BCL2
BCL2
BCL2 Apoptosis Regulator; PPP1R50; Bcl-2; Protein Phosphatase 1, Regulatory Subunit 50; Apoptosis Regulator Bcl-2; B-Cell CLL/Lymphoma 2; BCL2, Apoptosis Regulator 2
Tumor cells have many characteristics, including genomic instability and oncogene activation, which should lead to apoptosis.1 In a bid to survive, tumor cells may become dependent on the BCL-2 protein.2 Certain cancer cells will overexpress BCL-2, which in turn impedes apoptosis and facilitates tumor growth and resistance to chemotherapy.3 These malignant cells that depend on BCL-2 for survival are likely to be sensitive to BCL-2 modulation.4
Understanding the Role of BCL2
This animation discusses the role of BCL2 in normal cell function and explains the effects of disruptions in the BCL2 gene on cell signaling.
Expression in Cancer
High expression of BCL-2 occurs in a variety of cancer types. The graphic below displays cases in each cancer type (up to a certain percentage) that have been reported to overexpress BCL-2.
BCL2 Inhibitors
BCL2 inhibitors bind to and inhibit the activity of the BCL2 protein, regulating apoptosis and slowing the growth of cancer cells. This table outlines therapies targeting BCL2 both approved by the FDA and in the pipeline.
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BCL2 Inhibitors Approved by the FDA |
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Brand Name (Generic Drug Name) |
Indications |
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Venclexta (venetoclax)1 |
Treatment of adult patients with chronic lymphocytic leukemia or small lymphocytic lymphoma |
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Treatment in combination with azacitidine, or decitabine, or low-dose cytarabine for the treatment of newly diagnosed acute myeloid leukemia in adults 75 years or older, or who have comorbidities that preclude use of intensive induction chemotherapy |
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BCL2 Inhibitors in the Pipeline |
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Navitoclax2 |
Treatment being evaluated chronic lymphocytic leukemia, myelofibrosis, myeloproliferative neoplasms, and NSCLC |
