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Updated: Jun 22, 2025

Assessing Specificity of Anticancer Drugs In Vitro
Published on: March 23, 2016
Classification of anticancer drugs: an update with FDA- and EMA-approved drugs
Lorena Ostios-Garcia1, Daniel Martínez Pérez1, Beatriz Castelo1
1Department of Medical Oncology, Hospital Universitario La Paz, Madrid, Spain.
Abstract:
Anticancer systemic therapy comprises a complex and growing group of drugs. Some of the new agents with novel mechanisms of action that have appeared are difficult to fit in the groups of classical chemotherapy, hormones, tyrosine-kinase inhibitors, and monoclonal antibodies. We propose a classification based on two levels of information: the site of action and the mechanism of action. Regarding the former, drugs can exert their action in the tumor cell, the tumor vasculature, the immune system, or the endocrine system. The mechanism of action refers to the molecular target.
Insights
New anticancer drugs require a novel classification system. This system categorizes anticancer therapies by their site of action (tumor cell, vasculature, immune, or endocrine system) and molecular target mechanism.
Area of Science:
- Oncology
- Pharmacology
- Drug Discovery
Background:
- Anticancer systemic therapy encompasses a diverse and expanding range of drugs.
- Emerging novel agents often defy traditional classification categories like chemotherapy, hormones, tyrosine-kinase inhibitors, and monoclonal antibodies.
Purpose of the Study:
- To propose a new, two-level classification system for anticancer systemic therapy.
- To address the challenge of categorizing novel anticancer agents with unique mechanisms of action.
Main Methods:
- Classification based on the site of drug action.
- Classification based on the molecular mechanism of drug action.
Main Results:
- The proposed classification identifies four primary sites of action: tumor cell, tumor vasculature, immune system, and endocrine system.
- The mechanism of action is defined by the specific molecular target of the drug.
Conclusions:
- A dual-level classification system (site and mechanism of action) provides a more effective framework for understanding and categorizing modern anticancer therapies.
- This classification aids in organizing the growing complexity of systemic anticancer drug options.
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