KRAS mutations are among the most common genetic alterations in cancer and are considered particularly difficult to treat. In colon cancer, the second most common cause of cancer death, such mutations ...
Understanding the patterns of acquired resistance to epidermal growth factor receptor (EGFR) TKI treatment has led to more effective combination therapy and continues to drive development of novel ...
Structural insight into KRAS conformational cycling exposed temporary binding opportunities, overturning the “undruggable” ...
Clinically available KRAS inhibitors mainly target G12C, which is rare in PDAC and often acquires resistance. Oncogenic KRAS inactivates RB1 via CDK4/6, while RB1 mutation is rare. Thus, CDK4/6 ...
EO1001 demonstrates up to ~40-fold greater potency than osimertinib in EGFR ECD-mutant tumor models EO4426 (tezacitabine) demonstrates selective targeting of DNA replication machinery and resistance ...
BH-501284 demonstrated high potency (median IC50 of 0.83 nM) and prolonged residence time (>54 hours) in KRAS-mutant cell lines, offering ...
FDA NDA acceptance positions zipalertinib for post-systemic-therapy EGFR ex20ins NSCLC, with a February 27, 2027 PDUFA target ...