Abstract
Tumour resistance to anticancer agents remains a challenge in oncological practice, because it results in exposure to toxicities, unnecessary costs and, most importantly, delay of a potentially more effective treatment. Drug uptake by tumours may be impaired by several resistance pathways. Reasons for primary resistance may be that the drug is not delivered to the tumour or that its uptake by the tumour is not sufficient. Drug delivery depends on its distribution within the body, its bioavailability in the circulation and its transport to the tumour. Binding of drugs to circulating cells and proteins, formation of inactive metabolites as well as a rapid drug clearance may limit bioavailability. Furthermore, drug delivery to tumours is regulated by tumour vascularisation. Finally, tumour targets such as hormone receptors and efflux pumps also influence drug uptake by tumours. The use of specific PET tracers such as radiolabelled anticancer drugs (e.g. [18F]fluoropaclitaxel and [18F]5-fluorouracil) provide a unique means for individualized treatment planning and drug development. Combining these specific tracers with other less specific tracers, such as tracers for blood flow (e.g. [15O]H2O) and efflux (e.g. [11C]verapamil), may provide additional information on drug resistance mechanisms. Furthermore, radiolabelled anticancer agents may be valuable to evaluate the optimal timing of combination therapies. This review will focus on how PET can reveal different mechanisms of tumour resistance and thus may play a role in drug development and prediction of tumour response.
Keywords: Radiolabelled Anticancer Drugs, Oncology, Tumour, PET, fluoropaclitaxel, fluorouracil
Current Pharmaceutical Design
Title: Individualized Treatment Planning in Oncology: Role of PET and Radiolabelled Anticancer Drugs in Predicting Tumour Resistance
Volume: 14 Issue: 28
Author(s): Astrid A.M. van der Veldt, Gert Luurtsema, Mark Lubberink, Adriaan A. Lammertsma and N. Harry Hendrikse
Affiliation:
Keywords: Radiolabelled Anticancer Drugs, Oncology, Tumour, PET, fluoropaclitaxel, fluorouracil
Abstract: Tumour resistance to anticancer agents remains a challenge in oncological practice, because it results in exposure to toxicities, unnecessary costs and, most importantly, delay of a potentially more effective treatment. Drug uptake by tumours may be impaired by several resistance pathways. Reasons for primary resistance may be that the drug is not delivered to the tumour or that its uptake by the tumour is not sufficient. Drug delivery depends on its distribution within the body, its bioavailability in the circulation and its transport to the tumour. Binding of drugs to circulating cells and proteins, formation of inactive metabolites as well as a rapid drug clearance may limit bioavailability. Furthermore, drug delivery to tumours is regulated by tumour vascularisation. Finally, tumour targets such as hormone receptors and efflux pumps also influence drug uptake by tumours. The use of specific PET tracers such as radiolabelled anticancer drugs (e.g. [18F]fluoropaclitaxel and [18F]5-fluorouracil) provide a unique means for individualized treatment planning and drug development. Combining these specific tracers with other less specific tracers, such as tracers for blood flow (e.g. [15O]H2O) and efflux (e.g. [11C]verapamil), may provide additional information on drug resistance mechanisms. Furthermore, radiolabelled anticancer agents may be valuable to evaluate the optimal timing of combination therapies. This review will focus on how PET can reveal different mechanisms of tumour resistance and thus may play a role in drug development and prediction of tumour response.
Export Options
About this article
Cite this article as:
van der Veldt A.M. Astrid, Luurtsema Gert, Lubberink Mark, Lammertsma A. Adriaan and Hendrikse Harry N., Individualized Treatment Planning in Oncology: Role of PET and Radiolabelled Anticancer Drugs in Predicting Tumour Resistance, Current Pharmaceutical Design 2008; 14 (28) . https://dx.doi.org/10.2174/138161208786404344
DOI https://dx.doi.org/10.2174/138161208786404344 |
Print ISSN 1381-6128 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4286 |
Call for Papers in Thematic Issues
"Tuberculosis Prevention, Diagnosis and Drug Discovery"
The Nobel Prize-winning discoveries of Mycobacterium tuberculosis and streptomycin have enabled an appropriate diagnosis and an effective treatment of tuberculosis (TB). Since then, many newer diagnosis methods and drugs have been saving millions of lives. Despite advances in the past, TB is still a leading cause of infectious disease mortality ...read more
Current Pharmaceutical challenges in the treatment and diagnosis of neurological dysfunctions
Neurological dysfunctions (MND, ALS, MS, PD, AD, HD, ALS, Autism, OCD etc..) present significant challenges in both diagnosis and treatment, often necessitating innovative approaches and therapeutic interventions. This thematic issue aims to explore the current pharmaceutical landscape surrounding neurological disorders, shedding light on the challenges faced by researchers, clinicians, and ...read more
Emerging and re-emerging diseases
Faced with a possible endemic situation of COVID-19, the world has experienced two important phenomena, the emergence of new infectious diseases and/or the resurgence of previously eradicated infectious diseases. Furthermore, the geographic distribution of such diseases has also undergone changes. This context, in turn, may have a strong relationship with ...read more
Melanoma and Non-Melanoma Skin Cancer Treatment: Standard of Care and Recent Advances
In this thematic issue, we aim to provide a standard of care of the diagnosis and treatment of melanoma and non-melanoma skin cancer. The editor will invite authors from different countries who will write review articles of melanoma and non-melanoma skin cancers. The Diagnosis, Staging, Surgical Treatment, Non-Surgical Treatment all ...read more
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
- Announcements
Related Articles
-
Use of Insulin and Insulin Analogs and Risk of Cancer — Systematic Review and Meta-Analysis of Observational Studies
Current Drug Safety Pitavastatin and 4-Hydroxy-3-Methoxyacetophenone (HMAP) Reduce Cognitive Dysfunction in Vascular Dementia During Experimental Diabetes
Current Neurovascular Research Osteogenic Peptides in Bone Regeneration
Current Pharmaceutical Design Oncogene Suppression by Small Interfering RNAs
Current Pharmaceutical Biotechnology MicroRNAs: A Critical Regulator and a Promising Therapeutic and Diagnostic Molecule for Diabetic Cardiomyopathy
Current Gene Therapy Natural Compounds and Drug Discovery: Can Cnidarian Venom Play a Role?
Central Nervous System Agents in Medicinal Chemistry Lymphangiogenesis and Anti-Tumor Immune Responses
Current Molecular Medicine ABC Transporter Inhibitors in Reversing Multidrug Resistance to Chemotherapy
Current Drug Targets Bioactive Cyclohexenones: A Mini Review
Current Bioactive Compounds Targeting Never-In-Mitosis-A Related Kinase 5 in Cancer: A Review
Current Medicinal Chemistry Quinone-Based Drugs: An Important Class of Molecules in Medicinal Chemistry
Medicinal Chemistry MicroRNA Polymorphisms, MicroRNA Pharmacogenomics and Cancer Susceptibility
Current Pharmacogenomics and Personalized Medicine All for Statins and Statins for All; An Update
Current Pharmaceutical Design Anticancer Drugs Aimed at E6 and E7 Activity in HPV-Positive Cervical Cancer
Current Cancer Drug Targets Electrical Impedance Scanning - A New Diagnostic Tool in Cancer Detection: Current Status and Recent Developments
Current Medical Imaging Spirooxindoles as Potential Pharmacophores
Mini-Reviews in Medicinal Chemistry Utility of γH2AX as a Molecular Marker of DNA Double-Strand Breaks in Nuclear Medicine: Applications to Radionuclide Therapy Employing Auger Electron-Emitting Isotopes
Current Radiopharmaceuticals Latest Results for Anti-Angiogenic Drugs in Cancer Treatment
Current Pharmaceutical Design The Utilization of Gene Targeting Models During in Preclinical Study of Drug Discovery Process - Example of Phenotypic and Functional Analysis of Cacna1 βGene Product
Current Pharmaceutical Biotechnology Cucurbitacin IIb from Ibervillea sonorae Induces Apoptosis and Cell Cycle Arrest via STAT3 Inhibition
Anti-Cancer Agents in Medicinal Chemistry