(ven ET oh klax)

Trade Name: Venclexta™

Venetoclax is the generic name for the trade name drug Venclexta™. In some cases, health care professionals may use the trade name Venclexta™ when referring to the generic drug venetoclax.

Drug Type: Venetoclax is an Antineoplastic Agent; BCL-2 Inhibitor (for more detail, see "how this drug works" below).

What Venetoclax Is Used For:

• Indicated for the treatment of patients with chronic lymphocytic leukemia (CLL) or small lymphocytic lymphoma (SLL).
• In combination with azacitidine, or decitabine, or low-dose cytarabine to treat adults with newly-diagnosed acute myeloid leukemia (AML) who: are 75 years or older, or have other medical conditions that prevent the use of standard chemotherapy.

Note: If a drug has been approved for one use, physicians may elect to use this same drug for other problems if they believe it may be helpful.

How Venetoclax Is Given:

• Venetoclax is a tablet, taken by mouth.
• Venetoclax should be taken orally once daily with a meal and water.
• Dosage may be adjusted based on side effects.
• Take venetoclax exactly as prescribed.
• Swallow venetoclax tablets whole. Do not crush, chew, break or dissolve tablets.
• Do not change your dose or stop venetoclax.
• Take your dose of venetoclax at approximately the same time each day. If you miss a dose of venetoclax by less than 8 hours, take the missed dose right away. Then take your next dose as usual. If you miss a dose of venetoclax and it has been more than 8 hours, wait and take the next dose of venetoclax at your usual time.
• Do not take more than 1 dose of venetoclax at one time. Call your health care provider right away if you take too much.
• You should not drink grapefruit juice, eat grapefruit, Seville oranges (often used in marmalades), or starfruit while you are taking venetoclax. These foods may increase the amount of venetoclax in your blood.

The amount of venetoclax that you will receive depends on many factors, your general health or other health problems, and the type of cancer or condition being treated.

Side Effects:

Important things to remember about the side effects of venetoclax:

• Most people do not experience all of the side effects listed.
• Side effects are often predictable in terms of their onset and duration.
• Side effects are usually reversible and often improve or go away after treatment is stopped.
• There are many options to help minimize or prevent side effects.
• There is no relationship between the presence or severity of side effects and the effectiveness of the medication.

The following side effects are common (occurring in greater than 30%) for patients taking venetoclax:

• Low white blood cell counts (increases risk of infection)
• Diarrhea
• Nausea

These side effects are less common side effects (occurring in about 10-29%) of patients receiving venetoclax:

• Anemia
• Low platelets (increases risk of bleeding)
• Upper respiratory tract infection (cold symptoms)
• Fatigue
• High potassium in the blood
• Fever
• Vomiting
• Headache
• High phosphate in the blood
• Constipation
• Cough
• Low potassium in the blood
• Swelling
• Back pain

A serious, but very rare side effect of venetoclax may be:

Tumor Lysis Syndrome- may occur as a result of leukemia treatment. Tumor lysis syndrome occurs when large amounts of cancerous cells are rapidly killed by the therapy. These cells release uric acid, potassium, and phosphorous into the blood stream. Tumor lysis syndrome can lead to kidney failure. Tumor lysis syndrome usually occurs within 24-48 hours of therapy. Care must be taken to prevent the development of tumor lysis syndrome. Your health care provider will prescribe plenty of fluids to keep you hydrated. Drink at least two to three quarts of fluid every 24 hours, unless you are instructed otherwise. This is especially important starting 2 days before your first dose of venetoclax, on the day of your first dose, and any time your dose is increased. In some cases, your health care provider may prescribe other measures to lower your white blood count before therapy. Let your health care provider know immediately if you are unable to urinate. Your health care provider will monitor your progress.

Not all side effects are listed above. Some that are rare (occurring in less than 10% of patients) are not listed here. However, you should always inform your health care provider if you experience any unusual symptoms.

When to contact your doctor or health care provider:

Contact your health care provider immediately, day or night, if you should experience any of the following symptoms:

• Fever of 100.4° F (38° C) or higher, chills
• Sudden onset of shortness of breath, cough, difficulty breathing or wheezing
• New or worsening stomach pain, chills, fever, nausea, or vomiting
• Seizures, confusion, irregular heartbeat, dark or cloudy urine, extreme tiredness, muscle or joint pain

The following symptoms require medical attention, but are not an emergency. Contact your health care provider within 24 hours of noticing any of the following:

• Diarrhea (4-6 episodes in a 24-hour period)
• Nausea (interferes with ability to eat and unrelieved with prescribed medication).
• Unable to eat or drink for 24 hours or have signs of dehydration: tiredness, thirst, dry mouth, dark and decrease amount of urine, or dizziness
• Skin of the whites of your eyes turn yellow
• Decreased appetite
• Signs of an infection (cough with or without mucus, nasal drainage, burning with urination, redness or swelling, pus formation at the site of an injury or incision)
• Fatigue that interferes with activities of daily living (showering, bathing, making meals, etc.)
• Swelling
• Any signs of unusual bleeding (blood in the urine or stool, increased bruising, heavy menstrual bleeding)

Always inform your health care provider if you experience any unusual symptoms.

Precautions:

• Before starting venetoclax treatment, make sure you tell your doctor about any other medications you are taking (including prescription, over-the-counter, vitamins, herbal remedies, etc.)
• You should not drink grapefruit juice, eat grapefruit, Seville oranges (often used in marmalades), or starfruit while you are taking venetoclax. These foods may increase the amount of venetoclax in your blood.
• Do not receive any kind of immunization or vaccination without your doctor's approval while taking venetoclax.
• Inform your health care professional if you are pregnant or may be pregnant prior to starting this treatment. Venetoclax may be hazardous to the fetus. Women who are pregnant or become pregnant must be advised of the potential hazard to the fetus.
• For both men and women: Do not conceive a child (get pregnant) while taking venetoclaz. Barrier methods of contraception, such as condoms, are recommended during treatment and for at least 1 month after completing therapy. Discuss with your doctor when you may safely become pregnant or conceive a child after therapy.
• Venetoclax may cause fertility problems in males. This may affect your ability to father a child. Talk to your health care provider if you have concerns about fertility.
• Do not breast feed while taking this medication.

Self-Care Tips:

• Drink at least two to three quarts of fluid every 24 hours, unless you are instructed otherwise. This is especially important starting 2 days before your first dose of venetoclax, on the day of your first dose, and anytime your dose increased.
• If you should experience nausea, take anti-nausea medications as prescribed by your doctor, and eat small frequent meals. Sucking on lozenges and chewing gum may also help.
• Avoid sun exposure. Wear SPF 30 (or higher) sun block and protective clothing.
• In general, drinking alcoholic beverages should be kept to a minimum or avoided completely. You should discuss this with your doctor.
• Get plenty of rest.
• Maintain good nutrition.
• You may be at risk of infection so try to avoid crowds or people with colds, and report fever or any other signs of infection immediately to your healthcare provider.
• Wash your hands often. Do not touch your eyes or the inside of your nose unless you have just washed your hands and have not touched anything else in the meantime.
• Ask your doctor or nurse before scheduling dental appointment or procedures.
• Use an electric razor to minimize bleeding.
• If you experience symptoms or side effects, be sure to discuss them with your health care team. They can prescribe medications and/or offer other suggestions that are effective in managing such problems.

Monitoring and Testing:

you will be checked regularly by your health care professional while you are taking venetoclax to monitor side effects and check your response to therapy.

How Venetoclax Works:

Targeted therapy is the result of about 100 years of research dedicated to understanding the differences between cancer cells and normal cells. To date, cancer treatment has focused primarily on killing rapidly dividing cells because one feature of cancer cells is that they divide rapidly. Unfortunately, some of our normal cells divide rapidly too, causing multiple side effects.

Targeted therapy is about identifying other features of cancer cells. Scientists look for specific differences in the cancer cells and the normal cells. This information is used to create a targeted therapy to attack the cancer cells without damaging the normal cells, thus leading to fewer side effects. Each type of targeted therapy works a little bit differently but all interfere with the ability of the cancer cell to grow, divide, repair and/or communicate with other cells.

There are different types of targeted therapies, defined in three broad categories. Some targeted therapies focus on the internal components and function of the cancer cell. The targeted therapies use small molecules that can get into the cell and disrupt the function of the cells, causing them to die. There are several types of targeted therapy that focus on the inner parts of the cells. Other targeted therapies target receptors that are on the outside of the cell. Therapies that target receptors are also known as monoclonal antibodies. Antiangiogenesis inhibitors target the blood vessels that supply oxygen to the cells, ultimately causing the cells to starve.

Venetoclax is a small molecule type of targeted therapy. Venetoclax is a pill that promotes apoptosis, a common way by which cells die. It does this by binding to 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 chemotherapies. Venetoclax helps restore the process of apoptosis by binding directly to the BCL-2 protein, displacing pro-apoptotic proteins. Venetoclax blocks an important pathway that promotes cell survival in tumor cells that overexpress BCL-2, so venetoclax causes cells to die (pro-apoptotic).

Research continues to identify which cancers may be best treated with targeted therapies and to identify additional targets for more types of cancer.

Note: We strongly encourage you to talk with your health care professional about your specific medical condition and treatments. The information contained in this website is meant to be helpful and educational, but is not a substitute for medical advice.

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