Sprycel 70mg Tablets
It is used to treat a type of leukemia. It may be given to you for other reasons. Talk with the doctor.
Drug Class
Antineoplastic agent
Pharmacologic Class
Tyrosine Kinase Inhibitor (TKI); BCR-ABL inhibitor
Pregnancy Category
D
FDA Approved
Jun 2006
DEA Schedule
Not Controlled
Overview
What is this medicine?
Dasatinib is a medicine used to treat certain types of leukemia (blood cancer). It works by blocking specific proteins in cancer cells that help them grow and multiply. This helps to stop the growth of cancer cells.
How to Use This Medicine
Taking Your Medication Correctly
To get the most benefit from your medication, follow your doctor's instructions carefully. Read all the information provided with your prescription and follow the instructions closely.
Take your medication at the same time every day.
You can take it with or without food.
Swallow the tablet whole - do not chew, break, or crush it. If you have difficulty swallowing, consult your doctor.
Continue taking your medication as directed by your doctor or healthcare provider, even if you start feeling well.
Handling Your Medication
When handling your medication, take special precautions. Consult your doctor or pharmacist for guidance on how to handle it safely.
Avoid taking antacids within 2 hours before or 2 hours after taking your medication.
Storing and Disposing of Your Medication
To maintain the quality and effectiveness of your medication:
Store it at room temperature in a dry place, avoiding the bathroom.
* Some brands of this medication require storage in the original container. Do not remove the anti-moisture cube or packet. If you are unsure, consult your doctor or pharmacist.
Missing a Dose
If you miss a dose, skip it and resume your regular dosing schedule. Do not take two doses at the same time or take extra doses to make up for the missed one.
To get the most benefit from your medication, follow your doctor's instructions carefully. Read all the information provided with your prescription and follow the instructions closely.
Take your medication at the same time every day.
You can take it with or without food.
Swallow the tablet whole - do not chew, break, or crush it. If you have difficulty swallowing, consult your doctor.
Continue taking your medication as directed by your doctor or healthcare provider, even if you start feeling well.
Handling Your Medication
When handling your medication, take special precautions. Consult your doctor or pharmacist for guidance on how to handle it safely.
Avoid taking antacids within 2 hours before or 2 hours after taking your medication.
Storing and Disposing of Your Medication
To maintain the quality and effectiveness of your medication:
Store it at room temperature in a dry place, avoiding the bathroom.
* Some brands of this medication require storage in the original container. Do not remove the anti-moisture cube or packet. If you are unsure, consult your doctor or pharmacist.
Missing a Dose
If you miss a dose, skip it and resume your regular dosing schedule. Do not take two doses at the same time or take extra doses to make up for the missed one.
Lifestyle & Tips
- Take dasatinib at the same time each day, with or without food, but be consistent.
- Swallow tablets whole; do not crush, cut, or chew them.
- Avoid grapefruit and grapefruit juice during treatment, as they can increase the amount of dasatinib in your body.
- Avoid antacids, H2 blockers (like famotidine, ranitidine), and proton pump inhibitors (like omeprazole, pantoprazole) as they can reduce the absorption of dasatinib. If you need an antacid, take it at least 2 hours before or 2 hours after dasatinib.
- Report any signs of infection (fever, chills) or unusual bleeding/bruising immediately.
- Monitor for swelling in your ankles, legs, or abdomen, and report any sudden weight gain or shortness of breath.
- Use effective contraception during treatment and for a period after, as dasatinib can harm an unborn baby.
Available Forms & Alternatives
Available Strengths:
Generic Alternatives:
Dosing & Administration
Adult Dosing
Standard Dose:
For newly diagnosed chronic phase CML: 100 mg orally once daily. For chronic phase CML (resistant or intolerant to prior therapy): 100 mg orally once daily. For accelerated phase, myeloid or lymphoid blast phase CML, or Philadelphia chromosome-positive acute lymphoblastic leukemia (Ph+ ALL): 140 mg orally once daily. The 70mg tablet strength is commonly used for dose reductions due to toxicity or for specific maintenance regimens.
Condition-Specific Dosing:
Chronic Phase CML:
100 mg orally once daily
Advanced Phase CML (Accelerated, Myeloid/Lymphoid Blast) or Ph+ ALL:
140 mg orally once daily
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established
Child:
For pediatric patients with chronic phase CML: 60 mg/m² orally once daily (max 100 mg/day). For pediatric patients with advanced phase CML or Ph+ ALL: 90 mg/m² orally once daily (max 140 mg/day). Dosing is based on body surface area (BSA).
Adolescent:
For pediatric patients with chronic phase CML: 60 mg/m² orally once daily (max 100 mg/day). For pediatric patients with advanced phase CML or Ph+ ALL: 90 mg/m² orally once daily (max 140 mg/day). Dosing is based on body surface area (BSA).
Dose Adjustments
Renal Impairment:
Mild:
No dose adjustment required.
Moderate:
No dose adjustment required.
Severe:
No dose adjustment required. Use with caution in patients with severe renal impairment.
Dialysis:
No specific recommendations; Dasatinib is not significantly cleared by dialysis. Use with caution.
Hepatic Impairment:
Mild:
Child-Pugh A: No dose adjustment required.
Moderate:
Child-Pugh B: Reduce initial dose by 50% (e.g., 50 mg daily for CML-CP, 70 mg daily for advanced CML/Ph+ ALL).
Severe:
Child-Pugh C: Reduce initial dose by 50% (e.g., 50 mg daily for CML-CP, 70 mg daily for advanced CML/Ph+ ALL).
Pharmacology
Mechanism of Action
Dasatinib is a small-molecule tyrosine kinase inhibitor that inhibits multiple tyrosine kinases, including BCR-ABL, SRC family kinases (SRC, LCK, YES, FYN), c-KIT, EPHA2, and PDGFRβ. It binds to both the active and inactive conformations of the BCR-ABL kinase, making it effective against imatinib-resistant CML, including those with BCR-ABL mutations (except T315I). By inhibiting these kinases, dasatinib blocks proliferation and induces apoptosis in CML and Ph+ ALL cell lines overexpressing BCR-ABL.
Pharmacokinetics
Absorption:
Bioavailability:
Not precisely determined, but rapidly absorbed.
Tmax:
0.5 to 6 hours (median 0.5-2 hours)
FoodEffect:
High-fat meals may decrease Cmax and AUC. Can be taken with or without food, but consistency is recommended. Gastric pH affects solubility; increased pH (e.g., by PPIs, H2RAs, antacids) significantly decreases solubility and absorption.
Distribution:
Vd:
2505 L (suggests extensive extravascular distribution)
ProteinBinding:
Approximately 96% (primarily to albumin and alpha-1 acid glycoprotein)
CnssPenetration:
Limited, but detectable concentrations in CSF have been observed, particularly in patients with meningeal leukemia.
Elimination:
HalfLife:
3-5 hours (terminal half-life)
Clearance:
Not available (systemic clearance is high)
ExcretionRoute:
Mainly fecal (85%), with minor renal excretion (4%).
Unchanged:
Less than 0.1% excreted unchanged in urine, 19% in feces.
Pharmacodynamics
OnsetOfAction:
Rapid, within hours of first dose (based on kinase inhibition). Clinical response (hematologic) can be seen within weeks.
PeakEffect:
Steady-state concentrations are reached within 4 days of once-daily dosing.
DurationOfAction:
Sustained kinase inhibition throughout the dosing interval due to irreversible binding or prolonged cellular effects.
Safety & Warnings
BLACK BOX WARNING
Dasatinib can cause myelosuppression (neutropenia, thrombocytopenia, and anemia). Complete blood counts should be performed every 2 weeks for the first 3 months and then monthly or as clinically indicated. Dasatinib has been associated with fluid retention, including pleural effusion, pericardial effusion, and ascites. Severe fluid retention may require dose interruption or reduction, or diuretics. Pulmonary arterial hypertension (PAH) has been reported in patients treated with dasatinib. Patients should be evaluated for signs and symptoms of underlying cardiopulmonary disease prior to initiation of dasatinib and monitored for symptoms of PAH during treatment.
Side Effects
Important Side Effects to Report to Your Doctor Immediately
Although rare, some people may experience severe and potentially life-threatening side effects while taking this medication. If you experience any of the following symptoms, seek medical attention right away:
Allergic reactions: Rash, hives, itching, red, swollen, blistered, or peeling skin with or without fever, wheezing, tightness in the chest or throat, trouble breathing, swallowing, or talking, unusual hoarseness, or swelling of the mouth, face, lips, tongue, or throat.
Infections: Fever, chills, severe sore throat, ear or sinus pain, cough, increased or changed sputum production, painful urination, mouth sores, or wounds that won't heal.
Bleeding: Vomiting or coughing up blood, coffee ground-like vomit, blood in the urine, black, red, or tarry stools, bleeding gums, abnormal vaginal bleeding, unexplained bruises or bruises that get bigger, or uncontrollable bleeding.
Electrolyte problems: Mood changes, confusion, muscle pain, cramps, or spasms, weakness, shakiness, balance changes, abnormal heartbeat, seizures, loss of appetite, or severe nausea and vomiting.
High or low blood pressure: Severe headache or dizziness, fainting, or changes in vision.
Numbness or tingling: In the hands or feet.
Seizures: Convulsions or fits.
Fluid retention: Swelling, weight gain, or breathing difficulties.
Severe skin reactions: Stevens-Johnson syndrome (SJS), toxic epidermal necrolysis (TEN), or other severe skin reactions, which can be life-threatening. Symptoms include red, swollen, blistered, or peeling skin, skin irritation with or without fever, red or irritated eyes, or sores in the mouth, throat, nose, or eyes.
Tumor lysis syndrome (TLS): A potentially life-threatening condition that can occur in cancer patients. Symptoms include fast or abnormal heartbeat, fainting, difficulty urinating, muscle weakness or cramps, nausea, vomiting, diarrhea, loss of appetite, or feeling sluggish.
Heart problems: Abnormal heartbeat (such as prolonged QT interval), heart attack, or small strokes (TIAs). Symptoms include chest pain, fast or abnormal heartbeat, shortness of breath, sudden weight gain, swelling in the arms or legs, weakness on one side of the body, confusion, slurred speech, balance changes, drooping on one side of the face, vision changes, severe dizziness, or fainting.
Liver problems: Dark urine, fatigue, decreased appetite, nausea, stomach pain, light-colored stools, vomiting, or yellow skin and eyes.
Other Possible Side Effects
Most people experience no side effects or only mild side effects while taking this medication. However, if you experience any of the following side effects, consult your doctor:
Constipation
Stomach pain
Headache
Fatigue or weakness
Muscle or joint pain
Pain in the arms or legs
* Diarrhea, nausea, vomiting, or decreased appetite (common side effects that can be managed with your doctor's guidance)
If any of these side effects bother you, don't improve, or are severe, seek medical attention.
Reporting Side Effects
If you have questions about side effects or want to report a side effect, call your doctor or the FDA at 1-800-332-1088. You can also report side effects online at https://www.fda.gov/medwatch.
Although rare, some people may experience severe and potentially life-threatening side effects while taking this medication. If you experience any of the following symptoms, seek medical attention right away:
Allergic reactions: Rash, hives, itching, red, swollen, blistered, or peeling skin with or without fever, wheezing, tightness in the chest or throat, trouble breathing, swallowing, or talking, unusual hoarseness, or swelling of the mouth, face, lips, tongue, or throat.
Infections: Fever, chills, severe sore throat, ear or sinus pain, cough, increased or changed sputum production, painful urination, mouth sores, or wounds that won't heal.
Bleeding: Vomiting or coughing up blood, coffee ground-like vomit, blood in the urine, black, red, or tarry stools, bleeding gums, abnormal vaginal bleeding, unexplained bruises or bruises that get bigger, or uncontrollable bleeding.
Electrolyte problems: Mood changes, confusion, muscle pain, cramps, or spasms, weakness, shakiness, balance changes, abnormal heartbeat, seizures, loss of appetite, or severe nausea and vomiting.
High or low blood pressure: Severe headache or dizziness, fainting, or changes in vision.
Numbness or tingling: In the hands or feet.
Seizures: Convulsions or fits.
Fluid retention: Swelling, weight gain, or breathing difficulties.
Severe skin reactions: Stevens-Johnson syndrome (SJS), toxic epidermal necrolysis (TEN), or other severe skin reactions, which can be life-threatening. Symptoms include red, swollen, blistered, or peeling skin, skin irritation with or without fever, red or irritated eyes, or sores in the mouth, throat, nose, or eyes.
Tumor lysis syndrome (TLS): A potentially life-threatening condition that can occur in cancer patients. Symptoms include fast or abnormal heartbeat, fainting, difficulty urinating, muscle weakness or cramps, nausea, vomiting, diarrhea, loss of appetite, or feeling sluggish.
Heart problems: Abnormal heartbeat (such as prolonged QT interval), heart attack, or small strokes (TIAs). Symptoms include chest pain, fast or abnormal heartbeat, shortness of breath, sudden weight gain, swelling in the arms or legs, weakness on one side of the body, confusion, slurred speech, balance changes, drooping on one side of the face, vision changes, severe dizziness, or fainting.
Liver problems: Dark urine, fatigue, decreased appetite, nausea, stomach pain, light-colored stools, vomiting, or yellow skin and eyes.
Other Possible Side Effects
Most people experience no side effects or only mild side effects while taking this medication. However, if you experience any of the following side effects, consult your doctor:
Constipation
Stomach pain
Headache
Fatigue or weakness
Muscle or joint pain
Pain in the arms or legs
* Diarrhea, nausea, vomiting, or decreased appetite (common side effects that can be managed with your doctor's guidance)
If any of these side effects bother you, don't improve, or are severe, seek medical attention.
Reporting Side Effects
If you have questions about side effects or want to report a side effect, call your doctor or the FDA at 1-800-332-1088. You can also report side effects online at https://www.fda.gov/medwatch.
Seek Immediate Medical Attention If You Experience:
- Fever of 100.4°F (38°C) or higher, or other signs of infection
- Unusual bleeding (e.g., nosebleeds, bleeding gums, blood in urine or stool) or bruising
- Severe fatigue or weakness
- Shortness of breath, especially new or worsening
- Cough, especially new or worsening
- Chest pain or discomfort
- Swelling in the ankles, legs, feet, or abdomen
- Rapid weight gain
- Dizziness or lightheadedness
- Yellowing of the skin or eyes (jaundice)
- Dark urine or pale stools
- Severe nausea, vomiting, or diarrhea
- Severe skin rash
Before Using This Medicine
Before Taking This Medication: Important Information to Share with Your Doctor
It is essential to inform your doctor about the following:
Any allergies you have, including allergies to this medication, its components, or other substances. Be sure to describe the symptoms you experienced.
Certain health conditions, such as low potassium or magnesium levels.
If you are taking any of the following medications:
+ Cimetidine
+ Dexlansoprazole
+ Esomeprazole
+ Famotidine
+ Lansoprazole
+ Nizatidine
+ Omeprazole
+ Pantoprazole
+ Rabeprazole
+ Ranitidine
Any other medications you are taking, including prescription and over-the-counter (OTC) drugs, natural products, and vitamins. This medication can interact with various drugs, such as those used to treat HIV, infections, or seizures.
* If you are breastfeeding. You should not breastfeed while taking this medication and for 2 weeks after your last dose.
Please note that this is not an exhaustive list of all potential interactions. To ensure your safety, it is crucial to inform your doctor and pharmacist about all your medications and health conditions. Before starting, stopping, or changing the dose of any medication, consult with your doctor to verify that it is safe to take this medication in combination with your other medications and health conditions.
It is essential to inform your doctor about the following:
Any allergies you have, including allergies to this medication, its components, or other substances. Be sure to describe the symptoms you experienced.
Certain health conditions, such as low potassium or magnesium levels.
If you are taking any of the following medications:
+ Cimetidine
+ Dexlansoprazole
+ Esomeprazole
+ Famotidine
+ Lansoprazole
+ Nizatidine
+ Omeprazole
+ Pantoprazole
+ Rabeprazole
+ Ranitidine
Any other medications you are taking, including prescription and over-the-counter (OTC) drugs, natural products, and vitamins. This medication can interact with various drugs, such as those used to treat HIV, infections, or seizures.
* If you are breastfeeding. You should not breastfeed while taking this medication and for 2 weeks after your last dose.
Please note that this is not an exhaustive list of all potential interactions. To ensure your safety, it is crucial to inform your doctor and pharmacist about all your medications and health conditions. Before starting, stopping, or changing the dose of any medication, consult with your doctor to verify that it is safe to take this medication in combination with your other medications and health conditions.
Precautions & Cautions
Important Information for Patients Taking This Medication
It is crucial that you inform all your healthcare providers, including doctors, nurses, pharmacists, and dentists, that you are taking this drug. Regular monitoring of your blood work, heart function, and lung function is necessary, as directed by your doctor.
If you follow a lactose-free diet, consult with your doctor before taking this medication, as some products may contain lactose. Additionally, avoid consuming grapefruit and grapefruit juice while taking this drug.
Blood-Related Risks
This medication may suppress the bone marrow's ability to produce essential blood cells, increasing the risk of bleeding problems, infections, or anemia. If you have concerns, discuss them with your doctor. To minimize the risk of infection, practice good hygiene by washing your hands frequently and avoid close contact with individuals who have infections, colds, or flu.
You may also experience easier bleeding, so it is essential to be cautious and avoid injuries. Use a soft toothbrush and an electric razor to reduce the risk of bleeding. Although rare, some bleeding problems can be life-threatening.
Respiratory Risks
This drug may increase the risk of developing a severe lung condition called pulmonary arterial hypertension, which can occur at any time during treatment, even after more than a year. Discuss this risk with your doctor.
Special Considerations
If you are 65 years or older, use this medication with caution, as you may be more susceptible to side effects.
This drug has been shown to cause fertility problems in animal studies, which may affect your ability to conceive or father a child. If you are pregnant or may become pregnant, it is essential to handle this medication carefully. Pregnant individuals should not handle crushed or broken tablets, and if accidental contact occurs, wash the area with soap and water immediately.
Pregnancy and Contraception
This medication may harm the unborn baby if taken during pregnancy. If you may become pregnant, use effective birth control while taking this drug and for 30 days after your last dose, unless otherwise instructed by your doctor. If you become pregnant, notify your doctor promptly.
If your partner may become pregnant, use birth control while taking this medication and for 30 days after your last dose, unless otherwise instructed by your doctor. If your partner becomes pregnant, inform the doctor immediately.
Pediatric Patients
If you are giving this medication to a child and their weight changes, consult with your doctor, as the dosage may need to be adjusted. This drug may affect growth in children and teenagers, so regular growth checks may be necessary. Discuss this with your doctor.
It is crucial that you inform all your healthcare providers, including doctors, nurses, pharmacists, and dentists, that you are taking this drug. Regular monitoring of your blood work, heart function, and lung function is necessary, as directed by your doctor.
If you follow a lactose-free diet, consult with your doctor before taking this medication, as some products may contain lactose. Additionally, avoid consuming grapefruit and grapefruit juice while taking this drug.
Blood-Related Risks
This medication may suppress the bone marrow's ability to produce essential blood cells, increasing the risk of bleeding problems, infections, or anemia. If you have concerns, discuss them with your doctor. To minimize the risk of infection, practice good hygiene by washing your hands frequently and avoid close contact with individuals who have infections, colds, or flu.
You may also experience easier bleeding, so it is essential to be cautious and avoid injuries. Use a soft toothbrush and an electric razor to reduce the risk of bleeding. Although rare, some bleeding problems can be life-threatening.
Respiratory Risks
This drug may increase the risk of developing a severe lung condition called pulmonary arterial hypertension, which can occur at any time during treatment, even after more than a year. Discuss this risk with your doctor.
Special Considerations
If you are 65 years or older, use this medication with caution, as you may be more susceptible to side effects.
This drug has been shown to cause fertility problems in animal studies, which may affect your ability to conceive or father a child. If you are pregnant or may become pregnant, it is essential to handle this medication carefully. Pregnant individuals should not handle crushed or broken tablets, and if accidental contact occurs, wash the area with soap and water immediately.
Pregnancy and Contraception
This medication may harm the unborn baby if taken during pregnancy. If you may become pregnant, use effective birth control while taking this drug and for 30 days after your last dose, unless otherwise instructed by your doctor. If you become pregnant, notify your doctor promptly.
If your partner may become pregnant, use birth control while taking this medication and for 30 days after your last dose, unless otherwise instructed by your doctor. If your partner becomes pregnant, inform the doctor immediately.
Pediatric Patients
If you are giving this medication to a child and their weight changes, consult with your doctor, as the dosage may need to be adjusted. This drug may affect growth in children and teenagers, so regular growth checks may be necessary. Discuss this with your doctor.
Overdose Information
Overdose Symptoms:
- Myelosuppression (severe neutropenia, thrombocytopenia)
- Fluid retention (pleural effusion, pericardial effusion)
- Hepatotoxicity
What to Do:
There is no specific antidote for dasatinib overdose. Management should consist of general supportive measures and treatment of symptoms. Call 1-800-222-1222 (Poison Control Center) immediately.
Drug Interactions
Contraindicated Interactions
- Strong CYP3A4 inducers (e.g., Rifampin, Phenytoin, Carbamazepine, Phenobarbital, St. John's Wort)
- Proton Pump Inhibitors (PPIs) (e.g., Omeprazole, Esomeprazole, Lansoprazole, Pantoprazole, Rabeprazole)
Major Interactions
- Strong CYP3A4 inhibitors (e.g., Ketoconazole, Itraconazole, Clarithromycin, Ritonavir, Atazanavir, Indinavir, Nelfinavir, Saquinavir, Telithromycin, Voriconazole, Grapefruit juice) - significant increase in dasatinib exposure.
- H2-receptor antagonists (e.g., Famotidine, Ranitidine, Cimetidine) - significant decrease in dasatinib exposure.
Moderate Interactions
- Moderate CYP3A4 inhibitors (e.g., Erythromycin, Diltiazem, Verapamil, Fluconazole)
- Antacids (e.g., Aluminum hydroxide/Magnesium hydroxide) - separate administration by at least 2 hours.
Minor Interactions
- Not available
Monitoring
Baseline Monitoring
Complete Blood Count (CBC) with differential
Rationale: To establish baseline hematologic parameters and monitor for myelosuppression (neutropenia, thrombocytopenia, anemia).
Timing: Prior to initiation of therapy.
Liver Function Tests (LFTs) (AST, ALT, Bilirubin)
Rationale: To assess baseline hepatic function and monitor for hepatotoxicity.
Timing: Prior to initiation of therapy.
Renal Function Tests (Creatinine, BUN)
Rationale: To assess baseline renal function.
Timing: Prior to initiation of therapy.
Electrolytes (Potassium, Magnesium, Calcium)
Rationale: To assess baseline electrolyte status, as imbalances can contribute to QTc prolongation.
Timing: Prior to initiation of therapy.
Electrocardiogram (ECG)
Rationale: To assess baseline QTc interval and monitor for cardiac abnormalities.
Timing: Prior to initiation of therapy.
Pulmonary assessment (e.g., chest X-ray, pulmonary function tests if indicated)
Rationale: To establish baseline for potential pulmonary arterial hypertension (PAH) or pleural effusion.
Timing: Prior to initiation of therapy, especially if patient has pre-existing pulmonary conditions.
Routine Monitoring
Complete Blood Count (CBC) with differential
Frequency: Every 2 weeks for the first 3 months, then monthly or as clinically indicated.
Target: Maintain ANC > 1.0 x 10^9/L, Platelets > 50 x 10^9/L.
Action Threshold: Dose interruption or reduction for Grade 3/4 myelosuppression.
Liver Function Tests (LFTs)
Frequency: Monthly or as clinically indicated.
Target: Within normal limits or baseline.
Action Threshold: Dose interruption or reduction for Grade 3/4 elevations.
Renal Function Tests
Frequency: Periodically or as clinically indicated.
Target: Within normal limits or baseline.
Action Threshold: Not available (dose adjustment not typically needed for renal impairment).
Electrolytes (Potassium, Magnesium, Calcium)
Frequency: Periodically or as clinically indicated, especially if on diuretics or with cardiac risk factors.
Target: Within normal limits.
Action Threshold: Correct hypokalemia or hypomagnesemia prior to and during therapy.
Electrocardiogram (ECG)
Frequency: Periodically, especially if cardiac symptoms develop or with risk factors for QTc prolongation.
Target: QTc < 450 ms (men), < 470 ms (women).
Action Threshold: Dose interruption or reduction for QTc > 500 ms or significant prolongation.
Weight and Fluid Status
Frequency: Regularly (e.g., monthly or at each visit).
Target: Stable weight, no signs of significant fluid retention.
Action Threshold: Manage fluid retention with diuretics or dose modification if severe.
Pulmonary Symptoms (e.g., dyspnea, cough)
Frequency: Ongoing clinical assessment.
Target: Not applicable.
Action Threshold: Investigate new or worsening pulmonary symptoms for potential PAH or pleural effusion.
Symptom Monitoring
- Fever
- Chills
- Sore throat
- Unusual bleeding or bruising
- Fatigue
- Shortness of breath
- Cough
- Chest pain
- Swelling (ankles, legs, abdomen, face)
- Rapid weight gain
- Dizziness
- Lightheadedness
- Palpitations
- Muscle cramps or weakness
- Nausea
- Vomiting
- Diarrhea
- Rash
- Headache
Special Patient Groups
Pregnancy
Dasatinib can cause fetal harm when administered to a pregnant woman. Based on animal studies and its mechanism of action, dasatinib is classified as Pregnancy Category D. Advise pregnant women of the potential risk to a fetus. Advise females of reproductive potential to use effective contraception during treatment and for 30 days after the last dose. Advise males with female partners of reproductive potential to use effective contraception during treatment and for 90 days after the last dose.
Trimester-Specific Risks:
First Trimester:
Potential for major congenital malformations and embryo-fetal death based on animal data.
Second Trimester:
Potential for adverse developmental effects, including skeletal abnormalities and reduced fetal weight, based on animal data.
Third Trimester:
Potential for adverse developmental effects, including skeletal abnormalities and reduced fetal weight, based on animal data.
Lactation
It is not known whether dasatinib is excreted in human milk. Because many drugs are excreted in human milk and because of the potential for serious adverse reactions in breastfed infants, women should not breastfeed during treatment with dasatinib and for 2 weeks after the last dose.
Infant Risk:
High risk of serious adverse reactions in breastfed infants due to potential for myelosuppression, growth inhibition, and other toxicities.
Pediatric Use
Dasatinib is approved for pediatric patients with chronic myeloid leukemia (CML) and Philadelphia chromosome-positive acute lymphoblastic leukemia (Ph+ ALL). Dosing is based on body surface area (BSA). Safety and efficacy in pediatric patients younger than 1 year of age have not been established. Growth and development should be monitored.
Geriatric Use
No overall differences in safety or effectiveness were observed between elderly (≥65 years) and younger patients, but greater sensitivity of some older individuals cannot be ruled out. Elderly patients may be at increased risk for certain adverse events such as fluid retention and cardiac events. Dose adjustments are not routinely required based on age alone.
Clinical Information
Clinical Pearls
- Dasatinib is effective in patients with CML resistant or intolerant to imatinib, including those with most BCR-ABL mutations, but not T315I.
- Administer dasatinib consistently, either with or without food, but avoid taking it with grapefruit juice.
- Strictly avoid concomitant use of proton pump inhibitors (PPIs) and H2-receptor antagonists due to significant reduction in dasatinib absorption. If gastric acid suppression is needed, antacids can be used, but separate administration by at least 2 hours.
- Monitor patients closely for fluid retention, especially pleural effusion, which is a common side effect. Management may include diuretics or dose modification.
- Be vigilant for signs and symptoms of pulmonary arterial hypertension (PAH), which can occur months to years after initiation. Discontinuation of dasatinib may lead to improvement or reversal of PAH.
- Myelosuppression is a common and dose-limiting toxicity; frequent CBC monitoring is crucial, especially during the initial months of therapy.
- Dasatinib can prolong the QTc interval; correct hypokalemia and hypomagnesemia prior to and during therapy. Use with caution in patients with pre-existing cardiac conditions or those taking other QTc-prolonging drugs.
Alternative Therapies
- Imatinib (Gleevec)
- Nilotinib (Tasigna)
- Bosutinib (Bosulif)
- Ponatinib (Iclusig)
- Asciminib (Scemblix)
- Chemotherapy (for Ph+ ALL)
- Allogeneic hematopoietic stem cell transplantation
Cost & Coverage
Average Cost:
Varies widely, typically > $15,000 - $20,000 per 30 tablets
Generic Available:
Yes
Insurance Coverage:
Specialty Tier (requires prior authorization, often subject to high co-pays or co-insurance)
General Drug Facts
If your symptoms or health issues persist or worsen, it is essential to contact your doctor for further guidance. To ensure your safety, never share your medication with others or take someone else's medication. Some medications may come with an additional patient information leaflet, so it's a good idea to check with your pharmacist for more information. If you have any questions or concerns about this medication, don't hesitate to reach out to your doctor, nurse, pharmacist, or other healthcare provider. In the event of a suspected overdose, immediately call your local poison control center or seek medical attention. When seeking help, be prepared to provide details about the medication, including the amount taken and the time it happened, to facilitate prompt and effective treatment.