gefitinib / Generic mfg. - LARVOL DELTA

Haematological toxicities with targeted drugs in tumors: A systematic review and network meta-analysis of randomized controlled trials (ASH 2025) - "1 patient treated with sorafenib plus chemotherapy was reported to have died as a result of pancytopenia and 1 patient treated with chemotherapy (gemcitabine plus cisplatin) died due to anemia. Our study confirmed that chemotherapy with or without a placebo, one targeted drug with chemotherapy was associated with more severe hematologic toxicities compared with the use of one targeted drug, tepotinib plus gefitinib, tivantinib plus erlotinib. In the targeted drug monotherapy category, for the primary outcome, we found that alectinib and gefitinib had a higher risk of all-grade (grade 1-5) and severe-grade (grade 3-5) anemia, respectively...Ganitumab plus chemotherapy had the highest risk of grade 1-5 anemia and thrombocytopenia. Afatinib plus chemotherapy had the highest risk of grade 3-5 anemia and thrombocytopenia. Ramucirumab plus chemotherapy had the highest risk of grade 1-5 and 3-5 neutropenia. Veliparib plus chemotherapy had the highest risk of grade 1-5 and 3-5..."

Retrospective data • Review • Febrile Neutropenia • Leukopenia • Lung Cancer • Neutropenia • Non Small Cell Lung Cancer • Oncology • Solid Tumor • Thrombocytopenia

EGFR exon 19 duplications/insertions, rare but potential therapeutic targets for NSCLC: A real-world study and pooled analysis of case series (ESMO Asia 2025) - "Stratified by treatment, mPFS1 was 15.5 months with erlotinib (IQR: 9.4-20.0), 12.3 months with afatinib (IQR 7.8-14.3), 7.8 months with osimertinib (IQR 5.6-9.4), 10.9 months with icotinib (IQR 5.9-12.6), 5.3 months with gefitinib (IQR 4.7-9.2), and 6.0 months with immuno/chemotherapy (IQR 3.9-9.0). E19dup/ins are exceedingly rare EGFR genomic alterations with 4 variants reported to date. There is a potential PFS benefit with the use of erlotinib over immuno/chemotherapy as first-line treatment for these mutations. Further data are required to confirm the role of erlotinib in this setting."

Real-world • Real-world evidence • Retrospective data • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor • EGFR

Gefitinib plus pemetrexed-platinum chemotherapy versus gefitinib monotherapy in untreated EGFR-mutant advanced NSCLC (ESMO Asia 2025) - "In patients with EGFR-mutant NSCLC, using GPP over gefitinib monotherapy showed significantly improved PFS. However, it is associated with a higher incidence of adverse events. Therefore, individualized treatment decisions balancing efficacy and safety are of paramount importance to optimize the clinical outcomes."

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

Analysis of the efficacy and safety of radioactive seed Implantation combined with EGFR-TKI in the first-line treatment of classical EGFR mutation NSCLC (ESMO Asia 2025) - "Background: Representative EGFR-TKIs, such as gefitinib, afatinib, and osimertinib, have become the first-line standard treatment for patients with classical EGFR mutations (exon 19 deletions and exon 21 L858R) non-small cell lung cancer, with PFS ranging from 10 to 20 months...PFS has not yet reached for those receiving 2nd agents (only two patients, both treated with dacomitinib, still in follow-up currently), and 39.9m for those receiving 3rd agents. EGFR-TKI therapy combined with RSI confers a significant PFS benefit and merits further prospective investigation."

Clinical • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor • TP53

HIF1A-driven SLC16A3-mediated lactate export suppresses ferroptosis and promotes EGFR-TKI resistance in lung adenocarcinoma (ESMO Asia 2025) - "In vivo efficacy was evaluated in xenografts treated with gefitinib ± MSC-4381. SLC16A3 was upregulated in LUAD tumors and associated with poor prognosis... SLC16A3 suppresses ferroptosis and contributes to EGFR-TKI resistance by exporting lactate and maintaining redox homeostasis. Targeting SLC16A3 restores ferroptosis sensitivity and enhances EGFR-TKI efficacy, supporting its potential as a therapeutic target in LUAD."

Lung Adenocarcinoma • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor • GPX4 • HIF1A • SLC16A3 • SLC7A11

Drug utilisation evaluation of oral anticancer therapy in a south indian cancer centre (ESMO Asia 2025) - "Among targeted therapies, Gefitinib, Osimertinib, Crizotinib, Afatinib, Lorlatinib, and Nilotinib demonstrated consumption of 30 DDDs per patient over 30 days. Lower consumptions were observed with Lenvatinib and Cabozantinib with 13.3 DDDs and 11.25 DDDs per patient respectively. In the hormonal therapy group, Letrozole, Tamoxifen, Bicalutamide, Anastrozole, Enzalutamide, and Exemestane were all prescribed in line with WHO standards (30 DDDs per patient), whereas Abiraterone exhibited lower consumption of 15 DDDs per patient. Prescribing patterns and consumption metrics were largely consistent with WHO criteria, indicating rational oral anticancer drug use. Prescribing patterns and consumption metrics were largely consistent with WHO criteria, indicating rational oral anticancer drug use. Dose deviations occurred, though reasons were unclear and may relate to adverse effects, indication-specific or patient factors, or economic constraints. Further research is warranted..."

Oncology • Oral Cancer

CircZFAND6 suppresses gastric cancer metastasis and reduces resistance to TKI therapy. (PubMed, Mol Cancer) - No abstract available

Journal • Gastric Cancer • Oncology • Solid Tumor

ELK3-SERPINE1-PCBP2 axis promotes gefitinib resistance in lung cancer by inhibiting ferroptosis. (PubMed, Int Immunopharmacol) - "The ELK3-SERPINE1-PCBP2 axis promotes GEF resistance in lung cancer by inhibiting ferroptosis, providing a potential new therapeutic strategy for overcoming chemoresistance."

Journal • Lung Cancer • Oncology • Solid Tumor • Targeted Protein Degradation • PCBP2 • SERPINE1

DMAGCL: A dual-masked adaptive graph contrastive learning framework for predicting circRNA-drug sensitivity. (PubMed, Front Genet) - "Case studies on four representative anticancer drugs (doxorubicin, gefitinib, sorafenib, and paclitaxel) achieved an average experimental validation rate of 80%, highlighting the framework's predictive reliability and biological relevance. In conclusion, this study makes three primary contributions: (1) it introduces the novel DMAGCL framework, establishing a new paradigm for circRNA-drug association prediction via its synergistic dual-masking, adaptive learning, and attentive fusion components; (2) it delivers a highly robust and interpretable model with validated predictive reliability through extensive experiments and case studies (80% average validation rate); and (3) it provides a scalable computational tool that offers valuable insights for discovering novel circRNA-drug associations, understanding drug resistance mechanisms, and informing precision therapy design, with clear pathways for extension to other biological interaction tasks."

Journal • Oncology

Lung adenocarcinoma harboring uncommon EGFR exon 19 deletion L747_T751del and in cis K754E mutation: a case report and literature review. (PubMed, Discov Oncol) - "A 41-year-old male with metastatic lung adenocarcinoma received gefitinib as the first-line treatment. Drug binding dynamics simulation indicated reduced binding activity of osimertinib to L747_T751del and K754E mutation sites as compared to other third- or second-generation EGFR-targeted inhibitors. This study provides the first comprehensive investigation of the L747_T751del and in cis K754E mutation and its interaction with EGFR-targeted inhibitors, offering valuable clinical guidance for treating uncommon EGFR exon 19 mutations."

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

Survival benefit of targeted therapy in EGFR-mutant NSCLC patients with leptomeningeal metastases (SNO 2025) - "The interventions included Afatinib, Erlotinib, Furmonertinib, Gefitinib, Osimertinib, and Rociletinib. This meta-analysis provides the first pooled survival estimate in EGFR-mutant NSCLC patients with LMD receiving targeted therapies. The findings suggest that modern EGFR TKIs may offer clinically meaningful survival benefits in this otherwise high-risk group. Prospective studies are needed to validate these results and to define optimal treatment strategies."

Clinical • Lung Cancer • Non Small Cell Lung Cancer • Solid Tumor

Prognostic model for lung adenocarcinoma based on experimental drug-resistant cell lines and clinical patients. (PubMed, Front Mol Biosci) - "erlotinib-, gefitinib-, and osimertinib-resistant HCC827 cell lines were established by exposing them to increasing EGFR-TKIs concentrations. A nomogram (C-index = 0.7) integrated RiskScore with clinical factors for personalized prognosis. This model bridges in vitro resistance mechanisms with clinical immune landscapes, offering a tool to stratify patients for EGFR-TKIs, immunotherapies, or combinatorial strategies."

IO biomarker • Journal • Preclinical • Lung Adenocarcinoma • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor • LYPD3

Osimertinib Versus First-Generation Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitors for Metastatic EGFR-Mutant Non-Small Cell Lung Cancer: A Target Trial Emulation Study of Real-World Survival and Safety Outcomes. (PubMed, JCO Oncol Pract) - "In this large real-world comparative effectiveness study using target trial emulation, first-line osimertinib was associated with substantially prolonged OS and a favorable safety profile, including lower rates of severe infections and hospitalizations, compared with first-generation EGFR-TKIs in patients with metastatic EGFR-mutant NSCLC."

Journal • Real-world evidence • Hematological Disorders • Infectious Disease • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor • Thrombocytopenia • EGFR

ABCB1 and ABCC10 polymorphisms predict sensitivity to first- and third-generation EGFR-TKIs in EGFR-mutant NSCLC. (PubMed, Invest New Drugs) - "To assess clinical relevance, blood samples from 109 gefitinib/erlotinib- and 54 osimertinib-treated patients were analyzed for these SNPs. These findings suggest that ABC transporter SNPs could be valuable biomarkers for personalized medicine in NSCLC. These findings suggest that ABC transporter SNPs may serve as valuable biomarkers for predicting EGFR-TKI efficacy in NSCLC patients with EGFR mutations, which will contribute to personalized medicine."

Journal • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor • ABCB1 • ABCC10 • ABCC11 • ABCG2

Mechanisms of resistance to anti-HER2 therapies in brain metastatic derivatives of inflammatory HER2-positive breast cancer models (SABCS 2025) - "The HER2-selective tyrosine kinase inhibitor (TKI) tucatinib (Tuca) and the pan-HER TKI neratinib (Nrb), mostly used in the late line setting, are effective, including in treating brain metastases...Drug efficacy studies involved methylene blue-based cell growth and IC50 assays, and included the Akt inhibitor (i), capivasertib (Capi, 1uM), T-DXd (5ug/mL), and the EGFR-specific TKI gefitinib (Gef, 1uM) or monoclonal antibody cetuximab (Cetux, 10ug/mL)... Our findings suggest the role of high EGFR and PIK3CA mutations in resistance to Tuca, which warrants additional preclinical and clinical investigation. This underscores the importance of understanding if PIK3CA mutations are associated with reduced Tuca sensitivity and the testing of new mutant specific PIK3CAi or other PI3K/Akt pathway inhibitors. Our brain tropic TucaR cell and mouse models will be useful to understanding resistance in the brain metastatic setting, and future work will test the most promising..."

Metastases • Preclinical • Breast Cancer • HER2 Breast Cancer • HER2 Positive Breast Cancer • Oncology • Solid Tumor • PIK3CA

LAPTM4B Confers Resistance to EGFR-TKIs by Suppressing the Proteasomal Degradation of ATP1A1 in Non-small Cell Lung Cancer. (PubMed, Int J Biol Sci) - "In this study, we found that EGFR-TKI, including gefitinib and osimertinib, impaired WWP2-mediated proteasomal degradation of LAPTM4B. These compounds synergistically enhance the efficacy of EGFR-TKIs in NSCLC models in vitro and in vivo, with minimal toxicity. Integrative analyses of patient tissue samples, cellular models, an animal model, and cancer databases highlight the critical role of the LAPTM4B-ATP1A1-lysosomal acidification axis in EGFR-TKI resistance, providing a promising therapeutic avenue for overcoming resistance in EGFR-mutant NSCLC."

Journal • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor • Targeted Protein Degradation • ATP1A1 • LAPTM4B • WWP2

An Autologous NK/CIK Cell Product (PB101) in Combination With EGFR-TKI for Treating Lung Cancer (clinicaltrials.gov) - P1 | N=8 | Completed | Sponsor: Precision Biotech Taiwan Corp.

New P1 trial • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor

Construction of a survival prognosis model for epithelial-mesenchymal transition-related genes in gastric cancer. (PubMed, Eur J Med Res) - "Our study provides a prognostic assessment tool for GC based on EMT-related genes and offers novel insights into understanding the roles of EMT in GC progression and treatment resistance. These findings may aid in the development of precision therapy strategies for GC."

Journal • Gastric Cancer • Oncology • Solid Tumor • NPR3 • OLFML2B

Real-world use of and clinical outcomes with dacomitinib as first-line therapy in Asian patients with EGFR mutation-positive locally advanced or metastatic non-small cell lung cancer: Final analysis of the ARIA study. (PubMed, Lung Cancer) - P, P3 | "To our knowledge, ARIA is the largest real-world study of dacomitinib's efficacy and safety. Final analysis of this study showed substantial clinical efficacy of dacomitinib and revealed treatment patterns, such as starting dose, in the real world. Safety data were consistent with dacomitinib's known safety profile. These results support first-line dacomitinib use in Asian patients with EGFR mutation-positive advanced NSCLC."

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

Resistance to tucatinib associated with hyperactive EGFR could be overcome by co-targeting HER2 and EGFR in HER2-positive breast cancer models (SABCS 2025) - "NSG mice bearing GFP/Luc-tagged TucaR xenografts grown with estrogen supplementation were randomized to vehicle, Tuca (100mg/kg, once daily gavage, 7 days/week), or EGFR-specific inhibitors: 1) the TKI gefitinib (Gef 100 mg/kg, once daily gavage, 5 days/week) or 2) the monoclonal antibody cetuximab (Cetux, 30mg/kg, IP twice a week)), either alone or in combination, and monitored for primary tumor growth (caliper measurement) and spontaneous metastasis (by bioluminescence). Our novel findings have crucial therapeutic implications and suggest that HER2+ primary and metastatic tumors with high EGFR (~30% of HER2+ MBC) may not benefit from Tuca or EGFR inhibitors alone and need dual/pan-HER inhibitor therapy, a strategy that we intend to translate via a prospective trial. Our data also suggest the need for imaging-based endpoints in order to capture the minimal/microscopic residual disease that may otherwise be missed through routine tumor measurements, as well as the..."

Preclinical • Breast Cancer • HER2 Breast Cancer • HER2 Positive Breast Cancer • Oncology • Solid Tumor • EGFR • HER-2

RBM8A confers oxaliplatin resistance in gastric cancer by maintaining EGFR mRNA stability. (PubMed, Oncogene) - "Therapeutic targeting of this axis with the EGFR inhibitor gefitinib restored oxaliplatin sensitivity in vitro and synergistically suppressed RBM8A-driven xenograft growth in vivo. Additionally, single-cell RNA-seq revealed RBM8A enrichment in malignant gastric epithelial cells, while tissue microarrays confirmed that dual RBM8A/EGFR overexpression predicts the poorest survival outcomes. Collectively, our findings define the RBM8A-eIF4A3-EGFR axis as a druggable determinant of chemoresistance and establish RBM8A as both a prognostic biomarker and therapeutic target in GC."

Journal • Gastric Cancer • Oncology • Solid Tumor • EGFR • EIF4A3 • RBM8A

Pharmacophore-guided review of EGFR-targeted anticancer drugs with gefitinib as a reference. (PubMed, Eur J Med Chem) - "These patterns expose hidden trends in evasion of polypharmacology and lay groundwork for a versatile pharmacophore template suited to novel scaffold invention. Ultimately, this blended computational-experimental lens equips medicinal chemists with tools to accelerate lead optimization, crafting durable third- and fourth-generation options that adapt to shifting resistance landscapes and elevate EGFR-directed treatments."

Journal • Review • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor • TNFSF12

Discovering bioactive pharmaceuticals from natural products for type 2 diabetes mellitus using network pharmacology, molecular docking, and molecular dynamics. (PubMed, Sci Rep) - "72 natural compounds exhibited superior or comparable binding affinities to standard drugs of which, 17 ligands -Moracin D, Moracin P, Plantagineoside A, Pyrene (carcinogenic), Curcumin, Rohitukine, Berberine Chloride, Berberrubine, Apigenin, Emodin, Chelerythrine, Alvocidib, A-443,654, Xambioona, Altertoxin I, Ursolic Acid, and Oleanolic Acid -were selected as top candidates for further analysis. ADME/T analyses highlighted Pyrene, Guggulsterone, Melatonin, Gefitinib, Apigenin, Rotenone, Curcumin, Bavachinin A, Bavachinin, and Quinidine as particularly promising in terms of superior ADME and oral bioavailability...This study highlights the effectiveness of in-silico techniques to identify natural products as prospective alternative or adjunct therapies for T2DM. Further experimental validation is necessary to confirm compounds' efficacy and safety, paving the way for future clinical investigations."

Journal • Diabetes • Metabolic Disorders • Type 2 Diabetes Mellitus • AKT2 • AMPK • IR • MAPK8 • PPARG • PTPN1 • SLC2A4

Inhibition of primary ciliogenesis enhances efficacy of EGFR‑TKIs against non‑small cell lung cancer cells. (PubMed, Oncol Rep) - "Importantly, treatment with EGFR‑TKIs (gefitinib and dacomitinib) results in a dose‑dependent increase in cilia number and length in A549 and H23 cells, an effect not observed in HCC827 and PC9 cells. Furthermore, it was demonstrated by immunoblotting and immunofluorescence colocalization analysis that both the expression and ciliary localization of adenylate cyclase 3 (AC3) are significantly upregulated following EGFR‑TKIs treatment, and the reduction of AC3 expression effectively mitigates cellular drug resistance in A549 cells. These findings highlight a critical role for the cilia‑AC3 axis in modulating cellular response to EGFR‑TKIs, suggesting it as a potential therapeutic target for the treatment of NSCLC."

Journal • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Small Cell Lung Cancer • Solid Tumor • ARL13B

FDA-approved drug repurposing identifies small molecules with antitumor activity and temozolomide sensitization in glioblastoma (SNO 2025) - "Three agents - decitabine, raloxifene, and gefitinib – the targets of which are upregulated in GBM, demonstrated selective toxicity in ≥6 GBM models and collectively covered all 12. As a single agent, avapritinib significantly reduced viability in all GBM lines – especially of interest given its preliminary efficacy in pediatric high-grade glioma...Further in vitro and in vivo experiments are in progress. These findings nominate several drug candidates for rapid clinical evaluation in GBM."

Brain Cancer • Glioblastoma • Glioma • High Grade Glioma • Oncology • Solid Tumor • PDGFRA