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ZN-e4 is an orally bioavailable, irreversible, third-generation small molecule inhibitor of the epidermal growth factor receptor (EGFR). Developed by Zentalis Pharmaceuticals, it is engineered to selectively target EGFR mutations, specifically the T790M gatekeeper mutation and sensitizing mutations like Exon 19 deletions and L858R, while sparing wild-type EGFR to limit off-target toxicities such as skin rash and diarrhea. In 2020, Zentalis entered into an exclusive licensing agreement with SciClone Pharmaceuticals for the development and commercialization of ZN-e4 in Greater China, South Korea, Taiwan, and Vietnam. The compound is primarily investigated for the treatment of advanced non-small cell lung cancer (NSCLC) harboring these specific mutations.
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