Synonyms: Imbruvica® | PCI-32765
ibrutinib is an approved drug (FDA (2013), EMA (2014))
Compound class:
Synthetic organic
Comment: Ibrutinib is a clinically used inhibitor of Bruton's tyrosine kinase. It was originally approved with breakthrough therapy designation through the FDA's accelerated approval program.
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. ✖View more information in the IUPHAR Pharmacology Education Project: ibrutinib |
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Immunopharmacology Comments |
Ibrutinib inhibits BTK-mediated regulation of critical B cell pro-survival mechanisms, leading to decreased B cell activity and increased B cell apoptosis. This mechanism is exploited clinically for the treatment of B cell malignancies and to manage chronic GvHD. |
Immunopharmacology Disease | |||
Disease | X-Refs | Comment | References |
Graft versus host disease | Approved drug for chronic GvHD. | ||
Chronic lymphocytic leukemia |
Disease Ontology:
DOID:1040 OMIM: 151400 Orphanet: ORPHA67038 |
Approved drug for CLL. | |
Mantle cell lymphoma |
Disease Ontology:
DOID:0050746 Orphanet: ORPHA52416 |
Approved drug for MCL. | |
Waldenstrom macroglobulinemia |
Disease Ontology:
DOID:0050747 OMIM: 153600 Orphanet: ORPHA33226 |
Approved drug for WM. |