Effects of a T-type calcium channel blocker, ABT-639, on spontaneous activity in C-nociceptors in patients with painful diabetic neuropathy: a randomized controlled trial.

摘要: Abstract T-type calcium channels are a potential novel target for treatment of neuropathic pain such as painful diabetic neuropathy. ABT-639 is peripherally acting highly selective Cav3.2 channel blocker that has demonstrated analgesic efficacy in preclinical models and may have the to reduce spontaneous fiber activity. Microneurography unique technique directly assesses function peripheral sensory afferents measures abnormal activity single nociceptive C fibers. Abnormal C-nociceptors functions marker pain, reduction this could indicate efficacy. This randomized, double-blind controlled study evaluated effects 100-mg oral dose ABT-639, compared with placebo, on C-nociceptors, measured first time by microneurography adult patients Lidocaine was included placebo. Pharmacokinetics safety were evaluated. Thirty-nine total 56 analyzable identified 34 patients. There no significant differences C-nociceptor activities after vs Similar findings observed lidocaine clinically ABT-639. Further research targets neuropathy warranted. The utilization means measure human clinical studies opens new possibilities future compounds targeting nerve hyperexcitability. ClinicalTrials.gov identifier: NCT01589432.