erlotinib

P1, N=8, Completed, Precision Biotech Taiwan Corp.

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.

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.

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.

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.

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.

P=N/A, N=100, Completed, Taichung Veterans General Hospital

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.

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.

The docking protocol was validated by redocking (RMSD = 0.98 Å), and erlotinib (-8.96 kcal/mol) reproduced known interactions with ASP855, ALA859, and PHE723...In conclusion, PLA-EO exhibits selective cytotoxicity in ovarian cancer cells via ER stress pathways, supported by in silico evidence of EGFR targeting. The combined phytochemical, cellular, and docking results highlight P. loeflingii as a promising source of bioactive essential oils, warranting further in vivo validation.

Furthermore, evaluation of 7c in HCC827 (exon 19 deletion) mutation, which is a cell model highly sensitive to tyrosine kinase inhibitors, showed that the tested compound exhibited lower inhibition than erlotinib...Furthermore, 7c caused an increase in the levels of caspase 3 (4.68 folds) and caspase 9 (4.54 folds) in HCT-116 cells. Additionally, in silico studies of 7c showed a plausible binding mode that correlates with its potent inhibitory activity against the two enzymes, whereas ADME prediction revealed a favorable oral absorption.

Erlotinib induces oxidative and inflammatory optic nerve injury, while TPP co-treatment offers significant neuroprotection. These findings support TPP as a potential adjunct to reduce EGFR-TKI-related ocular toxicity and highlight importance of redox modulation in limiting treatment-associated side effects.