ABT-102 / AbbVie - LARVOL DELTA

Effects of the TRPV1 antagonist ABT-102 on body temperature in healthy volunteers: Pharmacokinetic/pharmacodynamic analysis of three phase 1 trials (Br J Clin Pharmacol) - P1, N=NA; The model estimates were: baseline oral body temperature, 36.3 (36.3-36.4)°C; baseline core body temperature, 37.0 (37.0-37.1)°C; oral circadian amplitude, 0.25 (0.22-0.28)°C; core circadian amplitude, 0.31 (0.28-0.34)°C; circadian phase shift, 7.6 (7.3-7.9) hr; ABT-102 E(max), 2.2 (1.9-2.7)°C; ABT-102 EC (50), 20 (15-28) ng/mL; tolerance T (50), 28 (20-43) hr

P1 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