Indications
Venetoclax is used together with Rituximab to treat adults with chronic lymphocytic leukemia (CLL) who have already had at least one earlier treatment. Venetoclax can also be given alone for CLL, in two situations. The first is when the patient has a 17p deletion or TP53 mutation and either can't take a B-cell receptor pathway inhibitor or has not responded to one. The second is when there is no 17p deletion or TP53 mutation, and the adult patient has not responded to both chemoimmunotherapy and a B-cell receptor pathway inhibitor.
⚠️ Always consult a registered physician before taking any medicine.
Pharmacology
Venetoclax is a selective small-molecule inhibitor of BCL-2, an antiapoptotic protein, and it is taken by mouth with good bioavailability. In CLL cells, BCL-2 has been shown to be overexpressed. This helps the tumor cells survive and has been linked with resistance to chemotherapeutics.
Venetoclax binds directly to the BCL-2 protein and displaces pro-apoptotic proteins such as BIM. This triggers mitochondrial outer membrane permeabilization and activates caspases, and so the process of apoptosis is restored. In nonclinical studies, venetoclax showed cytotoxic activity in tumor cells that overexpress BCL-2.
Pregnancy & Breastfeeding
Women should avoid becoming pregnant while taking Venetoclax and for at least 30 days after treatment ends. So women who could become pregnant must use highly effective contraception during treatment and for 30 days after stopping. It isn't known yet whether Venetoclax lowers the effectiveness of hormonal contraceptives, so women using them should add a barrier method.
Animal studies of embryo-foetal toxicity suggest the medicine may harm the fetus when given to pregnant women. There is no adequate, well-controlled data from its use in pregnant women, and animal studies have shown reproductive toxicity. Venetoclax is not recommended during pregnancy, or for women who could become pregnant and are not using highly effective contraception.
It is unknown whether Venetoclax or its metabolites pass into human milk. A risk to the breast-feeding child can't be excluded, so breast-feeding should be stopped during treatment.
No human data are available on the effect on fertility. Testicular toxicity was seen in dogs at clinically relevant exposures, so male fertility may be compromised by treatment. Before starting, counselling on sperm storage may be considered for some male patients.
⚠️ Talk to your doctor before taking any medicine during pregnancy or while breastfeeding.
Dosage Reference
⚠️ Reference ranges from official sources only. Consult your doctor for personalized dosing.
Side Effects & Interactions
Side Effects
No side-effect data recorded yet.