erlotinib / Generic mfg. - LARVOL DELTA

Design, synthesis, and biological evaluation of quinazoline-benzohydrazide and quinazoline-benzothiazole hybrids uncovering a dual EGFR/VEGFR-2 inhibitor with pronounced cytotoxic activity against triple-negative breast Cancer. (PubMed, Bioorg Med Chem) - "Among the tested compounds, 7a demonstrated the most potent activity, with IC₅₀ values ranging from 3.98 to 9.67 μM, comparable with doxorubicin...It also markedly inhibited EGFR and VEGFR-2 with IC₅₀ values of 1.67 and 6.72 μM, compared to Erlotinib and Sorafenib, respectively...Molecular docking studies confirmed the strong binding affinity of 7a within the active sites of both EGFR and VEGFR-2, supporting its proposed mechanism of action. These findings position compound 7a as a promising lead for further development as a dual EGFR/VEGFR-2-targeting anticancer agent, particularly for aggressive cancers such as TNBC."

IO biomarker • Journal • Breast Cancer • Oncology • Solid Tumor • Triple Negative Breast Cancer • BAX • BCL2 • CASP3 • CASP9 • EGFR

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

Underexplored mutations in plasma cell myeloma (ASH 2025) - "Many FDA-approved therapies exist in other cancers (such as sotorasib, selumetinib,vemurafenib, enasidenib, midostaurin, ruxolitinib, crizotinib, erlotinib), though these remain largelyunexplored in PCM. CHIP mutation burden in MM / PCM was 40%, Our analysis identified several potentially targetablemutations in pts with PCM, including KRAS, NRAS, BRAF, IDH2, FLT3, JAK2, ALK, and EGFR. Clonalhematopoiesis (CH/CHIP) mutations, such as DNMT3A, TET2, ASXL1, and SRSF2, were also observed.Although the lineage origin of several targetable mutations remains unclear, the likely high plasma cellburden in PCM cases suggests that many may originate within the malignant plasma cell clone. Thishypothesis warrants systematic investigation in future studies."

Tumor mutational burden • Hematological Malignancies • Multiple Myeloma • ALK • ASXL1 • BCOR • BRAF • CALR • CREBBP • CSF3R • DNMT3A • EGFR • FLT3 • GNAS • IDH2 • JAK2 • KRAS • NRAS • PHF6 • PPM1D • PRPF8 • SRSF2 • SUZ12 • TET2 • TMB • TP53

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

Comparative clinical efficacy of osimertinib versus erlotinib in stage IV EGFR and TP53 co-mutated lung adenocarcinoma (ESMO Asia 2025) - "Osimertinib demonstrated superior survival outcomes compared to erlotinib in patients with stage IV TP53 and EGFR co-mutated lung cancer. Further studies in larger cohorts are warranted to validate these findings and to explore predictors of response within each treatment group."

Clinical • IO biomarker • Metastases • Lung Adenocarcinoma • Lung Cancer • Microsatellite Instability • Non Small Cell Lung Cancer • Oncology • Solid Tumor • EGFR • MSI • PD-L1 • TP53

Impact of adding bevacizumab to erlotinib on progression-free and overall survival in EGFR-mutant advanced NSCLC with brain metastases: A meta-analysis (ESMO Asia 2025) - "In EGFR-positive advanced NSCLC patients with brain metastases, adding bevacizumab to erlotinib significantly improves progression-free survival (PFS) but does not provide a clear overall-survival (OS) benefit. This combination therapy represents an effective option to delay disease progression in this high-risk population. Further studies with longer follow-up are needed to determine its long-term impact on survival and quality of life."

Metastases • Retrospective data • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor • EGFR

Efficacy and safety of erlotinib and ramucirumab combination therapy in patients harboring EGFR mutations who have previously received osimertinib treatment for non-small cell lung cancer: CS-Lung006 Study (ESMO Asia 2025) - "In patients who received prior treatment with osimertinib, combination therapy with erlotinib and ramucirumab was suggested to be an effective treatment option when osimertinib treatment was discontinued due to toxicity."

Clinical • Combination therapy • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor • EGFR

Cancer therapy-related cardiac dysfunction associated with EGFR-TKIs in advanced EGFR-mutant non-small cell lung cancer: A single-center prospective observational study (ESMO Asia 2025) - "Global longitudinal strain (GLS), tricuspid regurgitation peak gradient (TRPG), E/e′ ratio, Troponin-T and N-terminal prohormone of B-type natriuretic peptide (NT-proBNP), were also analyzed using generalized estimating equations. Among 100 patients included in this study (median age 64; 39.0% male, 61.0% female; 72.0% non-smokers), 66.0% patients received osimertinib, 16.0% received erlotinib, 13.0% received afatinib, and 5.0% received dacomitinib. Our study demonstrates the incidence of CTRCD in patients with advanced or recurrent EGFR-mutant NSCLC receiving EGFR-TKI treatment, and compares the effect between osimertinib and first or second generation TKIs. Increased E/e′ ratio was found in osimertinib group, indicating increased diastolic dysfunction. These findings highlight the importance of clinical monitoring of cardiac function in patients receiving TKIs, particularly in those treated with osimertinib."

Clinical • Metastases • Observational data • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor

Osimertinib versus erlotinib plus an angiogenesis inhibitor for patients with EGFR-mutated non-small cell lung cancer and pleural effusion (ESMO Asia 2025) - "PFS of MPE (MPE-PFS), PFS, and overall survival (OS) were calculated using Kaplan-Meier curves, and log-rank tests were performed. Of 421 patients, median age was 73 years [range 28-92], 272 (65%) female, performance status 0 or 1 in 334 (79%) cases, adenocarcinoma in 417 (99%) cases, and 373 (89%) received osimertinib, 48 (11%) received erlotinib plus bevacizumab or ramucirumab (E/VEGF group). In patients with EGFR-mutated NSCLC and MPE, osimertinib was shown to be equally effective as erlotinib plus an angiogenesis inhibitor in controlling MPE."

Clinical • Pleural effusion • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor • EGFR

Real-world experience of low-dose nivolumab combined with metronomic chemotherapy in rural northeast India (ESMO Asia 2025) - "Low-dose nivolumab combined with triple metronomic chemotherapy with Erlotinib, Methotrexate and Celecoxib, demonstrated a favorable safety profile, with predominantly grade 1–2 adverse events; only 7% experienced grade 3 or higher toxicities, leading to dose modifications in 11% of cases. Low-dose nivolumab combined with metronomic chemotherapy is a feasible, well-tolerated, and effective option for advanced cancers in rural Northeast India, addressing critical barriers of cost and access. Given that prior studies show only about 3% of Indian patients eligible for immunotherapy can afford standard doses, this low-dose approach offers a practical strategy to expand immunotherapy availability in resource-limited settings."

Clinical • Real-world • Real-world evidence • Gastric Cancer • Gastrointestinal Cancer • Head and Neck Cancer • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor • Squamous Cell Carcinoma • Squamous Cell Carcinoma of Head and Neck

Efficacy & safety of taxane-platinum doublet chemotherapy with triple oral metronomic chemotherapy & low dose nivolumab as neoadjuvant therapy in locally advanced head and neck squamous cell carcinoma (ESMO Asia 2025) - "While the standard neoadjuvant TPF regimen (taxane, platinum, 5-fluorouracil) improves survival, it's use is limited by toxicity & resource constraints. A regimen with Taxane & Platinum—TP with triple oral metronomic chemotherapy (OMCT: methotrexate, erlotinib, celecoxib)—has shown favorable responses with lower toxicity. We assessed the efficacy and safety of adding low dose Nivolumab to TP-OMCT. This single-centre observational study- (Jan 2024–May 2025) -enrolled LA- HNSCC patients treated with neoadjuvant weekly paclitaxel (80mg/m2),carboplatin (AUC-2), triple-OMCT, and low-dose nivolumab (20, /40, or /80 mg)... Our chemo-immunotherapy regimen appears well-tolerated and highly effective. Compared to published literature, the pCR and survival outcomes were encouraging, warranting longer follow-up and validation in prospective studies."

Clinical • Metastases • Head and Neck Cancer • Oncology • Solid Tumor • Squamous Cell Carcinoma • Squamous Cell Carcinoma of Head and Neck

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

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

Identification of 2 Ubiquitin-Proteasome System-Related Subtypes in Esophageal Squamous Cell Carcinoma for Prognostic and Immunotherapeutic Response Prediction. (PubMed, J Immunother) - "Selumetinib, entinostat, and erlotinib were identified as candidate drugs for cluster 2, whereas tozasertib, alpelisib, and cediranib showed higher suitability for cluster 1. Ten potential biomarkers, 13 transcription factors, and 2 miRNAs were characterized. This study elucidates the role of UPS in ESCC progression and provides a framework for personalized treatment strategies."

IO biomarker • Journal • Esophageal Cancer • Esophageal Squamous Cell Carcinoma • Oncology • Squamous Cell Carcinoma • Targeted Protein Degradation • CD8 • TP53

Successful treatment of an MBTPS2-linked Olmsted syndrome patient using erlotinib. (PubMed, JAAD Case Rep) - No abstract available

Journal

Exploring the anticancer potential of Tinospora cordifolia with computational insights into EGFR inhibition. (PubMed, In Silico Pharmacol) - "Tinocordiside showed favorable frontier molecular orbital properties and strong binding affinity to the EGFR tyrosine kinase domain, forming multiple hydrogen bonds with critical residues and displaying a docking score comparable to Erlotinib...This underscores the need for apoptosis marker studies in vitro, in vivo validation, and advanced formulation strategies such as amorphous solid dispersions, lipid-based nanoparticles, or cyclodextrin complexes to enhance its therapeutic potential. In summary, T. cordifolia methanolic extract exhibits potent antioxidant and anticancer activity, with Tinocordiside as a promising EGFR-targeting lead compound for further therapeutic exploration."

Journal • Breast Cancer • Hematological Malignancies • Lymphoma • Oncology • Solid Tumor

Design, synthesis, and structural elucidation of ethyl 2-amino-5-oxo-4-aryl-4H-pyrano[3,2-c]quinoline-3-carboxylates as dual EGFR/HER-2 inhibitors endowed with antiproliferative activity. (PubMed, RSC Med Chem) - "Compounds 3a and 3f had the highest antiproliferative efficacy, especially against HT-29 colon cancer cells (IC50 = 23 and 25 nM, respectively), surpassing erlotinib (IC50 = 30 nM)...The compound showed strong binding affinities, forming critical hydrogen bonds and hydrophobic interactions with key active-site residues. Additionally, SwissADME analysis of 3a revealed full compliance with major drug-likeness filters, highlighting its potential as an orally available, dual EGFR/HER-2 inhibitor with favorable pharmacokinetic properties."

IO biomarker • Journal • Colon Cancer • Colorectal Cancer • Oncology • Solid Tumor • BAX • BCL2 • CASP8 • CASP9

Design, synthesis, and characterization of novel 5-ethylsulfonyl-indazole-3-carboxamides as dual VEGFR-2 and EGFR inhibitors: apoptotic antiproliferative and immunomodulatory evaluations. (PubMed, RSC Adv) - "Compounds 8g and 8h reduced TNF-α and IL-6 levels compared to dexamethasone. Additionally, SwissADME profiling demonstrated acceptable drug-likeness, moderate solubility, and a low CYP-inhibition profile, suggesting favorable pharmacokinetics compared to the reference inhibitor erlotinib. These integrated computational findings align with experimental data on antiproliferative effects and kinase inhibition, reinforcing compound 8h as a promising dual-target anticancer candidate."

Journal • Colorectal Cancer • Oncology • BCL2 • CASP3 • CASP8 • CASP9 • EGFR • IL6 • TNFA

Cancer Therapy-Related Cardiac Dysfunction Associated With EGFR-TKIs in Advanced EGFR-mutant Non-small Cell Lung Cancer (clinicaltrials.gov) - P=N/A | N=100 | Completed | Sponsor: Taichung Veterans General Hospital

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

Fused thiophene - benzimidazole conjugates targeting EGFR: Design, synthesis, anticancer evaluation and their mechanistic insights. (PubMed, Eur J Med Chem) - "Furthermore, Western blot analysis revealed that both compounds significantly inhibited the phosphorylation of the EGFR (pEGFR) and also upregulated the expression of LC3B-II (a key marker of autophagy) and cyclin-dependent kinase inhibitor p27, suggesting that activation of autophagy and cell cycle arrest occurred, respectively, thereby inhibiting EGFR phosphorylation and activating downstream cellular responses similar to those of Erlotinib...In silico ADME profiling further highlighted favourable pharmacokinetic properties, reinforcing the potential of 4d and 6d as promising lead candidates. Collectively, these results establish fused thiophene-benzimidazole hybrids as selective EGFR-targeted anticancer agents with strong therapeutic promise."

Journal • Lung Cancer • Oncology • Pancreatic Cancer • Solid Tumor • CDKN1B • EGFR

Clinical correlates of the diffuse glioma mechanical microenvironment - a systematic review (SNO 2025) - "Higher microenvironmental stiffness induced temozolomide resistance of glioma cells in 3D scaffolds in vitro. Tissue stiffness had a sensitizing effect for erlotinib, but not for doxorubicin... MME properties and downstream mechanosignalling correlate to diagnostic classification of brain tumors, and clinical outcome in glioma patients. MME characteristics based on neuroimaging and molecular mechanoprofiling may predict treatment response. Manipulation of the MME may add to drug repurposing in glioma, by improving efficacy of existing drugs that have been ineffective to date."

Clinical • Review • Brain Cancer • CNS Tumor • Glioblastoma • Glioma • Solid Tumor

Biological Medicines for Diffuse Intrinsic Pontine Gliomas (DIPG) Eradication (BIOMEDE). An International Randomized Phase II Biomarker-driven Platform Trial Comparing Three Targeted Therapies in Combination with Radiotherapy (SNO 2025) - "233 patients with biopsy-confirmed DIPG harboring H3K27me3 loss were randomized to one of the three drugs (erlotinib, everolimus or dasatinib) in addition to radiotherapy. Mutations in the mTOR pathway or its pathway activation on gene expression analysis were associated with a better response to everolimus. Four long-term survivors all treated with everolimus were alive more than six years from diagnosis."

Biomarker • Clinical • Combination therapy • P2 data • Brain Cancer • Diffuse Intrinsic Pontine Glioma • Glioma • Solid Tumor • TP53