{"id":"mequitazine","rwe":[{"pmid":"40670084","year":"2025","title":"Second-Generation H(1)-Receptor Antagonists, Mequitazine, Azelastine and Desloratadine Activate Caspase-8, Caspase-3, and Gasdermin E and Induce Cell Death Showing Pyroptotic-Like Features in Macrophages at Excessively High Concentrations.","finding":"","journal":"Biological & pharmaceutical bulletin","studyType":"Clinical Study"},{"pmid":"39885859","year":"2025","title":"Removal of active pharmaceutical compounds in Primalan and Diane using pumpkin biochar: synthesis, characterization, and adsorption study.","finding":"","journal":"RSC advances","studyType":"Clinical Study"},{"pmid":"39183717","year":"2024","title":"Overriding Cage Effect in Electron Donor-Acceptor Photoactivation of Diaryliodonium Reagents: Synthesis of Chalcogenides.","finding":"","journal":"Chemistry (Weinheim an der Bergstrasse, Germany)","studyType":"Clinical Study"},{"pmid":"38962307","year":"2024","title":"Development of radioiodine-labeled mequitazine for evaluation of hepatic CYP2D activity.","finding":"","journal":"Frontiers in pharmacology","studyType":"Clinical Study"},{"pmid":"36105086","year":"2022","title":"Experimental verification and validation of immune biomarkers based on chromatin regulators in ischemic stroke.","finding":"","journal":"Frontiers in genetics","studyType":"Clinical Study"}],"tags":[{"label":"mequitazine","category":"class"},{"label":"Small Molecule","category":"modality"},{"label":"Muscarinic acetylcholine receptor M3","category":"target"},{"label":"CHRM3","category":"gene"},{"label":"CHRM1","category":"gene"},{"label":"HRH1","category":"gene"},{"label":"R06AD07","category":"atc"},{"label":"Active","category":"status"},{"label":"Histamine Agents","category":"pharmacology"},{"label":"Histamine Antagonists","category":"pharmacology"},{"label":"Histamine H1 Antagonists","category":"pharmacology"},{"label":"Neurotransmitter Agents","category":"pharmacology"}],"phase":"phase_2","safety":{"safetySignals":[{"llr":46.049,"date":"","count":6,"signal":"Tubulointerstitial nephritis and uveitis syndrome","source":"DrugCentral FAERS","actionTaken":"Reported 6 times (LLR=46)"}],"commonSideEffects":[{"effect":"Tubulointerstitial nephritis and uveitis syndrome","drugRate":"LLR 46","severity":"common"}]},"trials":[],"aliases":[],"patents":[],"pricing":[],"allNames":"nipolazin","offLabel":[],"synonyms":["mequitazine","metaplexan","nipolazin"],"timeline":[],"approvals":[],"brandName":"Nipolazin","ecosystem":[],"mechanism":{"target":"Histamine H1 receptor, Muscarinic acetylcholine receptor M1, Muscarinic acetylcholine receptor M2","targets":[{"gene":"CHRM3","source":"DrugCentral","target":"Muscarinic acetylcholine receptor M3","protein":"Muscarinic acetylcholine receptor M3"},{"gene":"CHRM1","source":"DrugCentral","target":"Muscarinic acetylcholine receptor M1","protein":"Muscarinic acetylcholine receptor M1"},{"gene":"HRH1","source":"DrugCentral","target":"Histamine H1 receptor","protein":"Histamine H1 receptor"},{"gene":"CHRM5","source":"DrugCentral","target":"Muscarinic acetylcholine receptor M5","protein":"Muscarinic acetylcholine receptor M5"},{"gene":"CHRM4","source":"DrugCentral","target":"Muscarinic acetylcholine receptor M4","protein":"Muscarinic acetylcholine receptor M4"},{"gene":"CHRM2","source":"DrugCentral","target":"Muscarinic acetylcholine receptor M2","protein":"Muscarinic acetylcholine receptor M2"}],"modality":"Small Molecule","drugClass":"mequitazine","explanation":"Imagine your body has a system of messengers, called neurotransmitters, that help different parts work together. Acetylcholine is one of these messengers that helps control things like heart rate and breathing. Mequitazine blocks the action of acetylcholine at the M3 receptor, which can help reduce symptoms of allergic conditions.","oneSentence":"Mequitazine works by blocking the action of acetylcholine at the muscarinic acetylcholine receptor M3.","technicalDetail":"Mequitazine acts as a competitive antagonist at the M3 muscarinic acetylcholine receptor, inhibiting the binding of acetylcholine and subsequent downstream signaling pathways."},"commercial":{},"references":[{"id":1,"url":"https://drugcentral.org/drugcard/1707","fields":["approvals","synonyms","ATC","PK","indications","contraindications","DDIs","targets","patents","FAERS"],"source":"DrugCentral"},{"id":2,"url":"https://pubmed.ncbi.nlm.nih.gov/?term=MEQUITAZINE","fields":["publications"],"source":"PubMed/NCBI"}],"_enrichedAt":"2026-03-30T12:35:40.442939","biosimilars":[],"competitors":[{"drugName":"alimemazine","drugSlug":"alimemazine","fdaApproval":"","relationship":"same-class"},{"drugName":"promethazine","drugSlug":"promethazine","fdaApproval":"1951-03-29","genericCount":48,"patentStatus":"Off-patent — generic available","relationship":"same-class"},{"drugName":"thiethylperazine","drugSlug":"thiethylperazine","fdaApproval":"1961-07-18","patentStatus":"Unknown","relationship":"same-class"},{"drugName":"methdilazine","drugSlug":"methdilazine","fdaApproval":"","patentStatus":"Unknown","relationship":"same-class"}],"dataSources":[{"url":"https://drugcentral.org","name":"DrugCentral","fields":["indications","contraindications","safety","target","drugInteractions"],"retrievedDate":"2026-04-07"}],"genericName":"mequitazine","indications":{"approved":[],"offLabel":[],"pipeline":[]},"drugCategory":"active","labelChanges":[],"relatedDrugs":[{"drugId":"alimemazine","brandName":"alimemazine","genericName":"alimemazine","approvalYear":"","relationship":"same-class"},{"drugId":"promethazine","brandName":"promethazine","genericName":"promethazine","approvalYear":"1951","relationship":"same-class"},{"drugId":"thiethylperazine","brandName":"thiethylperazine","genericName":"thiethylperazine","approvalYear":"1961","relationship":"same-class"},{"drugId":"methdilazine","brandName":"methdilazine","genericName":"methdilazine","approvalYear":"","relationship":"same-class"}],"trialDetails":[],"genericFilers":[],"latestUpdates":[],"manufacturing":[],"administration":{},"crossReferences":{"NDDF":"004003","UNII":"Y463242LY2","CHEBI":"CHEBI:31821","INN_ID":"3672","RXNORM":"29528","UMLSCUI":"C0065972","ChEMBL_ID":"CHEMBL73451","KEGG_DRUG":"D01324","DRUGBANK_ID":"DB01071","PUBCHEM_CID":"4066","SNOMEDCT_US":"320756004","MESH_SUPPLEMENTAL_RECORD_UI":"C006069"},"formularyStatus":[],"_enricherVersion":"v2","developmentCodes":[],"ownershipHistory":[],"pharmacokinetics":{"source":"DrugCentral","fractionUnbound":"0.036%"},"publicationCount":136,"therapeuticAreas":["Neuroscience"],"atcClassification":{"source":"DrugCentral","atcCode":"R06AD07","allCodes":["R06AD07"]},"biosimilarFilings":[],"recentPublications":[{"date":"2025","pmid":"40670084","title":"Second-Generation H(1)-Receptor Antagonists, Mequitazine, Azelastine and Desloratadine Activate Caspase-8, Caspase-3, and Gasdermin E and Induce Cell Death Showing Pyroptotic-Like Features in Macrophages at Excessively High Concentrations.","journal":"Biological & pharmaceutical bulletin"},{"date":"2025 Jan 29","pmid":"39885859","title":"Removal of active pharmaceutical compounds in Primalan and Diane using pumpkin biochar: synthesis, characterization, and adsorption study.","journal":"RSC advances"},{"date":"2024 Nov 4","pmid":"39183717","title":"Overriding Cage Effect in Electron Donor-Acceptor Photoactivation of Diaryliodonium Reagents: Synthesis of Chalcogenides.","journal":"Chemistry (Weinheim an der Bergstrasse, Germany)"},{"date":"2024","pmid":"38962307","title":"Development of radioiodine-labeled mequitazine for evaluation of hepatic CYP2D activity.","journal":"Frontiers in pharmacology"},{"date":"2022","pmid":"36105086","title":"Experimental verification and validation of immune biomarkers based on chromatin regulators in ischemic stroke.","journal":"Frontiers in genetics"}],"companionDiagnostics":[],"genericManufacturerList":[],"status":"active","companyName":"","companyId":"","modality":"Small molecule","firstApprovalDate":"","aiSummary":"Nipolazin, also known as mequitazine, is a small molecule drug that targets the muscarinic acetylcholine receptor M3. It belongs to the mequitazine class and works by blocking the action of acetylcholine at this receptor, which is involved in various physiological processes. Mequitazine is used to treat allergic conditions, but its exact indications and commercial status are unknown. As a result, its half-life, bioavailability, and generic manufacturers are also unclear. Further research is needed to determine its full potential and safety profile.","enrichmentLevel":3,"visitCount":0,"trialStats":{"total":0,"withResults":0},"verificationStatus":"partial","dataCompleteness":{"mechanism":true,"indications":false,"safety":true,"trials":false,"score":2}}