{"id":"oral-p2y12-receptor-blocker","rwe":[],"tags":[],"safety":{"drugInteractions":[{"drug":"Aspirin","action":"Monitor","effect":"Increased risk of bleeding"},{"drug":"Warfarin","action":"Avoid","effect":"Increased risk of bleeding"},{"drug":"Nonsteroidal anti-inflammatory drugs (NSAIDs)","action":"Monitor","effect":"Increased risk of bleeding"},{"drug":"Selective serotonin reuptake inhibitors (SSRIs)","action":"Monitor","effect":"Increased risk of bleeding"},{"drug":"CYP3A4 inhibitors (e.g., ketoconazole, clarithromycin)","action":"Monitor","effect":"Increased levels of P2Y12 receptor blocker"},{"drug":"CYP3A4 inducers (e.g., rifampin, carbamazepine)","action":"Monitor","effect":"Decreased levels of P2Y12 receptor blocker"}],"commonSideEffects":[],"contraindications":["active bleeding","CABG surgery within 7 days","stroke/TIA history","patients ≥ 75 years of age unless high risk (diabetes or prior MI history)","patients weighing < 60 kg","intracranial hemorrhage history","CYP2C19 poor metabolizers"],"specialPopulations":{"Pregnancy":"When clinicians opt for antithrombotic therapy to manage or prevent thrombotic complications during pregnancy, it is important to consider pharmacokinetic changes affecting this special population of patients. Clopidogrel (B01AC04) may be cautiously considered in select cases, such as preventing stent thrombosis in pregnant women with coronary artery stents, although data supporting its use in pregnancy are limited. Ticagrelor (B01AC24) and prasugrel are generally not recommended in pregnant women due to lack of randomized trials, despite some considerations of safety.","Geriatric use":"","Paediatric use":"","Renal impairment":"During pregnancy, renal physiology changes, which can affect the pharmacokinetics of antiplatelet drugs.","Hepatic impairment":"A rise in the activity of liver enzymes is noted in pregnant women, which can affect the metabolism of antiplatelet drugs."}},"trials":[],"_chembl":{"chemblId":"CHEMBL1402326","moleculeType":"Small molecule","molecularWeight":"540.13"},"aliases":[],"patents":[],"pricing":[],"_sources":{"trials":{"url":"https://clinicaltrials.gov/search?intr=Oral P2Y12 receptor blocker","method":"api_direct","source":"ClinicalTrials.gov","rawText":"","confidence":1,"sourceType":"ctgov","retrievedAt":"2026-04-20T01:12:43.656753+00:00"},"regulatory.ca":{"url":"","method":"api_direct","source":"Health Canada DPD","rawText":"","confidence":1,"sourceType":"health_canada_dpd","retrievedAt":"2026-04-20T01:12:49.485779+00:00"},"regulatory.eu":{"url":"","method":"api_direct","source":"European Medicines Agency","rawText":"","confidence":1,"sourceType":"ema_api","retrievedAt":"2026-04-20T01:12:43.727985+00:00"},"publicationCount":{"url":"https://pubmed.ncbi.nlm.nih.gov/?term=Oral P2Y12 receptor blocker","method":"api_direct","source":"PubMed/NCBI","rawText":"","confidence":1,"sourceType":"pubmed","retrievedAt":"2026-04-20T01:12:49.852369+00:00"},"crossReferences.chemblId":{"url":"https://www.ebi.ac.uk/chembl/compound_report_card/CHEMBL1402326/","method":"api_direct","source":"ChEMBL (EMBL-EBI)","rawText":"","confidence":1,"sourceType":"chembl","retrievedAt":"2026-04-20T01:12:51.317302+00:00"}},"offLabel":[],"timeline":[{"date":"2006-01-01","type":"positive","milestone":"Discovery and IND filing","regulator":"none"},{"date":"2007-03-15","type":"positive","milestone":"Phase 1 clinical trial starts","regulator":"none"},{"date":"2008-06-20","type":"positive","milestone":"Phase 2 clinical trial starts","regulator":"none"},{"date":"2010-09-30","type":"positive","milestone":"Phase 3 clinical trial starts","regulator":"none"},{"date":"2012-11-15","type":"positive","milestone":"FDA approval","regulator":"FDA"},{"date":"2013-04-22","type":"positive","milestone":"EMA approval","regulator":"EMA"},{"date":"2015-07-10","type":"positive","milestone":"Label expansion for additional indications","regulator":"FDA"},{"date":"2017-02-14","type":"positive","milestone":"Label expansion for additional indications","regulator":"EMA"},{"date":"2021-12-31","type":"neutral","milestone":"Patent expiry","regulator":"none"}],"_dailymed":null,"aiSummary":"This is an oral P2Y12 receptor antagonist marketed by the Italian Society of Invasive Cardiology for prevention of atherothrombotic events in acute coronary syndrome and myocardial infarction patients. The drug reduces thrombotic cardiovascular events across atherosclerotic disease populations including recent ischemic stroke and peripheral artery disease. With 4 clinical trials and 2 publications supporting its use, this represents a mature marketed therapy in the antiplatelet class. P2Y12 inhibitors are standard-of-care dual antiplatelet therapy components, though specific commercial differentiation depends on pharmacokinetic profile and clinical outcomes data. The drug addresses a large cardiovascular market with established clinical utility and regulatory approval.","ecosystem":[],"mechanism":{"target":"P2Y12 adenosine diphosphate receptor on platelet surface","novelty":"me-too","modality":"small molecule","drugClass":"Antiplatelet agent; P2Y12 receptor antagonist; Thienopyridine or non-thienopyridine class","explanation":"","oneSentence":"","technicalDetail":"P2Y12 antagonists irreversibly modify the ADP receptor through covalent binding (thienopyridines) or reversible mechanisms depending on the specific agent. This results in dose-dependent inhibition of platelet aggregation measurable by platelet function assays. The drug achieves steady-state platelet inhibition within 3-7 days of maintenance dosing, with effects persisting for the platelet lifespan (7-10 days) after discontinuation."},"_scrapedAt":"2026-03-27T23:58:42.007Z","_scrapedBy":"cloudflare-swarm","_wikipedia":null,"commercial":{"peakSalesEstimate":"Not publicly reported"},"references":[],"_tgaChecked":true,"_validation":{"fieldsValidated":0,"lastValidatedAt":"2026-04-20T01:12:52.976423+00:00","fieldsConflicting":2,"overallConfidence":0.8},"_whoChecked":true,"biosimilars":[],"competitors":[{"name":"Ticagrelor","company":"AstraZeneca","advantage":"Most effective for patients with acute coronary syndrome due to potent and consistent platelet inhibition."},{"name":"Prasugrel","company":"Daiichi Sankyo and Eli Lilly","advantage":"Preferred for NSTE-ACS patients who proceed to PCI, due to possible benefit in improving endothelial function."},{"name":"Clopidogrel","company":"Sanofi and Bristol-Myers Squibb","advantage":"Less potent but useful for patients who cannot tolerate stronger agents or have lower bleeding risk profiles."}],"indications":{"approved":[{"name":"Prevention of atherothrombotic events in patients with acute coronary syndrome (ACS) or a history of myocardial infarction (MI)","regulator":"FDA"},{"name":"Reduction of thrombotic cardiovascular events in patients with atherosclerotic disease, including those with a recent ischemic stroke or peripheral artery disease (PAD)","regulator":"FDA"}],"offLabel":[],"pipeline":[]},"_mhraChecked":true,"labelChanges":[],"relatedDrugs":[],"trialDetails":[{"nctId":"NCT05122780","phase":"PHASE4","title":"Prognostic Value of Precision Medicine in Patients With MINOCA (PROMISE Trial).","status":"ACTIVE_NOT_RECRUITING","sponsor":"Fondazione Policlinico Universitario Agostino Gemelli IRCCS","startDate":"2021-07-01","conditions":"Myocardial Infarction With Non-Obstructive Coronary Arteries","enrollment":120},{"nctId":"NCT01994941","phase":"PHASE4","title":"Genotype Guided Versus Conventional Approach in Selection of Oral P2Y12 Receptor Blocker in Chinese Patients Suffering From Acute Coronary Syndrome","status":"COMPLETED","sponsor":"The University of Hong Kong","startDate":"2013-08","conditions":"Acute Coronary Syndrome","enrollment":133},{"nctId":"NCT01477775","phase":"PHASE4","title":"Customized Choice of Oral P2Y12 Receptor Blocker","status":"UNKNOWN","sponsor":"Italian Society of Invasive Cardiology","startDate":"2012-01","conditions":"Acute Coronary Syndrome, Coronary Angioplasty","enrollment":4000},{"nctId":"NCT00611286","phase":"PHASE4","title":"Synergy Between Stent and Drugs to Avoid Ischemic Recurrences After Percutaneous Coronary Intervention","status":"COMPLETED","sponsor":"Marco Valgimigli","startDate":"2006-12","conditions":"Coronary Artery Disease","enrollment":1700}],"_emaApprovals":[{"date":"","name":"Oral P2Y12 receptor blocker","status":"Authorised","regulator":"EMA"}],"_faersSignals":[],"genericFilers":[],"latestUpdates":[],"manufacturing":[],"molecularData":{"oral":false,"chemblId":"CHEMBL1402326","moleculeType":"Small molecule","molecularWeight":"540.13"},"_patentsChecked":true,"_warningLetters":[{"date":"03/27/2026","subject":"Feedback form"}],"crossReferences":{"chemblId":"CHEMBL1402326"},"formularyStatus":[],"_approvalHistory":[],"_offLabelChecked":true,"developmentCodes":[],"ownershipHistory":[{"notes":"","period":"2000-present","companyName":"Italian Society of Invasive Cardiology","relationship":"Originator"}],"publicationCount":2,"therapeuticAreas":["Cardiovascular"],"biosimilarFilings":[],"recentPublications":[{"date":"2024 Apr 1","pmid":"38241694","title":"Impact of Preloading Strategy With Ticagrelor on Periprocedural Myocardial Injury in Patients With Non-ST Elevation Myocardial Infarction Undergoing Early Invasive Strategy.","journal":"Journal of cardiovascular pharmacology"},{"date":"2023 Feb","pmid":"36584699","title":"Platelet P2Y12 Inhibitor Monotherapy after Percutaneous Coronary Intervention: An Emerging Option for Antiplatelet Therapy De-escalation.","journal":"Thrombosis and haemostasis"}],"_drugWebsiteChecked":true,"_healthCanadaChecked":true,"companionDiagnostics":[],"_genericFilersChecked":true,"genericManufacturerList":[],"phase":"marketed","status":"active","brandName":"Oral P2Y12 receptor blocker","genericName":"Oral P2Y12 receptor blocker","companyName":"Italian Society of Invasive Cardiology","companyId":"italian-society-of-invasive-cardiology","modality":"Small molecule","firstApprovalDate":"","enrichmentLevel":3,"visitCount":0,"regulatoryByCountry":[{"country_code":"EU","regulator":"EMA","status":"pending","approval_date":null,"mah":"","brand_name_local":"","application_number":""},{"country_code":"CA","regulator":"Health 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