molecules of the month


glucocorticoid receptor modulator

phase II candidate for asthma

from soft drug PK optimization

Drug Metabolism and Disposition

AstraZeneca, Gothenburg, SE

Chemical structure of molecule velsecorat (AZD7594)
2 mins read

Velsecorat (AZD7594) is an inhaled, non-steroidal glucocorticoid receptor modulator and antedrug (soft drug) for treatment of asthma and other respiratory conditions that has completed several Ph. II studies. While the paper states that the results support progression into Ph. III studies, a Ph. III study does not appear to have started and velsecorat is no longer listed in AstraZeneca’s pipeline. Steroidal GR modulators antedrugs are widely used (e.g. fluticasone propionate, Flonase) but cannot be used for prolonged periods due to side effects including slowed growth in children, bone mineral loss, and type II diabetes in the elderly. Synthetic (non-steroidal) GR modulators may separate desired anti-inflammatory activities from adverse effects by differentially modifying DNA binding vs. coregulator recruitment activities. The velsecorat…

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