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Synonyms: CAL-101/CAL101 | GS-1101 | Zydelig®
idelalisib is an approved drug (FDA & EMA (2014))
Compound class: Synthetic organic
Comment: Idelalisib is highly selective and potent oral inhibitor of phosphoinositide 3-kinase (PI3K) δ.
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.✖
View more information in the IUPHAR Pharmacology Education Project: idelalisib
|No information available.|
|Summary of Clinical Use|
|Idelalisib is a treatmet for difficult to treat leukemia and lymphomas. The potential of this drug was highlighted by the early termination of a phase 3 clinical trial, so that all participants could be given the drug . Idelalisib was approved in July 2014, for patients with relapsed chronic lymphocytic leukemia (CLL), in combination with rituximab. The FDA also granted the drug accelerated approval for the treatment of patients with relapsed follicular B-cell non-Hodgkin lymphoma (FL) and relapsed small lymphocytic lymphoma (SLL), particularly indicated for patients who have received at least two prior systemic therapies.
To view a full list of trials registered with ClinicalTrials.gov assessing idelalisib, click here.
|Mechanism Of Action and Pharmacodynamic Effects|
|PI3Kδ signaling is critical for the activation, proliferation, survival and trafficking of B lymphocytes and is hyperactive in many B-cell malignancies. Idelalisib inhibits this activity, ultimately leading to death of cancer cells.|
For extended ADME data see the following:
Electronic Medicines Compendium (eMC)
European Medicines Agency (EMA)