AKR1C3 Inhibition: A Strategy to Reverse Osimertinib Resistance in Non-small Cell Lung Cancer

Key Points

• The study aims to investigate whether inhibiting AKR1C3 can reverse osimertinib resistance in NSCLC cells harboring the EGFR C797S mutation.
• Utilized a novel selective AKR1C3 inhibitor, SG-55.
• Combined SG-55 with osimertinib in NSCLC cell lines with the C797S mutation.
• Conducted preclinical trials to assess drug efficacy and resistance reversal.
• Combining SG-55 with osimertinib restored sensitivity in C797S mutant NSCLC cells.
• AKR1C3 inhibition effectively reversed resistance to osimertinib.
• Highlights the potential for AKR1C3 as a therapeutic target in NSCLC.