Experimental Treatments: AZD 1981

AZD 1981 is an oral, non-steroidal, investigational therapy that has been studied in asthma patients. It is a CRTh2 receptor antagonist. The CRTh2 receptor is found on helper T-cells, which are essential in producing antibodies needed to control extracellular pathogens.

AZD 1981 studies

Helper T-cells have the CRTh2 receptor on their surface. Blocking a ligand in these receptors inhibits the movement of the cells, which is the potential therapeutic benefit for AZD 1981 for respiratory tract disorders.

Preclinical studies have shown that blocking the CRTh2 receptor inhibited inflammation induced by tobacco smoke and damage of the mucosa. Other studies have shown that the lungs of people with COPD have CRTh2 receptor production (expression) on respiratory mucosal epithelial cells and extracellular pathogens. Inhibition of the CRTh2 receptor could provide some therapeutic benefits to people with COPD.

Astra-Zeneca‘s AZD 1981 was well-tolerated in Phase 1 studies and has been studied in asthma. A Phase 2a study (NCT00690482) assessed the effectiveness and safety of AZD 1981 in people with moderate to severe COPD. Participants received either AZD 1981 1000 mg orally or a matching placebo twice daily for four weeks.

The primary objective of the study was to evaluate AZD 1981’s effectiveness compared with a placebo; the secondary objective was to evaluate its tolerability. However, there was no indication of a beneficial clinical effect of AZD 1981 in this group of participants, during the four weeks of treatment, although it was well tolerated and there were no safety concerns. Longer-term studies might reveal benefits in exacerbations or in slowing the rate of decline in lung function.


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