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Clinical Drug Investigation

Clinical Drug Investigation

IF: 2.89
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Safety, Tolerability, and Pharmacokinetics of the Novel Anti-influenza Agent Baloxavir Marboxil in Healthy Adults: Phase I Study Findings.

Published:1 December 2018 DOI: 10.1007/s40261-018-0710-9 PMID: 30288682
Hiroki Koshimichi, Toru Ishibashi, Nao Kawaguchi, Chisako Sato, Akira Kawasaki, Toshihiro Wajima

Abstract

Background and objective: Baloxavir marboxil, a prodrug that is metabolized to baloxavir acid, suppresses viral replication by inhibiting cap-dependent endonuclease. This first-in-human phase I study evaluated the safety, tolerability, and pharmacokinetics of baloxavir marboxil/baloxavir acid in healthy Japanese volunteers (Study 1), while food effects were evaluated in a separate phase I, crossover study in healthy Japanese volunteers (Study 2).

Methods: Study 1 participants were randomized to single-dose oral baloxavir marboxil (6, 20, 40, 60, or 80?mg; n?=?6 per dose) or placebo (n?=?10), while Study 2 participants (n?=?15) received single-dose oral baloxavir marboxil 20?mg in fasted, fed, and before-meal states.

Results: Baloxavir marboxil was well tolerated; there were few treatment-emergent adverse events and no serious adverse events/deaths. The mean plasma baloxavir acid concentration 24?h after single-dose (C24) oral baloxavir marboxil 6?mg was 6.92?ng/mL, exceeding the target C24 (6.85?ng/mL) estimated in nonclinical studies. In Study 1, baloxavir acid exposure demonstrated dose-proportional increases in the fasted state, with maximum plasma concentration generally attained within 3.5?h. Terminal elimination half-life ranged from 49 to 91?h. In Study 2, exposure was decreased and apparent clearance increased in the fed and before-meal states versus the fasted state; however, exposure exceeded the target C24 in all states.

Conclusion: Single-dose oral baloxavir marboxil was well tolerated, had a favorable safety profile, and had favorable pharmacokinetic characteristics, including a long half-life, supporting single oral dosing. The baloxavir acid area under the plasma concentration-time curve decreased with food intake by approximately 40%.

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Related products
Procduct Name CAS Molecular Formula Supplier Price
Baloxavir marboxil 1985606-14-1 C27H23F2N3O7S 298 suppliers Inquiry
Baloxavir 1985605-59-1 C24H19F2N3O4S 208 suppliers Inquiry
Baloxavir acid - Inquiry

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