维奈托克 (Venetoclax) 100mg
1. Composition:
The active ingredient of Venetoclax is Venetoclax, with the chemical name 4-(4-((4'-chloro-5'-(methylthio)-[1,1'-biphenyl]-2-yl)methyl)piperazin-1-yl)-N-((3-nitro-1H-pyrazol-1-yl)methyl)-3-(trifluoromethyl)benzamide. Its molecular formula is C45H50ClN7O7S, and the molecular weight is 868.44.
2. Pharmacological Effects:
Venetoclax is an oral small molecule drug that primarily acts by inhibiting BCL-2 protein. BCL-2 is an anti-apoptotic protein overexpressed in cancer cells, which prolongs their survival and prevents natural apoptosis. Venetoclax restores the apoptosis mechanism in cancer cells by binding to BCL-2, ultimately leading to cancer cell death.
The main efficacy of Venetoclax is demonstrated in:
- Chronic Lymphocytic Leukemia (CLL): It effectively reduces leukemia cells, shrinks lymph nodes, and improves patient survival rates.
- Acute Myeloid Leukemia (AML): When used in combination with other drugs, Venetoclax can increase the remission rates in AML patients, particularly the elderly or those unfit for chemotherapy.
3. Dosage and Administration:
Venetoclax is typically administered in oral tablet form, with a recommended dose of 100 mg; however, the dose is gradually increased during actual treatment. For CLL and SLL, the usual initial dose is 20 mg daily, which is then gradually increased weekly, ultimately reaching a maintenance dose of 400 mg daily. For AML, Venetoclax is usually combined with low-dose cytarabine or demethylating agents, with the dose adjusted according to the condition.
Patients should strictly adhere to the medication regimen under the guidance of a physician and avoid sudden discontinuation or self-adjustment of the dose. It is best taken with food to reduce gastrointestinal discomfort.
4. Research & Development History:
Venetoclax was co-developed by AbbVie and Roche, initially aimed at treating cancers with anti-apoptotic mechanisms. In 2016, the U.S. Food and Drug Administration (FDA) first approved Venetoclax for the treatment of CLL patients with a deletion of chromosome 17p, who are usually resistant to traditional treatments. Subsequently, Venetoclax was approved in multiple countries for treating CLL, SLL, and AML. With further research, Venetoclax has shown broad potential in cancer treatment, particularly in combination therapies.
5. Mechanism of Action:
Venetoclax selectively inhibits BCL-2 protein, relieving the anti-apoptotic mechanism of cancer cells and promoting natural apoptosis (programmed cell death). BCL-2 is a key anti-apoptotic protein, and its overexpression in hematological malignancies such as CLL and AML allows cancer cells to evade apoptosis, sustaining their growth and spread.
By blocking the action of BCL-2, Venetoclax effectively restores the apoptotic process, reducing the survival of cancer cells. This mechanism gives Venetoclax significant efficacy in treating BCL-2-dependent hematological cancers.
6. Summary:
Venetoclax is a potent BCL-2 inhibitor primarily used for treating malignant blood disorders such as CLL, SLL, and AML. It inhibits the growth and spread of cancer cells by blocking BCL-2 protein and restoring the apoptotic mechanism. Venetoclax performs excellently in the field of targeted therapy, especially for patients who are resistant or intolerant to traditional treatments.
