gefitinib / Generic mfg. - LARVOL DELTA

Double Primary Lung Adenocarcinomas Differentiated by Next-generation Sequencing: A Case Report (ATS 2025) - "The patient received gefitinib treatment and achieved a stable disease with a progression-free survival of three years...Owing to the heterogeneity of cancer, it is also difficult to select the optimal therapeutic strategy for patients with multiple primary lung cancer. Our case provides evidence for utility of NGS in facilitating diagnosis and treatment decisions of primary lung cancer diagnosis."

Biomarker • Case report • Clinical • IO biomarker • Next-generation sequencing • Lung Adenocarcinoma • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor • EGFR

When the Mediastinum Holds a Secret: A Journey to Uncover the Mysterious Lesion (ATS 2025) - "At another hospital, a CT guided biopsy from the lesion showed few atypical cells, and he was started on Gefitinib...He received Voriconazole for twelve months following which his symptoms improved and CT showed almost complete resolution of the lesions(Panel B).DiscussionMediastinal aspergillosis presenting as a mass is rare, and can mimic malignancy. In tuberculosis endemic countries, it can be misdiagnosed as tuberculosis which can result in delayed diagnosis and treatment. This case highlights that aspergillosis can affect immunocompetent individuals and efforts should be made to establish pathological or microbiological diagnosis of mediastinal mass."

Anorexia • Cough • Diabetes • Infectious Disease • Metabolic Disorders • Oncology • Otorhinolaryngology • Pain • Respiratory Diseases • Tuberculosis • AFP

A Case of Hidden Threats: Metastatic Right Middle Lobe Adenocarcinoma With Lymphangitic Carcinomatosis Mimicking Musculoskeletal Pain (ATS 2025) - "It also underscores the importance of initiating targeted therapy even in the absence of completed genetic testing when clinical suspicion and disease characteristics support it. Despite the patient's financial constraints preventing EGFR mutation analysis, starting Gefitinib empirically led to significant clinical improvement, illustrating the potential benefits of early targeted treatment in appropriate cases."

Clinical • Metastases • Cough • Lung Cancer • Musculoskeletal Diseases • Musculoskeletal Pain • Oncology • Pain • Pulmonary Disease • Respiratory Diseases • EGFR

Resistance to Anti EGFR Through the Successive and Cumulative Acquisition of Two New Oncogenic Addictions: BRAF and ALK (ATS 2025) - "She received Gefitinib on the first line...Following progression on chemotherapy, the patient receives targeted therapies combining Dabrafenib, Trametinib and Osimertinib. Due to a dissociated response after 4 months of treatment, a 5th line of Paclitaxel Bevacizumab was initiated. Following a new progression and the presence of an ALK rearrangement on the re-biopsy, treatment with Alectinib was then proposed. The response was dissociated and a final line was therefore proposed before stopping active treatments for toxicity and deterioration in general condition. This case reports a resistance to anti-EGFR by the successive and cumulative acquisition of two new oncogene addictions and emphasizes the importance of rebiopsy at each progression on targeted therapy if feasible."

CNS Disorders • Lung Adenocarcinoma • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Psychiatry • Solid Tumor • ALK • BRAF

The correlation of two SNPs in the DRACH motif with gefitinib-induced hepatotoxicity in patients with non-small cell lung cancer. (ASCO 2025) - P=N/A | "Clinical Trial Registration Number: NCT01994057 The abstract will be released to the public on May 22, 2025 at 4:00 PM CDT"

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

Clinical prognostic factors associated with progression-free survival in pts with metastatic EGFR-mutant non-small cell lung cancer treated with gefitinib first-line therapy. (ASCO 2025) - "The abstract will be released to the public on May 22, 2025 at 4:00 PM CDT"

Biomarker • Clinical • Metastases • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor • EGFR

Blood-based biomarkers for predicting treatment response to immune checkpoint inhibitors after EGFR-TKI resistance (AACR 2025) - "First-line EGFR-TKIs included erlotinib (n=15), afatinib (n=9), and gefitinib (n=4). T790M mutations were identified in 11 patients, of whom 10 received osimertinib and 1 received lazertinib. ICIs included atezolizumab (n=15), pembrolizumab (n=5), and nivolumab (n=8)... Plasma samples collected after EGFR-TKI resistance can predict ICI responses in EGFR-mutant NSCLC. Post-resistance plasma biomarker levels may serve as a minimally invasive approach to guide therapeutic decisions in this challenging patient population."

Biomarker • Checkpoint inhibition • IO biomarker • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor • Squamous Cell Carcinoma • GZMH • IL4 • IL6 • PD-L1

Potent Anti-Cancer Activity of Benzo[d]thiazole-Isatin Conjugates: Induces S Phase Arrest and Cell Necrosis in A549 and HepG2 Cells. (PubMed, Chem Biodivers) - "The preliminary antiproliferative results demonstrate that these synthetic derivatives are comparable to the well-known tyrosine kinase inhibitor (TKI) sunitinib. Mechanism of Action (MoA) studies reveled that compound 6g arrest the A549 and HepG2 cells at S phase, and the compound 6g on HepG2 cells resulting in a large number of cell necrosis.  Binding affinity of 6g with EGFR and CDK2 kinase give better results than reference drugs gefitinib and roscovitine, respectively."

Journal • Oncology • CDK2 • EGFR

Molecular characteristics and responses to EGFR tyrosine kinase inhibitors in non-small cell lung cancer patients with EGFR exon 19 insertions. (PubMed, BMC Med) - "Comprehensive analysis of EGFR 19ins in lung cancer patients revealed genomic characteristics and clinical response, helping better inform clinical action and might facilitate the development of more precise therapeutic options for patients with these uncommon driver mutations."

Journal • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor • CDKN2A • CTNNB1 • EGFR • LRP1B • PIK3CA • SMAD4 • TP53

Analytical Approaches to Estimate Medication Persistence From Electronic Health Record Data: A Study of Tyrosine Kinase Inhibitors in Patients With Epidermal Growth Factor Receptor-Positive Advanced Non-Small Cell Lung Cancer (ISPOR 2025) - "This study compared approaches for estimating the persistence of epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors (TKI), including erlotinib, gefitinib, dacomitinib, afatinib, osimertinib, and lazertinib, among patients with EGFR-positive advanced non-small cell lung cancer (advNSCLC). This retrospective study used the nationwide Flatiron Health EHR-derived deidentified database with a data cutoff of November 30, 2024. The non-TTE approach estimated higher EGFR TKI persistence than the TTE approach at all timepoints. The TTE approach accounts for censoring and estimates cumulative persistence, whereas the non-TTE approach provides a point-in-time snapshot. The TTE approach may also provide insights into other real-world outcomes, such as real-world treatment duration."

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

Establishment and evaluation cuproptosis-related gene signature for predicting the prognosis and immunotherapy response of hepatocellular carcinoma. (PubMed, Cancer Cell Int) - "This model demonstrates potential in predicting prognosis and immunotherapy response, providing insights into personalized treatment strategies for HCC. Additionally, our study suggests that BAMBI may serve as a novel biomarker and potential therapeutic target for HCC."

Gene Signature • IO biomarker • Journal • Tumor mutational burden • Hepatocellular Cancer • Oncology • Solid Tumor • BBOX1 • CXCL9 • IL7R • MPZL2 • TMB

Gefitinib Facilitates Bone Fracture Healing via Inhibition of the EGFR Pathway and Counteracting SOX9-driven Bone Metabolic Reprogramming. (PubMed, In Vivo) - "Gefitinib enhances bone fracture healing by modulating lipid metabolism through SOX9, suggesting its potential as a therapeutic agent for improving fracture outcomes."

Journal • Metabolic Disorders • Musculoskeletal Diseases • Orthopedics • SOX9

A Novel Strategy for Treating Gefitinib-Resistant Cancer: Correction of Multiple pathogenic single-nucleotide polymorphism (SNP) Using Adenine Base Editor- expressing adenovirus (ASGCT 2025) - "Collectively, this approach not only addresses the issue of drug resistance but also offers a more targeted and potentially more effective treatment option for cancer patients. Disease Focus of Abstract:Cancer Solid Tumors"

Oncology • Solid Tumor • EGFR • TP53

Engineering aptamer-directed phosphatase recruiting chimeras: a strategy for modulating receptor function and overcoming drug resistance. (PubMed, Nat Commun) - "Furthermore, it is discovered that the induced dephosphorylation could enhance the susceptibility to gefitinib in drug-resistant cancer cells and a xenograft mouse model, indicating the potential of Apt-PRCs to overcome drug resistance in cancer. This work offers a versatile methodology to design molecular mediators to modulate receptor phosphorylation so as to regulate the downstream signal transduction and overcome drug resistance."

Journal • Oncology • EGFR

Combined Use of Gefitinib and Bevacizumab in Advanced Non-Small-Cell Lung Cancer with EGFR G719S/S768I Mutations and Acquired C797S Without T790M After Osimertinib: A Case Report and Literature Review. (PubMed, Curr Oncol) - "Gefitinib combined with bevacizumab demonstrates efficacy in managing NSCLC with uncommon EGFR mutations and overcoming acquired C797S resistance. This combination therapy offers a promising treatment strategy for patients with limited options after resistance to second- and third-generation EGFR-TKIs."

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

Over 200! The largest BaF3-EGFR engineering cell lines collection, a useful platform for novel drug discovery (AACR 2025) - "Recognizing EGFR as a driver gene has accelerated the development of targeted anticancer therapies, such as monoclonal anti-EGFR antibodies (cetuximab, panitumumab) and small molecule receptor tyrosine kinase inhibitors (TKIs). The first generation of EGFR TKIs, like gefitinib and erlotinib, specifically target mutations such as L858R and exon 19 deletions. To address resistance to these early inhibitors, second-generation EGFR TKIs (afatinib, dacomitinib) were developed...Osimertinib, a third-generation TKI, was approved for use in EGFR-mutated NSCLC following the failure of first- and second-generation TKIs, although the EGFR C797S mutation limits its effectiveness. Fourth-generation EGFR TKIs, including BLU-945 and BBT-176, are under clinical evaluation but are not yet approved.We have created more than 200 Ba/F3-EGFR engineered cell lines, making this the largest in vitro and in vivo platform for drug discovery with the widest range of mutant cells. These cell lines..."

Preclinical • Brain Cancer • Breast Cancer • Colon Cancer • Colorectal Cancer • Head and Neck Cancer • HER2 Breast Cancer • HER2 Positive Breast Cancer • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Pancreatic Cancer • Solid Tumor • EGFR • EPGN • ERBB3 • ERBB4 • HBEGF • HER-2 • TGFA

Next-generation NSCLC drug development powered by PDCs and PDOs: Mimicking real responses (AACR 2025) - "The models response to afatinib sensitively. Another example is YUO-143, which harbors EGFR mutations E19del/T790M/C797S and was derived from a patient resistant to gefitinib and mavelertinib. YUO-143 was used in the development of the 4th gen TKI, BLU-945, and showed an IC50 of 43 nM.Conclusions : Patient-derived models could serve as a crucial tool in developing novel therapeutic strategies and next-generation drugs for NSCLC."

Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor • ALK • BRAF • CD74 • EML4 • KRAS • MET • ROS1

Characterization of EGFR C797S-mutant, osimertinib-resistant non-small cell lung cancer cells (AACR 2025) - "Originally, it was developed to target the T790M gatekeeper mutation which arises as acquired resistance mechanism to first-generation EGFR inhibitors such as gefitinib. In contrast, the fourth-generation EGFR inhibitors BLU-945 and JBJ-09-063 reduced viability of the parental and C797S-mutant clones with similar potency. While potencies in the clones were similar between 2D culture and 3D spheroids, BLU-945 and JBJ-09-063 reached a higher maximum effect in 3D spheroids compared to 2D culture.The successful generation and characterization of the NCI-H1975 C797S-mutant clones provides a valuable in vitro model in which additional next-generation EGFR inhibitors and drug combinations can be profiled to identify therapeutic strategies to overcome osimertinib resistance."

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

A Structural Insight Into Two Important ErbB Receptors (EGFR and HER2) and Their Relevance to Non-Small Cell Lung Cancer. (PubMed, Arch Pharm (Weinheim)) - "To develop treatment for EGFR-related NSCLC, several tyrosine kinase inhibitors (TKIs) were designed: gefitinib, erlotinib, as first-generation; neratinib, dacomitinib as second-generation; osimertinib, lazertinib as third-generation, as examples. Although structures obtained so far for the EGFR family provide meaningful insights into the mechanisms, the quality and the quantity of the EGFR family structures are insufficient to elucidate the complete structures and functions to overcome NSCLC. This review evaluates the structures of EGFR-HER2 and investigates their relation to NSCLC."

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

Targeting EZH2 to overcome osimertinib resistant non-small cell lung cancer (AACR 2025) - "Treatment for EGFR mutated lung cancers has evolved over the past two decades, starting with the EGFR tyrosine kinase inhibitors gefitinib and erlotinib, and more recently moving to osimertinib...Following generation of acquired resistance, we found that treatment with the EZH2 inhibitor tazemetostat (EPZ6438) was able to resensitize cell lines to osimertinib...This combination of changes may produce tumors that are more susceptible to immune surveillance, or that respond better to immune checkpoint inhibitors. Overall, this work highlights the ability of inhibiting EZH2 to overcome multiple osimertinib resistance mechanisms in human lung cancer cells and suggests that this drug combination may prolong the treatment benefit for many lung cancer patients."

IO biomarker • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor • EZH2 • MYC • PD-L1

Synergistic anti-cancer effects of dual IGF-1R and EGFR targeting in uveal melanoma (AACR 2025) - "Moreover, Linsitinib and gefitinib co-treatment dramatically increased cleaved PARP protein, an apoptotic maker. Our research suggests that dual targeting of IGF-1R and EGFR could be a novel treatment strategy to inhibit uveal melanoma metastatic dissemination and growth."

Eye Cancer • Melanoma • Oncology • Solid Tumor • Uveal Melanoma • EGFR

Design and discovery of BH-30643: A novel, reversible, mutant-selective macrocyclic EGFR inhibitor invulnerable to common resistance mutations (AACR 2025) - "First-generation (1G) (e.g. gefitinib) and second-generation (2G) (e.g. afatinib) EGFR TKIs share an anilinoquinazoline scaffold which is vulnerable to T790M gatekeeper resistance. Third-generation (3G) (e.g. osimertinib) EGFR TKIs employ a less potent pyrimidine scaffold and obtain good potency including T790M through introduction of an irreversible binding at C797...The unique profile of BH-30643 offers a promising strategy to target a range of classical and non-classical EGFR activating mutations without vulnerability to common on-target resistance mutations. Such an "OMNI-EGFRTM" inhibitor may represent a new generation of EGFR TKIs with potential to overcome some of the limitations of earlier agents."

Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor • ALK • HER-2 • ROS1

Drug tolerance mechanisms in patient-derived xenograft models with epidermal growth factor receptor mutated tumors treated with tyrosine kinase inhibitors (AACR 2025) - "Osimertinib (osi) is effective against common EGFR mutations as well as T790M, yet most patients eventually also develop resistance...Additionally, one progressed on gefitinib PHLC4223L858R and one on afatinib and gefitinib PHLC4192 Ex19delE746_A750del... The altered pathways in tolerance model appears to be unique to an osi-stable response compared to an osi-resistance response. PDX models from post-TKI patients may be useful to study the drug resistant mechanism."

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

Deciphering mechanism of resistance to anti EGFR treatment regimen in a NSCLC PDX model (AACR 2025) - "A deeper analysis comparing individual groups with each other (t-test: limma package, RStudio) revealed an upregulation of proteins that are involved in EMT (TLE1), bad prognosis (UBE2D2 and MAST4), or resistance (SORL1) in the Gefitinib-resistant clone1 under treatment with Cetuximab. The full analysis of the LC-MS data will elucidate the mechanism behind those resistance mechanism and will help to identify new targets as well as favorable combination regimen for pre-treated NSCLC patients. The currently ongoing metabolomics studies will help to build a more complete picture of the cellular regulations leading to the different outcomes observed in the current study."

Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor • HER-2 • MAST4 • NRAS • PTEN • SORL1 • UBE2D2

AMB304: A next generation ADC with topo I inhibitor, demonstrating robust preclinical efficacy against target overexpression tumors and high tolerability in non-human primate (NHP) (AACR 2025) - "Furthermore, elevated expression of the target is associated with resistance to anti-tumor drugs, such as EGFR TKIs (e.g., Gefitinib) and trastuzumab, via signaling. This study demonstrates that AMB304 is potent ADC with significant anticancer efficacy and an excellent safety profile. Moreover, its superior stability in plasma enhances its potential for clinical treatment. Therefore, AMB304 could be developed as a targeted therapy for advanced solid tumors with high target expression."

Preclinical • Breast Cancer • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor • Triple Negative Breast Cancer