Venetoclax is a small molecule inhibitor with high selectivity for B-cell lymphoma 2 (BCL-2) protein. It is used for the treatment of chronic lymphocytic leukemia (CLL) and small lymphocytic lymphoma (SLL). Venetoclax was approved by the US Food and Drug Administration (FDA) in 2016 and is marketed under the trade name Venclexta.
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Venetoclax has been shown to be highly effective in the treatment of CLL and SLL, which are two of the most common types of blood cancers. It works by inhibiting the BCL-2 protein, which is overexpressed in these cancers and helps the cancer cells survive. By inhibiting BCL-2, Venetoclax triggers apoptosis (cell death) in cancer cells, leading to tumor shrinkage and improved disease outcomes.
Besides CLL and SLL, Venetoclax is being studied for the treatment of other types of blood cancers, including acute myeloid leukemia (AML), multiple myeloma, and mantle cell lymphoma. It is also being evaluated in combination with other drugs, such as rituximab, to improve its efficacy and reduce the risk of resistance.
Venetoclax works by inhibiting the BCL-2 protein, which is a key regulator of apoptosis. In normal cells, BCL-2 helps to prevent cell death, but in cancer cells, it is overexpressed and contributes to the survival of the tumor. Venetoclax binds to BCL-2 and prevents it from inhibiting apoptosis, triggering cell death in cancer cells. Venetoclax is highly selective for BCL-2 and does not affect other proteins in the BCL-2 family, which reduces the risk of side effects.
Venetoclax has been shown to be generally safe and well-tolerated in clinical trials, with the most common side effects being diarrhea, nausea, and fatigue. However, there is a risk of serious side effects, including tumor lysis syndrome (TLS), which is a potentially life-threatening condition that can occur when large numbers of cancer cells are killed rapidly. TLS can cause kidney failure, cardiac arrhythmias, and other complications, so it is important to monitor patients closely and take steps to prevent it.