Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of ASP3652, a Reversible Fatty Acid Amide Hydrolase Inhibitor, in Healthy, Nonelderly, Japanese Men and Elderly, Japanese Men and Women: A Randomized, Double-blind, Placebo-controlled, Single and Multiple Oral Dose, Phase I Study

Masaomi Takizawa, Toshifumi Hatta, Hiromi Iitsuka, Masataka Katashima, Yuichiro Sato, Kentaro Kuroishi, Hirotaka Nagashima. Clin Ther. 2020;42(5):906-923.

Randomised controlled trialHumansWith ASP3652 (a FAAH inhibitor that raises endogenous PEA, tested alone)

This study tested palmitoylethanolamide together with ASP3652 (a FAAH inhibitor that raises endogenous PEA, tested alone). Its results cannot be assigned to palmitoylethanolamide alone. More combination studies.

Design

Randomised controlled trial

Subjects

40 healthy non-elderly men (single dose part) and 48 non-elderly men and elderly men and women (multiple dose part), Japanese

Dose used in the study

ASP3652 single oral doses of 30, 100, 300, 600 and 900 mg; multiple doses of 100 and 300 mg twice daily; or placebo

Duration

Multiple dosing reached near steady state at about 3 days; total length not stated in the abstract

What was measured

Adverse events, laboratory tests, vital signs, mood scale and ECGs; plasma and urine drug levels; FAAH activity and plasma anandamide, oleoylethanolamide and palmitoylethanolamide.

What the authors reported

This phase I study found:

• ASP3652 was absorbed rapidly, with exposure slightly more than dose-proportional and no accumulation.
• FAAH was inhibited dose-dependently and plasma anandamide, OEA and PEA rose in all dose groups.
• Adverse event rates after multiple doses ranged from 44.4% to 66.7% and were similar across groups including placebo.

Limits of this study

A phase I safety study in healthy volunteers, not a treatment trial. PEA was measured as a marker of FAAH inhibition, not given. Six authors are employees of Astellas Pharma and the investigator was paid by Astellas.

Source

PubMed 32456804 · doi:10.1016/j.clinthera.2020.03.021

Entry checked against the abstract on PubMed on 2026-09-22. The dose shown is the dose the researchers used. It is not a recommendation. How to read this page.