Targeting the EGFR signaling pathway in cancer therapy: What’s new in 2023?

Six‐Membered Aromatic Nitrogen Heterocyclic Anti‐Tumor Agents: Synthesis and Applications

“…The ARCHER 1050 trial, a phase III clinical trial, included individuals with newly diagnosed advanced NSCLC possessing an EGFR mutation. [220,221] This study showed that the administration of dacomitinib at a dosage of 45 mg/day resulted in a statistically significant extension of progression-free survival (14.7 months) compared to the use of gefitinib (250 mg/day) (9.2 months). Furthermore, the findings from the ARCHER 1009 and A7471028 studies further validate the superiority of dacomitinib over erlotinib in patients with NSCLC who have either an exon 19 deletion or L858R substitution in the EGFR exon 21.…”

“…It exhibited a prolonged half‐life of 59–85 h and an apparent volume of distribution of approximately 2600 L within the dosage range of 30–60 mg. The ARCHER 1050 trial, a phase III clinical trial, included individuals with newly diagnosed advanced NSCLC possessing an EGFR mutation [220,221] . This study showed that the administration of dacomitinib at a dosage of 45 mg/day resulted in a statistically significant extension of progression‐free survival (14.7 months) compared to the use of gefitinib (250 mg/day) (9.2 months).…”

Oncolytic herpes simplex viruses designed for targeted treatment of EGFR-bearing tumors

“… 8 Second, vector tropism can be restricted to cells expressing epidermal growth factor receptor (EGFR) or an EGFR mutant lacking exons 2–7 (EGFRvIII), 8 , 9 commonly upregulated in tumors such as GBM. 10 , 11 GBM are locally invasive brain tumors, although extraneural metastases to the regional lymph nodes, lungs, bone, and liver can occur late in the course of the disease. 12 EGFR is also overexpressed in cancers such as head and neck, lung, and breast, providing a cell surface marker with broad utility for targeted cancer therapy.…”

Design, Synthesis, and Biological Evaluation of Newly Synthesized Cinnamide-Fluorinated Containing Compounds as Bioactive Anticancer Agents

“…Epidermal growth factor receptor (EGFR) was the first receptor to be sequenced and discovered to possess tyrosine kinase activity . EGFR has been shown to be aberrantly expressed or activated in a number of tumors. , The downstream signaling effects of such aberration lead to impaired apoptosis, enhanced proliferation, angiogenesis, and metastatic spread. , Therefore, the inhibition of the EGFR signaling pathway has become a valuable approach in the treatment of cancer . One effective approach to inhibit EGFR-mediated signaling is to compete with ATP for binding to the tyrosine domain of EGFR utilizing small molecules of tyrosine kinase inhibitors (TKIs) .…”

“…13 , 14 Therefore, the inhibition of the EGFR signaling pathway has become a valuable approach in the treatment of cancer. 15 One effective approach to inhibit EGFR-mediated signaling is to compete with ATP for binding to the tyrosine domain of EGFR utilizing small molecules of tyrosine kinase inhibitors (TKIs). 16 Gefitinib, erlotinib, and lapatinib represent the most explored TKIs in the clinical setting for the treatment of various types of cancers.…”