ArticlePharmaceutics2021
Characterization of P-Glycoprotein Inhibitors for Evaluating the Effect of P-Glycoprotein on the Intestinal Absorption of Drugs.
Article in Pharmaceutics, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 14 papers, 1 of them a synthesis that pooled it.
What it found
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
14 citing papers in PubMed, 1 synthesis or guideline pooled it, 30 citations in OpenAlex.
- The effects of drug-drug interaction on linezolid pharmacokinetics: A systematic review.European journal of clinical pharmacology · 2024Pooled it
- Novel Fluorophenylated Dihydroimidazotriazinones as Potential Anticancer Agents: Design, Synthesis, In Vitro, Ex Vivo and In Silico Characterisation.International journal of molecular sciences · 2026Article
- N-Alkylated Monoterpene Indole Alkaloid Derivatives as Chemotherapy Adjuvants That Overcome P-glycoprotein-Mediated Multidrug Resistance in Cancer Cells, Spheroids and Patient-Derived Colorectal Cancer Organoids.Drug design, development and therapy · 2026Article
- Recent Advances in Synthetic Isoquinoline-Based Derivatives in Drug Design.Molecules (Basel, Switzerland) · 2025Review
- Virtual screening,Toxicology reports · 2025Article
- Structure-Based Design and In-Silico Evaluation of Computationally Proposed Curcumin Derivatives as Potential Inhibitors of the Coronaviral PLpro Enzymes.Pharmaceuticals (Basel, Switzerland) · 2025Article
- Article
- Parameterization of Physiologically Based Biopharmaceutics Models: Workshop Summary Report.Molecular pharmaceutics · 2024Review
- Knockout Transporter Cell Lines to Assess Substrate Potential Towards Efflux Transporters.The AAPS journal · 2024Article
- Role of P-glycoprotein in Regulating the Efficacy, Toxicity and Pharmacokinetics of Yunaconitine.Current drug metabolism · 2024Article
- Gut microbiome modulates tacrolimus pharmacokinetics through the transcriptional regulation of ABCB1.Microbiome · 2023Article
- Strategies and Mechanism in Reversing Intestinal Drug Efflux in Oral Drug Delivery.Pharmaceutics · 2022Review
- Oral etoposide and zosuquidar bioavailability in rats: Effect of co-administration andInternational journal of pharmaceutics: X · 2021Article
- Pharmaceutical Formulations with P-Glycoprotein Inhibitory Effect as Promising Approaches for Enhancing Oral Drug Absorption and Bioavailability.Pharmaceutics · 2021Review
Corrections and comments
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Authors and funding
7 authors at 2 institutions in 1 country.
Funding
Abstract
For developing oral drugs, it is necessary to predict the oral absorption of new chemical entities accurately. However, it is difficult because of the involvement of efflux transporters, including P-glycoprotein (P-gp), in their absorption process. In this study, we conducted a comparative analysis on the inhibitory activities of seven P-gp inhibitors (cyclosporin A, GF120918, LY335979, XR9576, WK-X-34, VX-710, and OC144-093) to evaluate the effect of P-gp on drug absorption. GF120918, LY335979, and XR9576 significantly decreased the basal-to-apical transport of paclitaxel, a P-gp substrate, across Caco-2 cell monolayers. GF120918 also inhibited the basal-to-apical transport of mitoxantrone, a breast cancer resistance protein (BCRP) substrate, in Caco-2 cells, whereas LY335979 hardly affected the mitoxantrone transport. In addition, the absorption rate of paclitaxel after oral administration in wild-type mice was significantly increased by pretreatment with LY335979, and it was similar to that in
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.