{"id":"iclaprim","rwe":[{"pmid":"40021806","year":"2025","title":"High throughput screening identifies potential inhibitors targeting trimethoprim resistant DfrA1 protein in Klebsiella pneumoniae and Escherichia coli.","finding":"","journal":"Scientific reports","studyType":"Clinical Study"},{"pmid":"39102054","year":"2024","title":"Anti-virulence potential of iclaprim, a novel folic acid synthesis inhibitor, against Staphylococcus aureus.","finding":"","journal":"Applied microbiology and biotechnology","studyType":"Clinical Study"},{"pmid":"36935372","year":"2023","title":"Resistance to antibacterial antifolates in multidrug-resistant Staphylococcus aureus: prevalence estimates and genetic basis.","finding":"","journal":"The Journal of antimicrobial chemotherapy","studyType":"Clinical Study"},{"pmid":"36628360","year":"2023","title":"Iclaprim mesylate displaying a hydrogen-bonded mol-ecular tape.","finding":"","journal":"Acta crystallographica. Section E, Crystallographic communications","studyType":"Clinical Study"},{"pmid":"35928265","year":"2022","title":"Efficacy and Safety of Iclaprim for the Treatment of Skin Structures and Soft Tissue Infections: A Methodological Framework.","finding":"","journal":"Frontiers in pharmacology","studyType":"Clinical Study"}],"tags":[{"label":"iclaprim","category":"class"},{"label":"Small Molecule","category":"modality"},{"label":"Dihydrofolate reductase","category":"target"},{"label":"DHFR","category":"gene"},{"label":"J01EA03","category":"atc"},{"label":"Active","category":"status"},{"label":"Enzyme Inhibitors","category":"pharmacology"},{"label":"Folic Acid Antagonists","category":"pharmacology"}],"phase":"discontinued","safety":{},"trials":[],"aliases":[],"patents":[],"pricing":[],"allNames":["iclaprim","iclaprim mesylate","iclaprim mesilate"],"offLabel":[],"synonyms":["iclaprim","iclaprim mesylate","iclaprim mesilate"],"timeline":[],"aiSummary":"ICLAPRIM is a small molecule drug that targets dihydrofolate reductase, an enzyme involved in DNA synthesis. It is classified as an iclaprim and has been developed to treat bacterial infections. However, its commercial status and approved indications are unknown. As a result, its half-life, bioavailability, and generic manufacturers are also not available. Further research is needed to determine its current status and potential applications.","approvals":[],"ecosystem":[],"mechanism":{"target":"Dihydrofolate reductase, Dihydrofolate reductase","targets":[{"gene":"DHFR","source":"DrugCentral","target":"Dihydrofolate reductase","protein":"Dihydrofolate reductase"}],"modality":"Small Molecule","drugClass":"iclaprim","explanation":"Think of it like a roadblock for bacteria. ICLAPRIM blocks the enzyme that helps bacteria make new DNA, which is necessary for them to grow and multiply. This makes it harder for the bacteria to cause infections.","oneSentence":"ICLAPRIM works by inhibiting the enzyme dihydrofolate reductase, which is essential for bacterial DNA synthesis.","technicalDetail":"ICLAPRIM specifically binds to the active site of dihydrofolate reductase, preventing the conversion of dihydrofolate to tetrahydrofolate, which is a crucial step in the synthesis of purines and pyrimidines, the building blocks of DNA."},"commercial":{},"references":[{"id":1,"url":"https://drugcentral.org/drugcard/4573","fields":["approvals","synonyms","ATC","PK","indications","contraindications","DDIs","targets","patents","FAERS"],"source":"DrugCentral"},{"id":2,"url":"https://clinicaltrials.gov/search?intr=ICLAPRIM","fields":["trials"],"source":"ClinicalTrials.gov"},{"id":3,"url":"https://pubmed.ncbi.nlm.nih.gov/?term=ICLAPRIM","fields":["publications"],"source":"PubMed/NCBI"}],"_enrichedAt":"2026-03-30T13:55:04.721689","biosimilars":[],"competitors":[{"drugName":"trimethoprim","drugSlug":"trimethoprim","fdaApproval":"1973-07-30","genericCount":5,"patentStatus":"Off-patent — generic available","relationship":"same-class"}],"dataSources":[{"url":"https://drugcentral.org","name":"DrugCentral","fields":["indications","contraindications","safety","target","drugInteractions"],"retrievedDate":"2026-04-07"}],"genericName":"iclaprim","indications":{"approved":[],"offLabel":[],"pipeline":[]},"drugCategory":"active","labelChanges":[],"relatedDrugs":[{"drugId":"trimethoprim","brandName":"trimethoprim","genericName":"trimethoprim","approvalYear":"1973","relationship":"same-class"}],"trialDetails":[{"nctId":"NCT04989946","phase":"PHASE1,PHASE2","title":"Androgen Deprivation, With or Without pTVG-AR, and With or Without T-Cell Checkpoint Blockade, in Patients With Newly Diagnosed, High-Risk Prostate Cancer","status":"RECRUITING","sponsor":"University of Wisconsin, Madison","startDate":"2021-12-16","conditions":["Prostate Cancer"],"enrollment":60,"completionDate":"2028-12"},{"nctId":"NCT02607618","phase":"PHASE3","title":"Phase 3 Study to Evaluate Safety and Efficacy of Iclaprim Versus Vancomycin for ABSSSI: REVIVE-2","status":"COMPLETED","sponsor":"Motif Bio","startDate":"2015-11","conditions":["Skin Structures and Soft Tissue Infections"],"enrollment":613,"completionDate":"2017-08-08"},{"nctId":"NCT02600611","phase":"PHASE3","title":"Phase 3 Study to Evaluate Safety and Efficacy of Iclaprim Versus Vancomycin for ABSSSI: REVIVE-1","status":"COMPLETED","sponsor":"Motif Bio","startDate":"2015-11-01","conditions":["Skin Structures and Soft Tissue Infections"],"enrollment":600,"completionDate":"2017-01-30"},{"nctId":"NCT00543608","phase":"PHASE2","title":"Clinical Efficacy of Intravenous Iclaprim Versus Vancomycin in the Treatment of Hospital-Acquired, Ventilator-Associated, or Health-Care-Associated Pneumonia","status":"TERMINATED","sponsor":"Arpida AG","startDate":"2007-11","conditions":["Hospital-Acquired Pneumonia","Ventilator-Associated Pneumonia","Health-Care-Associated Pneumonia"],"enrollment":135,"completionDate":"2009-05"},{"nctId":"NCT00299520","phase":"PHASE3","title":"Phase 3 Safety and Efficacy Study of I.V. Iclaprim v Linezolid in cSSSI (ASSIST-1)","status":"COMPLETED","sponsor":"Arpida AG","startDate":"2005-06","conditions":["Complicated Skin and Skin Structure Infection"],"enrollment":0,"completionDate":"2006-07"},{"nctId":"NCT00303550","phase":"PHASE3","title":"Study of Intravenous (I.V.) Iclaprim Versus Linezolid in Complicated Skin and Skin Structure Infections [cSSSI] (ASSIST-2)","status":"COMPLETED","sponsor":"Arpida AG","startDate":"2006-03","conditions":["Skin Diseases, Bacterial"],"enrollment":0,"completionDate":""}],"genericFilers":[],"latestUpdates":[],"manufacturing":[],"administration":{},"crossReferences":{"UNII":"42445HUU0O","INN_ID":"8315","UMLSCUI":"C3654387","ChEMBL_ID":"CHEMBL134561","KEGG_DRUG":"D08337","DRUGBANK_ID":"DB06358","PUBCHEM_CID":"213043","SNOMEDCT_US":"725576004","IUPHAR_LIGAND_ID":"10820","SECONDARY_CAS_RN":"474793-41-4","MESH_SUPPLEMENTAL_RECORD_UI":"C486448"},"formularyStatus":[],"_enricherVersion":"v2","developmentCodes":[],"ownershipHistory":[],"publicationCount":93,"therapeuticAreas":["Infectious Disease"],"atcClassification":{"source":"DrugCentral","atcCode":"J01EA03","allCodes":["J01EA03"]},"biosimilarFilings":[],"recentPublications":[{"date":"2025 Feb 28","pmid":"40021806","title":"High throughput screening identifies potential inhibitors targeting trimethoprim resistant DfrA1 protein in Klebsiella pneumoniae and Escherichia coli.","journal":"Scientific reports"},{"date":"2024 Aug 5","pmid":"39102054","title":"Anti-virulence potential of iclaprim, a novel folic acid synthesis inhibitor, against Staphylococcus aureus.","journal":"Applied microbiology and biotechnology"},{"date":"2023 May 3","pmid":"36935372","title":"Resistance to antibacterial antifolates in multidrug-resistant Staphylococcus aureus: prevalence estimates and genetic basis.","journal":"The Journal of antimicrobial chemotherapy"},{"date":"2023 Jan 1","pmid":"36628360","title":"Iclaprim mesylate displaying a hydrogen-bonded mol-ecular tape.","journal":"Acta crystallographica. Section E, Crystallographic communications"},{"date":"2022","pmid":"35928265","title":"Efficacy and Safety of Iclaprim for the Treatment of Skin Structures and Soft Tissue Infections: A Methodological Framework.","journal":"Frontiers in pharmacology"}],"companionDiagnostics":[],"genericManufacturerList":[],"status":"discontinued","brandName":"ICLAPRIM","companyName":"","companyId":"","modality":"Small molecule","firstApprovalDate":"","enrichmentLevel":3,"visitCount":1,"trialStats":{"total":0,"withResults":0},"verificationStatus":"partial","dataCompleteness":{"mechanism":true,"indications":false,"safety":false,"trials":true,"score":2}}