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Cancers
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Advances in Drug Repurposing to Overcome Cancers
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Advances in Drug Repurposing to Overcome Cancers

A special issue of Cancers (ISSN 2072-6694). This special issue belongs to the section "Cancer Drug Development".

Deadline for manuscript submissions: 30 August 2025 | Viewed by 6368

Special Issue Editor

Dr. Rafal Bartoszewski

E-Mail Website
Guest Editor
Department of Biophysics, Faculty of Biotechnology, University of Wroclaw, Wroclaw, Poland
Interests: HIFs; hypoxia; UPR; microRNA; miRNA; ER stress
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

The mortality rate of cancers is very high, mainly due to drug resistance. But there are some drawbacks to drug development, so we here present a better strategy, known as drug repurposing.

Due to the slow pace of the discovery of new drugs, accompanied by increasing costs and a high risk of attrition, the idea of reusing “known” drugs and molecules becomes very appealing. However, although multiple strategies have been proposed for the efficient, safe, and economic implementation of drug repurposing into therapies for both common and rare diseases, many obstacles have preventing them from benefiting patients. Today, we witness exponential research progress in fields that could propel drug repurposing, including the development of in vitro pharmacological profiling connected with multi-omics approaches, single-cell sequencing, as well as the dramatic expansion of artificial intelligence and quantum computing. These advances are accompanied by unlimited increases in publicly available datasets obtained during clinical or biomedical projects. Although all these breakthroughs could improve both the safety and efficiency of future drug repurposing strategies, they are also accompanied by specific challenges, some of which we are not aware of yet.

Thus, for this Special Issue, we welcome the submission of both experimental and review manuscripts relating to all aspects of modern drug repurposing, but especially ones which attempt to address future progress in this field and define related obstacles.

Dr. Rafal Bartoszewski
Guest Editor

Manuscript Submission Information

Manuscripts should be submitted online at www.mdpi.com by registering and logging in to this website. Once you are registered, click here to go to the submission form. Manuscripts can be submitted until the deadline. All submissions that pass pre-check are peer-reviewed. Accepted papers will be published continuously in the journal (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as communications are invited. For planned papers, a title and short abstract (about 100 words) can be sent to the Editorial Office for announcement on this website.

Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are thoroughly refereed through a single-blind peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. Cancers is an international peer-reviewed open access semimonthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 2900 CHF (Swiss Francs). Submitted papers should be well formatted and use good English. Authors may use MDPI's English editing service prior to publication or during author revisions.

Keywords

  • drug development
  • drug repurposing
  • drug resistance
  • pharmacological
  • cancers therapy

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Published Papers (5 papers)

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Research

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20 pages, 4025 KiB  
Article
Deciphering Nicotine-Driven Oncogenesis in Head and Neck Cancer: Integrative Transcriptomics and Drug Repurposing Insights
by Guo-Rung You, Daniel Yu Chang, Hung-Han Huang, Yin-Ju Chen, Joseph T. Chang and Ann-Joy Cheng
Cancers 2025, 17(9), 1430; https://doi.org/10.3390/cancers17091430 - 24 Apr 2025
Viewed by 128
Abstract
Background: Chronic nicotine exposure drives head and neck cancer (HNC) progression, yet its molecular mechanisms remain underexplored. This study examines nicotine-induced transcriptomic changes and potential therapies via drug repurposing. Methods: HNC cell lines (OECM1, SAS, and CGHNC9) were exposed to an [...] Read more.
Background: Chronic nicotine exposure drives head and neck cancer (HNC) progression, yet its molecular mechanisms remain underexplored. This study examines nicotine-induced transcriptomic changes and potential therapies via drug repurposing. Methods: HNC cell lines (OECM1, SAS, and CGHNC9) were exposed to an IC30 nicotine dose for three months to model chronic exposure in habitual smokers. Transcriptomic profiling of these sublines was integrated with TCGA-HNSC patient data. Differentially expressed genes (DEGs) underwent functional pathway enrichment analysis. Drug repurposing was conducted using gene–drug correlation analysis across GDSC, CTRP, and PRISM databases. Results: Transcriptomic analysis identified 1223 DEGs in nicotine-exposed HNC cells, and integration with TCGA-HNSC data defined a Nic-HNC gene set of 168 genes: 149 oncogenes and 19 tumor suppressors, with 36 oncogenes overexpressed in heavy smokers. Pathway analysis revealed the upregulation of oncogenic signaling, such as PI3K-AKT, alongside the suppression of immune regulation and metabolic reprogramming. Drug repurposing identified five compounds—AZD1332, JAK-8517, NU7441, BRD-K30748066, and neopeltolide—with the first two exhibiting the strongest inverse correlations with nicotine-induced oncogenes in heavy smokers, highlighting their potential as targeted therapies for tobacco-associated HNC. Conclusions: This study comprehensively characterizes nicotine-driven molecular dysregulation in HNC and proposes AZD1332 and JAK-8517 as promising therapeutic candidates through drug repurposing. These insights advance our understanding of nicotine’s oncogenic role and provide a foundation for translational research to develop targeted interventions for tobacco-associated HNC. Full article
(This article belongs to the Special Issue Advances in Drug Repurposing to Overcome Cancers)
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16 pages, 2316 KiB  
Article
A Network-Based Approach Exploiting Transcriptomics and Interactomics Data for Predicting Drug Repurposing Solutions Across Human Cancers
by Alessio Galimi and Giulia Fiscon
Cancers 2025, 17(7), 1144; https://doi.org/10.3390/cancers17071144 - 28 Mar 2025
Viewed by 266
Abstract
According to the European Federation of Pharmaceutical Industries and Association (EFPIA), a drug takes about 12–13 years from the first synthesis of a new active substance for the medicinal product to reach the market [...] Full article
(This article belongs to the Special Issue Advances in Drug Repurposing to Overcome Cancers)
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16 pages, 3569 KiB  
Article
Implications of GPIIB-IIIA Integrin and Liver X Receptor in Platelet-Induced Compression of Ovarian Cancer Multi-Cellular Spheroids
by Zitha Redempta Isingizwe, Virginie Sjoelund and Doris Mangiaracina Benbrook
Cancers 2024, 16(20), 3533; https://doi.org/10.3390/cancers16203533 - 19 Oct 2024
Viewed by 1208
Abstract
Background: Platelets have been shown to promote ovarian cancer; however, the mechanism is poorly understood. Previously, we demonstrated that platelets reduce the size and increase the density of multi-cellular ovarian cancer spheroids in cell cultures. The objectives of this study were to determine [...] Read more.
Background: Platelets have been shown to promote ovarian cancer; however, the mechanism is poorly understood. Previously, we demonstrated that platelets reduce the size and increase the density of multi-cellular ovarian cancer spheroids in cell cultures. The objectives of this study were to determine if platelet inhibitors could counteract these effects, and to explore the mechanisms involved. Methods: FDA-approved platelet inhibitors were screened for their abilities to alter platelet effects on ovarian cancer spheroids. Mass spectrometry was used to identify proteins significantly altered in cancer cells upon exposure to platelets. The effects of platelets and/or liver x receptor agonists or antagonists on LXR activity were measured using ES-2 ovarian cancer cells transduced with an LXR-reporter vector. Results: Eptifibatide, a GPIIB-IIIA integrin inhibitor, and dipyridamole, an adenosine reuptake inhibitor, reduced and enhanced platelet effects on ovarian cancer spheroids, respectively. Proteomic studies identified the LXR/RXR and integrin pathways as mediators of platelet effects on ovarian cancer, and downstream effectors of eptifibatide. Conclusions: Integrin pathways and their downstream LXR/RXR effectors are implicated in how platelets alter ovarian cancer spheroid morphology. These results support studying eptifibatide and LXR/RXR agonists as candidate drugs for repurposing as therapeutic strategies to counteract platelet promotion of ovarian cancer. Full article
(This article belongs to the Special Issue Advances in Drug Repurposing to Overcome Cancers)
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Review

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34 pages, 1418 KiB  
Review
Advances in the Repurposing and Blood–Brain Barrier Penetrance of Drugs in Pediatric Brain Tumors
by Julian S. Rechberger, Stephanie A. Toll, Subhasree Biswas, Hyo Bin You, William D. Chow, Nicholas Kendall, Pournima Navalkele and Soumen Khatua
Cancers 2025, 17(3), 439; https://doi.org/10.3390/cancers17030439 - 27 Jan 2025
Cited by 1 | Viewed by 1759
Abstract
Central nervous system (CNS) tumors are the leading cause of cancer-related mortality in children, with prognosis remaining dismal for some of these malignancies. Though the past two decades have seen advancements in surgery, radiation, and targeted therapy, major unresolved hurdles continue to undermine [...] Read more.
Central nervous system (CNS) tumors are the leading cause of cancer-related mortality in children, with prognosis remaining dismal for some of these malignancies. Though the past two decades have seen advancements in surgery, radiation, and targeted therapy, major unresolved hurdles continue to undermine the therapeutic efficacy. These include challenges in suboptimal drug delivery through the blood–brain barrier (BBB), marked intra-tumoral molecular heterogeneity, and the elusive tumor microenvironment. Drug repurposing or re-tasking FDA-approved drugs with evidence of penetration into the CNS, using newer methods of intracranial drug delivery facilitating optimal drug exposure, has been an area of intense research. This could be a valuable tool, as most of these agents have already gone through the lengthy process of drug development and the evaluation of safety risks and the optimal pharmacokinetic profile. They can now be used and tested in clinics with an accelerated and different approach. Conclusions: The next-generation therapeutic strategy should prioritize repurposing oncologic and non-oncologic drugs that have been used for other indication, and have demonstrated robust preclinical activity against pediatric brain tumors. In combination with novel drug delivery techniques, these drugs could hold significant therapeutic promise in pediatric neurooncology. Full article
(This article belongs to the Special Issue Advances in Drug Repurposing to Overcome Cancers)
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25 pages, 1395 KiB  
Review
H1 Antihistamines—Promising Candidates for Repurposing in the Context of the Development of New Therapeutic Approaches to Cancer Treatment
by Ewa Trybus and Wojciech Trybus
Cancers 2024, 16(24), 4253; https://doi.org/10.3390/cancers16244253 - 20 Dec 2024
Cited by 1 | Viewed by 2267
Abstract
Despite significant progress in the field of clinical oncology in terms of diagnostic and treatment methods, the results of anticancer therapy are still not fully satisfactory, especially due to limited response and high toxicity. This has forced the need for further research to [...] Read more.
Despite significant progress in the field of clinical oncology in terms of diagnostic and treatment methods, the results of anticancer therapy are still not fully satisfactory, especially due to limited response and high toxicity. This has forced the need for further research to finding alternative ways to improve success rates in oncological treatment. A good solution to this problem in the context of rapidly obtaining an effective drug that works on multiple levels of cancer and is also safe is the global strategy of repurposing an existing drug. Research into other applications of an existing drug enables a precise assessment of its possible mechanisms of action and, consequently, the broadening of therapeutic indications. This strategy is also supported by the fact that most non-oncological drugs have pleiotropic effects, and most of the diseases for which they were originally intended are multifactorial, which in turn is a very desirable phenomenon due to the heterogeneous and multifaceted biology of cancer. In this review, we will mainly focus on the anticancer potential of H1 antihistamines, especially the new generation that were not originally intended for cancer therapy, to highlight the relevant signaling pathways and discuss the properties of these agents for their judicious use based on the characteristic features of cancer. Full article
(This article belongs to the Special Issue Advances in Drug Repurposing to Overcome Cancers)
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