What is Venclexta/Venclyxto (venetoclax) for?
Venclexta/Venclyxto (venetoclax) is a B-Cell lymphoma-2 (BCL-2) inhibitor (chemotherapy) indicated as monotherapy for the treatment of people with chronic lymphocytic leukemia (CLL), with or without the 17p deletion, who have received at least one prior therapy1,2,3,4. The presence of 17p deletion can be assessed using specifically designed diagnostic tools3.
Venclexta/Venclyxto (venetoclax) in combination with rituximab is indicated for the treatment of adult patients with CLL who have received at least one prior therapy2,3,4. Venetoclax is marketed in the USA, Canada and Australia under the name Venclexta1,3,4, and in the European Union under the name Venclyxto2.
How does Venclexta/Venclyxto (venetoclax) work?
CLL is a slow-growing disease in which too many immature lymphocytes (white blood cells) accumulate in the blood and bone marrow5. About 10% of patients with untreated CLL and approximately 20% of patients with relapsed CLL have a particular chromosomal abnormality (17p deletion)6 that is related to a specific type of CLL named B-Cell lymphoma 2 (BCL-2).
Patients with CLL who have a 17p deletion lack a portion of the 17th chromosome the gene involved with the identification and elimination of faulty cells can be found7. This gene thus acts to suppress cancer growth. In the presence of a 17p deletion, healthy cells are unable to use this identification/elimination pathway to prevent and control malignant cells8.
Venetoclax is a selective inhibitor of a protein, named B-Cell lymphoma 2 (BCL-2 protein) that inhibits cell death (anti-apoptotic protein). Overexpression of the BCL-2 protein has been demonstrated in BCL-2 cells where it mediates tumour cell survival and has been associated with resistance to chemotherapeutics. Patients with the 17p deletion usually have poor outcomes with conventional chemo-immunotherapy9. Venetoclax is the first approved treatment that helps restore the process of apoptosis (cell death) by binding directly to the BCL-2 protein and preventing the inhibition of cell death1.
Where has Venclexta/Venclyxto (venetoclax) been approved?
Venclexta/Venclyxto (venetoclax) was approved by:
Food and Drug Administration (FDA), USA: April 11, 2016, for the treatment of patients with CLL or small lymphocytic lymphoma (SLL) with or without 17p deletion who have received at least one prior therapy1.
European Medical Agency (EMA), European Union, December 5, 2016 for the treatment of CLL in the presence of 17p deletion or mutation in adult patients who are unsuitable for or have failed a B-cell receptor pathway inhibitor and for the treatment of CLL in the absence of 17p deletion or TP53 mutation in adult patients who have failed both chemoimmunotherapy and a B-cell receptor pathway inhibitor2.
Therapeutic Goods Administration (TGA), Australia, January 5, 20179, in combination with rituximab, for the treatment of adult patients with CLL who have received at least one prior therapy. As monotherapy, it is indicated for the treatment of patients with relapsed or refractory CLL with 17p deletion or patients with relapsed or refractory CLL for whom there are no other suitable treatment options3.
Health Canada, Canada, September 2016, in combination with rituximab, for the treatment of patients with CLL who have received at least one prior therapy. As monotherapy it is indicated for the treatment of patients with CLL with 17p deletion who have received at least one prior therapy, or patients with CLL without the 17p deletion who have received at least one prior therapy and for whom there are no other available treatment options4.
Please note that this medicine may have also been approved in other regions than the ones we’ve listed. If you have a question about its approval in a specific country feel free to contact our support team.
How is Venclexta/Venclyxto (venetoclax) taken?
Venclexta/Venclyxto (venetoclax) as monotherapy
The standard dosage consists of a weekly ramp-up schedule over 5 weeks to the recommended daily dose of 400 mg taken orally:
Week 1: 20 mg daily.
Week 2: 50 mg daily.
Week 3: 100 mg daily.
Week 4: 200 mg daily
Week 5+: 400 mg daily.
The starter pack covers the treatment up to week 4. For week 5 and beyond venetoclax is dispensed as a one month supply in a bottle containing 120 100 mg tablets.
Concomitant use with strong inhibitors of CYP3A at initiation and during ramp-up phase is contraindicated1,2,3.
Venclexta/Venclyxto (venetoclax) in combination with Rituximab
Rituximab administration can be started for patients who have completed the 5-week dose ramp-up schedule with Venclexta and have received 400 mg dose of Venclexta for 7 days.
Complete information about Venclexta/Venclyxto (venetoclax) dosage and administration can be found in the official prescribing information listed in our resources section1,2,3.
Note: Please consult with your treating doctor for personalised dosing.
Are there any known side effects of Venclexta/Venclyxto (venetoclax)?
Common adverse reactions
The most common adverse reactions listed in the prescribing information include1,2,3,4:
neutropenia (neutrophil count decreased)
diarrhea
nausea
anemia
upper respiratory tract infection
fatigue.
Serious adverse reactions
The serious adverse reactions listed in the prescribing information include1,2,3,4:
pneumonia
febrile neutropenia
tumour lysis syndrome (TLS).
Use in specific populations
Venclexta/Venclyxto (venetoclax) can be fatal for a fetus, it is advised to avoid pregnancies and breast-feeding.
For a comprehensive list of side effects and adverse reactions please refer to the official prescribing information1,2,3,4.
