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Recent Advances of Novel Pharmaceutical Designs for Anti-Cancer Therapies, 3rd Edition

A special issue of International Journal of Molecular Sciences (ISSN 1422-0067). This special issue belongs to the section "Molecular Pharmacology".

Deadline for manuscript submissions: 20 June 2025 | Viewed by 1583

Special Issue Editor

Special Issue Information

Dear Colleagues,

The development of efficient and well-tolerated anticancer drugs is one of the main healthcare challenges of the century, with rising numbers of cancer patients worldwide. The close correspondence of clinicians, tumor biologists and medicinal chemists is mandatory for the successful establishment of new cancer treatments. Small-molecule protein binders and enzyme inhibitors, natural products, DNA-targeting alkylating agents and metal complexes form the main part of the current arsenal of anticancer drugs, which can serve as starting points for the development of new compounds with improved activity, bioavailability and potential to overcome drug resistance. Repurposed drugs and cost-effective new compounds obtained from multi-component reactions or few-step syntheses can become broadly available anticancer drugs. Computer-aided drug design contributes to the optimisation of existing drugs, as well as the identification of the first-generation inhibitors of new cancer targets. Sophisticated formulation systems improve pharmacokinetics and the tumor targeting properties of anticancer drugs. Recent drug research efforts aim at cancer epigenetics, cancer stem-like cells, tumor microenvironment and immunology. This Special Issue intends to showcase the current efforts on anticancer drug design and development. Original research articles, review articles, and short communications within (but not restricted to) the described research fields are welcome.

Dr. Bernhard Biersack
Guest Editor

Manuscript Submission Information

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Keywords

  • cancer
  • anticancer drugs
  • drug design
  • targeted therapy
  • immunotherapy
  • molecular target
  • molecular mechanism
  • drug resistance

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Published Papers (1 paper)

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Research

14 pages, 4539 KiB  
Article
Synergistic Enhancement of Antitumor Effects by Combining Abemaciclib with Desipramine
by Yan Li, Yeojin Sung, Young Eun Choi, Yongdoo Choi and Sung-Ho Goh
Int. J. Mol. Sci. 2024, 25(13), 7407; https://doi.org/10.3390/ijms25137407 - 5 Jul 2024
Viewed by 1106
Abstract
Cyclin-dependent kinase 4 and 6 (CDK4/6) inhibitors, including abemaciclib, have been approved for the treatment of hormone receptor-positive, human epidermal growth factor receptor 2 (HER2)-negative advanced, and metastatic breast cancer. Despite the high therapeutic efficacy of CDK4/6 inhibitors, they are associated with various [...] Read more.
Cyclin-dependent kinase 4 and 6 (CDK4/6) inhibitors, including abemaciclib, have been approved for the treatment of hormone receptor-positive, human epidermal growth factor receptor 2 (HER2)-negative advanced, and metastatic breast cancer. Despite the high therapeutic efficacy of CDK4/6 inhibitors, they are associated with various adverse effects, including potentially fatal interstitial lung disease. Therefore, a combination of CDK4/6 inhibitors with letrozole or fulvestrant has been attempted but has demonstrated limitations in reducing adverse effects, highlighting the need to develop new combination therapies. This study proposes a combination strategy using CDK4/6 inhibitors and tricyclic antidepressants to enhance the therapeutic outcomes of these inhibitors while reducing their side effects. The therapeutic efficacies of abemaciclib and desipramine were tested in different cancer cell lines (H460, MCF7, and HCT-116). The antitumor effects of the combined abemaciclib and desipramine treatment were evaluated in a xenograft colon tumor model. In vitro cell studies have shown the synergistic anticancer effects of combination therapy in the HCT-116 cell line. The combination treatment significantly reduced tumor size compared with control or single treatment without causing apparent toxicity to normal tissues. Although additional in vivo studies are necessary, this study suggests that the combination therapy of abemaciclib and desipramine may represent a novel therapeutic approach for treating solid tumors. Full article
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