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BIOMARKER:

EGFR S768I

i
Other names: EGFR, ERBB, ERBB1, Epidermal growth factor receptor
Entrez ID:
Related tests:
5d
An epidermal growth factor receptor compound mutation of L858R with S768I in advanced non-small-cell lung cancer: a case report. (PubMed, J Med Case Rep)
This case report is a compelling testimony to the evolving therapeutic landscape of non-small cell lung cancers, providing valuable insight into the potential therapeutic efficacy of epidermal growth factor receptor-tyrosine kinase inhibitors in the realm of rare and complex epidermal growth factor receptor mutations.
Journal • Metastases
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EGFR (Epidermal growth factor receptor)
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EGFR mutation • EGFR L858R • EGFR S768I • EGFR L858R + EGFR S765I
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Gilotrif (afatinib)
9d
Unveiling the Landscape of uncommon EGFR Mutations in Non-Small Cell Lung Cancer - A Systematic Review. (PubMed, J Thorac Oncol)
This systematic review supports the use of 2nd generation TKI afatinib for G719X, S768I, E709X and L747X mutations, as well as for compound uncommon mutations. For other uncommon mutations such as L861Q, 3rd generation TKI, such as osimertinib, could also be considered, given its activity and toxicity profile.
Review • Journal
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EGFR (Epidermal growth factor receptor)
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EGFR mutation • EGFR T790M • EGFR L861Q • EGFR G719X • EGFR S768I
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Tagrisso (osimertinib) • Gilotrif (afatinib)
26d
MET overexpression correlated with prognosis of EGFR-mutant treatment‑naïve advanced lung adenocarcinoma: a real‑world retrospective study. (PubMed, Clin Transl Oncol)
MET positive expression was an independent predictor of poor outcomes in untreated EGFR L858R mutation advanced LUAD patients treated with first-line EGFR-TKI monotherapy.
Retrospective data • Journal • Real-world evidence • Real-world • Metastases
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EGFR (Epidermal growth factor receptor) • MET (MET proto-oncogene, receptor tyrosine kinase)
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EGFR mutation • EGFR L858R • EGFR exon 19 deletion • EGFR expression • MET overexpression • EGFR L861Q • EGFR S768I • MET expression • MET positive • EGFR G719A • EGFR G719C
1m
A macrocyclic kinase inhibitor overcomes triple resistant mutations in EGFR-positive lung cancer. (PubMed, NPJ Precis Oncol)
Brigatinib-based therapy was effective against osimertinib-resistant EGFR C797S mutants and is undergoing clinical studies. Molecular dynamics simulation revealed the binding mode and affinity between BI-4020 and EGFR mutants. This study identified potential therapeutic strategies using the new-generation macrocyclic EGFR inhibitor to overcome the emerging ultimate resistance mutants.
Journal
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EGFR (Epidermal growth factor receptor)
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EGFR mutation • EGFR T790M • EGFR C797S • EGFR S768I • EGFR positive • EGFR L747P
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Tagrisso (osimertinib) • Alunbrig (brigatinib) • BI-4020
1m
ABC-lung: Atezolizumab, Bevacizumab and Chemotherapy in EGFR-mutant Non-small Cell Lung Carcinoma (clinicaltrials.gov)
P2, N=95, Active, not recruiting, ETOP IBCSG Partners Foundation | Trial primary completion date: Dec 2023 --> Mar 2024
Trial primary completion date
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EGFR mutation • EGFR L858R • EGFR T790M • EGFR G719X • EGFR S768I
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Avastin (bevacizumab) • Tecentriq (atezolizumab) • carboplatin • paclitaxel • pemetrexed
2ms
Current management of uncommon EGFR mutations in non-small cell lung cancer. (PubMed, Curr Probl Cancer)
It is crucial to understand these distinct variants and their specific responses to active treatment options to optimize care. In this review, we discuss these uncommon mutations in depth and dissect the current literature regarding their treatment outcomes and subsequent evidence-based management guidelines.
Journal
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EGFR (Epidermal growth factor receptor)
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EGFR mutation • EGFR L858R • EGFR L861Q • EGFR G719X • EGFR S768I • EGFR exon 18 mutation
2ms
Cerebrospinal fluid ctDNA testing shows an advantage over plasma ctDNA testing in advanced non-small cell lung cancer patients with brain metastases. (PubMed, Front Oncol)
Timely screening of patients with NSCLC for CSF ctDNA, especially for patients with positive plasma ctDNA, may facilitate the early detection of LM. Furthermore, patients with the EGFR 19del may have a higher risk of developing BPM.
Journal • Circulating tumor DNA • Metastases
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EGFR (Epidermal growth factor receptor) • ALK (Anaplastic lymphoma kinase) • ROS1 (Proto-Oncogene Tyrosine-Protein Kinase ROS)
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EGFR mutation • EGFR L858R • EGFR exon 19 deletion • EGFR S768I • EGFR L858R + EGFR S768I
3ms
Trial completion date • Trial primary completion date • Metastases
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HER-2 (Human epidermal growth factor receptor 2)
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HER-2 exon 20 insertion • EGFR G719X • EGFR S768I • EGFR G724S • HER-2 exon 23 mutation • EGFR R776C • EGFR V774M
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Ivesa (furmonertinib)
3ms
Osimertinib and Tegavivint as First-Line Therapy for the Treatment of Metastatic EGFR-Mutant Non-small Cell Lung Cancer (clinicaltrials.gov)
P1, N=18, Recruiting, Ohio State University Comprehensive Cancer Center | Trial primary completion date: Dec 2023 --> Dec 2024
Trial primary completion date • Metastases
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EGFR (Epidermal growth factor receptor) • NOTCH3 (Notch Receptor 3)
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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) • tegavivint (BC2059)
3ms
Comprehensive molecular analysis of driver mutations in non-small cell lung carcinomas and its correlation with PD-L1 expression, An Indian perspective. (PubMed, Pathol Res Pract)
This is one of the largest cohorts of NSCLC for comprehensive targeted mutational profiling and correlation with the PD-L1 expression. The mutations are more prevalent in non-smoker females for all genes, except ALK (non-smoker males). MET and BRAF mutations are more common in elderly population whereas EGFR mutations, and ALK and ROS1 genes rearrangements are more prevalent in younger population. The most common histopathologic subtype/feature associated with various mutations was as follows: acinar with EGFR, solid with ALK, macronucleoli with ROS1, signet ring with MET, and micropapillary with BRAF.
Journal • PD(L)-1 Biomarker • IO biomarker
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EGFR (Epidermal growth factor receptor) • HER-2 (Human epidermal growth factor receptor 2) • PD-L1 (Programmed death ligand 1) • KRAS (KRAS proto-oncogene GTPase) • BRAF (B-raf proto-oncogene) • ALK (Anaplastic lymphoma kinase) • MET (MET proto-oncogene, receptor tyrosine kinase) • ROS1 (Proto-Oncogene Tyrosine-Protein Kinase ROS)
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PD-L1 expression • BRAF V600E • KRAS mutation • EGFR mutation • BRAF V600 • EGFR L858R • EGFR exon 19 deletion • EGFR T790M • ALK rearrangement • MET exon 14 mutation • PD-L1 negative • EGFR L861Q • ALK mutation • ROS1 rearrangement • EGFR G719X • MET mutation • EGFR S768I
4ms
Exploring the conformational dynamics and thermodynamics of EGFR S768I and G719X + S768I mutations in non-small cell lung cancer: An in silico approaches. (PubMed, Open Life Sci)
The present study may be helpful in the development of new EGFR-targeted drugs based on the structure of rare mutations. Our findings may aid in developing new targeted treatments for patients with EGFR S768I and EGFR G719X + S768I mutations.
Journal
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EGFR (Epidermal growth factor receptor)
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EGFR mutation • EGFR wild-type • EGFR G719X • EGFR S768I • EGFR G719X + EGFR S768I • EGFR G719C
4ms
RC108 Combine With Furmonertinib With/Without Toripalimab in Patients With EGFR-mutated NSCLC (clinicaltrials.gov)
P1/2, N=106, Recruiting, RemeGen Co., Ltd. | Not yet recruiting --> Recruiting
Enrollment open
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PD-L1 (Programmed death ligand 1)
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PD-L1 expression • EGFR mutation • EGFR L858R • EGFR exon 19 deletion • EGFR T790M • EGFR G719X • EGFR S768I • MET expression • EGFR exon 18 mutation
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Loqtorzi (toripalimab-tpzi) • Ivesa (furmonertinib) • RC108
4ms
Phase classification • Metastases
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HER-2 (Human epidermal growth factor receptor 2)
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HER-2 exon 20 insertion • EGFR G719X • EGFR S768I • EGFR G724S • HER-2 exon 23 mutation • EGFR R776C • EGFR V774M
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Ivesa (furmonertinib)
4ms
Prognostic Outcomes and Recurrence Patterns in Resected Stage I Lung Adenocarcinoma Harboring Atypical Epidermal Growth Factor Receptor Mutation. (PubMed, Eur J Cardiothorac Surg)
Exon20 insertion mutation was correlated with favorable DFS and lower incidence of bone metastasis in radiological solid lung adenocarcinoma harboring atypical EGFR mutation.
Journal
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EGFR (Epidermal growth factor receptor)
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EGFR mutation • EGFR L861Q • EGFR G719X • EGFR S768I
4ms
First-Line Osimertinib for Previously Untreated Patients With NSCLC and Uncommon EGFR Mutations: The UNICORN Phase 2 Nonrandomized Clinical Trial. (PubMed, JAMA Oncol)
The results support the use of osimertinib as a treatment option for this patient population. Japan Registry of Clinical Trials Identifier: jRCTs071200002.
Clinical • P2 data • Journal
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EGFR (Epidermal growth factor receptor)
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EGFR mutation • EGFR L861Q • EGFR G719X • EGFR S768I
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Tagrisso (osimertinib)
5ms
TARGET: A Phase II, Open-Label, Single-Arm Study of 5-Year Adjuvant Osimertinib in Completely Resected EGFR-Mutated Stage II to IIIB NSCLC Post Complete Surgical Resection. (PubMed, Clin Lung Cancer)
Exploratory endpoints include: tissue/plasma concordance; analysis of circulating molecules in plasma samples using different profiling approaches to detect minimal residual disease; incidence and change over time of incidental pulmonary nodules. TARGET is currently recruiting, and completion is expected in 2029.
P2 data • 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 L861Q • EGFR G719X • EGFR S768I
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Tagrisso (osimertinib)
5ms
ABC-lung: Atezolizumab, Bevacizumab and Chemotherapy in EGFR-mutant Non-small Cell Lung Carcinoma (clinicaltrials.gov)
P2, N=95, Active, not recruiting, ETOP IBCSG Partners Foundation | Trial primary completion date: Sep 2023 --> Dec 2023
Trial primary completion date
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EGFR mutation • EGFR L858R • EGFR T790M • EGFR G719X • EGFR S768I
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Avastin (bevacizumab) • Tecentriq (atezolizumab) • carboplatin • paclitaxel • pemetrexed
5ms
EXCLAIM: A Study of TAK-788 in Adults With Non-Small Cell Lung Cancer (clinicaltrials.gov)
P1/2, N=334, Active, not recruiting, Takeda | Recruiting --> Active, not recruiting
Enrollment closed • HER2 exon 20
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HER-2 (Human epidermal growth factor receptor 2)
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EGFR mutation • EGFR L858R • HER-2 mutation • EGFR exon 19 deletion • EGFR T790M • EGFR exon 20 insertion • HER-2 exon 20 insertion • EGFR L861Q • EGFR G719X • EGFR S768I • EGFR exon 20 mutation • EGFR L861R • HER-2 exon 23 mutation
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Exkivity (mobocertinib)
5ms
Feasibility of Intratumoral Washing Fluid for Detecting EGFR Mutations in Lung Cancer (clinicaltrials.gov)
P=N/A, N=70, Recruiting, Pusan National University Hospital | Trial completion date: Dec 2023 --> Jun 2024 | Trial primary completion date: Aug 2023 --> Dec 2023
Trial completion date • Trial primary completion date • Metastases
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EGFR (Epidermal growth factor receptor)
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EGFR mutation • EGFR L858R • EGFR exon 19 deletion • EGFR T790M • EGFR exon 20 insertion • EGFR G719X • EGFR S768I
6ms
First-line osimertinib for patients with advanced NSCLC harboring EGFR mutations: A real-world study (ESMO Asia 2023)
Conclusions The result is consistent with FLAURA study for patients with EGFR-activating mutation. Osimeritinib showed clinical activity in patients with EGFR uncommon mutations as first-line treatment.
Clinical • Real-world evidence • Real-world • Metastases
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EGFR (Epidermal growth factor receptor)
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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)
6ms
New P1 trial • Metastases
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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) • RET (Ret Proto-Oncogene)
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EGFR mutation • HER-2 overexpression • BRAF mutation • HER-2 amplification • EGFR L858R • HER-2 mutation • EGFR exon 19 deletion • MET amplification • EGFR T790M • RET fusion • HER-2 exon 20 insertion • ALK fusion • EGFR L861Q • RAS mutation • EGFR G719X • EGFR S768I • HER-2 exon 20 mutation • BRAF amplification • HER-2 exon 23 mutation
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Erbitux (cetuximab) • Tagrisso (osimertinib) • Tukysa (tucatinib)
7ms
Sintilimab Combined With Anlotinib in Advanced NSCLC With EGFR Uncommon Mutations (clinicaltrials.gov)
P2, N=21, Completed, Zhejiang Cancer Hospital | Active, not recruiting --> Completed
Trial completion • Tumor mutational burden • IO biomarker • Metastases
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PD-L1 (Programmed death ligand 1)
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EGFR mutation • EGFR T790M • EGFR L861Q • EGFR G719X • EGFR S768I • EGFR G719X + EGFR L861Q + EGFR S768I
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Focus V (anlotinib) • Tyvyt (sintilimab)
7ms
New P2 trial • Circulating tumor DNA
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EGFR (Epidermal growth factor receptor)
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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)
7ms
The treatment of patients with non-small cell lung cancer carrying uncommon EGFR mutations, HER2 mutations, or brain metastases: a systematic review of pre-clinical and clinical findings for dacomitinib. (PubMed, Transl Cancer Res)
Last but not least, both pre-clinical and clinical data indicated that dacomitinib has an encouraging intracranial tumor control ability, regardless of uncommon mutations. Dacomitinib demonstrated good disease control on patients with NSCLC harboring major uncommon EGFR mutations and specific EGFR or HER2 mutation subtypes, and selective clinical application of dacomitinib is considerable in this setting, especially for those with intracranial metastases.
Preclinical • Review • 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 exon 20 insertion • EGFR L861Q • EGFR A763_Y764insFQEA • EGFR G719X • EGFR S768I • EGFR exon 20 mutation • EGFR L747P • HER-2 M774delinsWLV
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Vizimpro (dacomitinib)
7ms
New P2 trial • Metastases
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EGFR (Epidermal growth factor receptor)
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EGFR mutation • EGFR exon 20 insertion • EGFR L861Q • EGFR G719X • EGFR S768I • EGFR exon 18 mutation
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Nerlynx (neratinib)
7ms
Comparison of efficacy and safety of second- and third-generation TKIs for non-small-cell lung cancer with uncommon EGFR mutations. (PubMed, Cancer Med)
The efficacy of second- and third-generation TKIs for NSCLC with uncommon EGFR mutations does not differ, and so can be used to treat NSCLC patients with these mutations.
Journal
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EGFR (Epidermal growth factor receptor)
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EGFR mutation • EGFR L861Q • EGFR G719X • EGFR S768I
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Tagrisso (osimertinib) • Gilotrif (afatinib)
7ms
Real-word Study of Aumolertinib Treatment for Advanced NSCLC Patients with Uncommon EGFR Mutations in Late Permian Coal Area (IASLC-WCLC 2023)
This is the first prospective real-word study to explore the efficacy and safety of third-genaration EGFR-TKI aumolertinib as the first-line treatment for patients with uncommon EGFR mutation of C1 coal-accumulating areas, which can provide an opportunity to improve rates of cure. Trial recruitment is ongoing.
Clinical • Metastases
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EGFR (Epidermal growth factor receptor)
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EGFR mutation • EGFR T790M • EGFR G719X • EGFR S768I
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Ameile (aumolertinib)
8ms
NCI-2019-05913: Alisertib in Combination With Osimertinib in Metastatic EGFR-mutant Lung Cancer (clinicaltrials.gov)
P1, N=22, Active, not recruiting, Collin Blakely | Recruiting --> Active, not recruiting | N=38 --> 22 | Trial completion date: Feb 2025 --> May 2025 | Trial primary completion date: Feb 2025 --> May 2025
Enrollment closed • Enrollment change • Trial completion date • Trial primary completion date • Combination therapy • Metastases
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EGFR (Epidermal growth factor receptor) • TPX2 (TPX2 Microtubule Nucleation Factor)
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EGFR mutation • EGFR L858R • EGFR exon 19 deletion • EGFR T790M • EGFR L861Q • EGFR G719X • EGFR S768I • EGFR E709K • EGFR exon 19 insertion • EGFR H835L • EGFR L833V • EGFR V834L
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Tagrisso (osimertinib) • alisertib (MLN8237)
8ms
Real-world experience of dacomitinib in mEGFR Advanced NSCLC: A single centre experience (ESMO 2023)
Dacomitinib is active in pts with brain metastasis, uncommon EGFR mutation, in patients with poor PS, and at 30 mg starting dose. Dacomitinib showed very good PFS with manageable safety profile.
Clinical • Real-world evidence • Real-world • Metastases
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EGFR (Epidermal growth factor receptor)
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EGFR mutation • EGFR L858R • EGFR T790M • EGFR L861Q • EGFR G719X • EGFR S768I • EGFR G719X + EGFR S768I
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Vizimpro (dacomitinib)
8ms
First-line osimertinib in patients with EGFR mutated lung cancer with uncommon mutations (OCELOT study – interim analysis) (ESMO 2023)
Methods This is a multicentered Canadian phase II investigator-initiated study of (cohort A) osimertinib in the third-line (3L) rechallenge of patients with EGFR+ aNSCLC, following 1L treatment with osimertinib and 2L therapy with platinum pemetrexed chemotherapy; and (cohort B) 1L osimertinib in patients with uncommon EGFR mutations (exon 20 insertions are not permitted). Conclusions Osimertinib appears to be highly active and well tolerated in patients with the more frequent 'uncommon' EGFR mutations (G719X, L861X, and S768I). The OCELOT study will be the largest study to date of 1L osimertinib in patients with EGFR+ aNSCLC harboring uncommon mutations.
Clinical
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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 G719X • EGFR S768I • EGFR exon 20 mutation • EGFR positive
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Tagrisso (osimertinib) • pemetrexed
8ms
Clinical • Circulating tumor DNA • Metastases
|
EGFR (Epidermal growth factor receptor) • HER-2 (Human epidermal growth factor receptor 2) • KRAS (KRAS proto-oncogene GTPase) • BRAF (B-raf proto-oncogene) • NRAS (Neuroblastoma RAS viral oncogene homolog) • STK11 (Serine/threonine kinase 11) • KEAP1 (Kelch Like ECH Associated Protein 1)
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KRAS mutation • EGFR mutation • HER-2 overexpression • BRAF mutation • NRAS mutation • EGFR L858R • HER-2 mutation • EGFR T790M • STK11 mutation • RAS mutation • KEAP1 mutation • EGFR S768I • EGFR G719A • EGFR E746
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GuardantOMNI
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Enhertu (fam-trastuzumab deruxtecan-nxki)
8ms
TARGET: A Phase II Study of 5-year Adjuvant Osimertinib in Completely Resected EGFR-mutated Stage II-IIIB NSCLC (IASLC-WCLC 2023)
Exploratory endpoints include: plasma resistance markers; minimal residual disease and emerging resistance mutations; incidence and change over time of incidental pulmonary nodules. TARGET is currently recruiting; interim analyses of secondary efficacy endpoints are expected in 2027 and 2028, with final completion in 2029.
Clinical • P2 data
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EGFR (Epidermal growth factor receptor)
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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)
8ms
Real World Analysis Afatinib as a First Line Treatment Patients with Advanced Stage Non-small Cell Lung Cancer Harboring Uncommon EGFR Mutations (IASLC-WCLC 2023)
Afatinib was an effective treatment option in patients with locally advanced and metastatic NSCLC harboring uncommon EGFR mutations. Patients with the EGFR mutations at G719X, compound G719X-S768I and tolerated dose of 20 mg or 30 mg tended to achieve a longer median TTF than those with others.
Clinical • Real-world evidence • Real-world • Metastases
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EGFR (Epidermal growth factor receptor)
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EGFR mutation • EGFR G719X • EGFR S768I • EGFR G719X + EGFR S768I
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Gilotrif (afatinib)
8ms
Genomic Subtypes of EGFR-Mutant NSCLC and Real-World Progression-Free Survival (rwPFS) with Immunotherapy (IO) (IASLC-WCLC 2023)
Findings suggest that uncommon EGFR mutations may have a more immunogenic profile, however this does not translate into longer rwPFS with IO. Continued research on overcoming IO resistance in EGFR-mutant NSCLC is needed. Descriptive Cohort (N=8368)Exon 19del (n=427)L858R (n=342)Exon 20ins (n=66)G719/L861Q/S768I (n=86)WT (n=7447)Median Age66.8 a70.1 a63.7 a70.3 a68.3Female68.9% a67.8% a57.6%76.7% a48.7%Smoking History42.9% a49.4% a45.5% a70.9% a90.1%PD-L1 positive (1%)57.4% a56.1% a60.6%65.1%63.4%PD-L1 high (50%)20.8% a17.5% a24.2%22.1%31.1%TMB high (10 mut/Mb)4.9% a5.8% a6.1% a22.1% a40.5%IO Cohort (N=4073) bExon 19del (n=83)L858R (n=56)Exon 20ins (n=28)G719/L861Q/S768I (n=22)WT (n=3884)Median rwPFS1.9 m a2.7 m a2.2 m2.3 m a3.3 m(95% CI)(1.6 - 2.7)(2.4 - 3.5)(1.8 - 7.0)(1.6 - 4.9)(3.1 - 3.6)12-month % PFS9.1%5.1%12.1%8.1%21.7%a p-value<0.05 vs.
Clinical • Real-world evidence • Tumor mutational burden • PD(L)-1 Biomarker • IO biomarker • Real-world
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EGFR (Epidermal growth factor receptor) • TMB (Tumor Mutational Burden)
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PD-L1 expression • EGFR mutation • TMB-H • EGFR L858R • EGFR exon 19 deletion • EGFR wild-type • EGFR L861Q • EGFR G719X • EGFR S768I
8ms
Safety and Efficacy of Aumolertinib in Patients with advanced NSCLC Harboring Uncommon EGFR Mutations: Cohort 2 Updated (IASLC-WCLC 2023)
In patients with advanced NSCLC harboring uncommon EGFR mutations, high-dose aumolertinib demonstrated a tolerable safety profile and encouraging antitumor activity in NSCLC pts harboring uncommon EGFR mutations. High-dose aumolertinib is also currently being evaluated in a phase 3 clinical trial for patients with uncommon EGFR mutations (NCT04951648).
Clinical • Metastases
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EGFR (Epidermal growth factor receptor)
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EGFR mutation • EGFR L861Q • EGFR G719X • EGFR S768I • EGFR L747P • EGFR H773L • EGFR V774M
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Ameile (aumolertinib)
8ms
In Vivo Efficacy of AZD9592, an EGFR-cMET Bispecific ADC, in a Broad Panel of NSCLC Patient-Derived Xenograft Models (IASLC-WCLC 2023)
Comparable efficacy was observed across EGFR mutant (EGFRm) models previously treated with single or multiple lines of first- (gefitinib, erlotinib), second- (afatinib), and/or third-generation (osimertinib) EGFR TKIs. Additionally, TR was observed in 3/3 (100%) of models previously treated with an EGFR TKI in combination with the cMET TKI savolitinib; high cMET expression by IHC was seen in >90% of the cells in these three models. Notably, 4/5 (80%) of models with prior exposure to the ALK TKI crizotinib demonstrated TR... In vivo efficacy of AZD9592 was demonstrated in PDX models across a broad spectrum of NSCLC molecular profiles. These included EGFRwt and EGFRm tumours harbouring varied EGFR mutations; groups with and without prior chemotherapy; and groups with and without prior treatment with ALK, EGFR, and/or cMET TKI. These observations suggest that AZD9592 may provide clinical benefit in areas of unmet need, including in patients previously treated with chemotherapy or targeted agents.
Preclinical
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EGFR (Epidermal growth factor receptor) • ALK (Anaplastic lymphoma kinase)
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EGFR mutation • EGFR L858R • EGFR exon 19 deletion • EGFR exon 20 insertion • EGFR expression • EGFR wild-type • EGFR L861Q • EGFR S768I • EGFR exon 20 mutation • EGFR G719C
|
Xalkori (crizotinib) • Tagrisso (osimertinib) • erlotinib • Gilotrif (afatinib) • gefitinib • Orpathys (savolitinib) • tilatamig samrotecan (AZD9592)
8ms
A Multi-Center Observational Study of Effectiveness and Safety of First Line Afatinib in Major Uncommon EGFR mutated NSCLC (IASLC-WCLC 2023)
Afatinib was a treatment of choice for Vietnamese patients with NSCLC harboring major uncommon mutations, demonstrating an encouraging survival outcome, high response rate, and manageable tolerability profile. Brain and liver metastases might be poor prognostic factors and the incidence of secondary T790M mutation seems lower than those reported in common EGFR mutations.
Clinical • Observational data
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EGFR (Epidermal growth factor receptor)
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EGFR mutation • EGFR T790M • EGFR L861Q • EGFR G719X • EGFR S768I
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Gilotrif (afatinib)
8ms
Exceptional Response to Aumolertinib in an Advanced NSCLC Patient With Rare EGFR Exon20 V774M and S768I Mutations (IASLC-WCLC 2023)
The second-generation EGFR-TKI afatinib has been shown to be effective against complex rare EGFR mutations like H773L/V774M or G719X/S768I, meanwhile more adverse effects such as diarrhea and rash occur...Telephone follow-up revealed that the patient continued to take aumolertinib in combination with anlotinib until her death in July 2022... A previous report indicated that patients harboring two uncommon mutations were associated with poorer prognosis (mPFS: 6.5 months). However, the AIM study, recently published in ESMO ASIA 2022, demonstrated that aumolertinib had an impressive objective response rate (ORR) of 53.8% and disease control rate (DCR) of 100% in patients with the main rare mutations (G719X/L861Q/S768I). In summary, this case report suggests that EGFR V774M/S768I can be an activating mutation complex and the administration of aumolertinib monotherapy or a combination with anti-angiogenic drug can achieve outstanding clinical benefits for these patients.
Clinical • EGFR exon 20 • Metastases
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EGFR (Epidermal growth factor receptor)
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EGFR mutation • EGFR exon 20 insertion • EGFR L861Q • EGFR G719X • EGFR S768I • EGFR exon 20 mutation • EGFR exon 20 mutation + EGFR V774M + EGFR S768I • EGFR H773L • EGFR V774M
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Gilotrif (afatinib) • Focus V (anlotinib) • Ameile (aumolertinib)