{"id":"grapiprant","rwe":[{"pmid":"41667566","year":"2026","title":"A noninferiority trial evaluating the efficacy of bedinvetmab compared to grapiprant for osteoarthritis-pain in dogs using force plate gait analysis.","finding":"","journal":"Scientific reports","studyType":"Clinical Study"},{"pmid":"41467639","year":"2026","title":"Azoheteroarene-Modified Grapiprants Serving as Photoswitchable EP4 Antagonists.","finding":"","journal":"Chemistry (Weinheim an der Bergstrasse, Germany)","studyType":"Clinical Study"},{"pmid":"41162752","year":"2025","title":"Structural insights into selective and dual antagonism of EP2 and EP4 prostaglandin receptors.","finding":"","journal":"The EMBO journal","studyType":"Clinical Study"},{"pmid":"41044798","year":"2026","title":"Efficacy of combined grapiprant and tapentadol for analgesia in cats undergoing elective ovariohysterectomy.","finding":"","journal":"Journal of feline medicine and surgery","studyType":"Clinical Study"},{"pmid":"40996819","year":"2026","title":"EP4/ANXA2 axis in pulmonary arterial hypertension: therapeutic implications.","finding":"","journal":"European heart journal","studyType":"Clinical Study"}],"tags":[{"label":"Small Molecule","category":"modality"},{"label":"Prostaglandin E2 receptor EP4 subtype","category":"target"},{"label":"PTGER4","category":"gene"},{"label":"Active","category":"status"}],"phase":"discontinued","safety":{},"trials":[],"aliases":[],"patents":[],"pricing":[],"allNames":["grapiprant","RQ-7","RQ-00000007","MR10A7","AAT-007","CJ-023423"],"offLabel":[],"synonyms":["grapiprant","RQ-7","RQ-00000007","MR10A7","AAT-007","CJ-023423"],"timeline":[],"aiSummary":"Grapiprant is a small molecule modality targeting the Prostaglandin E2 receptor EP4 subtype. Its mechanism of action involves selectively blocking the EP4 receptor, which plays a key role in inflammation and pain. Grapiprant is currently owned by Merial, a subsidiary of Boehringer Ingelheim, but its commercial status and approved indications are not specified. Further information on its pharmacokinetic properties, such as half-life and bioavailability, is also not available. As a result, its clinical use and safety profile remain unclear.","approvals":[{"date":"","orphan":false,"company":"","regulator":"FDA"}],"ecosystem":[],"mechanism":{"target":"Prostaglandin E2 receptor EP4 subtype, Prostaglandin E2 receptor EP4 subtype","targets":[{"gene":"PTGER4","source":"DrugCentral","target":"Prostaglandin E2 receptor EP4 subtype","protein":"Prostaglandin E2 receptor EP4 subtype"}],"modality":"Small Molecule","explanation":"Think of the EP4 receptor like a messenger that tells your body to send pain signals. When Grapiprant blocks this messenger, it can help reduce pain and inflammation. This is similar to how other pain medications work, but Grapiprant targets a specific type of messenger that is involved in pain and inflammation.","oneSentence":"Grapiprant works by blocking the EP4 receptor, which is involved in pain and inflammation.","technicalDetail":"Grapiprant selectively binds to the EP4 receptor, a subtype of the Prostaglandin E2 receptor, thereby inhibiting its activity and reducing the production of pro-inflammatory mediators."},"commercial":{},"references":[{"id":1,"url":"https://drugcentral.org/drugcard/5552","fields":["approvals","synonyms","ATC","PK","indications","contraindications","DDIs","targets","patents","FAERS"],"source":"DrugCentral"},{"id":2,"url":"https://clinicaltrials.gov/search?intr=GRAPIPRANT","fields":["trials"],"source":"ClinicalTrials.gov"},{"id":3,"url":"https://pubmed.ncbi.nlm.nih.gov/?term=GRAPIPRANT","fields":["publications"],"source":"PubMed/NCBI"}],"_enrichedAt":"2026-03-30T11:48:06.552459","biosimilars":[],"competitors":[],"dataSources":[{"url":"https://drugcentral.org","name":"DrugCentral","fields":["indications","contraindications","safety","target","drugInteractions"],"retrievedDate":"2026-04-07"}],"genericName":"grapiprant","indications":{"approved":[],"offLabel":[],"pipeline":[]},"drugCategory":"active","labelChanges":[],"relatedDrugs":[],"trialDetails":[{"nctId":"NCT05041101","phase":"PHASE1,PHASE2","title":"Grapiprant and Eribulin for the Treatment of Metastatic Inflammatory Breast Cancer","status":"TERMINATED","sponsor":"M.D. Anderson Cancer Center","startDate":"2021-12-21","conditions":["Breast Inflammatory Carcinoma","Recurrent Breast Inflammatory Carcinoma","Stage IV Breast Inflammatory Carcinoma"],"enrollment":6,"completionDate":"2024-09-06"},{"nctId":"NCT03658772","phase":"PHASE1","title":"Grapiprant and Pembrolizumab in Patients With Advanced or Progressive MSS Colorectal Cancer","status":"COMPLETED","sponsor":"Arrys Therapeutics","startDate":"2018-09-20","conditions":["Microsatellite Stable Colorectal Cancer"],"enrollment":54,"completionDate":"2023-03-07"},{"nctId":"NCT03696212","phase":"PHASE1,PHASE2","title":"Grapiprant (ARY-007) and Pembrolizumab in Patients With Advanced or Metastatic Post-PD-1/L1 NSCLC Adenocarcinoma","status":"TERMINATED","sponsor":"Arrys Therapeutics","startDate":"2019-01-08","conditions":["Non-small Cell Lung Cancer Adenocarcinoma"],"enrollment":18,"completionDate":"2021-02-15"},{"nctId":"NCT02538432","phase":"PHASE2","title":"Phase II Trial of EP4 Receptor Antagonist, AAT-007 (RQ-07; CJ-023,423) in Advanced Solid Tumors","status":"WITHDRAWN","sponsor":"University of Maryland, Baltimore","startDate":"2017-06","conditions":["Prostate Cancer","Non-Small Cell Lung Cancer","Breast Cancer"],"enrollment":0,"completionDate":"2021-12"},{"nctId":"NCT00392080","phase":"PHASE1","title":"A Study Of The Effect Of CJ-023,423 On The Incidence Of Stomach Ulcers","status":"COMPLETED","sponsor":"Pfizer","startDate":"2006-11","conditions":["Osteoarthritis"],"enrollment":340,"completionDate":"2008-02"}],"genericFilers":[],"latestUpdates":[],"manufacturing":[],"administration":{},"crossReferences":{"NDDF":"017766","UNII":"J9F5ZPH7NB","INN_ID":"9763","RXNORM":"1862951","UMLSCUI":"C4278621","ChEMBL_ID":"CHEMBL3039498","KEGG_DRUG":"D10638","DRUGBANK_ID":"DB12836","PUBCHEM_CID":"11677589","IUPHAR_LIGAND_ID":"5858","MESH_SUPPLEMENTAL_RECORD_UI":"C522837"},"formularyStatus":[],"_enricherVersion":"v2","developmentCodes":[],"ownershipHistory":[],"publicationCount":43,"therapeuticAreas":["Pain"],"biosimilarFilings":[],"recentPublications":[{"date":"2026 Feb 10","pmid":"41667566","title":"A noninferiority trial evaluating the efficacy of bedinvetmab compared to grapiprant for osteoarthritis-pain in dogs using force plate gait analysis.","journal":"Scientific reports"},{"date":"2026 Feb 23","pmid":"41467639","title":"Azoheteroarene-Modified Grapiprants Serving as Photoswitchable EP4 Antagonists.","journal":"Chemistry (Weinheim an der Bergstrasse, Germany)"},{"date":"2025 Dec","pmid":"41162752","title":"Structural insights into selective and dual antagonism of EP2 and EP4 prostaglandin receptors.","journal":"The EMBO journal"},{"date":"2026 Jan","pmid":"41044798","title":"Efficacy of combined grapiprant and tapentadol for analgesia in cats undergoing elective ovariohysterectomy.","journal":"Journal of feline medicine and surgery"},{"date":"2026 Mar 9","pmid":"40996819","title":"EP4/ANXA2 axis in pulmonary arterial hypertension: therapeutic implications.","journal":"European heart journal"}],"companionDiagnostics":[],"genericManufacturerList":[],"status":"discontinued","brandName":"GRAPIPRANT","companyName":"","companyId":"","modality":"Small molecule","firstApprovalDate":"","enrichmentLevel":3,"visitCount":0,"regulatoryByCountry":[{"country_code":"US","regulator":"FDA","status":"approved","approval_date":null,"mah":"","brand_name_local":null,"application_number":""},{"country_code":"CA","regulator":"Health Canada","status":"likely_approved","approval_date":null,"mah":null,"brand_name_local":null,"application_number":null},{"country_code":"IL","regulator":"MOH","status":"likely_approved","approval_date":null,"mah":null,"brand_name_local":null,"application_number":null},{"country_code":"SG","regulator":"HSA","status":"likely_approved","approval_date":null,"mah":null,"brand_name_local":null,"application_number":null},{"country_code":"AE","regulator":"MOH","status":"likely_approved","approval_date":null,"mah":null,"brand_name_local":null,"application_number":null},{"country_code":"KR","regulator":"MFDS","status":"likely_approved","approval_date":null,"mah":null,"brand_name_local":null,"application_number":null},{"country_code":"AU","regulator":"TGA","status":"likely_approved","approval_date":null,"mah":null,"brand_name_local":null,"application_number":null},{"country_code":"GB","regulator":"MHRA","status":"likely_approved","approval_date":null,"mah":null,"brand_name_local":null,"application_number":null}],"trialStats":{"total":0,"withResults":0},"verificationStatus":"partial","dataCompleteness":{"mechanism":true,"indications":false,"safety":false,"trials":true,"score":2}}