Cargando…

Preclinical Pharmacokinetics and In Vitro Properties of GS-441524, a Potential Oral Drug Candidate for COVID-19 Treatment

Preclinical pharmacokinetics (PK) and In Vitro ADME properties of GS-441524, a potential oral agent for the treatment of Covid-19, were studied. GS-441524 was stable in vitro in liver microsomes, cytosols, and hepatocytes of mice, rats, monkeys, dogs, and humans. The plasma free fractions of GS-4415...

Descripción completa

Detalles Bibliográficos
Autores principales:	Wang, Amy Q., Hagen, Natalie R., Padilha, Elias C., Yang, Mengbi, Shah, Pranav, Chen, Catherine Z., Huang, Wenwei, Terse, Pramod, Sanderson, Philip, Zheng, Wei, Xu, Xin
Formato:	Online Artículo Texto
Lenguaje:	English
Publicado:	Frontiers Media S.A. 2022
Materias:	Pharmacology
Acceso en línea:	https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9424906/ https://www.ncbi.nlm.nih.gov/pubmed/36052127 http://dx.doi.org/10.3389/fphar.2022.918083

Ejemplares similares

Use of physiological based pharmacokinetic modeling for cross-species prediction of pharmacokinetic and tissue distribution profiles of a novel niclosamide prodrug
por: Yang, Mengbi, et al.
Publicado: (2023)

Population Pharmacokinetics of Remdesivir and GS-441524 in Hospitalized COVID-19 Patients
por: Leegwater, E., et al.
Publicado: (2022)

Pharmacokinetics of Orally Administered GS-441524 in Dogs
por: Yan, Victoria C., et al.
Publicado: (2021)

Potency and pharmacokinetics of GS-441524 derivatives against SARS-CoV-2
por: Wei, Daibao, et al.
Publicado: (2021)

Practical and Highly Efficient Synthesis of Remdesivir from GS-441524
por: Hu, Tianwen, et al.
Publicado: (2022)

Nucleoside analog GS‐441524: pharmacokinetics in different species, safety, and potential effectiveness against Covid‐19
por: Rasmussen, Henrik Berg, et al.
Publicado: (2022)

Interpatient variability in the pharmacokinetics of remdesivir and its main metabolite GS-441524 in treated COVID-19 subjects
por: Tempestilli, Massimo, et al.
Publicado: (2022)

Current knowledge about the antivirals remdesivir (GS-5734) and GS-441524 as therapeutic options for coronaviruses
por: Amirian, E. Susan, et al.
Publicado: (2020)

Population pharmacokinetic modeling of GS‐441524, the active metabolite of remdesivir, in Japanese COVID‐19 patients with renal dysfunction
por: Sukeishi, Asami, et al.
Publicado: (2021)

An efficient synthesis of RNA containing GS-441524: the nucleoside precursor of remdesivir
por: Moorthy, Ramkumar, et al.
Publicado: (2021)

Exploration of the optimal GS-441524 trough concentration for treating COVID-19
por: Nakano, Yuki, et al.
Publicado: (2023)

Transplacental transfer of Remdesivir and GS‐441524: An ex vivo perfusion study
por: Louchet, Margaux, et al.
Publicado: (2023)

Combination of the parent analogue of remdesivir (GS-441524) and molnupiravir results in a markedly potent antiviral effect in SARS-CoV-2 infected Syrian hamsters
por: Abdelnabi, Rana, et al.
Publicado: (2022)

Advantages of the Parent Nucleoside GS-441524 over Remdesivir for Covid-19 Treatment
por: Yan, Victoria C., et al.
Publicado: (2020)

Population pharmacokinetics and exposure–clinical outcome relationship of remdesivir major metabolite GS‐441524 in patients with moderate and severe COVID‐19
por: Tamura, Ryo, et al.
Publicado: (2023)

The preclinical inhibitor GS441524 in combination with GC376 efficaciously inhibited the proliferation of SARS-CoV-2 in the mouse respiratory tract
por: Shi, Yuejun, et al.
Publicado: (2021)

Synthesis and anti-SARS-CoV-2 activity of deuterated GS-441524 analogs
por: Zheng, Wei, et al.
Publicado: (2022)

Cellular Uptake and Intracellular Phosphorylation of GS-441524: Implications for Its Effectiveness against COVID-19
por: Rasmussen, Henrik Berg, et al.
Publicado: (2021)

Curing Cats with Feline Infectious Peritonitis with an Oral Multi-Component Drug Containing GS-441524
por: Krentz, Daniela, et al.
Publicado: (2021)

In vitro antiviral effects of GS-441524 and itraconazole combination against feline infectious peritonitis virus
por: Doki, Tomoyoshi, et al.
Publicado: (2022)

Biotransformation and transplacental transfer of the anti-viral remdesivir and predominant metabolite, GS-441524 in pregnant rats
por: Yang, Ling, et al.
Publicado: (2022)

Exploration for the effect of renal function and renal replacement therapy on pharmacokinetics of remdesivir and GS‐441524 in patients with COVID‐19: A limited case series
por: Choe, Pyoeng Gyun, et al.
Publicado: (2021)

Efficacy and safety of the nucleoside analog GS-441524 for treatment of cats with naturally occurring feline infectious peritonitis
por: Pedersen, Niels C, et al.
Publicado: (2019)

Removal of Remdesivir’s Metabolite GS-441524 by Hemodialysis in a Double Lung Transplant Recipient with COVID-19
por: Lê, Minh Patrick, et al.
Publicado: (2020)

Oral prodrug of remdesivir parent GS-441524 is efficacious against SARS-CoV-2 in ferrets
por: Cox, Robert M., et al.
Publicado: (2021)

Unlicensed GS-441524-Like Antiviral Therapy Can Be Effective for at-Home Treatment of Feline Infectious Peritonitis
por: Jones, Sarah, et al.
Publicado: (2021)

Quantification of GS-441524 concentration in feline plasma using high performance liquid chromatography with fluorescence detection
por: Kimble, Benjamin, et al.
Publicado: (2023)

An Optimized Bioassay for Screening Combined Anticoronaviral Compounds for Efficacy against Feline Infectious Peritonitis Virus with Pharmacokinetic Analyses of GS-441524, Remdesivir, and Molnupiravir in Cats
por: Cook, Sarah, et al.
Publicado: (2022)

Structural Insights into Plasticity and Discovery of Remdesivir Metabolite GS-441524 Binding in SARS-CoV-2 Macrodomain
por: Ni, Xiaomin, et al.
Publicado: (2021)

Intravenous delivery of GS-441524 is efficacious in the African green monkey model of SARS-CoV-2 infection
por: Pitts, Jared, et al.
Publicado: (2022)

Can remdesivir and its parent nucleoside GS-441524 be potential oral drugs? An in vitro and in vivo DMPK assessment
por: Xie, Jiashu, et al.
Publicado: (2021)

Antiviral treatment using the adenosine nucleoside analogue GS‐441524 in cats with clinically diagnosed neurological feline infectious peritonitis
por: Dickinson, Peter J., et al.
Publicado: (2020)

Fecal Feline Coronavirus RNA Shedding and Spike Gene Mutations in Cats with Feline Infectious Peritonitis Treated with GS-441524
por: Meli, Marina L., et al.
Publicado: (2022)

Binding Adaptation of GS-441524 Diversifies Macro Domains and Downregulates SARS-CoV-2 de-MARylation Capacity
por: Tsika, Aikaterini C., et al.
Publicado: (2022)

Oral GS-441524 derivatives: Next-generation inhibitors of SARS‐CoV‐2 RNA‐dependent RNA polymerase
por: Wang, Zhonglei, et al.
Publicado: (2022)

Nonsteroidal anti-inflammatory drugs (NSAIDs) and nucleotide analog GS-441524 conjugates with potent in vivo efficacy against coronaviruses
por: Zhou, Qifan, et al.
Publicado: (2023)

Thirty‐two cats with effusive or non‐effusive feline infectious peritonitis treated with a combination of remdesivir and GS‐441524
por: Green, Jodie, et al.
Publicado: (2023)

Validation of LC-MS/MS methods for determination of remdesivir and its metabolites GS-441524 and GS-704277 in acidified human plasma and their application in COVID-19 related clinical studies
por: Xiao, Deqing, et al.
Publicado: (2021)

Remdesivir and GS-441524 Retain Antiviral Activity against Delta, Omicron, and Other Emergent SARS-CoV-2 Variants
por: Pitts, Jared, et al.
Publicado: (2022)

The Potential Protective Role of GS-441524, a Metabolite of the Prodrug Remdesivir, in Vaccine Breakthrough SARS-CoV-2 Infections
por: Zhu, JiaYi, et al.
Publicado: (2022)

Cannot write session to /tmp/vufind_sessions/sess_pa6i42lavfl22d7k33akc0sb7o