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Design and Development of Novel Hybrids Based on Pyrrolo[2,1‐f][1,2,4]Triazine and 1‐(Methylpiperidin‐4‐yl) Aniline–Based Analogs: Exploring the Utility as Anticancer Agents via MERTK Inhibition

Chemical Biology and Drug Design

It plays a key role in cancer cell survival and proliferation and regulates immune responses in cancer. The synthesized molecules were assessed for their pharmacological potential via cell viability, drug metabolism and pharmacokinetics (DMPK), and MERTK inhibition studies corroborated by in silico studies.

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Pharmacokinetic study of the interaction between luteolin and magnoflorine in rats

Chemical Biology and Drug Design

Abstract Both luteolin and magnoflorine have been reported to regulate the development of breast cancer, which makes them easier to co-administrate. Magnoflorine significantly changed the pharmacokinetic profile of luteolin with increased area under the curve (AUC), prolonged t 1/2 , and reduced clearance rate.

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How GPCR agonists, including antibodies, are shaping the future of metabolic care

Drug Target Review

G protein-coupled receptors (GPCRs) represent a cornerstone of modern drug discovery due to their crucial role in regulating human physiology and their involvement in numerous diseases. A suitable pharmacokinetics profile can be achieved with the addition of half-life extending moieties to the molecule.

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The rising impact of biomarkers in early clinical development

Drug Target Review

For example, transcriptomic processes are showing the potential to identify and track failures in gene expression and gene regulation of amyloid and tau-related biomarkers, understood as precursors to the onset of Alzheimers disease (AD). Trial design and statistical methods are also key to determining the utility and validity of biomarkers.

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Factors influencing the Central Nervous System (CNS) distribution of the ATR inhibitor elimusertib (BAY1895344): Implications for the treatment of CNS tumors [Metabolism, Transport, and Pharmacogenetics]

ASPET

Various DDR inhibitors, targeting the key regulators of these pathways such as ataxia telangiectasia mutated and Rad3-related (ATR), are being explored as radio- and chemo-sensitizers. Standard of care GBM therapies include radiation and cytotoxic chemotherapy that lead to DNA damage.

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Understanding the Regulatory Environment in Japan for Generic Drug Development

Drug Patent Watch

Key Requirements for Generic Drug Approval Bioequivalence Studies : The PMDA requires bioequivalence studies to ensure that the generic drug is equivalent to the RLD in terms of its pharmacokinetic and pharmacodynamic properties. Pharmaceutical Regulations in Japan 2020. Freyr Solutions. Regulatory System on Generic Drugs in Japan.

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Mollugin Derivatives as Anti‐Inflammatory Agents: Design, Synthesis, and NF‐κB Inhibition

Chemical Biology and Drug Design

Investigation of the mechanism of action indicated that 5k down-regulated NF-B expression, possibly by suppressing LPS-induced expression of the p65 protein. ADMET prediction analysis indicated that compounds 5h and 5k showed good pharmacokinetic properties.