Effect of Strong CYP3A4 Inhibition, CYP3A4 Induction, and OATP1B1/3 Inhibition on the Pharmacokinetics of a Single Oral Dose of Sotorasib
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DOI: 10.1002/cpdd.1392
Abstract: Sotorasib is a small molecule that irreversibly inhibits the Kirsten rat sarcoma viral oncogene homolog (KRAS) protein with a G12C amino acid substitution mutant protein. The impact of cytochrome P450 (CYP) 3A4 inhibition and induction… read more here.
Keywords: cyp3a4 inhibition; cyp3a4; inhibition; cyp3a4 induction ... See more keywords
Advancing Predictions of Oral Drug Absorption, CYP3A4 Induction, and Transporter‐Mediated Interactions Using a Human Primary Intestinal 3D Model (EpiIntestinal™)
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DOI: 10.1002/cpt.70000
Abstract: Accurate prediction of oral drug absorption in humans is essential for early drug development; however, physiologically relevant human models are lacking. This study aims to comprehensively assess the EpiIntestinal™, a human primary intestinal 3D model,… read more here.
Keywords: drug; cyp3a4 induction; model; absorption ... See more keywords
Safety assessment of herbal supplement components targeting hepatotoxicity and CYP3A4 induction in cell-based assay using HepG2 cells.
Sign Up to like & getrecommendations! Published in 2022 at "Journal of food science"
DOI: 10.1111/1750-3841.16410
Abstract: Herbal supplements can cause hepatotoxicity and drug interactions via hepatic cytochrome P-450 (CYP) in some cases. However, there is no simple and stable cell-based assay to conduct a screening for hepatotoxicity and CYP induction. In… read more here.
Keywords: cell; safety; cyp3a4 induction; herbal supplements ... See more keywords
Effect of CYP3A4 Induction and Inhibition on the Pharmacokinetics of SHR0302 in Healthy Subjects.
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DOI: 10.1111/bcp.15733
Abstract: AIM SHR0302 is a selective Janus kinase (JAK) 1 inhibitor under clinical investigation for the treatment of rheumatoid arthritis. As SHR0302 is metabolized mainly by cytochrome P450 (CYP) 3A4, clinical studies were performed to evaluate… read more here.
Keywords: pharmacokinetics shr0302; effect; cyp3a4 induction; shr0302 healthy ... See more keywords
Evaluation of a Novel Renewable Hepatic Cell Model for Prediction of Clinical CYP3A4 Induction Using a Correlation-Based Relative Induction Score Approach
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DOI: 10.1124/dmd.116.072124
Abstract: Metabolism enzyme induction-mediated drug-drug interactions need to be carefully characterized in vitro for drug candidates to predict in vivo safety risk and therapeutic efficiency. Currently, both the Food and Drug Administration and European Medicines Agency… read more here.
Keywords: cyp3a4 induction; drug; induction; human hepatocytes ... See more keywords
High-performance PBPK model for predicting CYP3A4 induction-mediated drug interactions: a refined and validated approach
Sign Up to like & getrecommendations! Published in 2025 at "Frontiers in Pharmacology"
DOI: 10.3389/fphar.2025.1521068
Abstract: Introduction The cytochrome P450 enzyme 3A4 (CYP3A4) mediates numerous drug-drug interactions (DDIs) by inducing the metabolism of co-administered drugs, which can result in reduced therapeutic efficacy or increased toxicity. This study developed and validated a… read more here.
Keywords: induction mediated; cyp3a4 induction; pbpk model; drug ... See more keywords