erlotinib

A previous analysis of the RELAY phase 3 liquid biopsy addendum demonstrated suppressed EGFR-activating mutation allele count, increased total cell-free DNA (cfDNA) concentration, and shortened cfDNA fragment size with ramucirumab (RAM) plus erlotinib (ERL) versus placebo (PL) plus ERL in patients with EGFR-mutated NSCLC. This updated analysis revealed differences in total cfDNA concentration and T790M mutation rates between ex19del and L858R. RAM plus ERL may exhibit greater antitumor effects on L858R, supporting the favorable survival benefits observed previously in patients with a L858R.

Compounds SM-1F and SM-1 G exhibited good cytotoxic activity (IC50 = 0.5 and 0.7 µM) than standard drug erlotinib (IC50 = of 0.9 µM). Compound SM-1F showed a good binding score -8.93 kcal/mol and interactions with amino acid residues THR 854, THR 790, CYS 775, and PHE856. The results showed SM-1F may be used as a lead compound for further development of novel EGFR inhibitors.

Erlotinib (48.1%) and osimertinib (22.6%) were most frequently used. Conclusions TKIs demonstrated favorable disease control with low attributable ILD. Continued monitoring and structured risk assessment remain essential.

P2, N=50, Active, not recruiting, M.D. Anderson Cancer Center | Trial primary completion date: Jun 2026 --> May 2025

The expression patterns of these two genes did not align with the transcriptome, with only CEACAM5 exhibiting consistent gene and protein expressions. Our findings indicate that CEACAM5 serves as a biomarker for predicting the response of patients to ER and GB treatments.

Both compounds exhibited markedly lower cytotoxicity against normal WI-38 fibroblasts (IC50: 156.59 μM for T6 and 191.80 μM for T7) compared to the reference kinase inhibitor dasatinib (IC50: 37.87 μM), supporting a favorable in-vitro safety profile. Both quinazolinones effectively inhibited EGFR kinase activity with IC50 values of 0.198 μM and 0.131 μM, respectively, compared to 0.046 μM for the reference inhibitor erlotinib...Molecular docking suggested favorable initial EGFR binding of the synthesized quinazolinones, while molecular dynamics analysis supported improved dynamic stability of T7 relative to T6. The results support T6 and T7 as viable and safe candidates for further development in colorectal cancer treatment.

Molecular docking studies with the EGFR protein (PDB: 4HJO) indicate that compound P1 binds with a higher affinity (-8.8 kcal/mol) compared to the reference drug Erlotinib...In silico ADMET analysis reveals excellent oral absorption, low toxicity, and a favorable pharmacokinetic profile. These findings comprehensively validate P1's reactivity, affinity, and stability, positioning it as a promising anticancer drug candidate.

EGFR tyrosine kinase inhibitors, including osimertinib, generally exhibit lower efficacy in patients with the L858R-mutant NSCLC compared with those with exon 19 deletion (del19). Grade more than or equal to 3 adverse events occurred in 42% of patients. In real-world settings, RAM plus ERL demonstrated favorable efficacy in patients with L858R-mutant NSCLC and manageable toxicity.

Targeting HIF-1α disrupts metabolic reprogramming and hypoxia adaptation, thereby enhancing erlotinib efficacy. This combined approach highlights the therapeutic potential of HIF-1α inhibition as a novel strategy to overcome EGFR-TKI resistance in NSCLC.

P1, N=19, Active, not recruiting, National Cancer Institute (NCI) | Trial completion date: Mar 2026 --> Mar 2027

Molecular docking revealed higher binding affinities for both Idarubicin (- 9.98 kcal/mol) and Larotrectinib (- 9.42 kcal/mol) compared to the reference drug Erlotinib (-8.91 kcal/mol). Additionally, they demonstrated favorable predicted cytotoxicity against NSCLC cell lines. In conclusion, our integrated bioinformatics analysis identifies idarubicin and larotrectinib as putative candidates for drug repurposing targeting EGFR in NSCLC, providing a rational foundation for future experimental validation and further preclinical and clinical investigations.

There are a number of systemic and ocular side effects associated with erlotinib. Ocular adverse effects such as dry eye, epithelial keratopathy, nonhealing corneal epithelial defects, corneal ulceration, conjunctivitis, anterior uveitis, trichomegaly, and periorbital skin rash leading to ectropion and epiphora have been reported in the literature. To our knowledge, this is the first reported case of conjunctival ulceration associated with the use of erlotinib.