Preclinical and clinical evaluation of a novel TRPA1 antagonist LY3526318

• Published in: Pain (Amsterdam) Vol. 166; no. 8; pp. 1893 - 1908
• Main Authors: Broad, Lisa M., Suico, Jeffrey G., Turner, P. Kellie, Nie, Si, Johnson, Kirk W., Sanger, Helen E., Wegiel, Lindsay A., Sperry, David C., Remick, David, Moran, Magdalene, Malekiani, Sam, del Camino, Donato, Wu, Xinyuan, Chong, Jayhong A., Blair, Nathaniel T., Wilke, August V.
• Format: Journal Article
• Language: English
• Published: Philadelphia, PA Wolters Kluwer 01.08.2025
• Subjects: Adult; Analgesics - pharmacokinetics; Analgesics - pharmacology; Analgesics - therapeutic use; Animals; Disease Models, Animal; Dose-Response Relationship, Drug; Drug Evaluation, Preclinical; Female; Freund's Adjuvant - toxicity; Ganglia, Spinal - drug effects; HEK293 Cells; Humans; Hyperalgesia - drug therapy; Male; Pain - drug therapy; Pain Measurement - drug effects; Rats; Rats, Sprague-Dawley; TRPA1 Cation Channel - antagonists & inhibitors; TRPA1 Cation Channel - metabolism; TRPA1; Chronic pain

Supplemental Digital Content is Available in the Text.The transient receptor potential cation channel member A1 antagonist LY3526318 inhibited behavioral signs of enhanced nociception in animal models and was safe and well tolerated in phase 1 clinical studies. AbstractThe transient receptor potenti...