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Targeted Cancer Therapies

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The targeted cancer therapies, also known as “molecular targeted therapies,” take advantage of the molecular and genetic differences between the cancer cells and the normal cells. It needs a thorough understanding of the cancer cells to develop drugs that can target specific molecular aspects that drive the growth, progression, and spread of cancer cells without affecting the growth and survival of other normal cells in the body.
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Related Experiment Video

Updated: Mar 24, 2026

Establishment and Characterization of Three Afatinib-resistant Lung Adenocarcinoma PC-9 Cell Lines Developed with Increasing Doses of Afatinib

Establishment and Characterization of Three Afatinib-resistant Lung Adenocarcinoma PC-9 Cell Lines Developed with Increasing Doses of Afatinib

Published on: June 26, 2019

Recent progress on third generation covalent EGFR inhibitors.

Hengmiao Cheng¹, Sajiv K Nair¹, Brion W Murray²

¹Oncology Medicinal Chemistry, La Jolla Laboratories, Pfizer Worldwide Research and Development, 10770 Science Center Drive, San Diego, CA 92121, United States.

Bioorganic & Medicinal Chemistry Letters

|March 13, 2016

Summary

First-generation EGFR inhibitors are effective for NSCLC with specific mutations but lead to resistance. Third-generation inhibitors target resistance mutations like T790M, offering new treatment options.

Keywords:

Covalent inhibitor Drug resistance EGFR Lung cancer NSCLC Oncogenic mutation SBDD T790M

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Establishment and Characterization of Three Afatinib-resistant Lung Adenocarcinoma PC-9 Cell Lines Developed with Increasing Doses of Afatinib

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Published on: June 26, 2019

Establishing Dual Resistance to EGFR-TKI and MET-TKI in Lung Adenocarcinoma Cells In Vitro with a 2-step Dose-escalation Procedure

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Profiling Sensitivity to Targeted Therapies in EGFR-Mutant NSCLC Patient-Derived Organoids

Profiling Sensitivity to Targeted Therapies in EGFR-Mutant NSCLC Patient-Derived Organoids

Published on: November 22, 2021

Area of Science:

Oncology
Pharmacology
Molecular Biology

Background:

First-generation EGFR inhibitors (gefitinib, erlotinib) show efficacy in NSCLC with EGFR mutations (L858R, exon 19 deletions).
Drug resistance, often due to the EGFR-T790M mutation, limits long-term treatment success in approximately 60% of patients.

Purpose of the Study:

To review third-generation covalent EGFR inhibitors for NSCLC treatment.
To discuss novel drug discovery methodologies for these advanced inhibitors.

Main Methods:

Literature review of clinical trials involving third-generation EGFR inhibitors.
Analysis of drug discovery approaches for novel covalent EGFR inhibitors.

Main Results:

Third-generation covalent EGFR inhibitors exhibit high potency against T790M mutants.
These inhibitors demonstrate selectivity over wild-type (WT) EGFR, minimizing off-target effects.

Conclusions:

Third-generation EGFR inhibitors represent a promising therapeutic strategy for NSCLC patients with T790M-mediated resistance.
Ongoing research and novel discovery methods are crucial for developing next-generation EGFR-targeted therapies.