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2018 Price of Venclexta
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Venetoclax volume of distribution
The population estimate for apparent volume of distribution (Vdss/F) of venetoclax ranged from 256-321 L in patients.
Discount Cards 16,000+
Clients Benefit 29%
Total savings $4,735,080
What is Venetoclax
Venetoclax is an oral selective inhibitor of B-Cell Lymphoma-2 (BCL-2), an antiapoptotic protein that plays a key role in the development of chronic lymphocytic leukemia (CLL) cells. BCL-2 and its related proteins BCL-XL and MCL-1 bind to and sequester pro-apoptotic signals in the cell, causing a down-regulation of apoptosis. As an oncogene and an important regulator of apoptosis, BCL-2 overexpression therefore results in increased tumour cell survival and resistance to chemotherapy. Venetoclax helps restore the process of apoptosis by binding directly to the BCL-2 protein, displacing pro-apoptotic proteins like BIM, triggering mitochondrial outer membrane permeabilization and the activation of caspases. Compared to navitoclax, a duel inhibitor of BCL-2 and BCL-XL, venetoclax use results in significantly less platelet killing and thrombocytopenia. This is due to its specificity for BCL-2 and sparing of BCL-XL, which is required for platelet survival. In 2015, the United States Food and Drug Administration (FDA) granted Breakthrough Therapy Designation to venetoclax for patients with CLL who have relapsed or have been refractory to previous treatment and have the 17p deletion genetic mutation. It was approved by the FDA in April 2016.
Venetoclax mechanism of action
Venetoclax is a selective and orally bioavailable small-molecule inhibitor of BCL-2, an anti-apoptotic protein. Overexpression of BCL-2 has been demonstrated in CLL cells where it mediates tumor cell survival and has been associated with resistance to chemotherapeutics. Venetoclax helps restore the process of apoptosis by binding directly to the BCL-2 protein, displacing pro-apoptotic proteins like BIM, triggering mitochondrial outer membrane permeabilization and the activation of caspases. In nonclinical studies, venetoclax has demonstrated cytotoxic activity in tumor cells that overexpress BCL-2.
Dosage forms of Venetoclax
|Venclexta||10mg||1 dose pack (14 tablets)||$146|
Abb Vie Inc.
Indication of Venetoclax
For the treatment of patients with chronic lymphocytic leukemia (CLL) with 17p deletion, as detected by an FDA approved test, who have received at least one prior therapy.
Toxicity of Venetoclax
The most common adverse reactions ( 20%) were neutropenia, diarrhea, nausea, anemia, upper respiratory tract infection, thrombocytopenia, and fatigue. Patients should be monitored for development of tumor lysis syndrome and neutorpenia. Venetoclax may cause embryo-fetal harm when administered to a pregnant woman. Patients should therefore avoid pregnancy during treatment.
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