Synonyms: MK-3795 | MK3795 | PT-2385
Compound class:
Synthetic organic
Comment: PT2385 is a small-molecule antagonist of HIF2α that was designed for antitumour activity [1,3-5]. The molecule binds to an allosteric site on HIF2α and blocks its interaction with its dimerisation partner ARNT (aryl hydrocarbon receptor nuclear translocator, a.k.a. HIF1β). This action inhibits expression of HIF2α-dependent genes (e.g., VEGFA, PAI-1, and cyclin D1) in renal cancer models (cell lines and xenografts).
Ligand Activity Visualisation ChartsThese are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts. ✖ |
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No information available. |
Summary of Clinical Use |
PT2385 was advanced to clinical evaluations in patients with renal cell carcinomas or glioblastoma. |
Clinical Trials | |||||
Clinical Trial ID | Title | Type | Source | Comment | References |
NCT03216499 | HIF-2 Alpha Inhibitor PT2385 in Treating Patients With Recurrent Glioblastoma | Phase 2 Interventional | Sidney Kimmel Comprehensive Cancer Center at Johns Hopkins | ||
NCT02293980 | A Phase 1, Dose-Escalation Trial of PT2385 Tablets In Patients With Advanced Clear Cell Renal Cell Carcinoma (MK-3795-001) | Phase 1 Interventional | Peloton Therapeutics, Inc. | 2 |