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Pharmacokinetics of panobinostat: Inter-species difference in metabolic stability [Metabolism, Transport, and Pharmacogenetics]

ASPET

Panobinostat also showed inter-strain and inter-species differences in the in vitro plasma stability; and was stable in human plasma. Importantly, the plasma stability in various mouse strains was not reflected in the in vivo systemic pharmacokinetic behavior of panobinostat.

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Covalent Stapling of the Cereblon Sensor Loop Histidine Using Sulfur-Heterocycle Exchange

Covalent Modifiers

For example, sulfonyl imidazole EM12-SO2Im covalently blocked the CRBN binding site and possessed excellent metabolic stability in human plasma, liver microsomes, and hepatocytes.

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The Data-Driven Future of Drug Development

DrugBank

Data science has emerged as an innovative tool in the biopharmaceutical industry, leveraging the power of machine learning and artificial intelligence to drive innovation and efficiency across the entire drug development lifecycle. These complex molecules require precise engineering to ensure optimal efficacy and safety.

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Fixing drug discovery’s most persistent problem with AI

Drug Target Review

These core ADMET properties are fundamental to drug development across the industry, making them well-suited for pre-competitive collaboration. ADMET refers to absorption, distribution, metabolism, excretion and toxicity. Image credit: UGREEN 3S / Shutterstock.

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Computational Design of a Bicyclic Peptide Inhibitor Targeting the ICOS/ICOS‐L Protein–Protein Interaction

Chemical Biology and Drug Design

Notably, CP5 demonstrated satisfactory invitro pharmacokinetic properties, such as metabolic stability and lipophilicity, positioning it as a promising candidate for further drug development. Importantly, we validated the ICOS/ICOS-L inhibitory activity of CP5 using both TR-FRET assay and ELISA.

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Obstacles and innovations of macrocyclic drug development

Drug Target Review

Cyclic Peptide Design, Chapter 2: Strategies to Enhance Metabolic Stabilities. Cyclic peptides in pipeline: What future for these great molecules? Pharmaceuticals , 16(7):996, 2023. Khatri B, Nuthakki VR, Chatterjee J. Springer, 2019. Jain AN, Cleves AE, Gao Q, et al. Journal of Computer-Aided Molecular Design , 33:531558, 2019.