Table 2.

Randomized studies of oral antagonists targeting the human P2X7 receptor

Antagonist to human P2X7	Trial	Numbers randomized	Adverse events	Drug dosage	Drug efficacy	Markers of inflammation	Ref
AZD9056	Phase 2a study in rheumatoid arthritis	n = 71	Mild nausea, vomiting, diarrhoea	100 and 400 mg daily for 4 weeks	Improvement in swollen, tender joint counts	No improvement	Keystone et al. (2012)
AZD9056	Phase 2b study in rheumatoid arthritis	n = 385	Nausea, vomiting, diarrhoea	50, 100, 200 and 400 mg daily for 24 weeks	No improvement in ACR20 criteria	No Improvement	Keystone et al. (2012)
AZD9056	Phase 2a study in active Crohn's disease	n = 34	Nausea, diarrhoea	200 mg daily for 4 weeks	Decrease in disease pain	No Improvement	Eser et al. (2015)
CE‐224535	Phase 2a study in rheumatoid arthritis	n = 153	Nausea, diarrhoea	500 mg BID for 12 weeks	No efficacy in ACR20 criteria	No improvement	Stock et al. (2012)
GSK1482160	Randomized placebo‐controlled in healthy humans	n = 24	Headache, arrhythmia in one subject	Escalating, single doses of up to 1 g on four occasions	No progression to clinical trials	No in vivo markers measured	Ali et al. (2013)