A clinical review on third and fourth generation EGFR tyrosine kinase inhibitors for the treatment of non-small cell lung cancer.
Explore this paper's citation graph
Summary
This review delves into the current clinical status, efficacy, safety profiles, and regulatory approvals of third-generation EGFR TKIs, including Osimertinib, Lazertinib, Furmonertinib, Aumolertinib, Rezivertinib, Befotertinib, Sunvozertinib, and explores emerging fourth-generation EGFR TKIs designed to address resistance mechanisms beyond those targeted by their predecessors.
- Type
- review
- Published
- 2025-03-01
- Cited by
- 21
- References
- 136
- OpenAlex
- https://openalex.org/W4408662124
- Semantic Scholar
- https://api.semanticscholar.org/CorpusID:277211341
Keywords
Chemistry, Tyrosine kinase, Cancer research, Cancer, Lung cancer
References
- Parallel phase 1 clinical trials in the US and in China: accelerating the test of avitinib in lung cancer as a novel inhibitor selectively targeting mutated EGFR and overcoming T790M-induced resistance
- Acquired resistance to TKIs in solid tumours: learning from lung cancer
- EGFR mutation and resistance of non-small-cell lung cancer to gefitinib.
- Non-small cell lung cancer: epidemiology, risk factors, treatment, and survivorship.
- Rociletinib in EGFR-mutated non-small-cell lung cancer.
- Gefitinib or chemotherapy for non-small-cell lung cancer with mutated EGFR.
- Novel mutant-selective EGFR kinase inhibitors against EGFR T790M
- Common EGFR-mutated subgroups (Del19/L858R) in advanced non-small-cell lung cancer: chasing better outcomes with tyrosine kinase inhibitors.
- Next-generation epidermal growth factor receptor tyrosine kinase inhibitors in epidermal growth factor receptor -mutant non-small cell lung cancer.
- Osimertinib: First Global Approval
- Rociletinib: has the TIGER lost a few of its stripes?
- Olmutinib: First Global Approval
- Discovery of (R,E)-N-(7-Chloro-1-(1-[4-(dimethylamino)but-2-enoyl]azepan-3-yl)-1H-benzo[d]imidazol-2-yl)-2-methylisonicotinamide (EGF816), a Novel, Potent, and WT Sparing Covalent Inhibitor of Oncogenic (L858R, ex19del) and Resistant (T790M) EGFR Mutants for the Treatment of EGFR Mutant Non-Small-Ce
- Profile of rociletinib and its potential in the treatment of non-small-cell lung cancer
- Rociletinib—An Investigational Therapy in Patients with Previously Treated EGFR Mutant-positive Non-small Cell Lung Cancer
- Osimertinib or Platinum–Pemetrexed in EGFR T790M–Positive Lung Cancer
- Targeting EGFR T790M mutation in NSCLC: From biology to evaluation and treatment
- First-in-human study of AC0010, a novel irreversible, mutant-selective EGFR inhibitor in patients with 1st generation EGFR TKI-resistant non-small cell lung cancer (NSCLC)
- Synergy between next generation EGFR tyrosine kinase inhibitors and miR-34a in the inhibition of non-small cell lung cancer.
- C-2 (E)-4-(Styryl)aniline substituted diphenylpyrimidine derivatives (Sty-DPPYs) as specific kinase inhibitors targeting clinical resistance related EGFRT790M mutant.
Cited by
- Prevalence of osimertinib-induced cardiotoxicity in non-small cell lung cancer patients: a systematic review and meta-analysis.
- Quinazoline-based fourth-generation EGFR tyrosine kinase inhibitors to overcome C797S-mediated resistance in non-small cell lung Cancer (NSCLC).
- Lung cancer in non-smoking women (LCINSW): from risk factors to precision therapy
- Advancing EGFR-targeted anticancer strategies: the potential of thiazole, pyrazole, and thiazole–pyrazole hybrids
- Efficacy and Safety of EGF/EGFR Vaccines in EGFR‐Driven Solid Tumors: A Systematic Review and Meta‐Analysis of Controlled and Single‐Arm Studies
- Recent advances in Pyrazolo[3,4-d]pyrimidine-based dual inhibitors in the treatment of cancers.
- Design, synthesis, and antiproliferative efficacy of an innovative series of triazino[5,6-b]indole derivatives targeting EGFR, CD1, Hsp90, PI3K, and ERK/AKT as key molecular targets in cancer therapy.
- First‐Line Third‐Generation EGFR Tyrosine Kinase Inhibitor Monotherapy for Advanced EGFR‐Mutated Non‐Small Cell Lung Cancer: A Systematic Review and Network Meta‐Analysis
- Comparing the effect of traditional and novel tyrosine kinase inhibitors for epidermal growth factor receptor exon 20 insertions by molecular dynamics simulation
- Osimertinib acquired resistance among patients with EGFR-mutated NSCLC: from molecular mechanisms to clinical therapeutic strategies
- Hydrazonylthiazole Derivatives as Dual EGFR and ALR2 Inhibitors: Design, Synthesis, and Comprehensive In Vitro and In Silico Evaluation for Potential Anticancer Activity
- Design, catalyst-free synthesis, DFT study and anticancer assessment of new 2,9-disubstituted purine-6-carboxamides.
- Properties of FDA-approved small molecule protein kinase inhibitors: a 2026 update.
- What Happens in Successful Optimizations? A Survey of 2018-2024 Literature.
- Design, synthesis and biological evaluation of selective inhibitors against the L858R/T790M/C797S mutant EGFR kinase based on the scaffold of brigatinib
- LncRNA HCP5 remodels G6PD dual post-translational modification to mediate metabolic adaptations driving osimertinib resistance in lung adenocarcinoma.
- Intestinal Organoid‐Based Mathematical Modeling Predicts Clinical Gastrointestinal Toxicity of Oral Oncology Drugs
- Design, synthesis and biological evaluation of selective inhibitors against the L858R/T790 M/C797S mutant EGFR kinase based on the scaffold of brigatinib
Related papers
- ASH Annual Meeting 2012—Chronic Myeloid Leukemia Update
- Small molecule tyrosine kinase inhibitors: potential role in pediatric malignant solid tumors.
- Pharmacokinetics of Four Tyrosine Kinase Inhibitors in Adult and Paediatric Chronic Myeloid Leukaemia Patients
- Pharmacokinetics of Four Tyrosine Kinase Inhibitors in Adult and Paediatric Chronic Myeloid Leukaemia Patients
- Analysis of onset mechanism for tyrosine kinase inhibitor imatinib induced-left ventricular diastolic dysfunction
- Moving on up: Second-Line Agents as Initial Treatment for Newly-Diagnosed Patients with Chronic Phase CML
- Targeting heterodimeric EGFR/ErbB2-receptor complexes with novel bispecific small-molecule tyrosine kinase inhibitors in combination with an experimental radiotherapy in human malignant glioma cells
- Features of the etythropoesis upon treatment of chronic myeloid leukemia with tyrosine kinase inhibitor
- Imatinib-mesylate for all patients with hypereosinophilic syndrome?
- The role of allogeneic stem cell transplantation for CML in the tyrosine kinase inhibitor era