Dasatinib

What is Dasatinib?

• Dasatinib (Sprycel) is a kinase inhibitor used to treat certain cases of chronic myelogenous leukemia (CML) and acute lymphoblastic leukemia (ALL).

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Dasatinib ball-and-stick

What are the uses of this medicine?

Dasatinib (Sprycel) is a prescription medicine used to treat:

• adults with newly diagnosed Philadelphia chromosome-positive (Ph+) chronic myeloid leukemia (CML) in chronic phase.
• adults with Ph+ CML who no longer benefit from, or did not tolerate, other treatment, including imatinib.
• adults with Ph+ acute lymphoblastic leukemia (Ph+ ALL) who no longer benefit from, or did not tolerate, other treatment.
• children 1 year of age and older with Ph+ CML in chronic phase.
• children 1 year of age and older with newly diagnosed Ph+ ALL in combination with chemotherapy.

How does this medicine work?

• Dasatinib is an orally available, small molecule inhibitor of the unique BCR-ABL tyrosine kinase receptor, which is the product of a fusion gene resulting from the translocation between chromosomes 9 and 22 that underlies the Philadelphia chromosome of chronic myelogenous leukemia (CML).
• The abnormal tyrosine kinase receptor is constitutively expressed and causes abnormal cell growth and proliferation.
• Inhibition of the enzyme can lead to dramatic reversal of progression of leukemia and is highly effective, although limited by the development of tumor resistance caused by mutations in the kinase.
• Dasatinib is actually a multi-kinase inhibitor and also has activity against scr, c-Kit and ephrin receptors, among others.

Who Should Not Use this medicine ?

• This medicine have no usage limitations.

What drug interactions can this medicine cause?

• Avoid concomitant use of strong CYP3A4 inhibitors. If concomitant administration of a strong CYP3A4 inhibitor cannot be avoided, consider a Sprycel dose reduction
• The coadministration of Sprycel with strong CYP3A inducers may decrease dasatinib concentrations. If concomitant administration of a strong CYP3A4 inducer cannot be avoided, consider a Sprycel dose increase.
• The coadministration of Sprycel with a gastric acid reducing agent may decrease the concentrations of dasatinib. Do not administer H2 antagonists or proton pump inhibitors with Sprycel. Consider the use of antacids in place of H2 antagonists or proton pump inhibitors. Administer the antacid at least 2 hours prior to or 2 hours after the dose of Sprycel. Avoid simultaneous administration of Sprycel with antacids.

Is this medicine FDA approved?

• Dasatanib received approval for use in the United States in 2006 and is one of five such specific inhibitors of BCR-ABL approved for clinical use, the others being imatinib [2001], nilotinib [2007], bosutinib [2012] and ponatinib [2012].

How should this medicine be used?

Recommended dosage: In Chronic phase CML in adults:

• 100 mg once daily.

In Accelerated phase CML, myeloid or lymphoid blast phase CML, or Ph+ ALL in adults:

• 140 mg once daily.

Chronic phase CML and ALL in pediatrics:

• starting dose based on body weight as below

Dosage of Sprycel for Pediatric Patients

Body Weight (kg)	Daily Dose (mg)
10 to less than 20	40mg
20 to less than 30	60 mg
30 to less than 45	70 mg
at least 45	100 mg

Administration:

• Take Sprycel 1 time a day.
• Take Sprycel with or without food, either in the morning or in the evening.
• Swallow Sprycel tablets whole. Do not crush, cut or chew the tablets.
• If your child cannot swallow tablets whole, talk with your healthcare provider.
• You should not drink grapefruit juice during treatment with Sprycel.
• If you miss a dose of Sprycel, take your next scheduled dose at your regular time. Do not take two doses at the same time.
• If you take too much Sprycel, call your healthcare provider or go to the nearest hospital emergency room right away.

What are the dosage forms and brand names of this medicine?

This medicine is available in fallowing doasage form:

• As Tablets: 20 mg, 50 mg, 70 mg, 80 mg, 100 mg, and 140 mg.

This medicine is available in fallowing brand namesː

• Sprycel

What side effects can this medication cause?

The most common side effects of Sprycel in adults and children receiving Sprycel alone include:

• diarrhea
• headache
• skin rash
• shortness of breath
• tiredness
• nausea
• muscle pain

The most common side effects of Sprycel in children receiving Sprycel with chemotherapy include:

• swelling, pain and redness of the lining of your mouth, throat, stomach and bowel (mucositis)
• low white blood cell counts with fever
• fever
• diarrhea
• nausea
• vomiting
• muscle pain
• stomach-area (abdominal) pain
• cough
• headache
• rash
• tiredness
• constipation
• abnormal heart rate
• high blood pressure (hypertension)
• swelling
• infections
• low blood pressure
• decreased appetite
• allergic reactions
• shortness of breath
• nose bleed
• numbness or tingling of your hands and feet
• feeling confused or disoriented

Sprycel may cause serious side effects, including:

• Low blood cell counts
• Bleeding problems
• Your body may hold too much fluid (fluid retention)
• Heart and blood vessel (cardiovascular) problems
• Pulmonary Arterial Hypertension (PAH)
• Severe skin reactions
• Tumor Lysis Syndrome (TLS)
• Slowing of growth and development in children

What special precautions should I follow?

• Treatment with Sprycel is associated with severe (NCI CTCAE Grade 3 or 4) thrombocytopenia, neutropenia, and anemia. Use caution if used concomitantly with medications that inhibit platelet function or anticoagulants. Monitor complete blood counts regularly. Transfuse and interrupt Sprycel when indicated.
• Sprycel can cause serious and fatal bleeding.
• Sprycel may cause fluid retention. Manage with supportive care measures and/or dose modification.
• Sprycel can cause cardiac dysfunction. Monitor patients for signs or symptoms and treat appropriately.
• Sprycel may increase the risk of developing pulmonary arterial hypertension (PAH) in adult and pediatric patients which may occur any time after initiation, including after more than 1 year of treatment. Consider baseline risk and evaluate patients for signs and symptoms of PAH during treatment. Stop Sprycel if PAH is confirmed.
• Sprycel may increase the risk of prolongation of QTc. Use Sprycel with caution in patients who have or may develop prolongation of the QT interval.
• Cases of severe mucocutaneous dermatologic reactions, including Stevens-Johnson syndrome and erythema multiforme, have been reported in patients treated with Sprycel.
• Tumor lysis syndrome has been reported in patients with resistance to prior imatinib therapy, primarily in advanced phase disease. Maintain adequate hydration and correct uric acid levels prior to initiating therapy with Sprycel.
• Based on limited human data, Sprycel can cause fetal harm when administered to a pregnant woman. Advise patients of reproductive potential of potential risk to fetus and to use effective contraception.
• In pediatric trials of Sprycel in chronic phase CML after at least 2 years of treatment, adverse reactions associated with bone growth and development. Epiphyses delayed fusion, osteopenia, growth retardation, and gynecomastia have been reported. Monitor bone growth and development in pediatric patients.

What to do in case of emergency/overdose?

Symptoms of overdosage may include:

• myelosuppression
• bleeding

Management of overdosage:

• Since Sprycel is associated with severe myelosuppression , monitor patients who ingest more than the recommended dosage closely for myelosuppression and give appropriate supportive treatment.

Can this medicine be used in pregnancy?

• Based on limited human data, Sprycel can cause fetal harm when administered to a pregnant woman.
• Adverse pharmacologic effects including hydrops fetalis, fetal leukopenia, and fetal thrombocytopenia have been reported with maternal exposure to Sprycel.

Can this medicine be used in children?

• The safety and effectiveness of Sprycel monotherapy have been demonstrated in pediatric patients with newly diagnosed chronic phase CML.
• The safety and effectiveness of Sprycel in combination with chemotherapy have been demonstrated in pediatric patients one year and over with newly diagnosed Ph+ ALL.
• It is not known if Sprycel is safe and effective in children under 1 year of age.

What are the active and inactive ingredients in this medicine?

• Active ingredient: dasatinib
• Inactive ingredients: lactose monohydrate, microcrystalline cellulose, croscarmellose sodium, hydroxypropyl cellulose, and magnesium stearate. The tablet coating consists of hypromellose, titanium dioxide, and polyethylene glycol.

Who manufactures and distributes this medicine?

• Distributed by: Bristol-Myers Squibb Company, Princeton, NJ USA

What should I know about storage and disposal of this medication?

• Store Sprycel 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 expired or unused Sprycel.
• Wear latex or nitrile gloves when handling tablets that have accidentally been crushed or broken.
• Females who are pregnant should not handle crushed or broken Sprycel tablets.

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• Dailymed label info on Dasatinib
• FDA Dasatinib

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