Pharmacokinetics of Edaravone Oral Suspension in Patients With Amyotrophic Lateral Sclerosis

This report aimed to assess the pharmacokinetics and safety of an edaravone oral suspension in patients with ALS after oral and percutaneous endoscopic gastrostomy (PEG) tube administration.METHODS: Two single-dose, open-label phase 1 clinical studies were conducted. Edaravone oral suspension (105 mg of edaravone in 5 mL aqueous suspension) was administered orally and via PEG tube to 9 and 6 Japanese patients with ALS, respectively. Plasma and urinary pharmacokinetics of unchanged edaravone and its metabolites (sulfate and glucuronide conjugates) were determined. Safety was also evaluated.FINDINGS: After reaching maximum plasma concentration, the mean plasma concentration-time of unchanged edaravone showed a triphasic elimination. Mean plasma concentration-time profiles of the metabolites were higher than those of unchanged edaravone. The mean urinary excretion ratios were higher for the glucuronide conjugate than for either unchanged edaravone or the sulfate conjugate. In patients administered edaravone orally, a single adverse event occurred (blood urine present), which was mild and improved without medical intervention. No adverse drug reactions or serious adverse events were reported. In patients administered edaravone via PEG tube, 5 treatment-emergent adverse events were reported in 3 patients; none were related to the study drug. No adverse drug reactions were reported.IMPLICATIONS: In patients with ALS, a single dose of edaravone oral suspension was well absorbed and ...

Source: Clinical Therapeutics - November 12, 2023 Category: Drugs & Pharmacology Authors: Hidetoshi Shimizu Yukiko Nishimura Youichi Shiide Makoto Akimoto Makiko Yashiro Masaki Ueda Manabu Hirai Hiide Yoshino Tomohiko Mizutani Kazuaki Kanai Osamu Kano Hideki Kimura Hisakuni Sekino Kimiko Ito Source Type: research