ArticleBiochemical pharmacology2020
Pharmacokinetics of gemcitabine and its amino acid ester prodrug following intravenous and oral administrations in mice.
Article in Biochemical pharmacology, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 18 papers.
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Who cites it
18 citing papers in PubMed, 34 citations in OpenAlex.
- Dipeptide Transport Systems at the Interface of Peptide Metabolism and Drug Delivery in Cancer.International journal of molecular sciences · 2026Review
- Improving Laboratory-Based Cancer Drug Discovery Study Designs for Better Research Translations.Methods and protocols · 2026Review
- Baicalin nano-micelles for dry eye disease: LC-MS/MS method validation, pharmacokinetics and pharmacodynamics in preclinical models.Saudi pharmaceutical journal : SPJ : the official publication of the Saudi Pharmaceutical Society · 2025Article
- Dual Stimuli-Responsive Gemcitabine-Conjugated Alginate-Chitosan Nanoparticles for Triple-Negative Breast Cancer Therapy: A Smart Approach.Bioconjugate chemistry · 2025Article
- NIR Responsive Polymeric Prodrug Micelles ZnPc@P(PEG-CMA-TKGEM) for Combating Gemcitabine Drug Delivery in Anticancer Chemotherapy.Materials (Basel, Switzerland) · 2025Article
- Lysine Acetyltransferase 8: A Target for Natural Compounds in Cancer Therapy.International journal of molecular sciences · 2025Review
- Phase I study of oral metronomic gemcitabine (D07001) in patients with advanced solid tumors.The oncologist · 2025Article
- Clinical application and drug resistance mechanism of gemcitabine.Frontiers in cell and developmental biology · 2025Review
- Metal Complexation for the Rational Design of Gemcitabine Formulations in Cancer Therapy.ACS applied materials & interfaces · 2024Article
- Evaluation of the effects of a dasatinib-containing, self-emulsifying, drug delivery system on HT29 and SW420 human colorectal carcinoma cells, and MCF7 human breast adenocarcinoma cells.Journal of Taibah University Medical Sciences · 2024Article
- Article
- Improved Antitumor Efficiency ofInternational journal of nanomedicine · 2024Article
- The Role of Solute Carrier Transporters in Efficient Anticancer Drug Delivery and Therapy.Pharmaceutics · 2023Review
- Design of an L-Valine-Modified Nanomicelle-Based Drug Delivery System for Overcoming Ocular Surface Barriers.Pharmaceutics · 2022Article
- Precise engineering of hybrid molecules-loaded macromolecular nanoparticles showsDrug delivery · 2021Article
- Acetylation turns leucine into a drug by membrane transporter switching.Scientific reports · 2021Article
- Epigenetic regulation of intestinal peptide transporter PEPT1 as a potential strategy for colorectal cancer sensitization.Cell death & disease · 2021Article
- Combinational dual drug delivery system to enhance the care and treatment of gastric cancer patients.Drug delivery · 2020Article
Corrections and comments
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Authors and funding
4 authors at 1 institution in 1 country.
Funding
Abstract
Gemcitabine is an intravenously administered anti-cancer nucleoside analogue. Systemic exposure following oral administration of gemcitabine is limited by extensive first-pass metabolism via cytidine deaminase (CDA) and potentially by saturation of nucleoside transporter-mediated intestinal uptake. An amino acid ester prodrug of gemcitabine, 5'-l-valyl-gemcitabine (V-Gem), was previously shown to be a substrate of the intestinally expressed peptide transporter 1 (PEPT1) and stable against CDA-mediated metabolism. However, preliminary studies did not evaluate the in vivo oral performance of V-Gem as compared to parent drug. In the present study, we evaluated the pharmacokinetics and in vivo oral absorption of gemcitabine and V-Gem following intravenous and oral administrations in mice. These studies revealed that V-Gem undergoes rapid systemic elimination (half-life < 1 min) and has a low oral bioavailability (<1%). Most importantly, the systemic exposure of gemcitabine was not different following oral administration of equimolar doses of gemcitabine (gemcitabine bioavailability of 18.3%) and V-Gem (gemcitabine bioavailability of 16.7%). Single-pass intestinal perfusions with portal blood sampling in mice revealed that V-Gem undergoes extensive activation in intestinal epithelial cells and that gemcitabine undergoes first-pass metabolism in intestinal epithelial cells. Thus, formulation of gemcitabine as the prodrug V-Gem does not increase systemic gemcitabine exposure following oral dosing, due, in part, to the instability of V-Gem in intestinal epithelial cells.
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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.