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Synonyms: Entocort® | Eohilia® (budesonide oral suspension) | Jorveza® | Pulmicort® | S-1320 | Uceris®
budesonide is an approved drug (FDA (1997), EMA (2018))
Compound class: Natural product or derivative
Comment: Budesonide is a glucocorticoid steroid. The INN document specifies that the approved drug consists of a racemic mixture of two epimers, based on the stereocentre of the carbon where the butyl chain meets the rest of the molecule. Our structure does not specify strereochemistry at this point and represents the mixture. The two epimers are represented by CID 40000 and CID 63006.
COVID-19: Results from a Phase 2 clinical trial have shown that a short duration administration of budesonide in the early phase of SARS-CoV-2 infection reduces both the likelihood of needing urgent medical care and time to recovery .
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: budesonide
|No information available.|
|Summary of Clinical Use|
|Used by inhalation to treat asthma and severe chronic obstructive pulmonary disease (COPD). EMA approvals (2014) are for products containing budesonide and formoterol. May be used to treat Crohn's disease (inflammatory bowel disease) , inflammatory skin disorders, allergic rhinitis and in an extended release formulation, ulcerative colitis . Symbicort® inhalers contain a fixed-dose formualtion of budesonide and the β2-adrenoceptor bronchodilator formoterol.
Oral formulations of this drug have EMA orphan disease approval to treat graft-versus-host disease (2006) and eosinophilic oesophagitis (2013). Takeda are developing their oral solution formulation of budesonide (Eohilia®, TAK-721) for the treatment for eosninophilic oesophagitis.
In October 2014, the US FDA approved a rectal foam formulation containing budesonide (Uceris®) for the treatment of ulcerative colitis.
|Mechanism Of Action and Pharmacodynamic Effects|
|Budesonide binds to the glucocorticoid receptor (GR) and the drug-receptor complex translocates to the nucleus and acts as transcription factor for target gene expression. The antiinflammatory actions of budesonide are thought to involve phospholipase A2 inhibitory proteins such as the annexins (aka lipocortins), which control the biosynthesis of the major mediators of inflammation, prostaglandins and leukotrienes. Increased expression of the gene coding for annexin-1 is one of the mechanisms by which glucocorticoids inhibit inflammation.|
|Clinical Trial ID||Title||Type||Source||Comment||References|
|NCT04416399||STerOids in COVID-19 Study||Phase 2 Interventional||University of Oxford||5|
|NCT04331470||Evaluation of Efficacy of Levamisole and Formoterol+Budesonide in Treatment of COVID-19||Phase 2/Phase 3 Interventional||Fasa University of Medical Sciences|
For extended ADME data see the following:
Electronic Medicines Compendium (eMC)