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Synonyms: XC-302 | XC302
Compound class: Synthetic organic
Comment: Puquitinib is an orally active, PI3 kinase inhibitor that induces autophagy by inhibiting the PI3K/AKT/mTOR signaling pathway. Puquitinib is selective for p110δ relative to other PI3K class I enzymes. It is a clinical lead developed for antitumour activity .
Puquitinib is a 'pseudo' INN, that takes the form of an INN, but has not been submitted to the World Health Organisation for ratification.
Ligand Activity Visualisation Charts
These 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.✖
|No information available.|
|Summary of Clinical Use|
|Puquitinib was found to be safe, with a promising tolerability and efficacy profile against relapsed/refractory non-Hodgkin's lymphoma in phase 1 clinical trial . It is currently undergoing phase 2 clinical trials in China .|
|Mechanism Of Action and Pharmacodynamic Effects|
|PI3Kδ and its downstream target, AKT, are frequently activated in leukemic blasts from patients with B‐cell malignancies or acute myeloid leukemia (AML), and selective inhibitors of the δ isoform show efficacy in certain B-cell malignancies [1-2]. PI3Kδ inhibition is suggested to release leukemia and lymphoma cells from their protective niche by disrupting signals from the lymphoid microenvironment .|