AZD1386 / AstraZeneca - LARVOL DELTA

Randomized clinical trial: inhibition of the TRPV1 system in patients with nonerosive gastroesophageal reflux disease and a partial response to PPI treatment is not associated with analgesia to esophageal experimental pain (Scand J Gastroenterol) - P2, N=14; NCT01019928; Pubmed ID: 23320520; "In the esophagus AZD1386 did not significantly change the moderate pain threshold for heat [-3%, 95% confidence interval (CI), -22;20%], distension (-11%, 95% CI, -28;10%), or electrical current (6%, 95% CI, -10;25%). Mean cutaneous heat tolerance increased by 4.9°C (95% CI, 3.7;6.2°C). AZD1386 increased the maximum body temperature by a mean of 0.59°C (95% CI, 0.40-0.79°C), normalizing within 4 h."

P2 data • Pain

TRPV1 antagonistic analgesic effect: A randomized study of AZD1386 in pain following third molar extraction (Pain Journal Online) - P2, N=103; NCT00672646; Sponsor: Astra Zeneca; "SPID%0-8hrs showed no significant difference between AZD1386 and placebo (p=0.132) but between naproxen and placebo (p=0.038). AZD1386 had a rapid short lasting analgesia and compared to placebo, PID% was significantly higher (p⩽0.026) at 0.25, 0.50, 0.75 and 1.00 hours after drug administration...AZD1386 was well tolerated with a rapid analgesia that was short lasting despite sustained plasma concentration."

P2 data • Pain

Hyperthermia induced by transient receptor potential vanilloid-1 (TRPV1) antagonists in human clinical trials: Insights from mathematical modeling and meta-analysis. (PubMed, Pharmacol Ther) - "We also conducted a meta-analysis of T data from human trials and found that polymodal TRPV1 antagonists (ABT-102, AZD1386, and V116517) increase T, whereas the mode-selective blocker NEO6860 does not. Several strategies of harnessing the thermoregulatory effects of TRPV1 antagonists in humans are discussed."

Journal • Retrospective data • Review