Inhaled glucocorticoids are the main treatment for asthma. In fact, this therapeutic agent can effectively interfere with many of asthma’s pathogenic circuits. Of these drugs, Budesonide has probably been the most used molecule in experimental research and clinical practice over the past few decades.

Budesonide, an inhaled glucocortical steroid, is an orally active glucocorticoid receptor agonist.

Budesonide is an inhaled glucocorticoid steroid that acts as an orally active glucocorticoid receptor agonist. It is widely used as an anti-inflammatory agent for the treatment of asthma.

Here’s mechanism of action:
Budesonide is a liposoluble molecule that easily crosses cell membranes. It binds to the glucocorticoid receptor (GR) in the cytoplasm. Upon binding, the GR undergoes a conformational change and translocates into the nucleus. In the nucleus, activated GRs bind to specific DNA sequences called glucocorticoid response elements (GRE). This binding enhances the transcription of anti-inflammatory proteins and inhibits pro-inflammatory transcription factors like NF-κB and AP-1.

Budesonide has a high receptor-binding affinity and a relative GR affinity of 935. It exhibits a potent transcriptional effect, surpassing other inhaled glucocorticoids. Budesonide can also interact with NF-κB and AP-1 proteins, further suppressing their pro-inflammatory functions.

On the other hand, Budesonide decreases the size of lung tumors, reverses DNA hypomethylation and modulates mRNA expression of genes. Studies have shown that budesonide can decrease the size of lung tumors and reverse DNA hypomethylation. It has been found to modulate mRNA expression of genes and suppress the activation of the NLRP3 inflammasome. Budesonide pretreatment has shown promising results in reducing lung injury in mice with acute lung injury (ALI).

References:

[1] Pelaia G, et al. Pulm Pharmacol Ther. 2016 Oct; 40:15-21.

[2] Dong L, et al. J Immunol Res. 2019 Feb 27;2019:7264383.

[3] Pereira MA, et al. Int J Cancer. 2007 Mar 1;120(5):1150-3.