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LFB-190 is a small molecule inhibitor targeting the bromodomain and extra-terminal domain (BET) family of proteins. Developed by Leapfrog Bio, it is designed as an antineoplastic agent for the treatment of solid tumors, with a particular focus on cancers characterized by loss-of-function mutations in the EP300 gene. BET proteins regulate transcription of multiple cancer-related genes and pathways; inhibition disrupts oncogenic transcriptional programs. Leapfrog Bio’s research has identified a synthetically lethal relationship between BET inhibition and EP300 loss-of-function mutations, suggesting enhanced efficacy in this genetically defined patient population. The drug is currently being evaluated in phase II clinical trials for solid tumors, including lung, colon, and bladder cancers[1][3][4].
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