Gemcitabine versus Modified Gemcitabine: A Review of Several Promising Chemical Modifications

Moysan, Elodie; Bastiat, Guillaume; Benoit, Jean-Pierre

doi:10.1021/mp300370t

Cited by 232Synthesis and biological activityCancer therapeutics and mechanismsDrug Transport and Resistance Mechanisms

Gemcitabine versus Modified Gemcitabine: A Review of Several Promising Chemical Modifications

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Moysan, Elodie, Bastiat, Guillaume, Benoit, Jean-Pierre·2013·Molecular Pharmaceutics

DOI 10.1021/mp300370t

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Abstract

Gemcitabine, an anticancer agent which acts against a wide range of solid tumors, is known to be rapidly deaminated in blood to the inactive metabolite 2',2'-difluorodeoxyuridine and to be rapidly excreted by the urine. Moreover, many cancers develop resistance against this drug, such as loss of transporters and kinases responsible for the first phosphorylation step. To increase its therapeutic levels, gemcitabine is administered at high doses (1000 mg/m(2)) causing side effects (neutropenia, nausea, and so forth). To improve its metabolic stability and cytotoxic activity and to limit the phenomena of resistance many alternatives have emerged, such as the synthesis of prodrugs. Modifying an anticancer agent is not new; paclitaxel or ara-C has been subjected to such changes. This review summarizes the various chemical modifications that can be found in the 4-(N)- and 5'-positions of gemcitabine. They can provide (i) a protection against deamination, (ii) a better storage and (iii) a prolonged release in the cell, (iv) a possible use in the case of deoxycytidine kinase deficiency, and (v) transporter deficiency. These new gemcitabine-based sysems have the potential to improve the clinical outcome of a chemotherapy strategy.

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The effective in vivo dosage of SSK1 was approximately 60-fold lower than the clinical dosage of gemcitabine (30 mg/kg).
“our effective in vivo dosage of SSK1 was approximately 60-fold lower than the clinical dosage of gemcitabine (30 mg/kg)”
From Elimination of senescent cells by β-galactosidase-targeted prodrug attenuates inflammation and restores physical function in aged mice (2020) · cites this paper as [24]

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Research Highlights
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Authors: Moysan, E., Bastiat, G., & Benoit, J.-P.
Affiliations: Inserm (FR)
LUNAM Université—Micro et Nanomédecines Biomimétiques, F-49933 Angers, France
Corresponding author: Bastiat, Guillaume
ORCID: Bastiat, Guillaume
Venue: Molecular Pharmaceutics
Publisher: American Chemical Society (ACS)
Published: 2012-10-08
Volume: 10
Issue: 2
Pages: 430-444
ISSN: 1543-8384 (ISSN-L)
1543-8392
DOI: 10.1021/mp300370t
OpenAlex: W2095221067
Cited by: 225
References: 123
Citations by year: 2026: 13 · 2025: 23 · 2024: 10 · 2023: 18 · 2022: 21 · 2021: 19 · 2020: 23 · 2019: 13 · 2018: 21 · 2017: 18 · 2016: 14 · 2015: 14 · 2014: 14 · 2013: 4
FWCI: 0.51
Type: journal article
Language: en
Open access: green
inserm.hal.science
Licence: other-oa
Locations: Molecular Pharmaceutics (publishedVersion)
PubMed (publishedVersion)
HAL (submittedVersion, other-oa)
Funders: Eli Lilly and Company
Conseil Régional des Pays de la Loire
Topics: Physical Sciences › Chemistry › Organic Chemistry › Synthesis and biological activity
Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Cancer therapeutics and mechanisms
Health Sciences › Medicine › Oncology › Drug Transport and Resistance Mechanisms
Keywords: gemcitabine, prodrugs, chemical modification, 2',2'-difluorodeoxyuridine, deamination, drug resistance, nucleoside transporters, metabolic stability, cytotoxicity
MeSH terms: Gemcitabine, Animals, Antimetabolites, Antineoplastic, Deoxycytidine, Humans, Models, Biological, Phosphorylation, Prodrugs, Kaplan-Meier Estimate

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Gemcitabine versus Modified Gemcitabine: A Review of Several Promising Chemical Modifications

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