Synonyms: compound 2b [PMID: 21375264] | Ro 4402257 | Ro-4402257 | Ro4402257
Compound class:
Synthetic organic
Comment: Pamapimod is an ATP-competitive (Type I), orally bioavailable and highly selective inhibitor of p38α mitogen-activated protein kinase (MAPK14), that was developed for immunomodulatory potential [4].
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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Immunopharmacology Comments |
Pamapimod is a mitogen-activated protein kinase p38α/β (MAPK14/MAPK11) inhibitor that was developed for immunomodulatory potential [4]. Proof-of-concept of the clinical potential of p38 inhibition as an immunomodulatory modality in RA was published by Zhang et al. (2010) [6]. |
Immunopharmacology Disease | |||
Disease | X-Refs | Comment | References |
Rheumatoid arthritis |
Disease Ontology:
DOID:7148 OMIM: 180300 |
Phase 2 clinical studies evaluating pamapimod (RO4402257) in RA patients either as a monotherapy (NCT00303563), or as an adjunct to methotrexate therapy (NCT00316771) have been completed. As a monotherapy pamapimod was not as effective as methotrexate, and in patients on a stable methotrexate regimen pamapimod showed no significant improvement in efficacy outcomes compared to placebo. | 1 |