2023 World Conference on Lung Cancer (Posters)-P2.09. Design, Synthesis and Assessment of Novel Molecule against Drug-Resistant Dual Mutant EGFR (T790M/L858R) to Treat NSCLC

P2.09. Design, Synthesis and Assessment of Novel Molecule against Drug-Resistant Dual Mutant EGFR (T790M/L858R) to Treat NSCLC - PDF(Abstract)

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This presentation discusses the design, synthesis, and assessment of a novel molecule, KKI04, to treat drug-resistant dual mutant EGFR (T790M/L858R) in non-small cell lung cancer (NSCLC). The development of acquired resistance to current EGFR tyrosine kinase inhibitors (TKIs) is a major challenge in the treatment of EGFR mutant NSCLC. The molecule KKI04 shows significant inhibition activity against drug-resistant EGFR kinases at both the molecular and cellular levels. <br /><br />The researchers used a lead modification approach to develop the efficient drug against drug-resistant EGFR tyrosine kinases. They synthesized the designed molecule and determined its efficacy through in vitro kinase inhibition assays and cell viability assays. The results showed that KKI04 is a potent inhibitor of EGFR T790M/L858R, with higher affinity and lower IC50 values compared to Osimertinib, a third-generation EGFR TKI. <br /><br />In conclusion, KKI04 has shown promising activity against drug-resistant dual mutant EGFR kinases. It has superior inhibition activity compared to existing EGFR kinase inhibitors. However, further studies are needed to evaluate its tumor-reducing and clinical translatable ability through in vivo mice xenografts. <br /><br />This research is valuable for the development of new targeted therapies for metastatic non-small cell lung cancer, particularly for patients with drug-resistant EGFR mutations. It presents a potential breakthrough in overcoming acquired resistance to current EGFR TKIs and provides hope for improved treatment options in the future.

Asset Subtitle

Vikas Kumar

Meta Tag

Speaker Vikas Kumar

Topic Metastatic NSCLC: Targeted Therapy - EGFR/HER2

Keywords

KKI04

drug-resistant

dual mutant EGFR

NSCLC

acquired resistance

EGFR TKIs

inhibition activity

potent inhibitor

Osimertinib

tumor-reducing