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BIOMARKER:

EGFR L858R

i
Entrez ID:
Related tests:
1d
Enhanced the Trans-Cleavage Activity of CRISPR-Cas12a Using Metal-Organic Frameworks as Stimulants for Efficient Electrochemical Sensing of Circulating Tumor DNA. (PubMed, Adv Sci (Weinh))
More importantly, it has been successfully used to detect the targets in clinical practice, requiring low-dose samples and a short time. This strategy is believed to shed new light on the applications of cancer diagnosis, treatment, and surveillance.
Journal • Circulating tumor DNA
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EGFR (Epidermal growth factor receptor)
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EGFR mutation • EGFR L858R
1d
Enrollment open
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EGFR mutation • EGFR L858R • EGFR exon 19 deletion • EGFR T790M
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Ivesa (firmonertinib)
2d
AST2818 in Advanced Non-Small Cell Lung Cancer With EGFR Mutations (clinicaltrials.gov)
P=N/A, N=116, Terminated, Allist Pharmaceuticals, Inc. | Unknown status --> Terminated; Indications have been approved for marketing
Trial termination
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EGFR mutation • EGFR L858R • EGFR exon 19 deletion • EGFR T790M • EGFR L861Q • EGFR G719X
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Ivesa (firmonertinib)
2d
Safety, Tolerability, Pharmacokinetics and Anti-tumour Activity of Alflutinib in Advanced Non Small Cell Lung Cancer (clinicaltrials.gov)
P1, N=14, Terminated, Allist Pharmaceuticals, Inc. | Unknown status --> Terminated; Indications have been approved for marketing
Trial termination
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EGFR mutation • EGFR L858R • EGFR exon 19 deletion • EGFR T790M • EGFR L861Q • EGFR G719X
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Ivesa (firmonertinib)
3d
Localization of epidermal growth factor receptor-mutations using PNA:DNA probes in clinical specimens from patients with non-small cell lung cancer. (PubMed, Sci Rep)
TIL analysis of L858R-mutated tumors revealed that CD8+PD-1+ T cells and CD68+ macrophages were scarce in tumors, but in the cytokeratin-positive intra-tumoral regions, CD4+, FoxP3+, and CD204+ cells tended to be more abundant in the L858R-positive tumor area than in the negative area. Thus, PNA:DNA probes specific for EGFR-mutations can detect areas with heterogeneous EGFR mutants in whole cancer tissues and can be used to evaluate the mutation-associated TIL status in EGFR-mutant cancer tissues.
Journal • PD(L)-1 Biomarker • IO biomarker
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EGFR (Epidermal growth factor receptor) • CD8 (cluster of differentiation 8) • PD-1 (Programmed cell death 1) • CD4 (CD4 Molecule) • CD68 (CD68 Molecule) • FOXP3 (Forkhead Box P3) • MSR1 (Macrophage Scavenger Receptor 1)
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EGFR mutation • EGFR L858R
3d
New trial
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EGFR (Epidermal growth factor receptor)
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EGFR L858R • EGFR exon 19 deletion
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Tagrisso (osimertinib)
3d
Registration study on advanced non-small cell lung cancer (ChiCTR2500098714)
P=N/A, N=10000, Not yet recruiting, Henan Cancer Hospital; Henan Cancer Hospital
New trial
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EGFR (Epidermal growth factor receptor) • HER-2 (Human epidermal growth factor receptor 2) • KRAS (KRAS proto-oncogene GTPase) • BRAF (B-raf proto-oncogene) • ALK (Anaplastic lymphoma kinase) • TP53 (Tumor protein P53) • PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha) • MET (MET proto-oncogene, receptor tyrosine kinase) • RET (Ret Proto-Oncogene) • PTEN (Phosphatase and tensin homolog) • ROS1 (Proto-Oncogene Tyrosine-Protein Kinase ROS) • NTRK1 (Neurotrophic tyrosine kinase, receptor, type 1) • NTRK3 (Neurotrophic tyrosine kinase, receptor, type 3) • NTRK2 (Neurotrophic tyrosine kinase, receptor, type 2) • KEAP1 (Kelch Like ECH Associated Protein 1) • MDM2 (E3 ubiquitin protein ligase) • FBXW7 (F-Box And WD Repeat Domain Containing 7) • NFE2L2 (Nuclear Factor, Erythroid 2 Like 2) • RUNX1T1 (RUNX1 Partner Transcriptional Co-Repressor 1) • EPHA2 (EPH receptor A2)
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TP53 mutation • KRAS mutation • EGFR mutation • KRAS G12C • BRAF mutation • BRAF V600 • EGFR L858R • HER-2 mutation • EGFR exon 19 deletion • ALK positive • RET fusion • PTEN mutation • ALK rearrangement • MET exon 14 mutation • EGFR L861Q • KEAP1 mutation • ROS1 positive • EGFR G719X • MET mutation • EGFR S768I • RET rearrangement • KRAS G12 • NFE2L2 mutation
3d
160mg furmonertinib for the first-line treatment of EGFR-sensitive mutations NSCLC with BM/LM : a single-arm, prospective clinical study (ChiCTR2500099395)
P4, N=30, Not yet recruiting, The Fourth Hospital of Hebei Medical University; The Fourth Hospital of Hebei Medical University
New P4 trial
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EGFR (Epidermal growth factor receptor)
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EGFR mutation • EGFR L858R • EGFR exon 19 deletion • EGFR positive
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Ivesa (firmonertinib)
3d
The effect of adjuvant EGFR-TKI therapy on the prognosis of pathological stage I invasive lung adenocarcinoma with EGFR mutation (ChiCTR2500098187)
P=N/A, N=1000, Not yet recruiting, West China Hospital, Sichuan University; West China Hospital, Sichuan University
New trial
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EGFR mutation • EGFR L858R • EGFR exon 19 deletion • EGFR T790M • EGFR L861Q • EGFR G719X • EGFR S768I
4d
ALCINA 2: Analysis of Circulating Tumor Markers in Blood (clinicaltrials.gov)
P=N/A, N=992, Recruiting, Institut du Cancer de Montpellier - Val d'Aurelle | N=620 --> 992
Enrollment change
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PD-L1 (Programmed death ligand 1) • KRAS (KRAS proto-oncogene GTPase)
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KRAS G12C • EGFR L858R • KRAS G12
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CELLSEARCH®
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Enhertu (fam-trastuzumab deruxtecan-nxki)
4d
New P4 trial
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EGFR (Epidermal growth factor receptor)
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EGFR mutation • EGFR L858R • EGFR exon 19 deletion • EGFR T790M
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Ivesa (firmonertinib)
4d
New trial
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EGFR mutation • EGFR L858R • EGFR exon 19 deletion • EGFR L861Q • EGFR G719X • EGFR S768I • EGFR positive
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Ivesa (firmonertinib)
4d
New P1 trial
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TP53 (Tumor protein P53)
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TP53 mutation • EGFR mutation • EGFR L858R • EGFR exon 19 deletion
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Tagrisso (osimertinib) • Focus V (anlotinib)
4d
AK112-RWS-IIT: Real-world clinical studies of Ivonescimab in locally advanced or metastatic non-squamous NSCLC with EGFR-TKI treatment failure (ChiCTR2500096483)
P4, N=30, Recruiting, Higher Education Mega Center Hospital of Guangdong Provincial Hospital of Chinese Medicine; Higher Education Mega Center Hospital of Guangdong Provi
New P4 trial
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EGFR mutation • EGFR L858R • EGFR exon 19 deletion • EGFR T790M • EGFR L861Q • EGFR G719X • EGFR S768I • EGFR positive
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Yidafan (ivonescimab)
4d
New P3 trial
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TACSTD2 (Tumor Associated Calcium Signal Transducer 2)
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EGFR mutation • EGFR L858R • EGFR exon 19 deletion • EGFR T790M • EGFR L861Q • EGFR G719X • EGFR S768I
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Tagrisso (osimertinib) • Datroway (datopotamab deruxtecan)
4d
New P2 trial
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EGFR (Epidermal growth factor receptor)
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EGFR mutation • EGFR L858R • EGFR exon 19 deletion
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Tyvyt (sintilimab)
4d
New trial
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EGFR mutation • EGFR L858R • EGFR exon 19 deletion
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Focus V (anlotinib)
4d
A phase I, multicenter, open-label, first-in-human, dose escalation and expansion study of DM005 in patients with advanced solid tumors (ChiCTR2500095720)
P1, N=176, Not yet recruiting, Guangdong Provincial People's Hospital(Guangdong Academy of Medical Sciences); Guangdong Provincial People's Hospital(Guangdong Academy of Medical Sci
New P1 trial
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HER-2 (Human epidermal growth factor receptor 2) • BRAF (B-raf proto-oncogene) • ALK (Anaplastic lymphoma kinase) • MET (MET proto-oncogene, receptor tyrosine kinase) • ROS1 (Proto-Oncogene Tyrosine-Protein Kinase ROS) • NTRK (Neurotrophic receptor tyrosine kinase)
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EGFR mutation • EGFR L858R • EGFR exon 19 deletion • EGFR exon 20 insertion • EGFR wild-type
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DM005
4d
A Multicenter, Single-Arm, Phase II Study of High-Dose Almonertinib as First-Line Treatment for Patients with EGFR Exon 21 L858R-Mutated Advanced Lung Adenocarcinoma (LUAD) (ChiCTR2500095661)
P2, N=122, Recruiting, The Affiliated Panyu Central Hospital of Guangzhou Medical University; The Affiliated Panyu Central Hospital of Guangzhou Medical University
New P2 trial
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EGFR (Epidermal growth factor receptor)
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EGFR mutation • EGFR L858R
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Ameile (aumolertinib)
5d
Randomized Phase III Study of EGFR Tyrosine Kinase Inhibitor and Intercalated Platinum-doublet Chemotherapy for Non-small Cell Lung Cancer Harboring EGFR Mutation. (PubMed, Clin Cancer Res)
The intercalation of cisplatin plus pemetrexed after the response to EGFR-TKI improved PFS but not OS compared with EGFR-TKI monotherapy as the first-line treatment for advanced NSqNSCLC harboring EGFR mutation.
P3 data • Journal
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EGFR (Epidermal growth factor receptor)
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EGFR mutation • EGFR L858R • EGFR exon 19 deletion
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cisplatin • Tagrisso (osimertinib) • gefitinib • pemetrexed
5d
Trial completion date
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EGFR (Epidermal growth factor receptor) • PD-L1 (Programmed death ligand 1) • BRAF (B-raf proto-oncogene) • ALK (Anaplastic lymphoma kinase) • MET (MET proto-oncogene, receptor tyrosine kinase) • RET (Ret Proto-Oncogene) • ROS1 (Proto-Oncogene Tyrosine-Protein Kinase ROS) • NTRK (Neurotrophic receptor tyrosine kinase)
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EGFR mutation • EGFR L858R • EGFR exon 19 deletion • MET exon 14 mutation
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docetaxel • Datroway (datopotamab deruxtecan)
7d
Journal
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EGFR (Epidermal growth factor receptor)
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EGFR mutation • EGFR L858R • EGFR exon 19 deletion
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Tagrisso (osimertinib)
7d
Metal ion-enhanced ZIC-cHILIC StageTip for N-Glycoproteomic and Phosphoproteomic Profiling in EGFR-mutated Lung Cancer Cells. (PubMed, Mol Cell Proteomics)
Most prominent alterations were observed in EGFR (auto-phosphorylation Y1197 and 10 bi- and triantennary fucosyl-sialo glycans at N603), downstream PI3K-Akt pathway (ERBB2-T1240, MET-S990/T992, AKT-S124/S126) and integrin family (sialo-fucosyl glycans), suggesting site-specific alteration between N-glycosylation and phosphorylation interplay in the TKI resistant L858R-T790M mutant NSCLC cells. The glycoproteomic and phosphoproteomic landscape may help to unravel the complex modification alterations underlying the resistant mechanism, offering insights for improving therapeutic strategies and patient outcomes.
Journal
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EGFR (Epidermal growth factor receptor) • HER-2 (Human epidermal growth factor receptor 2)
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EGFR mutation • EGFR L858R • EGFR T790M • EGFR L858R + EGFR T790M
9d
Discovery of novel dual-target inhibitors of LSD1/EGFR for non-small cell lung cancer therapy. (PubMed, Acta Pharmacol Sin)
L-1 that shows the highest biological activity across BaF3 cell, mutant EGFR kinase and LSD1 assays due to its dual targeting of LSD1/EGFR, emerges as a promising lead compound for non-small cell lung cancer treatment. This study demonstrates that L-1 efficiently inhibits lung cancer growth in vitro and in vivo, suggesting it as a potential lead for non-small cell lung cancer treatment, highlighting the utility of virtual screening methods in discovering multi-target inhibitors and strategies for other diseases.
Journal
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EGFR (Epidermal growth factor receptor) • KDM1A (Lysine Demethylase 1A)
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EGFR mutation • EGFR L858R • EGFR T790M • EGFR expression
9d
Enrollment change
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EGFR (Epidermal growth factor receptor)
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EGFR L858R • EGFR exon 19 deletion
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Rybrevant (amivantamab-vmjw) • Lazcluze (lazertinib) • amivantamab SC (Ami-LC) • minocycline
9d
Targeting EGFR-Mcl-1 Axis by Piperlongumine as a Novel Strategy for Non-Small Cell Lung Cancer Therapy. (PubMed, Am J Chin Med)
Furthermore, Piperlongumine significantly inhibited tumor growth in both Osimertinib-sensitive and resistant NSCLC xenograft models. These findings highlight the potential of Piperlongumine as an effective agent in overcoming EGFR-targeted therapy resistance and suggest new avenues for its clinical application in NSCLC treatment.
Journal
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EGFR (Epidermal growth factor receptor)
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EGFR mutation • EGFR L858R • EGFR exon 19 deletion • EGFR T790M • EGFR L858R + EGFR T790M
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Tagrisso (osimertinib)
9d
EGFR status assessment using reflex testing targeted next-generation sequencing for resected non-squamous non-small cell lung cancer. (PubMed, Virchows Arch)
Shorter median event-free survival (EFS) in patients with an EGFR exon 18 mutation and those with TP53 exon 7 co-mutation was recorded. The EGFR status should be systematically evaluated using targeted NGS reflex testing for resected NS-NSCLC since future therapeutic decision-making could soon consider integrating the presence of co-occurring mutations.
Retrospective data • Journal • Next-generation sequencing • PD(L)-1 Biomarker • IO biomarker
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EGFR (Epidermal growth factor receptor) • PD-L1 (Programmed death ligand 1) • TP53 (Tumor protein P53)
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PD-L1 expression • TP53 mutation • EGFR mutation • EGFR L858R • EGFR expression • TP53 wild-type
12d
Therapeutic insights into epidermal growth factor receptor/reactive oxygen species proto-oncogene 1-receptor co-mutated non-small cell lung cancer: Crizotinib as a promising option. (PubMed, World J Clin Oncol)
While third-generation EGFR tyrosine kinase inhibitors (TKIs), such as osimertinib, are commonly regarded as first-line therapies, recent studies indicate that crizotinib may offer superior disease control in certain EGFR-mutant patients, particularly those who exhibit poor responses to EGFR TKIs...In patients with EGFR/ROS1 co-mutation, gefitinib is generally effective as a first-line treatment; however, its efficacy can be limited, whereas crizotinib has demonstrated improved disease control. Future research should focus on identifying optimal treatment strategies for patients with EGFR/ROS1 co-mutation to enhance patient outcomes. In conclusion, this case report not only illustrates the effectiveness of crizotinib in managing patients with EGFR/ROS1 co-mutation but also underscores the importance of personalized treatment approaches, offering valuable insights for improving clinical outcomes in NSCLC patients with complex genetic profiles.
Journal
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EGFR (Epidermal growth factor receptor) • ROS1 (Proto-Oncogene Tyrosine-Protein Kinase ROS)
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EGFR mutation • EGFR L858R • ROS1 rearrangement
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Xalkori (crizotinib) • Tagrisso (osimertinib) • gefitinib
16d
Pathologic complete response following salvage surgery after lazertinib treatment in advanced EGFR-mutated lung adenocarcinoma: case report and literature review. (PubMed, Transl Lung Cancer Res)
The patient remained disease-free for 1 year following lazertinib treatment. This case suggests that salvage surgery after treatment with lazertinib may be a safe and effective approach for NSCLC with common EGFR mutations.
Journal
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EGFR (Epidermal growth factor receptor)
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EGFR mutation • EGFR L858R
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Lazcluze (lazertinib)
16d
Rapid detection of non-small cell lung cancer driver mutations using droplet digital polymerase chain reaction analysis of bronchial washings: a prospective multicenter study. (PubMed, Transl Lung Cancer Res)
This approach represents a promising alternative to tissue biopsy for molecular profiling, potentially expediting treatment decisions. While serum ddPCR showed limited utility, it may complement tissue genotyping in specific clinical scenarios.
Clinical • Journal • Polymerase Chain Reaction
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EGFR (Epidermal growth factor receptor) • KRAS (KRAS proto-oncogene GTPase) • BRAF (B-raf proto-oncogene)
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BRAF V600E • KRAS mutation • EGFR mutation • BRAF V600 • EGFR L858R • EGFR exon 19 deletion • EGFR G719X • KRAS G12
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Oncomine™ Dx Target Test
16d
Immunotherapy efficacy between exon 19 deletion and exon 21 L858R mutation in advanced EGFR mutant non-small-cell lung cancer: a direct and indirect meta-analysis. (PubMed, Transl Lung Cancer Res)
Subgroup analyses also showed similar tendency that 21 L858R had more clinical benefit compared to 19 Del no matter whether IO monotherapy or IO combination. For advanced EGFR mutant NSCLC patients, 21 L858R had superior IO efficacy compared with 19 Del.
Retrospective data • Journal • IO biomarker
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EGFR (Epidermal growth factor receptor)
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EGFR mutation • EGFR L858R • EGFR exon 19 deletion • EGFR L858R + EGFR exon 19 deletion
16d
Testing the Addition of the Pill Chemotherapy, Cabozantinib, to the Standard Immune Therapy Nivolumab Compared to Standard Chemotherapy for Non-small Cell Lung Cancer (clinicaltrials.gov)
P2, N=117, Active, not recruiting, National Cancer Institute (NCI) | Trial completion date: Jun 2025 --> Sep 2025 | Trial primary completion date: Jun 2025 --> Sep 2025
Trial completion date • Trial primary completion date
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EGFR (Epidermal growth factor receptor) • PD-L1 (Programmed death ligand 1) • KRAS (KRAS proto-oncogene GTPase) • BRAF (B-raf proto-oncogene) • ALK (Anaplastic lymphoma kinase) • ROS1 (Proto-Oncogene Tyrosine-Protein Kinase ROS)
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KRAS G12C • EGFR L858R • EGFR exon 19 deletion • EGFR exon 20 insertion • ALK rearrangement • EGFR L861Q • ROS1 positive • KRAS G12 • EGFR exon 20 mutation • MET positive • EGFR negative
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Opdivo (nivolumab) • gemcitabine • docetaxel • Cabometyx (cabozantinib tablet) • albumin-bound paclitaxel • Cyramza (ramucirumab) • Cometriq (cabozantinib capsule) • ABP 206 (nivolumab biosimilar)
18d
Severe denosumab-induced hypocalcemia requiring long-term intensified medication in a patient with EGFR-mutant lung cancer and diffuse osteoblastic bone metastases. (PubMed, Respir Med Case Rep)
Tartrate-resistant acid phosphatase-5b (TRACP-5b), a marker of bone resorption, was a biomarker for the required amount of calcium in this case. Patients with lung cancer with diffuse osteoblastic bone metastases could develop severe hypocalcemia and require long-term calcium supplementation.
Journal
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EGFR (Epidermal growth factor receptor)
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EGFR mutation • EGFR L858R
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Prolia (denosumab)
19d
EXCLAIM-2: TAK-788 as First-Line Treatment Versus Platinum-Based Chemotherapy for Non-Small Cell Lung Cancer (NSCLC) With EGFR Exon 20 Insertion Mutations (clinicaltrials.gov)
P3, N=354, Active, not recruiting, Takeda | Trial completion date: Jul 2025 --> Sep 2026 | Trial primary completion date: Dec 2024 --> Sep 2026
Trial completion date • Trial primary completion date
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HER-2 (Human epidermal growth factor receptor 2)
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EGFR L858R • EGFR exon 19 deletion • EGFR T790M • EGFR exon 20 insertion • EGFR L861Q • EGFR G719X • EGFR S768I • EGFR exon 20 mutation
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cisplatin • carboplatin • pemetrexed • Exkivity (mobocertinib)
21d
Aumolertinib plus chemotherapy as first-line treatment for advanced NSCLC with EGFR exon 19 deletion or exon 21 L858R: a phase II trial. (PubMed, Oncologist)
Aumolertinib plus chemotherapy shows potential as first-line treatment for patients with EGFR-mutant advanced NSCLC, which deserves to be investigated in randomized controlled trials. CtDNA clearance may be a prognostic marker.
P2 data • Journal
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EGFR (Epidermal growth factor receptor)
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EGFR L858R • EGFR exon 19 deletion
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carboplatin • pemetrexed • Ameile (aumolertinib)
21d
Inherited rare epidermal growth factor receptor mutation and somatic mutations in patients with non-small cell lung cancer: a case report. (PubMed, BMC Med Genomics)
The investigation and comprehension of the significance of each individual EGFR mutation hold the promise for potential in cancer prevention or early diagnosis within family cohorts and understanding the mechanisms of tumorigenesis in sporadic cases.
Journal
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EGFR (Epidermal growth factor receptor)
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EGFR mutation • EGFR L858R
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Tagrisso (osimertinib)
24d
Distribution of EGFR and KRAS Mutations in Patients with Surgically Resected Non-Small Cell Lung Cancer from Southern Italy: Real-Life Data from a Single Institution and Literature Review. (PubMed, Cancers (Basel))
Our findings improve the understanding of lung cancer genetics in a small and homogeneous area of Southern Italy and guide future research. The EGFR and KRAS mutations in NSCLC resected patients from Southern Italy showed a global similar incidence compared to other recently described Italian cohorts of advanced and early-stage NSCLC, with a higher frequency of exon19 EGFR deletions. No prognostic impact was observed for both EGFR and KRAS status, but additional investigations on a larger cohort are needed.
Journal
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EGFR (Epidermal growth factor receptor) • KRAS (KRAS proto-oncogene GTPase)
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KRAS mutation • EGFR mutation • KRAS G12C • EGFR L858R • EGFR exon 19 deletion • KRAS G12D • KRAS G12
25d
Trial completion date
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EGFR mutation • EGFR L858R • EGFR exon 19 deletion • EGFR T790M
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Erbitux (cetuximab) • Gilotrif (afatinib)
26d
A Study of NX-019 in Patients with Advanced, Epidermal Growth Factor Receptor (EGFR) Mutant Cancer (clinicaltrials.gov)
P1, N=258, Active, not recruiting, Nalo Therapeutics Inc. | Recruiting --> Active, not recruiting | Trial completion date: Oct 2027 --> Dec 2025 | Trial primary completion date: Feb 2027 --> Jun 2025
Enrollment closed • Trial completion date • Trial primary completion date
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EGFR (Epidermal growth factor receptor)
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EGFR mutation • EGFR L858R • EGFR L861Q
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NX-019
26d
Racial Diversity and Co-Mutational Analysis of Biologically Relevant Alterations in EGFR Mutant Lung Cancers. (PubMed, Clin Lung Cancer)
EGFR mutation subtypes and co-mutations differ by race. KMT2C may influence TMB and immunotherapy response, while GLI1 is linked to TKI resistance. TP53 alterations were more commen in smokers, and patients with high PDL-1 and TMB, highlighting additional factors that drive tumors with these alterations.
Journal • Tumor mutational burden • PD(L)-1 Biomarker • IO biomarker
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EGFR (Epidermal growth factor receptor) • PD-L1 (Programmed death ligand 1) • TP53 (Tumor protein P53) • TMB (Tumor Mutational Burden) • KMT2C (Lysine Methyltransferase 2C) • GLI1 (GLI Family Zinc Finger 1)
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EGFR mutation • TMB-H • EGFR L858R • EGFR exon 19 deletion
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Tempus xT Assay
27d
Long-term benefit of afatinib combined with bevacizumab in a lung adenocarcinoma patient with a novel rare EGFR Q787L mutation. (PubMed, Int Immunopharmacol)
Our findings suggest that the combination of afatinib and bevacizumab may offer long-term clinical benefits for LUAC patients harboring the novel and rare EGFR Q787L mutation. This case highlights a potential therapeutic strategy warranting further investigation in clinical studies.
Journal
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EGFR (Epidermal growth factor receptor)
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EGFR mutation • EGFR L858R • EGFR exon 19 deletion • EGFR exon 20 insertion • EGFR exon 20 mutation
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Avastin (bevacizumab) • Gilotrif (afatinib) • Conmana (icotinib)
29d
Identification of Novel Fourth-Generation Allosteric Inhibitors Targeting Inactive State of EGFR T790M/L858R/C797S and T790M/L858R Mutations: A Combined Machine Learning and Molecular Dynamics Approach. (PubMed, J Phys Chem B)
Recently, fourth-generation AIs, EAI045, have been discovered to potently and selectively inhibit various EGFR mutations but limited antiproliferative effects in the absence of the antibody cetuximab...However, path-independent alchemical approaches like streamlined alchemical free energy perturbation and binding free energy estimator 2 (BFEE2) were employed to validate the results and identify potent compounds. These findings pave the way to identification of novel potential fourth-generation AIs, which require further experimental validation.
Journal
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EGFR (Epidermal growth factor receptor)
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EGFR mutation • EGFR L858R • EGFR T790M • EGFR L858R + EGFR T790M
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Erbitux (cetuximab)