Preclinically, BLU-222 showed significant antitumor activity in a CCNE1-amplified ovarian cancer model, and BLU-222 in combination with standard of care agents led to sustained tumor regression even after treatment cessation. 1 Early biomarker testing using a non-invasive, highly sensitive, and quantitative KIT D816V test may reduce a patient’s time to diagnosis. In subsets of patients with ovarian cancer and other tumor types, aberrant CCNE1 hyperactivates CDK2, resulting in cell cycle dysregulation and tumor growth. Systemic Mastocytosis (SM) is a rare disorder characterized by neoplastic proliferation of mast cells driven by the KIT D816V mutation in greater than 90 of cases. However, prior drug discovery efforts targeting CDK2 have been hindered by challenges in achieving selectivity over other CDK family members associated with toxicity.ĬDK2 is believed to play an important role in tumor proliferation for patients with HR-positive, HER2-negative metastatic breast cancer. CDK2 and CCNE1 are central to regulating the cell cycle, which is involved in the process of cell growth and division. View clinical trials of avapritinib.īLU-222 is a potent and selective CDK2 inhibitor for the treatment of patients with CDK2-vulnerable cancers, including hormone receptor (HR)-positive, HER2-negative breast cancer and CCNE1 aberrant tumors. Food and Drug Administration (FDA) for the treatment of moderate to severe indolent SM.īlueprint Medicines is developing avapritinib as a potential treatment for a broad population of patients with SM globally, including advanced and non-advanced SM. – A minority of patients have advanced SM in addition to mast cell activation symptoms, it is associated with organ damage due to mast cell infiltration and poor overall survival.Īvapritinib has received breakthrough therapy designation from the U.S. – The vast majority of those affected have non-advanced (indolent or smoldering) SM, with debilitating symptoms that lead to a profound, negative impact on quality of life. SM comprises a disease spectrum ranging from indolent SM, which is predominantly characterized by severe constitutional symptoms caused by mast cell degranulation and mediator release, to advanced SM, which is characterized by organ dysfunction and reduced survival due to mast cell infiltration. Systemic mastocytosis (SM) is a rare disease that results from the abnormal proliferation of mast cells across all forms of SM, the KIT D816V mutation is the primary driver of disease.
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