Synonyms: compound 20 [PMID: 31749910] | IBI376 | INCB-050465
Compound class:
Synthetic organic
Comment: Parsaclisib (INCB050465) is a PI3Kδ inhibitor that was developed by Incyte Corporation as an antineoplastic and immunomodulatory agent, as claimed in their patent WO2014134426A1 [1]. The chemical structure is one of those claimed in patent WO2013033569A1, but it was not immediately clear which example it was from a mixture of diastereoisomers 345-348 (347 and 348 had the highest inhibitory potency vs. PI3Kδ and 347 was tested in vivo) [2]. The 2019 disclosure by Yue et al. confirmed the structure as patent example 346 [4]. Preclinical and phase 1/2 clinical evidence suggests that compared to first-generation PI3Kδ inhibitors, parsaclisib has reduced hepatotoxicity [3].
![]() 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 ![]() |
Parsaclisib (INCB50465) has advanced to Phase 2 clinical trial. It is being evaluated in multiple studies looking at its efficacy in various lymphomas and B cell malignancies, and in Sjögren's syndrome and autoimmune hemolytic anemia. NCT04142554 will evaluate parsaclisib in patients with triple negative or HER2+ breast cancers. Click here to link to ClinicalTrials.gov's full list of INCB50465 trials. |
Mechanism Of Action and Pharmacodynamic Effects ![]() |
Parsaclisib's antitumour mechanism involves targeting PI3Kδ-mediated proliferative signalling in malignant B cells and inhibiting Treg immunosuppression in the tumour microenvironment [3-4]. |
Clinical Trials | |||||
Clinical Trial ID | Title | Type | Source | Comment | References |
NCT03627065 | A Study of INCB050465 in Primary Sjögren's Syndrome | Phase 2 Interventional | Incyte Corporation | ||
NCT03538041 | A Study of INCB050465 in Participants With Autoimmune Hemolytic Anemia | Phase 2 Interventional | Incyte Corporation | ||
NCT02718300 | A Study of INCB050465 in Combination With Ruxolitinib in Subjects With Myelofibrosis | Phase 2 Interventional | Incyte Corporation | ||
NCT03235544 | A Study of INCB050465 in Relapsed or Refractory Mantle Cell Lymphoma Previously Treated With or Without a BTK Inhibitor (CITADEL-205) | Phase 2 Interventional | Incyte Corporation |