- Targeted Drugs Ibrutinib(CAS:936563-96-1)
- Ibrutinib Mechanism of Action
- What Ibrutinib Is Used For
- Ibrutinib Benefits/Effects
- How Should We Take Ibrutinib
- Ibrutinib Side Effects
- Ibrutinib Storage
Targeted Drugs Ibrutinib(CAS:936563-96-1)
Many newer treatments for lymphoma are targeted drugs. Targeted drugs aim to kill the type of cell that has turned cancerous or stop signals that make cancerous cells grow or divide. In lymphoma, the type of cell that becomes cancerous is called a “lymphocyte” (a type of white blood cell that fights infection). There are several types of lymphocyte that can become cancerous. Ibrutinib targets B lymphocytes (B cells) and is therefore used to treat B-cell lymphomas.
Cells send and receive signals to other cells. Some of these signals keep cells alive and make them divide. There are lots of signalling pathways and signals are sent along one or more of these pathways. Ibrutinib is a cell signal blocker that targets a protein called ‘Bruton’ s tyrosine kinase’ (BTK). BTK is a part of a pathway that helps B cells to stay alive and divide. Blocking BTK can make B cells die or prevent them dividing. This treatment can therefore stop the spread of cancerous B cells.
Ibrutinib Mechanism of Action
Ibrutinib(936563-96-1) is not a chemotherapy drug but one of what are termed “targeted therapies.” Targeted therapy is the result of 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.
Ibrutinib inhibits the function of Bruton’s tyrosine kinase (BTK). BTK is a key signaling molecule of the B-cell receptor signaling complex that plays an important role in the survival of malignant B cells. Ibrutinib blocks signals that stimulate malignant B cells to grow and divide uncontrollably. 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 web site is meant to be helpful and educational, but is not a substitute for medical advice.
What Ibrutinib Is Used For
❶ To treat people with mantle cell lymphoma (MCL; a fast-growing cancer that begins in the cells of the immune system) who have already been treated with at least one other chemotherapy medication.
❷ To treat people with chronic lymphocytic leukemia (CLL; a type of cancer that begins in the white blood cells) and small lymphocytic lymphoma (SLL; a type of cancer that begins mostly in the lymph nodes).
❸ To treat people with Waldenstrom’s macroglobulinemia (WM; a slow-growing cancer that begins in certain white blood cells in your bone marrow).
❹ To treat people with marginal zone lymphoma (MZL; a slow growing cancer that begins in a type of white blood cells that normally fights infection) who have already been treated with a certain type of chemotherapy medication.
❺ To treat people with chronic graft vs host disease (cGVHD; a complication of hematopoietic stem-cell transplant [HSCT; a procedure that replaces diseased bone marrow with healthy bone marrow] that may start a while after the transplant and last for a long time) after being treated unsuccessfully with 1 or more medications.
Ibrutinib is in a class of medications called kinase inhibitors. It works by blocking the action of the abnormal protein that signals cancer cells to multiply. This helps stop the spread of cancer cells.
Ibrutinib is considered by many experts to be a ‘breakthrough treatment’ for some types of lymphoma. It gives higher response rates compared with other therapies for the same types of lymphoma. The main trials that led to approval of ibrutinib are briefly described below.
(1) Benefits in mantle cell lymphoma
Mantle cell lymphoma that has relapsed or not responded to first-line therapy can be difficult to treat. However, the main study in this area showed that more than two-thirds of 111 people treated with ibrutinib responded to the treatment (their lymphoma shrank or disappeared).
A second study in 280 people compared ibrutinib with another cancer drug, temsirolimus, in people with relapsed or refractory mantle cell lymphoma. People lived for an average of 15 months without their lymphoma getting worse when treated with ibrutinib compared with an average of 6 months when treated with temsirolimus.
(2) Benefits in chronic lymphocytic leukaemia (CLL)
Long-lasting responses have been seen in people with CLL treated with ibrutinib. In the main trial involving 391 people with relapsed or refractory CLL, ibrutinib was compared with ofatumumab, which is often used for people with CLL that has come back. One year after starting treatment, around 66 in 100 people taking ibrutinib had CLL that had stayed under control (this is called ‘progression-free survival’) compared with around 6 in 100 people treated with ofatumumab.
In a second study involving 269 people who hadn’ t yet received any treatment for their CLL, ibrutinib was compared with the chemotherapy drug chlorambucil. After 1.5 years of treatment, around 90 in 100 people taking ibrutinib had CLL that had stayed under control compared with around 52 in 100 people treated with chlorambucil.
Adding ibrutinib to bendamustine and rituximab for people with relapsed or refractory CLL was also effective in a study involving 578 people. The risk of CLL progressing was reduced by taking ibrutinib instead of a placebo (dummy treatment).
(3) Benefits in Waldenström’ s macroglobulinaemia (WM)
A high response rate has also been seen in people with WM – about 9 in 10 people with WM responded to ibrutinib treatment in a trial in 63 people. This trial was a significant breakthrough for WM as it is an uncommon form of lymphoma and it is therefore difficult to recruit enough people to take part in a clinical trial. This trial led to the approval of ibrutinib for WM in Europe.
How Should We Take Ibrutinib
You will be given ibrutinib as tablets. It may be given in combination with other targeted therapy drugs and chemotherapy. During treatment you usually see a cance¬r doctor, a cancer nurse or a specialist nurse, and a specialist pharmacist. This is who we mean when we mention doctor, nurse or pharmacist in this information.
Before or on the day of treatment, a nurse or person trained to take blood (phlebotomist) will take a blood sample from you. This is to check that your blood cells are at a safe level for you to have treatment.
You will see a doctor or nurse before you have treatment. They will ask you how you have been feeling. If your blood results are okay, the pharmacist will prepare your treatment. Your nurse will tell you when your treatment is likely to be ready.
The nurse or pharmacist will give you the ibrutinib tablets to take home. Always take them exactly as explained. This is important to make sure they work as well as possible for you. You may be given tablets of different strengths. You usually keep taking ibrutinib every day for as long as it keeps the cancer under control. Your nurse or pharmacist may also give you anti-sickness drugs and other medicines to take home. Take all your tablets exactly as they have been explained to you.
Warm Reminder on Self-Care:
♦ While taking ibrutinib, drink at least two to three quarts of fluid every 24 hours, unless you are instructed otherwise.
♦ Wash your hands often and after taking each dose of ibrutinib.
♦ 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 health care provider.
♦ To help treat/prevent mouth sores while taking ibrutinib, use a soft toothbrush, and rinse three times a day with 1 teaspoon of baking soda mixed with 8 ounces of water.
♦ Use an electric razor and a soft toothbrush to minimize bleeding.
♦ Avoid contact sports or activities that could cause injury.
♦ To reduce nausea, take anti-nausea medications as prescribed by your doctor, and eat small, frequent meals while taking ibrutinib.
♦ Eat foods that may help reduce diarrhea-see Managing Side Effects – Diarrhea
♦ Follow regimen of anti-diarrhea medication as prescribed by your health care professional.
♦ Avoid sun exposure. Wear SPF 15 (or higher) sun block and protective clothing. Ibrutinib may make you more sensitive to the sun and you may sunburn more easily.
♦ In general, drinking alcoholic beverages should be kept to a minimum or avoided completely while you are taking ibrutinib. You should discuss this with your doctor.
♦ Get plenty of rest.
♦ Maintain good nutrition while being treated with ibrutinib.
♦ If you experience symptoms or side effects while being treated with ibrutinib, 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.
Ibrutinib Side Effects
Get emergency medical help if you have signs of an allergic reaction: hives; difficult breathing; swelling of your face, lips, tongue, or throat.
Stop using ibrutinib and call your doctor at once if you have:
♦ Signs of infection–fever, chills, weakness, mouth sores, cough with mucus, trouble breathing;
♦ Signs of bleeding inside your body–dizziness, weakness, confusion, problems with speech, prolonged headache, black or bloody stools, pink or brown urine, or coughing up blood or vomit that looks like coffee grounds;
♦ Severe or ongoing diarrhea;
♦ Chest pain, pounding heartbeats or fluttering in your chest, feeling like you might pass out;
♦ Severe headache, blurred vision, pounding in your neck or ears;
♦ Easy bruising, unusual bleeding, purple or red spots under your skin;
♦ Pale skin, cold hands and feet;
♦ Kidney problems–little or no urinating, swelling in your feet or ankles; or
♦ Signs of tumor cell breakdown–confusion, weakness, muscle cramps, nausea, vomiting, fast or slow heart rate, decreased urination, tingling in your hands and feet or around your mouth.
Common side effects may include:
♦ Diarrhea, nausea;
♦ Fever, cough, trouble breathing;
♦ Blisters or ulcers in your mouth;
♦ Feeling tired;
♦ Bruising, rash; or
♦ Muscle pain, bone pain.
This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.
Keep Ibrutinib in the container it came in, tightly closed, and out of reach of children. Store it at room temperature and away from light, excess heat and moisture not in the bathroom.
Unneeded Ibrutinib should be disposed of in special ways to ensure that pets, children, and other people cannot consume them. However, you should not flush this Ibrutinib down the toilet. Instead, the best way to dispose of your medication is through a medicine take-back program. Talk to your pharmacist or contact your local garbage/recycling department to learn about take-back programs in your community. See the FDA’s Safe Disposal of
It is important to keep all medication out of sight and reach of children as many containers (such as weekly pill minders and those for eye drops, creams, patches, and inhalers) are not child-resistant and young children can open them easily. To protect young children from poisoning, always lock safety caps and immediately place the medication in a safe location – one that is up and away and out of their sight and reach.
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