gefitinib / Generic mfg. - LARVOL DELTA

TAS3351 is a brain penetrable EGFR-TKI that overcomes T790M and C797S resistant mutations. (PubMed, Commun Med (Lond)) - "These findings indicate that TAS3351 is a promising therapeutic candidate for patients with NSCLC whose tumors have relapsed or are refractory to treatment due to the C797S and T790M mutations, and the brain metastases."

Journal • Breast Cancer • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor

Kasugamycin Inhibits Melanoma Lung Metastasis and CHI3L1-Driven M2-Like Tumor-Associated Macrophage Differentiation. (PubMed, Immunotargets Ther) - "Pharmacologic inhibition studies were conducted using the epidermal growth factor receptor (EGFR) inhibitor gefitinib to validate mechanistic links...These findings identify a previously unrecognized anti-tumor mechanism of KSM through inhibition of CHI3L1-EGFR-STAT3 signaling and suppression of M2-like TAM differentiation. KSM may therefore represent a promising immunomodulatory strategy for treating melanoma lung metastasis and other CHI3L1-driven malignancies."

IO biomarker • Journal • Melanoma • Oncology • Solid Tumor • CD163 • CHI3L1 • MRC1 • PD-L1

Tumor Angiogenesis and EGFR-Mutated Cancers: Structural Insights, Mutation Dynamics, and Innovative Therapeutic Strategies. (PubMed, Curr Top Med Chem) - "A focused translational approach that combines structural insights with innovative therapeutic strategies is urgently needed to achieve lasting clinical benefits in EGFR-driven cancers."

Journal • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor • EGFR • MET

Yifei Sanjie pill combined with gefitinib reduces the progression of EGFR-TKIs-resistant non-small cell lung cancer via YAP/ANKRD1 axis. (PubMed, Phytomedicine) - "Co-administration of YFSJ and gefitinib suppresses the growth and migration of NSCLC. ANKRD1 may be a potential biomarker for EGFR exon 20 mutation-driven resistance. This therapy reduces resistance to first-generation EGFR-TKIs by blocking YAP/ANKRD1 axis to suppress cell proliferation and promoting apoptosis. Based on our previous clinical investigations and the present preclinical findings, YFSJ-particularly in combination with gefitinib-may represent a novel therapeutic strategy and warrants further exploration for the treatment of NSCLC resistant to EGFR exon 20 mutations."

Journal • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor • ANKRD1 • CASP3 • YAP1

Integrated analysis of therapeutic strategies and prognostic factors in advanced lung adenocarcinoma: Retrospective study with emphasis on gene assays, multimodality treatment approaches and predictive machine learning models. (PubMed, Oncol Lett) - "First-line treatment with the tyrosine kinase inhibitor afatinib was associated with improved OS compared with that of patients treated with erotinib or gefitinib. In addition, combination therapy with the angiogenesis inhibitor bevacizumab had a positive impact on OS...These findings highlight the importance of molecular profiling and individualized treatment strategies in optimizing OS for patients with advanced lung adenocarcinoma. Furthermore, the validated machine learning models may serve as useful tools for risk stratification and personalized prognostic assessment to support clinical decision-making."

Biomarker • Journal • Retrospective data • Lung Adenocarcinoma • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor • EGFR • PD-L1

Real-world outcomes of EGFR–TP53 co-mutated lung cancer from Western India: A retrospective analysis (ELCC 2026) - "First-line systemic therapy was administered in 92.2% (n=106) mainly EGFR-TKI–based regimens: gefitinib (48.2%),osimertinib(24.1%) & afatinib(17.2%) either as monotherapy(n=55)or in combination with chemotherapy (n=31) with ORR of 76%. mOS was 32.8 mo in adenocarcinoma vs 14.9 mo in other histologies (p=0.022). mOS for TKI alone was 32.8 mo vs 24.2 mo with TKI + chemotherapy (p = 0.884) with distribution of TKI types similar in both the groups (p=0.325).Conclusions This study presents Western Indian real-world data on TP53 co-mutation heterogeneity and outcomes with EGFR-TKI regimens informing routine clinical practice."

IO biomarker • Real-world • Real-world evidence • Retrospective data • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor • ALK • EGFR • HER-2 • KRAS • PD-L1 • PIK3CA • TP53

First-line limertinib versus gefitinib in EGFR-mutated advanced NSCLC: Updated overall survival results from a randomized, double-blind, phase III trial (ELCC 2026) - P3 | "No new safety signals were identified with long-term exposure to limertinib.Conclusions With over 41 months of follow-up, limertinib had a clinically substantial OS benefit, with a 9-month improvement in median OS and a 10% increase in 3-year OS rate compared with gefitinib, and a manageable long-term safety profile. These results demonstrated limertinib as a preferred first-line treatment option for patients with EGFR-mutated advanced NSCLC."

Clinical • Metastases • P3 data • Lung Cancer • Non Small Cell Lung Cancer • Solid Tumor • EGFR

Real-world outcomes (RWO) of oral MET-inhibition in EGFR MET-amplified (MET-amp) NSCLC (ELCC 2026) - "Treatment regimens included tepotinib (tepo) with osimertinib (Osi) (n=14), capmatinib (Cap) with nazartinib (n=3), savolitinib with Osi (n=1), vebreltinib with Osi (n=1), Cap with Erlotinib/Gefitinib (n=3). MET-treated patients with MET:CEP7 ratio ≥2 (n=10) had similar responses to those with ratio <2 (n=5) (mOS 45.4 vs 49.8m, mPFS on MET-i 8.2 v 6.8m, DOR 8.9 v 6.2m).Conclusions Combination EGFR and MET inhibition benefited both denovo Met-amp and post TKI MET resistant EGFR patients. Oral combinations remain an important option for patients."

Clinical • Real-world • Real-world evidence • Lung Cancer • Non Small Cell Lung Cancer • Solid Tumor • EGFR

Real-world effectiveness of different EGFR TKI treatment strategies in advanced non-small cell lung cancer (ELCC 2026) - "Background Frontline osimertinib (OSI) is the standard of care for advanced non-small cell lung cancer (NSCLC) harboring sensitizing EGFR mutations and has demonstrated superior overall survival (OS) compared with first-generation EGFR TKIs (1G; erlotinib and gefitinib). OS was comparable between OSI and SEQ (HR 1.15; 95% CI: 0.89–1.48; p=0.294).Conclusions In real-world practice, both frontline OSI and SEQ strategies significantly improved OS compared with frontline 1G therapy without subsequent OSI, with comparable OS between OSI and SEQ. These findings support further economic evaluation to identify the most cost-effective treatment strategy in resource-limited settings."

Clinical • Metastases • Real-world • Real-world effectiveness • Real-world evidence • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor

RELAY+: Final Overall Survival With Ramucirumab Plus Gefitinib in Patients With Untreated EGFR-Mutated Metastatic NSCLC. (PubMed, JTO Clin Res Rep) - "Patients received RAM (10 mg/kg every 2 wk) plus GEF (250 mg once daily) until disease progression (period 1); patients with disease progression who acquired a T790M mutation received RAM plus osimertinib (80 mg once daily) (period 2). Treatment-emergent T790M rate post progression was 81.3%. RELAY+ revealed a favorable benefit-risk profile for RAM plus GEF in East Asian patients with untreated EGFR-mutated metastatic NSCLC, supporting RAM plus GEF as an alternative first-line treatment option, particularly in those with an L858R mutation."

Journal • Cardiovascular • Hypertension • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor • EGFR

Disparity in the Markers of Affordability Across Targeted- and Immune-Therapy Drugs Used in Head and Neck Cancers. (PubMed, Head Neck) - "Despite modest survival benefits, current immunotherapy pricing severely limits global accessibility. Policy reform and pricing strategies are needed to ensure equitable cancer care."

IO biomarker • Journal • Head and Neck Cancer • Oncology • Solid Tumor

A Study of Gefitinib, Trametinib, Disulfiram, and Sunitinib in Addition to Standard Chemotherapy in People With Osteosarcoma (clinicaltrials.gov) - P2 | N=45 | Recruiting | Sponsor: Memorial Sloan Kettering Cancer Center

New P2 trial • Oncology • Osteosarcoma • Sarcoma • Solid Tumor

Preclinical evaluation of EO1001 in EGFR-ECD mutant solid tumor models: Toward biomarker-directed therapy (AACR 2026) - P1/2 | "EGFR-ECD mutations are intrinsically resistant to approved EGFR TKIs, including osimertinib, erlotinib, gefitinib, and afatinib, because the structural alterations lie outside the ATP-binding pocket and preserve receptor signaling despite drug engagement. This preclinical program will further explore mechanisms of EO1001's activity in EGFR-ECD mutant cancers, providing support for biomarker-guided clinical development."

Preclinical • Brain Cancer • Gastrointestinal Cancer • Glioblastoma • Oncology • Solid Tumor • EGFR

The EGFR-PROTAC molecule TY-2719 attenuates acquired resistance to 3rd-generation EGFR TKIs and augments the efficacy of KRAS mutant inhibitors in solid tumors (AACR 2026) - "TY-2719 overcame osimertinib resistance in BaF3 L858R/C797S and BaF3 del19/C797S CDX mouse models and enhanced the efficacy of Divarasib (GDC-6036) and pan-KRASi Daroxonrasib (RMC-6236) in NSCLC H1972 and H2122 cells, as well as Daroxonrasib in MiaPaca 2 (PDAC, KRAS G12D), AsPC-1, SU.86.86, PANC-1 (PDAC, KRAS G12D), and Capan-1 (PDAC KRAS G12V). TY-2719 effectively degraded EGFR with the L858R mutation in NSCLC H3255 cells and the L858R/T790M/C797S and 19del/C797S mutations in BaF3 cells. However, it did not degrade EGFR in cells expressing wild-type EGFR, such as A549 and H358 cells. It demonstrated excellent antiproliferative activity against EGFR mutants but did not inhibit the growth of normal cells, including NHEK, MCF-10A, IOSE-80, and FHC cells."

Clinical • Preclinical • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Pancreatic Ductal Adenocarcinoma • Solid Tumor • KRAS

FOXM1 as a drug target in NF1-associated malignant peripheral nerve sheath tumors (AACR 2026) - "Synergistic killing of MPNST cells was obtained by combining thiostrepton with a MEK inhibitor (mirdametinib), CDK4/6 inhibitor (palbociclib), or EGFR inhibitor (gefitinib), while NB drugs synergized best with gefitinib. Our data demonstrate FOXM1 is an important driver of MPNST pathogenesis. FOXM1 expression and transcriptional activity are greatly increased in MPNSTs compared to benign precursors from the same patients. In agreement, genetic and therapeutic inactivation of FOXM1 promoted MPNST cell arrest and death."

Brain Cancer • Neurofibrosarcoma • Oncology • Sarcoma • Solid Tumor • CDKN2A • FOXM1 • NF1

Understanding evolutionary and ecological mechanisms of sotorasib resistance in KRAS G12C-mutant non-small cell lung cancer (AACR 2026) - "Drug sensitivity shifted over time and resistant replicates evolved cross-resistance to EGFR/HER2-targeted inhibitors (e.g. Gefitinib and Lapatinib). In contrast, a statistically significant increase in paclitaxel sensitivity was detected, suggesting a collateral vulnerability associated with altered cell-cycle regulation as a compensatory response to KRAS inhibition...Competition outcomes shifted across sotorasib concentrations, indicating that ecological interactions are dose-dependent, highlighting the potential for ecology-informed dosing strategies to reduce competitive release and delay resistance. Together, we provide novel insights into the eco-evolutionary processes underlying sotorasib resistance and identify vulnerabilities that may be leveraged to design therapies that delay or redirect resistance."

Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor • EGFR • HER-2 • KRAS

Deep-learning prediction of progression-free survival to EGFR inhibitors from H&E tissue slides in advanced EGFR-mutated non-small cell lung cancer (AACR 2026) - "Performance was evaluated with C-index for continuous PFS and AUC for 1-year PFS, using bootstrapping. In total, 141 patients were included (n=73 osimertinib; n=68 erlotinib/gefitinib). This is the first study to predict PFS to EGFR-TKIs from H&E slides. Despite limited sample size, these findings support further investigation of digital pathology for PFS prediction in EGFR-mutated NSCLC. Results on additional cohorts, combination of the model with clinical variables, and interpretability will be presented at the congress."

Metastases • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor

Preclinical validation of tetrahydroquinoline derivatives as EGFR inhibitor inducing glioblastoma cell death. (PubMed, Eur J Pharm Sci) - "The half maximum inhibitory concentration (IC50) for THQPMP and gefitinib was established to be 40.6 µM and 46 µM for LN229 cells and 38.3 µM and 68 µM for SNB19 cells, respectively...THQPMP was validated to cross the blood-brain barrier with moderate permeability. Overall, THQPMP has shown efficient preclinical activity against GBM by modulating EGFR signaling pathways, warranting further in vivo validation for phase clinical trials."

Journal • Preclinical • Brain Cancer • Glioblastoma • Oncology • Solid Tumor

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."

Journal • P3 data • Lung Cancer • Lung Non-Squamous Non-Small Cell Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor • EGFR

Farnesyltransferase inhibitor LB42708 disables oncogenic RAS signaling and overcomes gefitinib resistance in NSCLC via FTase α-subunit and RAS degradation. (PubMed, Cell Commun Signal) - No abstract available

Journal • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor

SAFETY AND EFFECTIVENESS OF EGFR-TKI RECHALLENGE AFTER EGFR-TKI-ASSOCIATED INTERSTITIAL LUNG DISEASE IN ADVANCED NON-SMALL CELL LUNG CANCER: A RETROSPECTIVE COHORT STUDY IN TAIWAN (ISPOR 2026) - "We conducted a retrospective cohort study to compare the safety and effectiveness of EGFR-TKI rechallenge versus chemotherapy in patients with advanced NSCLC who experienced ILD during first-line EGFR-TKIs treatment. Using the Taiwan National Health Insurance Research Database (NHIRD), we identified patients with advanced NSCLC between 2011 and 2020 whose first-line therapy (gefitinib, erlotinib, or afatinib) was interrupted by ILD. EGFR-TKI rechallenge is a feasible and effective strategy for advanced NSCLC patients who have recovered from initial EGFR-TKI-associated ILD. Rechallenge offers a significant survival benefit without a marked increase in ILD recurrence risk compared to chemotherapy. These findings provide robust real-world evidence to support clinical decision-making and insurance reimbursement considerations for this challenging patient population."

Metastases • Retrospective data • Interstitial Lung Disease • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Pulmonary Disease • Respiratory Diseases • Solid Tumor

Patient-derived extracellular matrix scaffolds enable physiologically relevant ex vivo models of vulvar cancer (ESGO 2026) - "Proteomic analysis further revealed increased expression of laminins and matrix-remodelling enzymes in dhECM cultures. Treatment with gefitinib, afatinib, or binimetinib significantly reduced cancer cell invasion and viability in dhECM organotypics.Conclusion Decellularised human ECM hydrogels provide physiologically relevant, tissue-specific scaffolds for ex vivo modelling of vulvar cancer and enable effective preclinical evaluation of targeted therapies."

Preclinical • Gynecologic Cancers • Oncology • Solid Tumor • Squamous Cell Carcinoma • Vulvar Cancer • COL1A1 • COL1A2 • COL2A1 • COL3A1

Regulatory Role of Ribosome Biogenesis-Related Genes in Hepatocellular Carcinoma Prognosis and Construction of a Risk Prediction Model. (PubMed, Dig Dis Sci) - "A novel prediction model was constructed based on seven RB-related signature genes for prognostic prediction in HCC patients. Targeted inhibition of CGREF1 may represent a potential strategy to improve therapeutic outcomes in HCC."

Journal • Hepatocellular Cancer • Oncology • Solid Tumor • SLC7A11

Aumolertinib combined with targeting ETV4 in the treatment of non-small cell lung cancer. (PubMed, J Thorac Dis) - "In vitro experiments using PC-9 cells included Cell Counting Kit-8 (CCK-8) assays (cell viability), wound healing assays (migration), flow cytometry (apoptosis/cell cycle), RNA sequencing (RNA-seq), public transcriptome datasets (GSE193258, GSE178975) were analyzed to compare ETS variant transcription factor 4 (ETV4) expression across EGFR-TKIs (aumolertinib, osimertinib, and gefitinib). ETV4 knockdown enhanced aumolertinib-induced apoptosis/G2/M arrest in vitro and synergistically suppressed tumor growth in vivo. These findings revealed that ETV4 enhanced the therapeutic efficacy of aumolertinib in vitro and in vivo, indicating that ETV4 is a potential therapeutic co-target, serving as a treatment strategy to prevent the acquired resistance induced by aumolertinib."

Journal • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor • ETV4 • TCF4

Dose dependent intracranial response to sotorasib in KRASG12C-mutated lung cancer brain metastases (DKK 2026) - "Likewise, clinical studies reported a dose-dependent increase of the EGFR-TKI gefitinib in the cerebrospinal fluid during radiotherapy (3). Our case suggests a dose dependent intracranial activity of sotorasib. Tolerance-adapted dose escalation may offer a therapeutic option for patients experiencing central disease progression under standard dosing. It also underscores the importance of carefully evaluating individual dose reductions."

IO biomarker • Brain Cancer • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor • ABCB1 • KRAS