Dasatinib

Dasatinib is a prescription medication used to treat certain types of leukemia (cancers of the white blood cells). Dasatinib belongs to a group of drugs kinase inhibitors. It works by blocking the action of proteins that signal cancer cells to grow.

​This medication comes in tablet form. It is usually taken by mouth once a day, with or without food.

Common side effects of dasatinib are diarrhea, headache, and cough.

Leukemia is a cancer that forms in the blood cells. Some patients who have chronic myeloid leukemia have Philadelphia chromosome-positive chronic myelogenous leukemia (Ph+ CML). Other patients have Philadelphia chromosome-positive acute lymphoblastic leukemia (Ph+ ALL). The Philadelphia chromosome contains a gene that codes for a protein called Bcr-Abl. Bcr-Abl makes leukemia cells divide more rapidly. This gene can also make leukemia cells resistant to certain types of treatment.

Testing for the Philadelphia chromosome is done to see whether treatment with dasatinib is likely to be effective in treating chronic myelogenous leukemia (CML) or acute lymphoblastic leukemia (ALL). If testing is not done, treatment with dasatinib may not be effective.

Dasatinib is approved for treatment of Philadelphia chromosome-positive chronic myelogenous leukemia (Ph+ CML). It is also approved for Philadelphia chromosome-positive acute lymphoblastic leukemia (Ph+ ALL). It works by targeting the Bcr-Abl protein found on leukemia cells. By binding to the Bcr-Abl protein, dasatinib prevents the growth of cancer cells.

Dasatinib is a prescription medicine used to treat adults who have:

• newly diagnosed Philadelphia chromosome-positive (Ph+) chronic myeloid leukemia (CML) in chronic phase.
• Ph+ CML who no longer benefit from, or did not tolerate, other treatment, including Gleevec (imatinib mesylate).
• Philadelphia chromosome-positive acute lymphoblastic leukemia (Ph+ ALL) who no longer benefit from, or did not tolerate, other treatment.

Dasatinib is also used to treat children who have:

• Philadelphia chromosome-positive (Ph+) chronic myeloid leukemia (CML) in chronic phase.

This medication may be prescribed for other uses. Ask your doctor or pharmacist for more information.

Dasatinib may be found in some form under the following brand names:

• Sprycel

Dasatinib may cause serious side effects, see "Dasatinib Precautions" section.

Common side effects of dasatinib include:

• diarrhea
• headache
• cough
• skin rash
• fever
• nausea
• tiredness
• vomiting
• muscle pain
• weakness
• infections

Tell your healthcare provider if you have any side effect that bothers you or that does not go away.

These are not all of the possible side effects of dasatinib. For more information, ask your healthcare provider or pharmacist.

Tell your healthcare provider about all the medicines you take, including prescription and non-prescription medicines, vitamins, antacids, and herbal supplements.

Especially tell your healthcare provider if you take:

• medicines that increase the amount of dasatinib in your bloodstream, such as:
  • Nizoral (ketoconazole),
  • Sporanox (itraconazole),
  • Norvir (ritonavir),
  • Reyataz (atazanavir sulfate),
  • Crixivan (indinavir),
  • Viracept (nelfinavir),
  • Nefazodone (serzone, nefadar),
  • Invirase (saquinavir),
  • Ketek (telithromycin),
  • E-mycin (erythromycin),
  • Biaxin (clarithromycin).
• medicines that decrease the amount of dasatinib in your bloodstream, such as:
  • Decadron (dexamethasone),
  • Dilantin (phenytoin),
  • Tegretol (carbamazepine),
  • Rimactane (rifampin),
  • Luminal (phenobarbital).
• medicines whose blood levels might change by taking dasatinib, such as:
  • Sandimmune (cyclosporine),
  • Alfenta (alfentanil),
  • Fentanyl (fentanyl),
  • Orap (pimozide),
  • Rapamune (sirolimus),
  • Prograf (tacrolimus),
  • Ergomar (ergotamine).

Dasatinib is best absorbed from your stomach into your bloodstream in the presence of stomach acid. You should avoid taking medicines that reduce stomach acid, such as:

• Tagamet (cimetidine),
• Pepcid (famotidine),
• Zantac (ranitidine),
• Prilosec (omeprazole),
• Protonix (pantoprazole sodium),
• Nexium (esomeprazole),
• AcipHex (rabeprazole),
• Prevacid (lansoprazole).

Medicines that neutralize stomach acid, such as Maalox (aluminum hydroxide/magnesium hydroxide), Tums (calcium carbonate), or Rolaids (calcium carbonate and magnesia), may be taken up to 2 hours before or 2 hours after dasatinib.

Since dasatinib therapy may cause bleeding, tell your healthcare provider if you are using blood thinner medicine, such as Coumadin (warfarin sodium) or aspirin.

Know the medicines you take. Keep a list of your medicines and show it to your healthcare provider and pharmacist when you get a new medicine.

Dasatinib may cause serious side effects, including:

• Low Blood Cell Counts: Dasatinib may cause low red blood cell counts (anemia), low white blood cell counts (neutropenia), and low platelet counts (thrombocytopenia). Your healthcare provider will do blood tests to check your blood cell counts regularly during your treatment with dasatinib. Call your healthcare provider right away if you have a fever or any signs of an infection while taking dasatinib.
• Bleeding: Dasatinib may cause severe bleeding that can lead to death. Call your healthcare provider right away if you have:
  • unusual bleeding or bruising of your skin
  • bright red or dark tar-like stools
  • a decrease in your level of consciousness, headache, or change in speech.
• Your body may hold too much fluid (fluid retention): In severe cases, fluid may build up in the lining of your lungs, the sac around your heart, or your stomach cavity. Call your healthcare provider right away if you get any of these symptoms during treatment with dasatinib:
  • swelling all over your body
  • weight gain
  • shortness of breath and cough.
• Heart problems. Dasatinib may cause an abnormal heart rate, heart problems or a heart attack. Your healthcare provider will monitor the potassium and magnesium levels in your blood, and your heart function.
• Pulmonary Arterial Hypertension (PAH). Dasatinib may cause high blood pressure in the vessels of your lungs. PAH may happen at anytime during your treatment with dasatinib. Your healthcare provider should check your heart and lungs before and during your treatment with dasatinib. Call your healthcare provider right away if you have shortness of breath, tiredness, or swelling all over your body (fluid retention).
• Fetal harm. Dasatinib may cause harm to an unborn baby (fetus). It is recommended to avoid dasatinib during pregnancy.
• In children, Dasatinib may cause slow bone growth and lower bone densities. In addition, it may cause swelling or tenderness in the breast tissues (gynecomastia). It is recommended to monitor bone growth and development in children.

Grapefruit and grapefruit juice may interact with dasatinib and lead to potentially dangerous effects. Discuss the use of grapefruit products with your doctor.

Before you take dasatinib, tell your healthcare provider if you:

• have problems with your immune system
• have liver problems
• have heart problems
• are lactose intolerant
• have any other medical conditions
• are pregnant or planning to become pregnant.
• are breastfeeding or plan to breastfeed. 

Tell your healthcare provider about all the medicines you take, including prescription and non-prescription medicines, vitamins, antacids, and herbal supplements.

Tell your doctor if you are pregnant or plan to become pregnant.

The FDA categorizes medications based on safety for use during pregnancy. Five categories - A, B, C, D, and X, are used to classify the possible risks to an unborn baby when a medication is taken during pregnancy.

This medication falls into category D. Dasatinib may harm your unborn baby. Women should not become pregnant while taking dasatinib. Talk to your healthcare provider right away if you are pregnant or plan to become pregnant.

Tell  your healthcare provider if you are breastfeeding or plan to breastfeed. It is not known if dasatinib passes into your breast milk or if it can harm your baby. You and your healthcare provider should decide if you will take dasatinib or breastfeed. You should not do both.

Take dasatinib exactly as prescribed by your healthcare provider.

• Take dasatinib with or without food. Try to take dasatinib at the same time each day.
• Swallow dasatinib tablets whole. Do not break, cut, or crush the tablets.
• You should not drink grapefruit juice while taking dasatinib.
• Your healthcare provider may:
  • change your dose of dasatinib, or
  • tell you to temporarily stop taking dasatinib.
• Do not change your dose or stop taking dasatinib without first talking with your healthcare provider.
• If you miss a dose of dasatinib, take your next scheduled dose at its regular time. Do not take two doses at the same time. Call your healthcare provider or pharmacist if you are not sure what to do.
• If you take too much dasatinib, call your healthcare provider or go to the nearest hospital emergency room right away.

The recommended starting dosage of dasatinib for chronic phase CML is 100 mg taken by mouth once daily. The recommended starting dosage of dasatinib for accelerated phase CML, myeloid or lymphoid blast phase CML, or Ph+ ALL is 140 mg taken by mouth once daily. In children with chronic phase CML the starting dose is based on their body weight.

If you take too much dasatinib call your healthcare provider or local Poison Control Center, or seek emergency medical attention right away.

If dasatinib is administered by a healthcare provider in a medical setting, it is unlikely that an overdose will occur. However, if overdose is suspected, seek emergency medical attention.

• Store dasatinib at room temperature, between 68°F to 77°F (20°C to 25°C).
• Ask your healthcare provider or pharmacist about the right way to throw away outdated or unused dasatinib.
• Women who are pregnant should not handle crushed or broken dasatinib tablets.
• Keep dasatinib and all medicines out of the reach of children and pets.