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Repurposing FDA-approved drugs for COVID-19: targeting the main protease through multi-phase approach.
Antivir Ther
December 2024
Pharmaceutical Medicinal Chemistry & Drug Design Department, Faculty of Pharmacy (Boys), Al-Azhar University, Cairo, Egypt.
Background: The COVID-19 pandemic has created an urgent need for effective therapeutic agents. The SARS-CoV-2 Main Protease (M) plays a crucial role in viral replication and immune evasion, making it a key target for drug development. While several studies have explored M inhibition, identifying FDA-approved drugs with potential efficacy remains a critical research focus.
View Article and Find Full Text PDFIdentification of Malaria-Selective Proteasome β5 Inhibitors Through Pharmacophore Modeling, Molecular Docking, and Molecular Dynamics Simulation.
Int J Mol Sci
November 2024
Department of Pharmacology, Kangwon National University School of Medicine, Chuncheon 24341, Republic of Korea.
Malaria remains a global health challenge, with increasing resistance to frontline antimalarial treatments such as artemisinin (ART) threatening the efficacy of current therapies. In this study, we investigated the potential of FDA-approved drugs to selectively inhibit the malarial proteasome, a novel target for antimalarial drug development. By leveraging pharmacophore modeling, molecular docking, molecular dynamics (MD) simulations, and binding free-energy calculations, we screened a library of compounds to identify inhibitors selective for the Plasmodium proteasome over the human proteasome.
View Article and Find Full Text PDFPhysiologically based pharmacokinetic modeling of drug-drug interactions between ritonavir-boosted atazanavir and rifampicin in pregnancy.
CPT Pharmacometrics Syst Pharmacol
November 2024
Department of Pharmacology and Therapeutics, University of Liverpool, Liverpool, UK.
Ritonavir-boosted atazanavir (ATV/r) and rifampicin are mainstays of second-line antiretroviral and multiple anti-TB regimens, respectively. Rifampicin induces CYP3A4, a major enzyme involved in atazanavir metabolism, causing a drug-drug interaction (DDI) which might be exaggerated in pregnancy. Having demonstrated that increasing the dose of ATV/r from once daily (OD) to twice daily (BD) in non-pregnant adults can safely overcome this DDI, we developed a pregnancy physiologically based pharmacokinetic (PBPK) model to explore the impact of pregnancy.
View Article and Find Full Text PDFImpact of dissolution medium pH and ionization state of the drug on the release performance of amorphous solid dispersions.
J Pharm Sci
January 2025
Small Molecule CMC Development, Research and Development, AbbVie Inc., North Chicago, IL 60064, United States.
Amorphous solid dispersions (ASDs) are widely employed as a strategy to improve oral bioavailability of poorly water soluble compounds. Typically, optimal dissolution performance from a polyvinylpyrrolidone vinyl acetate (PVPVA) based ASD is observed at relatively low drug loading limit. Above a certain drug load, termed limit of congruency (LoC), the release from ASDs significantly decreases.
View Article and Find Full Text PDFDissolution, phase behavior and mass transport of amorphous solid dispersions in aspirated human intestinal fluids.
J Pharm Sci
January 2025
Department of Industrial and Molecular Pharmaceutics, College of Pharmacy, Purdue University, West Lafayette, Indiana, USA. Electronic address:
Amorphous solid dispersions (ASDs) typically show improved dissolution and generate supersaturated solutions, enhancing the oral bioavailability of poorly soluble drugs. To gain insights into intraluminal ASD behavior, we utilized two poorly soluble drugs with different crystallization tendencies, atazanavir and posaconazole, prepared as ASDs at a 10% drug loading with hydroxypropyl methylcellulose acetyl succinate (HPMCAS). We evaluated their release in aspirated fasted-state human intestinal fluid (FaHIF), and multi-component fasted-state simulated intestinal fluid (composite-FaSSIF), characterizing the supersaturation profiles and drug-rich nanodroplets that formed.
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