gefitinib / Generic mfg. - LARVOL DELTA

Structure-Driven Mechanisms and Synergistic Approaches of Polyphyllin VII in Breast Cancer Therapy. (PubMed, Arch Pharm (Weinheim)) - "Additionally, PP7 exhibits synergistic effects with chemotherapeutic agents like cisplatin, bortezomib, and gefitinib, enhancing cancer cell apoptosis and mitigating drug resistance. However, further research is necessary to clarify its specific role in breast cancer subtypes, ensure its safety in clinical applications, and optimize its broad-scale biosynthesis. This review highlights the structure-driven mechanisms underlying PP7 actions and its therapeutic potential as a standalone agent or adjunct in breast cancer therapy."

Journal • Review • Breast Cancer • Oncology • Pain • Rheumatology • Solid Tumor

Mechanism Study on Inhibition of EPHA2 Expression Impaired Skin Barrier Function by Gefitinib. (PubMed, Exp Dermatol) - "Ephrin-A1 Fc, an EPHA2 agonist, effectively mitigated gefitinib-induced cutaneous damage and inflammation, while concurrently downregulating K10, K17, IL-6, and TNF-α expression in HaCaT cells and upregulating CLDN4 expression. Gefitinib appears to induce dermal barrier dysfunction via the downregulation of EPHA2 expression."

Journal • Dermatology • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor • CLDN4 • EFNA1 • EPHA2 • IL6 • TNFA

Ginsenoside Rg3 Adjunctively Increases the Efficacy of Gefitinib Against NSCLC by Regulating EGFR Copy Number. (PubMed, Pharmaceuticals (Basel)) - "The results of in vivo pharmacodynamic assays confirmed that sequential administration of ginsenoside Rg3 with TKI drugs could achieve a gainful complementary effect. Ginsenoside Rg3 down-regulates the copy number of EGFR important exons in EGFR-mutant cells of lung adenocarcinoma and reduces EGFR protein expression, thus providing a high gainful complementary effect in combination with EGFR-TKI."

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

Recent Advances in the Use of Ganoderma lucidum and Coriolus versicolor Mushrooms to Enhance the Anticancer Efficacy of EGFR-Targeted Drugs in Lung Cancer. (PubMed, Pharmaceutics) - "Depending on their binding interactions with EGFRs, EGFR-TKIs are classified as reversible (first-generation: gefitinib and erlotinib) or irreversible inhibitors (second-generation: afatinib and dacomitinib; third-generation: osimertinib). The involvement of drug transporters and cytochrome P450 enzymes in these herb-drug interactions is summarized. Finally, we also discuss the opportunities and future prospects regarding the combined use of Lingzhi/Yunzhi and EGFR-TKIs in cancer patients."

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

Beyond the Basics: Exploring Pharmacokinetic Interactions and Safety in Tyrosine-Kinase Inhibitor Oral Therapy for Solid Tumors. (PubMed, Pharmaceuticals (Basel)) - "Pharmacokinetic DDIs can critically impact the efficacy and safety of TKIs such as erlotinib, gefitinib, and pazopanib by affecting their absorption, distribution, and metabolism. Drug-specific toxicities, such as hyperlipidemia with lorlatinib or visual disturbances with crizotinib, must be assessed using specific criteria, with dose adjustments and supportive care tailored to individual patient responses. Thus, optimal TKI therapy relies on managing drug interactions through multidisciplinary care, monitoring, and patient education to ensure safety and treatment efficacy."

Journal • PK/PD data • Review • Cardiovascular • Dyslipidemia • Fatigue • Oncology • Solid Tumor

Predictive and Prognostic Significance of Serum Neuron-Specific Enolase in Patients with Metastatic Non-Small Cell Lung Cancer Receiving Gefitinib: A Prospective Study from South Egypt Cancer Institute. (PubMed, Asian Pac J Cancer Prev) - "Baseline serum NSE is an independent poor predictive and prognostic factor for patients with metastatic EGFR-mutated NSCLC receiving gefitinib therapy."

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

Molecular Docking and Drug-Likeness of Salicornia-Derived Phytochemicals Against HER Receptors. (PubMed, Curr Issues Mol Biol) - "Among them, 3,5-di-O-caffeoylquinic acid, 3-O-caffeoylquinic acid, myricetin, quercetin, stigmasterol, kaempferol, isorhamnetin, rhamnetin, and hesperitin featured strong predicted binding affinities to the HER1, HER2, and HER4 growth factor receptors, comparable to those of standard anti-cancer drugs such as gefitinib and dovitinib. Further pharmacokinetic assessments, including bioavailability and toxicity analyses, identified compounds with favorable drug-likeness properties and minimal toxicity risks, except for myricetin and quercetin. These findings underscore the potential of Salicornia-derived phytochemicals as promising candidates for the development of safe, novel, and effective anti-cancer agents targeting GFRs, contributing to the advances in precision oncology, pending further validation through in vitro and/or in vivo experiments."

Journal • Oncology • EGFR • ERBB4 • HER-2

Case Report: Gefitinib in EGFR 19del recurrent aggressive fibromatosis. (PubMed, Front Oncol) - "82003061] and the Shanghai Sailing Program [20YF1408800] to Yanjing Guo, the Natural Science Foundation of Shanghai [Grant No. 24ZR1412800] to Xin Liu)."

Journal • Desmoid Tumors • Fibrosis • Genetic Disorders • Sarcoma • Solid Tumor • EGFR

Efficacy and safety of first-line treatment options for advanced non-small cell lung cancer: A retrospective study. (PubMed, Medicine (Baltimore)) - "In conclusion, the combination of carboplatin, paclitaxel, bevacizumab, or gefitinib significantly improved progression-free survival and overall survival in patients with advanced NSCLC, offering superior efficacy over conventional regimens, with manageable side effects. These findings warrant further investigation to confirm the long-term benefits and optimize treatment strategies for advanced NSCLC."

IO biomarker • Journal • Retrospective data • Cardiovascular • Constipation • Gastroenterology • Gastrointestinal Disorder • Hypertension • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor • EGFR

Investigating the potential of the SI306 Src inhibitor and its liposomal formulation in the non-small cell lung cancer treatment. (PubMed, Int J Pharm) - "Furthermore, both SI306 and Lipo-SI306 exhibited lower cytotoxicity towards HaCaT cells than dasatinib and gefitinib, with CC50s approximately one order of magnitude higher. Hemolytic activity (ranging from 1.85 % as liposomal formulation, to 3.81 % in DMSO and to 14.83 % in Tween80 MIX, respectively) and the median lethal dose (LD50) of 200 mg/kg on Tenebrio molitor coleoptera confirmed the favorable safety profile of SI306. Finally, pharmacokinetic and biodistribution studies in healthy mice showed prolonged circulation time and increased lung accumulation of SI306 when administered as liposomal formulation, highlighting the potential therapeutic advantages of this drug delivery system for NSCLC treatment."

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

Flemiphilippinin A induces paraptosis in lung cancer cells via c-Myc-driven endoplasmic reticulum stress and CHOP-mediated mitochondrial dysfunction. (PubMed, Phytomedicine) - "This research demonstrates that Flp-A exerts potent anti-tumor effects against lung cancer by targeting c-Myc to induce excessive ER stress and mediating mitochondrial dysfunction through CHOP, ultimately triggering paraptosis. Furthermore, Flp-A increases sensitivity of lung carcinoma cells to gefitinib through paraptosis induction. Our work provides the first evidence for Flp-A's anti-lung cancer mechanism via the paraptosis pathway and confirms its safety profile. Additionally, we reveal Flp-A's capacity to bypass gefitinib resistance in lung carcinoma. These findings position Flp-A as a encouraging novel medical agent for lung cancer treatment, particularly for addressing drug resistance."

Journal • Lung Cancer • Metabolic Disorders • Oncology • Solid Tumor • MYC

Phosphoproteomic analysis reveals the diversity of signaling behind ErbB-inhibitor-induced phenotypes. (PubMed, FEBS J) - "Here, we performed a phosphoproteomic analysis in embryonic zebrafish to identify the signaling pathways perturbed by ErbB receptor tyrosine-protein kinase inhibitors gefitinib, lapatinib, and AG1478 at the organism level. The treatment with the inhibitors targeting the PI3K/Akt, p38 MAPK, and Notch signaling pathways, along with the ErbB inhibitors AG1478 and lapatinib, perturbed the overall movement and ventricle wall growth of zebrafish embryos. Taken together, these results indicate that inhibitors with overlapping primary targets can affect different signaling pathways while eliciting similar physiological phenotypes."

Journal

Retreatment With EGFR-Tyrosine Kinase Inhibitor After Disease Progression Following Gefitinib Induction and Chemoradiotherapy in EGFR-Mutant Stage III Non-small Lung Cancer: An Efficacy and Safety Analysis of the LOGIK0902/OLCSG0905 Study. (PubMed, Cureus) - "Background and objective We had previously conducted a phase II study (LOGIK0902/OLCSG0905 study) involving the eight-week administration of gefitinib, followed by cisplatin-based chemoradiotherapy, to treat locally advanced, epidermal growth factor receptor (EGFR)-mutated, non-small cell lung cancer (NSCLC)...After relapse, 9/14 patients (64.3%) received gefitinib, 3/14 (21.4%) received afatinib, and 2/14 (14.3%) received erlotinib monotherapy, respectively...Adverse events were comparable to those previously reported. Conclusions Patients with disease progression after protocol therapy demonstrated sensitivity to retreatment with an EGFR-TKI, with acceptable safety."

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

Cell-in-cell associated lncRNA signature predicts prognosis and immunotherapy response in gastric cancer. (PubMed, Front Oncol) - "Drug sensitivity analysis revealed low-risk patients responded better to gefitinib/entinostat, while high-risk patients benefited from dasatinib/foretinib. Experimental validation confirmed AP000695.2 promoted proliferation and invasion in GC cells (P <0.01). This study establishes CICRlncRNAs as prognostic biomarkers and provides insights for precision therapy, though clinical applicability requires prospective validation."

IO biomarker • Journal • Gastric Cancer • Oncology • Solid Tumor

Adding Gefitinib to Target Acquired C797S Mutation After Progression on First-Line Osimertinib in EGFR-Mutant Advanced NSCLC (IASLC-WCLC 2025) - "Abstract is embargoed at this time."

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

The Combination of USP24-i-101-Astemizole Sensitizes the Cytotoxicity of Taxol and Gefitinib in Drug-Resistant Lung Cancer (IASLC-WCLC 2025) - "Abstract is embargoed at this time."

Lung Cancer • Oncology • Solid Tumor

The targeting of AKR1C1 synergizes with gefitinib via the STAT3 signaling pathway in EGFR-mutated NSCLC. (PubMed, Genes Dis) - No abstract available

Journal • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor • AKR1C1 • EGFR

Effectiveness of afatinib after long-term gefitinib treatment for EGFR L858R and S768I compound mutation-positive lung adenocarcinoma: A case report. (PubMed, Respir Med Case Rep) - "Furthermore, immunohistochemical analysis revealed an increase in HER2 and HER3 protein expression in the gefitinib-resistant specimens. These findings suggest that HER2 and HER3 upregulation may contribute to gefitinib resistance, and that afatinib may effectively target these resistance mechanisms."

Journal • Lung Adenocarcinoma • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Respiratory Diseases • Solid Tumor • EGFR • ERBB3 • HER-2

EGCG-releasing nanofibrous scaffold enhances wound healing via γδ T cells modulation. (PubMed, Biomaterials) - "Inhibition of AREG and EGFR function via monoclonal antibodies against AREG and EGFR antagonist Gefitinib similarly delayed wound healing, the therapeutic advantage of APEMS over APS was abolished, emphasizing its critical role in the process. These findings provide a framework for developing advanced wound management materials and highlight the therapeutic potential of targeting γδ T cells and AREG-EGFR signaling to enhance tissue regeneration."

Journal • Inflammation

Therapeutic evaluation of paclitaxel co-loaded PLGA nanoparticles with imatinib, protamine-imatinib, and gefitinib: comparative in vitro studies in MDA-MB-231 breast cancer cells and in vivo investigations in rats. (PubMed, Naunyn Schmiedebergs Arch Pharmacol) - "Our findings thus highlight the superior potential of co-loaded polymeric NPs in targeted cancer therapy, with an enhanced safety profile, therapeutic outcomes, and modulation of systemic inflammation. The co-loaded formulation of PX with IMT and GF presents a promising strategy for advancing breast cancer treatment."

Journal • Preclinical • Breast Cancer • Fibrosis • Immunology • Oncology • Solid Tumor • Triple Negative Breast Cancer • MUC1 • TNFA

Development of a 3D-3 co-culture microbead consisting of cancer-associated fibroblasts and human umbilical vein endothelial cells for the anti-tumor drug assessment of lung cancer. (PubMed, Transl Lung Cancer Res) - "Moreover, the results also showed that after co-culturing CRLCs with CAFs and HUVECs, the cytotoxicity induced by chemotherapeutic agents (cisplatin, paclitaxel, vinorelbine, and gemcitabine) as well as TKIs (gefitinib, afatinib) was reduced. These findings suggest that the patient-derived in vitro 3D-3 co-culture model, which highlighted the close association between tumor cell resistance and the TME, offers innovative ideas and methods for addressing treatment resistance in lung cancer patients. By closely mirroring human lung tumors, this model not only enhances our understanding of the disease but also paves the way for the development of more effective and personalized therapeutic strategies."

Journal • Lung Cancer • Oncology • Solid Tumor • ALDH1A1 • CAFs • NANOG • SOX9

Overcoming refractory leptomeningeal metastasis in nonsmall cell lung cancer with intrathecal pemetrexed and osimertinib: a case report. (PubMed, Anticancer Drugs) - "Here, we present a case of a 58-year-old female with advanced epidermal growth factor receptor (EGFR)-mutated (exon 19 deletion) lung adenocarcinoma who developed LM after failing first-line gefitinib therapy. Upon disease recurrence after 6 months, therapeutic intensification through increased intrathecal pemetrexed frequency and high-dose osimertinib (160 mg/day) resulted in sustained neurological improvement and prolonged survival with manageable toxicity. This case demonstrates the potential of optimized intrathecal/systemic TKI combination strategies for EGFR-mutant NSCLC with LM, providing clinical insights for this therapeutic dilemma."

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

Potential interactions between traditional Chinese medicine and osimertinib: a Case Report. (PubMed, Front Pharmacol) - "A 57-year-old female was diagnosed with stage IV lung adenocarcinoma, who switched from gefitinib to osimertinib after disease progression. After adjusting the TCM prescription, the patient's osimertinib Ctrough was stable within the range of 145 and 228 ng/mL without significant adverse reactions and carcinoembryonic antigen levels stabilized. This case underscored the importance of monitoring drug concentrations in patients concurrently using TCM and osimertinib to optimize treatment outcomes and minimize potential drug-drug interactions."

Journal • Embryonal Tumor • Lung Adenocarcinoma • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor • CEACAM5 • EGFR

Computer prediction and genetic analysis identifies retinoic acid modulation as a driver of conserved longevity pathways in genetically-diverse Caenorhabditis nematodes. (PubMed, bioRxiv) - "While eleven compounds (aldosterone, arecoline, bortezomib, dasatinib, decitabine, dexamethasone, erlotinib, everolimus, gefitinib, temsirolimus, and thalidomide) either had no effect on median lifespan or were toxic, five compounds (all-trans retinoic acid, berberine, fisetin, propranolol, and ritonavir) extended lifespan in Caenorhabditis elegans . Evolutionary conservation of retinoic acid as a signaling ligand and the structure of the downstream effector network of retinoic acid combine to suggest that the all-trans retinoic acid pathway is an ancient metabolic regulatory system that can modulate lifespan. Our results highlight the potential of combining computational prediction of longevity interventions with the power of nematode functional genetics and underscore that the manipulation of a conserved metabolic regulatory circuit by co-opting endogenous signaling molecules is a powerful approach for discovering aging interventions."

Journal • Acne Vulgaris • Acute Promyelocytic Leukemia • Hematological Malignancies • Leukemia • Oncology • AKT1 • AKT2 • AMPK • HSF1

AKT/mTOR as a targetable hub to overcome multimodal resistance to EGFR inhibitors in oesophageal squamous cell carcinoma. (PubMed, Br J Cancer) - "Combining AKT/mTOR inhibitors with EGFR inhibitors in EGFR-driven ESCC shows synergism but with elevated toxicity. Monotherapy AKT/mTOR inhibitors or combined therapy at reduced doses could offer improved, cost-effective therapy options for gefitinib-resistant cancer."

Journal • Esophageal Cancer • Esophageal Squamous Cell Carcinoma • Oncology • Squamous Cell Carcinoma • IGF1 • IGFBP3 • PDGFRB • TGFB1