Novel Anti-cancer Compounds: Drug Metabolism and Absorption

A special issue of Pharmaceutics (ISSN 1999-4923). This special issue belongs to the section "Pharmacokinetics and Pharmacodynamics".

Deadline for manuscript submissions: 31 July 2024 | Viewed by 995

Special Issue Editors


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Guest Editor
Department of Pharmacology and PharmacoGenomics Research Center, Inje University College of Medicine, Inje University, Busan 47392, Republic of Korea
Interests: drug–drug interaction; metabolomics; drug metabolism and pharmacokinetics
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Guest Editor
Faculty of Chemistry, Gdańsk University of Technology, Gdańsk, Poland
Interests: anticancer drugs; biotransformation; detoxification; reactive intermediates; drug metabolizing enzymes; cytochrome P450; glutathione conjugates; glutathione S-transferase; metabolite identification; metabolite electrosynthesis; high-performance liquid chromatography; mass spectrometry

Special Issue Information

Dear Colleagues,

The success of cancer chemotherapy depends on the selection of safe and effective medication. Thus, the development of a new anti-cancer drug requires careful consideration of its absorption and metabolism in the patient, which determine a drug’s systemic bioavailability, therapeutic effect, and toxicity. Research in this area provides, i.e., knowledge about the activation and detoxification metabolism of a drug candidate as well as its affinity to interact with drug transporters and/or drug-metabolizing enzymes. The evaluation of reactive drug metabolites, which usually are responsible for the majority of rapid and unexpected drug toxic effects, is particularly challenging. Critically, progress in these studies depends on the development and improvement of different approaches for the generation, identification, and characterization of various types of drug metabolites. Especially, in silico and in vitro methods that are able to predict metabolic reactions that take place in the human body, but do not involve living organisms, are focused on.

This Special Issue aims to collect up-to-date information regarding the study of novel anti-cancer compounds in different areas, including drug delivery, the assessment of drug metabolites and metabolic pathways, and the prediction of transporter- or enzyme-mediated drug interactions using different in silico, in vitro and in vivo strategies.

All researchers actively involved in anti-cancer drug discovery and development are invited to contribute to this Special Issue. Original research articles and review articles on the abovementioned topics are particularly welcome.

We look forward to receiving your contributions.

Prof. Dr. Dong Hyun Kim
Dr. Agnieszka Potęga
Guest Editors

Manuscript Submission Information

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Keywords

  • absorption
  • anti-cancer activity
  • biotransformation
  • detoxification
  • drug transporters
  • drug-metabolizing enzymes
  • metabolic activation
  • metabolite identification
  • reactive metabolites

Published Papers (1 paper)

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Review

34 pages, 3426 KiB  
Review
Enhancing the Bioavailability of Resveratrol: Combine It, Derivatize It, or Encapsulate It?
by Mohamed Salla, Nadine Karaki, Belal El Kaderi, Abeer J. Ayoub, Samar Younes, Maya N. Abou Chahla, Shairaz Baksh and Sami El Khatib
Pharmaceutics 2024, 16(4), 569; https://doi.org/10.3390/pharmaceutics16040569 - 22 Apr 2024
Viewed by 544
Abstract
Overcoming the limited bioavailability and extensive metabolism of effective in vitro drugs remains a challenge that limits the translation of promising drugs into clinical trials. Resveratrol, despite its well-reported therapeutic benefits, is not metabolically stable and thus has not been utilized as an [...] Read more.
Overcoming the limited bioavailability and extensive metabolism of effective in vitro drugs remains a challenge that limits the translation of promising drugs into clinical trials. Resveratrol, despite its well-reported therapeutic benefits, is not metabolically stable and thus has not been utilized as an effective clinical drug. This is because it needs to be consumed in large amounts to overcome the burdens of bioavailability and conversion into less effective metabolites. Herein, we summarize the more relevant approaches to modify resveratrol, aiming to increase its biological and therapeutic efficacy. We discuss combination therapies, derivatization, and the use of resveratrol nanoparticles. Interestingly, the combination of resveratrol with established chemotherapeutic drugs has shown promising therapeutic effects on colon cancer (with oxaliplatin), liver cancer (with cisplatin, 5-FU), and gastric cancer (with doxorubicin). On the other hand, derivatizing resveratrol, including hydroxylation, amination, amidation, imidation, methoxylation, prenylation, halogenation, glycosylation, and oligomerization, differentially modifies its bioavailability and could be used for preferential therapeutic outcomes. Moreover, the encapsulation of resveratrol allows its trapping within different forms of shells for targeted therapy. Depending on the nanoparticle used, it can enhance its solubility and absorption, increasing its bioavailability and efficacy. These include polymers, metals, solid lipids, and other nanoparticles that have shown promising preclinical results, adding more “hype” to the research on resveratrol. This review provides a platform to compare the different approaches to allow directed research into better treatment options with resveratrol. Full article
(This article belongs to the Special Issue Novel Anti-cancer Compounds: Drug Metabolism and Absorption)
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