PF-06818883 / Pfizer - LARVOL DELTA

A novel approach for modeling in vivo enzyme turnover in the presence of a suicide inhibitor drug: A proof-of-concept brain PET study on MAG lipase. (PubMed, J Cereb Blood Flow Metab) - "We analyzed nonhuman primate PET data with monoacyglycerol lipase (MAGL) tracer [11C]PF-06809247, and suicide inhibitor PF-06818883 (0.03-1.27 mg/kg, active compound PF-06807893)...Serial PET experiments and measuring the drug's plasma concentration allowed to estimate correcting for residual suicide inhibition. This approach can be extended to other PET enzyme targets, improving our understanding of enzyme pathological alterations and suicide inhibitor-based therapies."

Journal • Preclinical

Target occupancy study and whole-body dosimetry with a MAGL PET ligand [C]PF-06809247 in non-human primates. (PubMed, EJNMMI Res) - "[C]PF-06809247 is a promising PET ligand for further studies of MAGL in the human brain."

Journal • Inflammation