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Class: Biological Therapy
Generic Name: Ponatinib
Trade Name: Iclusig®

How is Iclusig used? Iclusig is indicated for adult patients with:

· Chronic phase chronic myeloid leukemia (CML) who have been treated with at least two prior kinase inhibitors and experienced resistance or intolerance to treatment

· Accelerated phase or blast phase CML or Philadelphia chromosome positive acute lymphoblastic leukemia (Ph+ ALL) whose cancer has no other kinase inhibitors indicated

· T315I-positive CML (chronic, accelerated or blast phase) or T315I-positive PH+ ALL

Iclusig was approved with a black box warning disclosing the following risk:

· Blood clots or blockage in arteries or veins which may lead to heart attack, stroke or death; can prevent proper blood flow to your heart, brain, intestines, legs, eyes and other parts of your body; may result in requiring emergency surgery or treatment. The risk of blood clots or blockage has been experienced in patients with and without cardiovascular risk factors including patients under the age of 50.

· Heart problems including heart failure which can lead to death; Iclusig can also cause irregular heartbeats (slow or fast) and heart attack.

· Liver problems including liver failure which could lead to death.

What is the mechanism of action? Iclusig is a tyrosine kinase inhibitor (TKI). Most often, resistance to tyrosine kinase inhibitors (TKI) used to treat chronic myeloid leukemia (CML) is caused by changes (mutations) in the part of the BCR-ABL gene that makes the BCR-ABL protein. Mutations change the shape of the BCR-ABL protein so that certain TKIs can no longer bind to it effectively. This can cause the TKI to stop working. Because each TKI drug works slightly differently, one TKI drug may be able to overcome the resistance from the mutation that another TKI cannot. Iclusig is a multi-targeted tyrosine-kinase inhibitor that primarily functions as a BCR-ABL inhibitor. It was designed to overcome the T3151 mutation, which is notoriously resistant and difficult to treat.

Switching to a different TKI may result in a treatment response after CML stops responding or becomes resistant to a prior TKI.

How is Iclusig given (administered)? Iclusig is administered orally once daily, with or without food. The dose depends on the CML phase, and also depends on the health of the patient.

How are patients monitored? Patients will have scheduled meetings with their healthcare provider while they are being treated with Iclusig. Typically, blood will be drawn to check levels of blood cells and to monitor functions of some organ systems such as the pancreas and liver. Your healthcare provider will also check you for heart problems during your treatment with Iclusig. Patients may also undergo physical examinations, scans or other measures to assess side effects and response to therapy.

What are the most common side effects of treatment with Iclusig?

  • Rash
  • Joint Pain
  • Stomach-area pain
  • Headache
  • Constipation
  • Dry skin
  • High blood pressure
  • Tiredness
  • Fluid retention and swelling
  • Fever
  • Nausea
  • Inflammation of the pancreas
  • Increase in lipase levels
  • Bleeding
  • Anemia
  • Liver problems
  • Blood clots or blockages in blood vessels
  • Low blood platelet counts
  • Low blood levels of white blood cells

This is not a complete list of side effects. Some patients may experience other side effects that are not listed here and this drug was approved with a black box warning highlighting risk of very serious side effects.

Some side effects may require medical attention. Other side effects do not require medical attention and may go away during treatment. Patients should check with their physician about any side effects that continue or are bothersome.

What can patients do to help alleviate or prevent discomfort and side effects?

  • Pay careful attention to the physician’s instructions and inform the physician of any and all side effects. Seek immediate medical attention right away for symptoms of blood clots, blood vessel blockages, heart problems and/or liver problems.
  • Maintain adequate rest and nutrition.
  • If possible, avoid large crowds or people who are sick or not feeling well
  • Wash hands often to reduce the risk of infection.
  • Avoid activities that may cause injury or bruising.
  • Drink plenty of water.
  • Avoid grapefruit or grapefruit juice during treatment with Iclusig.

Are there any special precautions patients should be aware of before starting treatment?

  • Patients should inform their physician of any other medication they are taking (whether prescription or over-the-counter, including vitamins, herbs, etc.) as they may interact with treatment.
  • Patients should inform their physician if they are pregnant, breastfeeding or planning a family in the near future. You should not become pregnant during treatment with Iclusig. It is important to use some kind of birth control while undergoing treatment. It is not known if Iclusig passes into breast milk; avoid breastfeeding during treatment and for 6 days after your last dose.
  • Patients should inform their physician about all medical conditions, including history of blood clots, heart problems, irregular heartbeat, liver problems, history of pancreatitis, diabetes, high cholesterol, high blood pressure or bleeding problems.
  • Patients should inform their physician if they are lactose intolerant as Iclusig tablets contain lactose.
  • Patients should inform their physician if they have had surgery recently or plan to have surgery.

When should patients notify their physician?

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Tell your doctor if you experience any side effect that bothers you or does not go away. Get medical help right away if you experience:

· Symptoms of blood clots or blockage in your blood vessels including: chest pain or pressure; pain in arms, legs, back, neck or jaw; shortness of breath, numbness/weakness on one side of the body; leg swelling; trouble talking; headache; dizziness; severe stomach pain; decreased or loss of vision.

· Symptoms of heart problems including: shortness of breath, chest pain, fast or irregular heartbeats, dizziness, or feel faint.

· Symptoms of liver problems including: yellowing of skin or whites of the eyes, dark “tea-colored” urine, sleepiness, loss of appetite, bleeding or bruising.

Call your doctor right away if you experience:

· Symptoms of high blood pressure including confusion, headaches, dizziness, chest pain or shortness of breath.

· Symptoms of inflammation of the pancreas including sudden stomach-area pain or discomfort, nausea and vomiting.

· Symptoms of neuropathy including muscle weakness, tingling, burning, pain, discomfort/loss of feeling in hands or feet, double vision, eyesight problems, drooping of the face or eyelids, change in taste.

· Symptoms of eye problems.

· Symptoms of serious bleeding.

· Symptoms of fluid retention including swelling, weight gain, shortness of breath and cough.

· Symptoms of irregular heartbeat.

· Symptoms of low blood cell counts including a fever or signs of infection.

· Symptoms of tumor lysis syndrome.

· Symptoms of posterior leukoencephalopathy syndrome including headaches, seizures, confusion, changes in vision or problems thinking.

· Symptoms of wound healing problems.

· Symptoms of a tear in your stomach or intestinal wall including sever pain in your abdomen, abdominal swelling, or high fever.

What is a package insert?
A package insert is required by the FDA and contains a summary of the essential scientific information needed for the safe and effective use of the drug for healthcare providers and consumers. A package insert typically includes information regarding specific indications, administration schedules, dosing, side effects, contraindications, results from some clinical trials, chemical structure, pharmacokinetics and metabolism of the specific drug. By carefully reviewing the package insert, you will get the most complete and current information about how to safely use this drug. If you do not have the package insert for the drug you are using, your pharmacist or physician may be able to provide you with a copy.

Important Limitations of Use
The information provided above on the drug you have selected is provided for your information only and is not a substitute for consultation with an appropriate medical doctor. We are providing this information solely as a courtesy and, as such, it is in no way a recommendation as to the safety, efficacy or appropriateness of any particular drug, regimen, dosing schedule for any particular cancer, condition or patient nor is it in any way to be considered medical advice. Patients should discuss the appropriateness of a particular drug or chemotherapy regimen with their physician.

As with any printed reference, the use of particular drugs, regimens and drug dosages may become out-of-date over time, since new information may have been published and become generally accepted after the latest update to this printed information. Please keep in mind that health care professionals are fully responsible for practicing within current standards, avoiding use of outdated regimens, employing good clinical judgment in selecting drugs and/or regimens, in calculating doses for individual patients, and verifying all dosage calculations.