Drug Metabolism and New Drug Development for Cancers

A special issue of Metabolites (ISSN 2218-1989). This special issue belongs to the section "Pharmacology and Drug Metabolism".

Deadline for manuscript submissions: 31 August 2025 | Viewed by 4802

Special Issue Editors


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Guest Editor
Department of Pharmaceutical Chemistry, Poznan University of Medical Sciences, 60-780 Poznan, Poland
Interests: drug analysis; drug stability; pharmaceutical chemistry
Special Issues, Collections and Topics in MDPI journals

E-Mail Website
Guest Editor
Department of Pharmaceutical Chemistry, Poznan University of Medical Sciences, 60-780 Poznan, Poland
Interests: parenteral nutrition; drug interaction; pharmaceutical chemistry; nanoformulation; nano-delivery system; drug stability

Special Issue Information

Dear Colleagues,

We invite you to contribute to this Special Issue. Cancer is one of the top causes of death worldwide. However, medical sciences do not remain indifferent and the race is on, the primary goal of which is to help patients through the development of new anticancer drugs and treatments. Understanding metabolic pathways and developing new molecules and formulations for drug delivery are only some of the possible weapons in this unequal fight. The path from developing an active ingredient to implementing the drug into clinical practice is long and involves the work of many specialists.

This Special Issue is devoted to Drug Metabolism and New Drug Development for Cancers and aims to publish original articles as well as interesting review articles on the following topics:

  • The biochemistry of anticancer molecules.
  • The impact of anticancer drugs/substances on metabolism.
  • Natural compounds/extracts and plant screening for antineoplastic activity metabolites.
  • Studies in pharmaceutical chemistry: drug structure and activity relationships or the development of new molecules.
  • Developing new delivery methods for known substances, for example, formulating new nanoforms such as liposomes, micelles, nanospheres, etc.

Additionally, this Special Issue will be a summary of important research in the development of medical sciences.

Prof. Dr. Anna Jelińska
Dr. Szymon Tomczak
Guest Editors

Manuscript Submission Information

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Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 2700 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

  • cancer
  • new drug development
  • metabolites
  • secondary plant metabolites
  • drug delivery
  • nanoformulation
  • anticancer treatment

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Published Papers (3 papers)

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Research

16 pages, 2315 KiB  
Article
Potential Use of Common Administration of Emulsion for Parenteral Nutrition and Vinpocetine: Compatibility Study and Prospect
by Szymon Tomczak, Kornelia Kaszuba, Jagoda Szkudlarek, Ludwika Piwowarczyk and Anna Jelińska
Metabolites 2024, 14(8), 439; https://doi.org/10.3390/metabo14080439 - 7 Aug 2024
Cited by 1 | Viewed by 1173
Abstract
Vinpocetine (VP) is distributed after oral and intravenous administration, and its uptake in the thalamus, basal ganglia, and visual cortex. Due to poor bioavailability (~7%) and marked first-pass effect (~75%), including a short half-life (2–3 h), oral administration of VP is limited. It [...] Read more.
Vinpocetine (VP) is distributed after oral and intravenous administration, and its uptake in the thalamus, basal ganglia, and visual cortex. Due to poor bioavailability (~7%) and marked first-pass effect (~75%), including a short half-life (2–3 h), oral administration of VP is limited. It requires frequent administration of the drug to obtain a therapeutic effect. Attempts to overcome these difficulties include the use of new drug delivery systems and/or alternative routes of drug administration. One possibility is the common administration of lipid emulsion and drug using the same catheter. However, this procedure is not recommended due to potential interaction and lack of safety data. For this purpose, we checked the compatibility of VP solutions with eight commercially available parenteral nutrition admixtures, i.e., Lipoflex special, Omegaflex special, Lipoflex peri, Omegaflex peri, Kabiven, SmofKabiven, Kabiven Peripheral, and Olimel Peri N4E. Coadministration is only possible if the stability of the drug and the lipid emulsion is confirmed. The available data are scarce and only concern the incompatibility of VP with ibuprofen. Compatibility tests were carried out in simulated administration through a Y-site connector using clinical flow rates. The stability of the drug and lipid emulsion was assessed by visual inspection and measurement of pH, osmolality, particle size as mean droplet diameter (MDD) and percentage of lipids residing in globules larger than 5 µm (PFAT5), zeta potential, polydispersity index, and lipid-free parenteral nutrition admixture(PNA) turbidity. The results of the compatibility of VP with eight commercial PN admixtures showed that all lipid emulsions show different signs of destabilization. In the studied samples, particles larger than 1000 nm, a significant increase in MDD, zeta potential, and loss of homogeneity visible as an increase in the polydispersity index were observed. Most of the samples had PFAT5 above the USP limit (0.05%). Taking into account the obtained data, VP should not be administered with the studied lipid emulsions for parenteral nutrition. Full article
(This article belongs to the Special Issue Drug Metabolism and New Drug Development for Cancers)
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18 pages, 5522 KiB  
Article
The Comparative Metabolism of a Novel Hepatocellular Carcinoma Therapeutic Agent, 2,3-Diamino-N-(4-(benzo[d]thiazol-2-yl)phenyl)propanamide, in Human and Animal Hepatocytes
by Young-Heun Jung, Dong-Cheol Lee, Ye-Min Kwon, Eunbee Jang, Garam Choi, Yeoun-Hee Kim, Tae Hwan Kim and Ju-Hyun Kim
Metabolites 2024, 14(8), 425; https://doi.org/10.3390/metabo14080425 - 1 Aug 2024
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Abstract
[2,3-diamino-N-(4-(benzo[d]thiazol-2-yl)phenyl)propanamide], named as ETN101, is a novel therapeutic agent for hepatocellular carcinoma. In vitro studies examined ETN101 metabolites in human, mouse, rat, dog, and monkey hepatocytes and identified the drug-metabolizing enzymes involved using cDNA-expressed human recombinant cytochrome P450s (CYPs), carboxylesterases (CESs), [...] Read more.
[2,3-diamino-N-(4-(benzo[d]thiazol-2-yl)phenyl)propanamide], named as ETN101, is a novel therapeutic agent for hepatocellular carcinoma. In vitro studies examined ETN101 metabolites in human, mouse, rat, dog, and monkey hepatocytes and identified the drug-metabolizing enzymes involved using cDNA-expressed human recombinant cytochrome P450s (CYPs), carboxylesterases (CESs), N-acetyltransferase (NAT) 1, and human liver cytosol. ETN101 showed similar metabolic stability across hepatocytes from five species, with particularly comparable stability in humans, rats, and monkeys. Its half-life was 75.0 min in humans, 68.9 in rats, 73.1 in monkeys, 120.4 in mice, and 112.7 in dogs. Thirty-four ETN101 metabolites, including the major metabolite M1, were identified using liquid chromatography–high-resolution mass spectrometry. ETN101 was primarily metabolized to M1 and CYP1A2 is exclusively responsible for M1 metabolism. Both NAT1 and NAT2 were responsible for the N-acetylation of M1 to M2. ETN101 remained stable in human CESs. In conclusion, this study provides comprehensive insights into the metabolic characteristics of ETN101, valuable for its toxicological and clinical development. Full article
(This article belongs to the Special Issue Drug Metabolism and New Drug Development for Cancers)
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16 pages, 4416 KiB  
Article
Elucidation and Regulation of Tyrosine Kinase Inhibitor Resistance in Renal Cell Carcinoma Cells from the Perspective of Glutamine Metabolism
by Kento Morozumi, Yoshihide Kawasaki, Tomonori Sato, Masamitsu Maekawa, Shinya Takasaki, Shuichi Shimada, Takanari Sakai, Shinichi Yamashita, Nariyasu Mano and Akihiro Ito
Metabolites 2024, 14(3), 170; https://doi.org/10.3390/metabo14030170 - 19 Mar 2024
Cited by 1 | Viewed by 1767
Abstract
Tyrosine kinase inhibitors (TKIs) play a crucial role in the treatment of advanced renal cell carcinoma (RCC). However, there is a lack of useful biomarkers for assessing treatment efficacy. Through urinary metabolite analysis, we identified the metabolites and pathways involved in TKI resistance [...] Read more.
Tyrosine kinase inhibitors (TKIs) play a crucial role in the treatment of advanced renal cell carcinoma (RCC). However, there is a lack of useful biomarkers for assessing treatment efficacy. Through urinary metabolite analysis, we identified the metabolites and pathways involved in TKI resistance and elucidated the mechanism of TKI resistance. To verify the involvement of the identified metabolites obtained from urine metabolite analysis, we established sunitinib-resistant RCC cells and elucidated the antitumor effects of controlling the identified metabolic pathways in sunitinib-resistant RCC cells. Through the analysis of VEGFR signaling, we aimed to explore the mechanisms underlying the antitumor effects of metabolic control. Glutamine metabolism has emerged as a significant pathway in urinary metabolite analyses. In vitro and in vivo studies have revealed the antitumor effects of sunitinib-resistant RCC cells via knockdown of glutamine transporters. Furthermore, this antitumor effect is mediated by the control of VEGFR signaling via PTEN. Our findings highlight the involvement of glutamine metabolism in the prognosis and sunitinib resistance in patients with advanced RCC. Additionally, the regulating glutamine metabolism resulted in antitumor effects through sunitinib re-sensitivity in sunitinib-resistant RCC. Our results are expected to contribute to the more effective utilization of TKIs with further improvements in prognosis through current drug therapies. Full article
(This article belongs to the Special Issue Drug Metabolism and New Drug Development for Cancers)
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