition where the heart's blood vessels are narrowed, which can lead to chest pain and increase the risk of future heart attacks.
- Safety and Pharmacokinetic Studies: A significant portion of the research involves understanding how selatogrel works in the body and its safety profile. Two trials have been conducted in Healthy Subjects and one in Healthy Volunteers. These studies typically assess how the drug is absorbed, distributed, metabolized, and eliminated (pharmacokinetics), and identify potential side effects in individuals without the target condition. This helps establish a baseline for its effects.
- Hepatic Impairment: One trial specifically examines selatogrel in individuals with Hepatic Impairment. This type of study is crucial to understand how liver function might affect the drug's processing in the body. Adjustments to dosing might be necessary for patients with liver conditions to ensure both effectiveness and safety.
In total, 6 clinical trials involving 14,474 participants have been conducted or are ongoing for selatogrel. The earliest trial began on 2017-12-28, and the latest is expected to conclude on 2025-08-20.
Dosing
Selatogrel has been studied in various formulations and strengths for subcutaneous administration. The drug is designed for a single dose application.
- Formulations: Selatogrel has been investigated in several forms. These include a liquid formulation delivered via an autoinjector or a syringe. Another formulation studied is a lyophilizate-based formulation, which is a freeze-dried powder that would be reconstituted with liquid before administration via a syringe. The autoinjector system is designed to be a ready-to-use, single-dose drug delivery system for convenience.
- Strengths Studied: Clinical trials have explored different strengths of selatogrel. Doses of 8 mg and 16 mg have been administered as single subcutaneous injections. Some trials mention the drug being supplied in sealed glass vials at a strength of 20 mg, which would then be reconstituted and further diluted to achieve the target doses of 8 mg or 16 mg.
- Administration: Selatogrel is intended for subcutaneous administration, meaning it is injected under the skin. Participants in some studies were instructed to self-administer the 16 mg dose using an autoinjector upon experiencing symptoms suggestive of an acute event.
Specific dosing regimens for participants with mild or moderate hepatic impairment have also been part of the investigation to understand how liver function affects the drug's metabolism and to determine appropriate dosing adjustments if needed.
Side Effects
In a clinical trial involving Selatogrel, the most commonly reported side effect was dyspnoea (shortness of breath). This occurred in 3.7% of patients taking Selatogrel, compared to 0.0% of patients receiving a placebo. Other common side effects reported more frequently with Selatogrel than with placebo included:
- Dizziness: 2.2% of patients on Selatogrel experienced dizziness, compared to 0.4% on placebo.
- Diarrhea: 1.5% of patients on Selatogrel experienced diarrhea, compared to 0.4% on placebo.
- Injection site bruise: 1.1% of patients on Selatogrel experienced a bruise at the injection site, compared to 0.0% on placebo.
- Oedema peripheral (swelling in the limbs): 0.4% of patients on Selatogrel experienced this, compared to 0.0% on placebo.
Some side effects were reported less frequently in patients taking Selatogrel compared to placebo. For example, headache was reported by 1.3% of patients on Selatogrel versus 2.2% on placebo. Vessel puncture site bruise occurred in 0.9% of Selatogrel patients compared to 1.3% on placebo, and contusion (bruising) occurred in 0.7% of Selatogrel patients compared to 1.3% on placebo.
Clinical Trial Results
Clinical trials have evaluated the effects of Selatogrel in adults with coronary artery disease and those who have experienced a heart attack. The drug's ability to inhibit platelet activity, which is important for preventing blood clots, was a key focus.
Study in Adults With Coronary Artery Disease (NCT03384966)
This study assessed the effects of Selatogrel in adults with coronary artery disease. A key measure was the pharmacodynamic response, which indicates how well the drug inhibits platelet aggregation (clumping of platelets). Approximately 34% of patients taking either 16 mg or 8 mg of Selatogrel showed a pharmacodynamic response, compared to 6% of patients on placebo.
Selatogrel significantly reduced platelet reactivity, as measured by P2Y12 reaction units (PRU) and maximum platelet aggregation (MPA). For example, Selatogrel 16 mg reduced platelet reactivity from approximately 160 PRU to a range of 5 to 12 PRU at predefined time points. Similarly, maximum platelet aggregation was reduced from 63-65% to 13-32% with Selatogrel 16 mg. The 8 mg dose also showed significant reductions in both measures.
Selatogrel was rapidly absorbed into the bloodstream, with maximum plasma concentrations reached within approximately 0.5 hours for both the 8 mg and 16 mg doses. Bleeding events were observed in both the Selatogrel and placebo groups during the study.
Study in Adults With Heart Attack (NCT03487445)
This study investigated Selatogrel in adults who had experienced a heart attack. The results showed a strong pharmacodynamic response. Approximately 95% of participants receiving Selatogrel 16 mg and 100% of participants receiving Selatogrel 8 mg achieved a pharmacodynamic response, indicating effective inhibition of platelet aggregation.
Platelet reactivity, measured in P2Y12 reaction units (PRU), was substantially reduced. The 16 mg dose of Selatogrel decreased median platelet reactivity from approximately 181 PRU to 7-9 PRU. The 8 mg dose reduced median platelet reactivity from approximately 194 PRU to 9-51 PRU at various time points.
Similar to the other study, Selatogrel was quickly absorbed, reaching maximum plasma concentrations within approximately 1 hour for both the 8 mg and 16 mg doses.
Currently Recruiting Trials
Clinical trials are essential for developing new treatments and understanding how they work. Selatogrel is currently being investigated in a significant study for individuals who have experienced a heart attack.
The "Selatogrel Outcome Study in Suspected Acute Myocardial Infarction" (NCT04957719) is a Phase 3 clinical trial sponsored by Viatris Innovation GmbH. This large study aims to enroll approximately 14,000 participants to evaluate Selatogrel. It is designed for patients who have recently been discharged from the hospital after experiencing a specific type of heart attack, known as type 1 acute myocardial infarction, and who also have additional cardiovascular risk factors. The trial seeks to understand the potential benefits of Selatogrel in this patient population.
Where to Participate
The clinical trial for Selatogrel is actively recruiting participants across a wide geographic area, with sites established in 31 states, covering 72 cities and 82 locations in total. This extensive network aims to make participation accessible to many eligible individuals.
Some of the top cities with participating sites include:
- Birmingham, Alabama (4 sites)
- Pensacola, Florida (2 sites)
- Greenville, South Carolina (2 sites)
- Newark, New Jersey (2 sites)
- Amarillo, Texas (2 sites)
- Falls Church, Virginia (2 sites)
- Jacksonville, Florida (2 sites)
- Jonesboro, Arkansas (1 site)
- Tucson, Arizona (1 site)
- Huntsville, Alabama (1 site)
To be eligible for participation, individuals must be between 18 and 80 years of age. The study is open to participants of all genders, but it is not seeking healthy volunteers or children.
Development Timeline
The journey of Selatogrel in clinical development began on December 28, 2017, with its first clinical trial. Since then, Viatris Innovation GmbH has consistently sponsored all 6 trials for Selatogrel, guiding its progression through various research stages. The latest trial is projected to conclude by August 20, 2025.
Initially, Selatogrel was explored for conditions such as Irritable Bowel Syndrome with Constipation (IBS-C) and hyperphosphatemia. As research advanced, the development pipeline expanded to include studies involving healthy volunteers and individuals with hepatic impairment, allowing researchers to gather crucial safety and pharmacokinetic data. The drug's focus then broadened significantly to cardiovascular health, with studies in stable coronary artery disease, culminating in the current large-scale Phase 3 trial for acute myocardial infarction. This comprehensive approach has involved 3 Phase 1 trials, 2 Phase 2 trials, and 1 pivotal Phase 3 trial, collectively enrolling 14,474 participants to date.