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Synonyms: Celsentri® | Selzentry® | UK 427857 | UK-427,857
maraviroc is an approved drug (EMA and FDA (2007))
Compound class: Synthetic organic
Comment: Maraviroc is a small molecule antagonist of the C-C chemokine receptor type 5 (CCR5) expressed on T cells.
The stereochemistry of maraviroc as specified by the PDB compound link varies from that specified in our structure and that of CID 3002977.The compound is represented on ChEMBL by CHEMBL1201187.
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|
|Maraviroc is approved for use in combination antiretroviral treatment of patients infected with CCR5-tropic HIV-1 virus.
Maraviroc-induced CCR5 blockade was investigated for action in treating rheumatoid arthritis, but with discouraging clinical trial results. Other CCR5 antagonists (AZD5672 and ancriviroc) have also proven ineffective in RA clinical trials 
|Mechanism Of Action and Pharmacodynamic Effects|
|CCR5 is a co-receptor for HIV-1 and other viruses, allowing these viruses to enter cells. Maraviroc selectively antagonises the interaction between the human CCR5 receptor and HIV-1 envelope glycoprotein gp120. This prevents the CCR5-tropic HIV-1 from entering the cells . Maraviroc has also been shown to inhibit leukocyte trafficking and mucosal inflammation in a mouse colitis model , suggesting a CCR5-based interventional strategy with therapeutic potential in inflammatory bowel diseases.|
For extended ADME data see the following:
Electronic Medicines Compendium (eMC)
European Medicines Agency (EMA)