Review Article

The Purinergic System and Glial Cells: Emerging Costars in Nociception

Table 1

Summary of past and current clinical trials evaluating purinergic ligands in pain.

Name of ligandCompanyClinical trial numberType of painMain outcomes

AF219
(P2X3 antagonist)
Afferent PharmaceuticalsNCT01554579Osteoarthritis of the kneeNo published results yet
NCT01569438Interstitial cystitis/bladder pain syndromeNo published results yet

CE-224,535
(P2X7 antagonist)
PfizerNCT00628095Rheumatoid arthritisCE-224,535 was not efficacious, compared with placebo, for the treatment of RA in patients with an inadequate response to metotrexate [72]
NCT00418782Osteoarthritis of the kneeCE-224,535 failed to demonstrate efficacy in a 2-week study of knee pain in osteoarthritis patients

AZD9056AstraZenecaNCT00520572Rheumatoid arthritisAZD9056 does not have significant efficacy in the treatment of RA [73]

GSK1482160
(P2X7 antagonist)
GlaxoSmithKlineNCT00849134“First-in-human” study to assess the pharmacokinetic profile of the drugNo major safety or tolerability concerns were identified in this study. Nevertheless, monitoring the release of IL-1β in subjects led to the decision to discontinue drug development for inflammatory pain conditions [74]

Adenosine
(e.v.)
Wake Forest School of MedicineNCT00349921Neuropathic pain (comparison with clonidine)No published results yet
Xsira PharmaceuticalsNCT00298636Perioperative pain (hysterectomy/myomectomy)No published results yet

GW493838GlaxoSmithKlineNCT00376454Neuropathic pain as a result of postherpetic neuralgia or nerve injuryNo published results yet