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Tibremciclib is a novel, potent, and selective small molecule inhibitor of cyclin-dependent kinase 4 and 6 (CDK4/6). It is being developed for the treatment of hormone receptor-positive (HR+), human epidermal growth factor receptor 2-negative (HER2-) advanced breast cancer. Clinical trials have demonstrated that tibremciclib, particularly in combination with fulvestrant, significantly improves progression-free survival (PFS) in patients who have experienced disease progression after prior endocrine therapy. While showing promising antitumor activity and a manageable safety profile, its global integration requires broader clinical trials to assess generalizability across diverse populations. It has recently been approved in China for HR+/HER2- advanced breast cancer.
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