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Updated: Jan 26, 2026
Predictive Immune Modeling of Solid Tumors
Published on: February 25, 2020
Rethinking Alkylating(-Like) Agents for Solid Tumor Management
Hélène Lajous1, Bénédicte Lelièvre2, Elodie Vauléon3
1CRCINA, INSERM, Université de Nantes, Université d'Angers, Angers, France; Center for Education and Research on Macromolecules (CERM), CESAM Research Unit, University of Liege, B6a Sart-Tilman, B-4000 Liege, Belgium.
Abstract:
Although old molecules, alkylating agents and platinum derivatives are still widely used in the treatment of various solid tumors. However, systemic toxicity and cellular resistance mechanisms impede their efficacy. Innovative strategies, including local administration, optimization of treatment schedule/dosage, synergistic combinations, and the encapsulation of bioactive molecules in smart, multifunctional drug delivery systems, have shown promising results in potentiating anticancer activity while circumventing such hurdles. Furthermore, questioning of the old paradigm according to which nuclear DNA is the critical target of their anticancer activity has shed light on subcellular alternative and neglected targets that obviously participate in the mediation of cytotoxicity or resistance. Thus, rethinking of the use of these pivotal antineoplastic agents appears critical to improve clinical outcomes in the management of solid tumors.
Insights
Alkylating agents and platinum derivatives show promise in solid tumor treatment. Innovative strategies and exploring new targets can enhance their anticancer activity and overcome resistance.
Area of Science:
- Oncology
- Pharmacology
- Drug Delivery
Background:
- Alkylating agents and platinum derivatives are established treatments for solid tumors.
- Systemic toxicity and cellular resistance limit the efficacy of these traditional chemotherapeutics.
- The critical target of these agents has traditionally been considered nuclear DNA.
Purpose of the Study:
- To review innovative strategies for enhancing the efficacy of alkylating agents and platinum derivatives.
- To explore alternative subcellular targets beyond nuclear DNA for these antineoplastic agents.
- To re-evaluate the clinical application of these pivotal anticancer drugs.
Main Methods:
- Literature review of existing and emerging strategies for alkylating agent and platinum derivative therapy.
- Analysis of research on drug delivery systems and combination therapies.
- Investigation into studies examining non-nuclear DNA targets and their role in cytotoxicity and resistance.
Main Results:
- Innovative strategies like local administration, optimized dosing, and synergistic combinations show potential.
- Smart drug delivery systems can enhance anticancer activity and mitigate toxicity.
- Alternative subcellular targets are implicated in mediating cytotoxicity and resistance, challenging the nuclear DNA-centric view.
Conclusions:
- Rethinking the application of alkylating agents and platinum derivatives is crucial for improving solid tumor treatment outcomes.
- Exploring novel targets and advanced drug delivery systems can overcome current therapeutic limitations.
- A paradigm shift towards understanding broader cellular targets may unlock greater clinical efficacy.
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