What are BCL-2 inhibitors?
Table of Contents
A selective inhibitor of the anti-apoptotic protein B-cell lymphoma 2 (Bcl-2), with potential pro-apoptotic and antineoplastic activities. Upon administration, Bcl-2 inhibitor BCL201 binds to and inhibits the activity of Bcl-2. This restores apoptotic processes in tumor cells.
Which of the following is an inhibitor of BCL-2?
Venetoclax is the first selective BCL2 inhibitor, and the first of a new class of anticancer drug (BH3-mimetics) to be approved for routine clinical practice, currently in chronic lymphocytic leukemia (CLL) and acute myeloid leukemia (AML).
Is Venetoclax a BCL-2 inhibitor?
Venetoclax (ABT-199, GDC-0199) is a highly selective BCL-2 inhibitor that represents the first approved agent of this class and is currently widely used in the treatment of chronic lymphocytic leukemia (CLL) as well as acute myeloid leukemia (AML).
What is the result of developing an inhibitor that targets BCL-2?
Inhibitors of BCL-2, such as venetoclax and navitoclax, were shown to selectively induce apoptosis in malignant cells and have been extensively investigated as single agents and in combination with other drugs in several malignancies, including acute leukemia, lymphomas, and solid tumors.
Is Navitoclax FDA approved?
FDA approves new drug for chronic lymphocytic leukemia in patients with a specific chromosomal abnormality. 2016.
Does BCL2 inhibit apoptosis?
Bcl-2 inhibits apoptosis by increasing the time-to-death and intrinsic cell-to-cell variations in the mitochondrial pathway of cell death.
When was Venclexta FDA approved?
On October 16, 2020, the Food and Drug Administration granted regular approval to venetoclax (VENCLEXTA ®, AbbVie Inc. and Genentech Inc.)
What class of drug is Venetoclax?
Venetoclax is in a class of medications called B-cell lymphoma-2 (BCL-2) inhibitors. It works by blocking the action of a certain protein in the body that helps cancer cells survive.
How do Senolytics work?
Senolytic drugs are agents that selectively induce apoptosis of senescent cells. These cells accumulate in many tissues with aging and at sites of pathology in multiple chronic diseases.
Is Bcl-2 an oncogene or tumor suppressor?
Apoptosis-Suppressing Oncoprotein Bcl-2 Bcl-2 is widely believed to be an apoptosis suppressor gene. Overexpression of the protein in cancer cells may block or delay onset of apoptosis, by selecting and maintaining long-living cells and arresting cells in the G0 phase of the cell cycle.