ReviewMolecules (Basel, Switzerland)2021
Globally Approved EGFR Inhibitors: Insights into Their Syntheses, Target Kinases, Biological Activities, Receptor Interactions, and Metabolism.
Review in Molecules (Basel, Switzerland), 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 105 papers, 3 of them syntheses that pooled it.
What it found
Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.
The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
105 citing papers in PubMed, 3 syntheses or guidelines pooled it.
- Unravelling the biological nexus of smoking and postpartum depression: a meta-analysis and functional genomics approach.Archives of women's mental health · 2026Pooled it
- Receptor tyrosine kinase targeted therapies in glioblastoma: a systematic review.Frontiers in medicine · 2026Pooled it
- Progress and prospects of targeted therapy and immunotherapy for urachal carcinoma.Frontiers in pharmacology · 2023Pooled it
- Design, synthesis, and biological evaluation of quinolin-2-one/thiazole hybrids as multi-targeted antiproliferative agents inducing caspase-dependent apoptosis.Scientific reports · 2026Article
- Exploring tyrosine kinase inhibitors for HER2-positive breast cancer: comprehensive review on a complete pharmacology-molecular mechanisms, safety profiles, and insights from preclinical and clinical studies.Clinical & translational oncology : official publication of the Federation of Spanish Oncology Societies and of the National Cancer Institute of Mexico · 2026Review
- On-resin Heck coupling enables small-molecule ligand discovery with covalent peptide-encoded libraries.Chemical science · 2026Article
- Post-marketing safety surveillance of EGFR-targeted agents and disseminated intravascular coagulation risk: a disproportionality analysis based on the FDA Adverse Event Reporting System.International journal of clinical pharmacy · 2026Article
- Structure-Activity Relationship Evaluation of Melatonin and Its Derivatives for Wound-Healing Applications: A Combined Network Pharmacology, Molecular Docking, and Biological Validation Approach.International journal of molecular sciences · 2026Article
- Identification of miR-21-5p and miR-21-3p regulated hub genes and drug repurposing targets in cervical cancer: an integrative computational analysis.Naunyn-Schmiedeberg's archives of pharmacology · 2026Article
- Design, Synthesis of Novel Quinazolinone Derivatives and Evaluation of EGFR Kinase Inhibition Activity via In Vitro and In Silico Studies.Chemical biology & drug design · 2026Article
- Design, click-based synthesis, molecular docking, molecular dynamics and anticancer activity of new isoindoline-1,3-dione- triazole-glycopyranosyl hybrids.Scientific reports · 2026Article
- Multi-target regulation by artemether in MAFLD through EGFR/HSP90 pathways.Journal of advanced research · 2026Article
- Novel "C-Clamp" Design of Highly Selective Small-Molecule Sensors for Kinase Proteins.Chemical & biomedical imaging · 2026Article
- Molecularly Targeted Therapies in Oncology: Mechanisms, Resistance, and Combination Strategies.Molecules (Basel, Switzerland) · 2026Review
- Exploiting Methyl Triazenes as Attractive Alternatives to Temozolomide and Dacarbazine for Cancer Therapy.Molecules (Basel, Switzerland) · 2026Review
- DeepDrugs: a mechanism-aware tri-linear attention framework for synergistic drug-combination prediction.Briefings in bioinformatics · 2026Article
- Benzo[ACS omega · 2026Article
- Article
- Lipopeptides fromBiotech (Basel (Switzerland)) · 2026Article
- A Review on EGFR-Tyrosine Kinase Inhibitors and their Resistance Mechanisms.Current pharmaceutical design · 2026Review
45 more citing papers are in PubMed but not listed here.
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
4 authors.
Funding
Abstract
Targeting the EGFR with small-molecule inhibitors is a confirmed valid strategy in cancer therapy. Since the FDA approval of the first EGFR-TKI, erlotinib, great efforts have been devoted to the discovery of new potent inhibitors. Until now, fourteen EGFR small-molecule inhibitors have been globally approved for the treatment of different types of cancers. Although these drugs showed high efficacy in cancer therapy, EGFR mutations have emerged as a big challenge for these drugs. In this review, we focus on the EGFR small-molecule inhibitors that have been approved for clinical uses in cancer therapy. These drugs are classified based on their chemical structures, target kinases, and pharmacological uses. The synthetic routes of these drugs are also discussed. The crystal structures of these drugs with their target kinases are also summarized and their bonding modes and interactions are visualized. Based on their binding interactions with the EGFR, these drugs are also classified into reversible and irreversible inhibitors. The cytotoxicity of these drugs against different types of cancer cell lines is also summarized. In addition, the proposed metabolic pathways and metabolites of the fourteen drugs are discussed, with a primary focus on the active and reactive metabolites. Taken together, this review highlights the syntheses, target kinases, crystal structures, binding interactions, cytotoxicity, and metabolism of the fourteen globally approved EGFR inhibitors. These data should greatly help in the design of new EGFR inhibitors.
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What OpenQuestion holds
Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.