What are the Challenges and Limitations of BET Inhibitors?
While BET inhibitors hold promise for cancer therapy, there are several challenges and limitations. One major challenge is the development of resistance, which can occur through various mechanisms such as mutations in BET proteins or compensatory activation of parallel signaling pathways. Additionally, BETi can have off-target effects and toxicity, potentially leading to side effects like thrombocytopenia and gastrointestinal issues. The narrow therapeutic window and the need for combination therapies to enhance efficacy and overcome resistance are also significant concerns.
