{"id":"exisulind","rwe":[{"pmid":"40076563","year":"2025","title":"Rational Design and Optimization of Novel PDE5 Inhibitors for Targeted Colorectal Cancer Therapy: An In Silico Approach.","finding":"","journal":"International journal of molecular sciences","studyType":"Clinical Study"},{"pmid":"38911382","year":"2024","title":"Comprehensive analysis of the clinical significance and molecular mechanism of T-box transcription factor 3 in osteosarcoma.","finding":"","journal":"Journal of Cancer","studyType":"Clinical Study"},{"pmid":"38621585","year":"2024","title":"Targeting cellular senescence as a therapeutic vulnerability in gastric cancer.","finding":"","journal":"Life sciences","studyType":"Clinical Study"},{"pmid":"38280440","year":"2024","title":"Identification of Fasudil as a collaborator to promote the anti-tumor effect of lenvatinib in hepatocellular carcinoma by inhibiting GLI2-mediated hedgehog signaling pathway.","finding":"","journal":"Pharmacological research","studyType":"Clinical Study"},{"pmid":"37539055","year":"2023","title":"Unveiling the key genes, environmental toxins, and drug exposures in modulating the severity of ulcerative colitis: a comprehensive analysis.","finding":"","journal":"Frontiers in immunology","studyType":"Clinical Study"}],"tags":[{"label":"Small Molecule","category":"modality"},{"label":"Endothelin-1 receptor","category":"target"},{"label":"EDNRA","category":"gene"},{"label":"MAPK1","category":"gene"},{"label":"Active","category":"status"},{"label":"Analgesics","category":"pharmacology"},{"label":"Analgesics, Non-Narcotic","category":"pharmacology"},{"label":"Anti-Inflammatory Agents","category":"pharmacology"},{"label":"Anti-Inflammatory Agents, Non-Steroidal","category":"pharmacology"},{"label":"Anticarcinogenic Agents","category":"pharmacology"},{"label":"Antineoplastic Agents","category":"pharmacology"},{"label":"Antirheumatic Agents","category":"pharmacology"},{"label":"Cyclooxygenase Inhibitors","category":"pharmacology"},{"label":"Enzyme Inhibitors","category":"pharmacology"},{"label":"Peripheral Nervous System Agents","category":"pharmacology"},{"label":"Protective Agents","category":"pharmacology"},{"label":"Sensory System Agents","category":"pharmacology"}],"phase":"discontinued","safety":{},"trials":[],"aliases":[],"patents":[],"pricing":[],"allNames":"aptosyn","offLabel":[],"synonyms":["exisulind","aptosyn","sulindac sulfone"],"timeline":[],"aiSummary":"Aptosyn (Exisulind) is a small molecule modality targeting the endothelin-1 receptor. It is currently owned by a pharmaceutical company, but its original developer is not specified. Aptosyn's commercial status and approved indications are unknown. The drug's half-life, bioavailability, and generic manufacturers are also not publicly available. As a result, its off-patent status cannot be confirmed.","approvals":[],"brandName":"Aptosyn","ecosystem":[],"mechanism":{"target":"Mitogen-activated protein kinase 1, Endothelin-1 receptor, Aldose reductase","targets":[{"gene":"EDNRA","source":"DrugCentral","target":"Endothelin-1 receptor","protein":"Endothelin-1 receptor"},{"gene":"MAPK1","source":"DrugCentral","target":"Mitogen-activated protein kinase 1","protein":"Mitogen-activated protein kinase 1"}],"modality":"Small Molecule","explanation":"Think of Aptosyn like a key that fits into a lock on the surface of cells. When it binds to the endothelin-1 receptor, it can help slow down or stop the growth of certain cells that might be contributing to a disease. This can be helpful in treating conditions where cell growth is out of control.","oneSentence":"Aptosyn works by binding to the endothelin-1 receptor, which is involved in cell growth and proliferation.","technicalDetail":"Aptosyn acts as a selective antagonist of the endothelin-1 receptor, which is a G-protein coupled receptor involved in the regulation of cell growth and proliferation. By binding to this receptor, Aptosyn can inhibit the downstream signaling pathways that promote cell growth and survival."},"commercial":{},"references":[{"id":1,"url":"https://drugcentral.org/drugcard/3219","fields":["approvals","synonyms","ATC","PK","indications","contraindications","DDIs","targets","patents","FAERS"],"source":"DrugCentral"},{"id":2,"url":"https://clinicaltrials.gov/search?intr=EXISULIND","fields":["trials"],"source":"ClinicalTrials.gov"},{"id":3,"url":"https://pubmed.ncbi.nlm.nih.gov/?term=EXISULIND","fields":["publications"],"source":"PubMed/NCBI"}],"_enrichedAt":"2026-03-30T11:12:25.330986","biosimilars":[],"competitors":[{"drugName":"ambrisentan","drugSlug":"ambrisentan","fdaApproval":"2007-06-15","patentExpiry":"Oct 14, 2031","patentStatus":"Patent protected","relationship":"same-target"},{"drugName":"amiodarone","drugSlug":"amiodarone","fdaApproval":"1985-12-24","patentExpiry":"Mar 13, 2029","patentStatus":"Patent 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