Related Experiment Video
Updated: Mar 26, 2026
Author Spotlight: Advancements in Molecular Biomarker Testing for Non-Squamous Non-Small Cell Lung Cancer
Published on: September 8, 2023
Evaluation of Three Small Molecular Drugs for Targeted Therapy to Treat Nonsmall Cell Lung Cancer
1Department of Respiratory Medicine, Peking Union Medical College Hospital, Peking Union Medical College and Chinese Academy of Medical Sciences, Beijing 100730, China.
Objective:
To guide the optimal selection among first-generation epidermal growth factor receptor-tyrosine kinase inhibitors (EGFR-TKIs) in clinical practice. This review attempted to provide a thorough comparison among three first-generation EGFR-TKIs, namely icotinib, erlotinib, and gefitinib, with regard to their molecular structure, pharmacokinetic parameters, clinical data, adverse reactions, and contraindications.
Data Sources:
An electronic literature search of the PubMed database and Google Scholar for all the available articles regarding gefitinib, icotinib, and erlotinib in the English language from January 2005 to December 2014 was used.
Study Selection:
The search terms or keywords included but not limited to "lung cancer", "nonsmall cell lung cancer (NSCLC)", "epidemiology", "EGFR", "TKIs", and "optimal selection ".
Results:
As suggested by this review, even though the three first-generation EGFR-TKIs share the quinazoline structure, erlotinib had the strongest apoptosis induction activity because of its use of a different side-chain. The pharmacokinetic parameters indicated that both erlotinib and icotinib are affected by food. The therapeutic window of erlotinib is narrow, and the recommended dosage is close to the maximum tolerable dosage. Icotinib enjoys a wider therapeutic window, and its concentration in the blood is within a safe dosage range even if it is administered with food. Based on multiple large-scale clinical trials, erlotinib is universally applied as the first-line treatment. In marked contrast, icotinib is available only in China as the second- or third-line therapeutic approach for treating advanced lung cancer. In addition, it exhibits a similar efficacy but better safety profile than gefitinib.
Conclusions:
Although there is a paucity of literature regarding whether icotinib is superior to erlotinib, its superior toxicity profile, noninferior efficacy, and lower cost indicate that it is a better alternative for Chinese patients living with advanced NSCLC.
Insights
This review compares first-generation epidermal growth factor receptor-tyrosine kinase inhibitors (EGFR-TKIs) for optimal lung cancer treatment selection. Icotinib shows a better safety profile and lower cost, making it a preferred choice for Chinese patients with advanced non-small cell lung cancer (NSCLC).
Area of Science:
- Oncology
- Pharmacology
- Medical Chemistry
Background:
- First-generation epidermal growth factor receptor-tyrosine kinase inhibitors (EGFR-TKIs) are crucial in treating non-small cell lung cancer (NSCLC).
- Optimal selection among icotinib, erlotinib, and gefitinib requires a comprehensive understanding of their properties.
- Clinical practice needs clear guidance for choosing the most effective and safe first-generation EGFR-TKI.
Purpose of the Study:
- To compare three first-generation EGFR-TKIs: icotinib, erlotinib, and gefitinib.
- To evaluate their molecular structure, pharmacokinetics, clinical data, and safety profiles.
- To guide optimal selection of these EGFR-TKIs in clinical practice for NSCLC.
Main Methods:
- Conducted an electronic literature search of PubMed and Google Scholar.
- Included English-language articles published from January 2005 to December 2014.
- Utilized keywords such as "lung cancer", "NSCLC", "EGFR", and "TKIs" for comprehensive data retrieval.
Main Results:
- Erlotinib demonstrated the strongest apoptosis induction activity due to its unique side-chain.
- Icotinib and erlotinib pharmacokinetics are affected by food; icotinib has a wider therapeutic window and safer blood concentration.
- Erlotinib is a universal first-line treatment, while icotinib, available in China, shows similar efficacy with better safety than gefitinib for advanced NSCLC.
Conclusions:
- Icotinib presents a superior toxicity profile, non-inferior efficacy, and lower cost compared to erlotinib.
- Icotinib is a more favorable alternative for Chinese patients with advanced NSCLC.
- Further literature is needed to definitively establish icotinib's superiority over erlotinib.
Related Concept Videos
02:57Targeted Cancer Therapies
There are several types of targeted therapies against...
02:57Targeted Cancer Therapies
02:50Combination Therapies and Personalized Medicine
The combination of the drug acetazolamide and sulforaphane is a good example of combination therapy to treat cancer. The cells in the interior of a large tumor often die due to the hypoxic and...
01:26Targets for Drug Action: Overview
Receptors are either membrane-spanning or intracellular proteins, which upon binding a ligand, get activated and transmit the signal downstream to elicit a response. Drugs bind receptors, either mimicking the action of endogenous ligands or blocking the receptor activity to bring about a modified response. Nearly 35% of approved drugs target the G...