Tag: EGFR

Olafertinib is a Third-Generation EGFR TKI

Non-small-cell lung carcinoma (NSCLC) is any type of epithelial lung cancer other than small-cell lung carcinoma (SCLC). NSCLC patients with activating EGFR mutations initially respond to first-generation EGFR inhibitors. Epidermal growth factor receptor (EGFR) is a transmembrane glycoprotein with an extracellular epidermal growth factor binding domain and an intracellular...

DBPR112 is an Orally Active EGFR (both WT and Mutant) Inhibitor

Epidermal growth factor receptor (EGFR), a transmembrane protein, is a receptor of EGF family members of extracellular protein ligands. Specifically, EGFR expresses at elevated levels in different forms of cancer and is usually positively relevant to cancer progression and adverse prognosis. Different mutant forms of this protein also contribute...

Afatinib is an Irreversible and Orally Active EGFR Family Inhibitor

Lung cancer continues to be the leading cause of cancer-related mortality. Members of the ERBB receptor tyrosine kinase family include EGFR, HER2, HER3, and HER4. They present an attractive option for targeted therapy in patients with NSCLC, due to observed patterns of oncogenic mutation of EGFR and HER2. In addition, esophageal...

EMI56 is a Superior Mutant EGFR Inhibitor

Receptor Tyrosine Kinases (RTKs) play critical roles in embryogenesis, normal physiology, and several diseases. Epidermal growth factor receptor (EGFR) is a transmembrane protein with cytoplasmic kinase activity that transduces important growth factor signaling from the extracellular milieu to the cell. Furthermore, EGFR common double mutations include 19Del, L858R, and...

Mavelertinib is a Selective and Irreversible EGFR TKI

Mutant EGFRs are one of the major drivers of non-small-cell lung cancer (NSCLC). While reversible first-generation EGFR inhibitors are initially an effective treatment. However, a drug-resistant gatekeeper T790M mutation accounts for ∼50% of disease progression in patients with first-generation agents. Irreversible second-generation EGFR inhibitors are more potent against the...

AG-494 is a Potent and Selective EGFR Inhibitor

Epidermal growth factor (EGF) receptor (EGFR), is the prototype of the EGFR family that also includes ErbB2/HER2/Neu, ErbB3/HER3, and ErbB4/HER4. EGFR is commonly upregulated in cancers such as in non-small-cell lung cancer, metastatic colorectal cancer, glioblastoma, head and neck cancer, pancreatic cancer, and breast cancer. Various mechanisms mediate the upregulation...