Safety, Tolerability, and Pharmacokinetics of the Novel Antiviral Agent Ensitrelvir Fumaric Acid, a SARS-CoV-2 3CL Protease Inhibitor, in Healthy Adults
Ryosuke Shimizu, Takuhiro Sonoyama, Takahiro Fukuhara, Aya Kuwata, Yumiko Matsuo, Ryuji Kubota
Abstract
of ensitrelvir but did not impact the area under the curve (AUC), suggesting suitability for administration without food restriction. Compared with Japanese participants, plasma exposures were slightly lower for white participants. Ensitrelvir affected the pharmacokinetics of CYP3A substrates because of increase in AUC of midazolam coadministered with ensitrelvir 750/250 mg on day 6. In conclusion, ensitrelvir was well-tolerated and demonstrated favorable pharmacokinetics, including a long half-life, supporting once-daily oral dosing. These results validate further assessments of ensitrelvir in participants with SARS-CoV-2 infection.
Topics & Concepts
TolerabilityPharmacokineticsProtease inhibitor (pharmacology)PharmacologySevere acute respiratory syndrome coronavirus 2 (SARS-CoV-2)VirologyCoronavirus disease 2019 (COVID-19)MedicineFumaric acidAdverse effectChemistryViral loadVirusInternal medicineInfectious disease (medical specialty)BiochemistryDiseaseAntiretroviral therapySARS-CoV-2 and COVID-19 ResearchCOVID-19 Clinical Research StudiesMosquito-borne diseases and control