PLB-1001 is a selective small-molecule inhibitor primarily investigated for its use in targeted cancer therapy. It shows potent activity against specific mutant forms of the epidermal growth factor receptor (EGFR), particularly those associated with non-small cell lung cancer (NSCLC). Due to its ability to cross the blood-brain barrier, PLB-1001 has demonstrated promising efficacy in treating brain metastases, which are often challenging to address with conventional EGFR inhibitors. It is being evaluated in clinical trials for patients who have developed resistance to earlier generations of EGFR inhibitors, offering a potential therapeutic option for those with limited treatment alternatives. Its selectivity helps minimize off-target effects, potentially improving patient tolerance and safety profiles during long-term treatment.