Sprycel 50mg 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)
Pregnancy Category
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. By blocking these proteins, dasatinib helps to stop the growth of cancer cells.
How to Use This Medicine
Taking Your Medication Correctly
To ensure you get the most out of your medication, follow these steps:
Take your medication exactly as directed by your doctor.
Read all the information provided with your medication and follow the instructions carefully.
Take your medication at the same time every day.
You can take your medication with or without food.
Swallow the tablet whole - do not chew, break, or crush it.
If you have difficulty swallowing, consult your doctor for guidance.
Continue taking your medication as prescribed by your doctor or healthcare provider, even if you start to feel better.
Handling Your Medication
When handling your medication, take special precautions. Consult your doctor or pharmacist for instructions on how to handle your medication safely.
Important Interactions
Do not take antacids within 2 hours before or 2 hours after taking your medication.
Storing and Disposing of Your Medication
Store your medication at room temperature in a dry place, away from 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 ensure you get the most out of your medication, follow these steps:
Take your medication exactly as directed by your doctor.
Read all the information provided with your medication and follow the instructions carefully.
Take your medication at the same time every day.
You can take your medication with or without food.
Swallow the tablet whole - do not chew, break, or crush it.
If you have difficulty swallowing, consult your doctor for guidance.
Continue taking your medication as prescribed by your doctor or healthcare provider, even if you start to feel better.
Handling Your Medication
When handling your medication, take special precautions. Consult your doctor or pharmacist for instructions on how to handle your medication safely.
Important Interactions
Do not take antacids within 2 hours before or 2 hours after taking your medication.
Storing and Disposing of Your Medication
Store your medication at room temperature in a dry place, away from 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.
Lifestyle & Tips
- Take dasatinib exactly as prescribed by your doctor, usually once a day, with or without food.
- Swallow tablets whole; do not crush, cut, or chew them.
- Avoid grapefruit and grapefruit juice while taking dasatinib, as they can increase the amount of medicine in your body.
- Avoid antacids, H2 blockers (like famotidine), and proton pump inhibitors (like omeprazole) while taking dasatinib. If you need an antacid, take it at least 2 hours before or 2 hours after your dasatinib dose.
- Report any signs of infection (fever, chills, sore throat) immediately.
- Report any unusual bleeding or bruising.
- Report any swelling, shortness of breath, or sudden weight gain, as these could be signs of fluid retention.
- Do not stop taking dasatinib without talking to your doctor first.
Available Forms & Alternatives
Available Strengths:
Generic Alternatives:
Dosing & Administration
Adult Dosing
Standard Dose:
Chronic Myeloid Leukemia (CML) in chronic phase (CML-CP): 100 mg orally once daily. CML in accelerated phase (CML-AP), myeloid or lymphoid blast phase (CML-BP), or Philadelphia chromosome-positive acute lymphoblastic leukemia (Ph+ ALL): 140 mg orally once daily. Doses may be adjusted based on response and tolerability.
Dose Range:
20 - 180 mg
Condition-Specific Dosing:
CML-CP:
100 mg orally once daily
CML-AP/BP, Ph+ ALL:
140 mg orally once daily
Dose reduction for toxicity:
Consider 80 mg, 50 mg, or 20 mg once daily
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established
Child:
CML-CP: 60 mg/m² orally once daily (max 100 mg/day). CML-AP/BP, Ph+ ALL: 90 mg/m² orally once daily (max 140 mg/day). Dosing based on body surface area.
Adolescent:
CML-CP: 60 mg/m² orally once daily (max 100 mg/day). CML-AP/BP, Ph+ ALL: 90 mg/m² orally once daily (max 140 mg/day). Dosing based on body surface area.
Dose Adjustments
Renal Impairment:
Mild:
No dose adjustment required.
Moderate:
No dose adjustment required.
Severe:
No dose adjustment required, but caution is advised due to limited data.
Dialysis:
Not available. Dasatinib is highly protein bound and unlikely to be removed by dialysis.
Hepatic Impairment:
Mild:
No dose adjustment required (Child-Pugh A).
Moderate:
Reduce initial dose by 20-30% (e.g., 80 mg for 100 mg standard dose, 100 mg for 140 mg standard dose) (Child-Pugh B). Monitor closely.
Severe:
Reduce initial dose by 30-50% (e.g., 50 mg for 100 mg standard dose, 70 mg for 140 mg standard dose) (Child-Pugh C). Monitor closely.
Pharmacology
Mechanism of Action
Dasatinib is a small molecule kinase inhibitor that inhibits multiple tyrosine kinases, including BCR-ABL, SRC family (SRC, LCK, YES, FYN), c-KIT, EPHA2, and PDGFRβ. It binds to both active and inactive conformations of the ABL kinase domain, making it effective against imatinib-resistant CML and Ph+ ALL, including those with BCR-ABL mutations (except T315I).
Pharmacokinetics
Absorption:
Bioavailability:
Not precisely determined, but rapidly absorbed.
Tmax:
0.5 to 6 hours (median 0.5-3 hours)
FoodEffect:
High-fat meal increases AUC by 14% and Cmax by 23%. Not clinically significant, can be taken with or without food. However, gastric pH affects solubility and absorption.
Distribution:
Vd:
2505 L (apparent volume of distribution)
ProteinBinding:
Approximately 96% (primarily to albumin and alpha-1 acid glycoprotein)
CnssPenetration:
Limited, but detectable concentrations in CSF have been observed in some patients.
Elimination:
HalfLife:
3 to 5 hours (terminal half-life)
Clearance:
Not available (apparent oral clearance 318 L/h)
ExcretionRoute:
Mainly feces (85%), minor urine (4%)
Unchanged:
Less than 0.1% in urine, 19% in feces
Pharmacodynamics
OnsetOfAction:
Rapid, within hours for kinase inhibition.
PeakEffect:
Not directly applicable for anti-cancer effect, but peak plasma concentrations reached within hours.
DurationOfAction:
Sustained kinase inhibition due to irreversible binding or slow dissociation, allowing once-daily dosing.
Safety & Warnings
Side Effects
Urgent Side Effects: Seek Medical Help Immediately
Although rare, this medication can cause severe and potentially life-threatening side effects. If you experience any of the following symptoms, contact your doctor or 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 unhealing wounds.
Bleeding: Vomiting or coughing up blood, coffee ground-like vomit, blood in urine, black, red, or tarry stools, gum bleeding, abnormal vaginal bleeding, unexplained bruises or enlarging bruises, 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.
Blood pressure changes: Severe headache, dizziness, fainting, or vision changes.
Numbness or tingling: In the hands or feet.
Seizures: Convulsions or loss of consciousness.
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. Seek medical help immediately if you experience red, swollen, blistered, or peeling skin; skin irritation with or without fever; red or irritated eyes; or sores in your mouth, throat, nose, or eyes.
Tumor lysis syndrome (TLS): If you have cancer, you may be at increased risk of developing TLS, a potentially life-threatening condition. Contact your doctor immediately if you experience a fast or abnormal heartbeat, fainting, difficulty urinating, muscle weakness or cramps, nausea, vomiting, diarrhea, loss of appetite, or feeling sluggish.
Heart problems: Abnormal heartbeat (including prolonged QT interval), heart attack, or small strokes (TIAs). Seek medical help immediately if you experience chest pain, fast or abnormal heartbeat, shortness of breath, significant 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. If you already have liver problems, your risk of developing liver problems may be higher.
Common Side Effects
Most people experience no side effects or only mild side effects. However, if you experience any of the following, contact your doctor or seek medical attention:
Constipation
Stomach pain
Headache
Fatigue or weakness
Muscle or joint pain
Pain in the arms or legs
* Diarrhea, vomiting, nausea, or decreased appetite (common side effects that can be managed with your doctor's guidance)
If any of these side effects bother you, do not improve, or are severe, contact your doctor for advice.
Reporting Side Effects
You can report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch. If you have questions about side effects, contact your doctor for medical advice.
Although rare, this medication can cause severe and potentially life-threatening side effects. If you experience any of the following symptoms, contact your doctor or 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 unhealing wounds.
Bleeding: Vomiting or coughing up blood, coffee ground-like vomit, blood in urine, black, red, or tarry stools, gum bleeding, abnormal vaginal bleeding, unexplained bruises or enlarging bruises, 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.
Blood pressure changes: Severe headache, dizziness, fainting, or vision changes.
Numbness or tingling: In the hands or feet.
Seizures: Convulsions or loss of consciousness.
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. Seek medical help immediately if you experience red, swollen, blistered, or peeling skin; skin irritation with or without fever; red or irritated eyes; or sores in your mouth, throat, nose, or eyes.
Tumor lysis syndrome (TLS): If you have cancer, you may be at increased risk of developing TLS, a potentially life-threatening condition. Contact your doctor immediately if you experience a fast or abnormal heartbeat, fainting, difficulty urinating, muscle weakness or cramps, nausea, vomiting, diarrhea, loss of appetite, or feeling sluggish.
Heart problems: Abnormal heartbeat (including prolonged QT interval), heart attack, or small strokes (TIAs). Seek medical help immediately if you experience chest pain, fast or abnormal heartbeat, shortness of breath, significant 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. If you already have liver problems, your risk of developing liver problems may be higher.
Common Side Effects
Most people experience no side effects or only mild side effects. However, if you experience any of the following, contact your doctor or seek medical attention:
Constipation
Stomach pain
Headache
Fatigue or weakness
Muscle or joint pain
Pain in the arms or legs
* Diarrhea, vomiting, nausea, or decreased appetite (common side effects that can be managed with your doctor's guidance)
If any of these side effects bother you, do not improve, or are severe, contact your doctor for advice.
Reporting Side Effects
You can report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch. If you have questions about side effects, contact your doctor for medical advice.
Seek Immediate Medical Attention If You Experience:
- Fever, chills, or other signs of infection
- Unusual bleeding or bruising
- Severe fatigue or weakness
- Shortness of breath, cough, or chest pain
- Swelling in your ankles, feet, or hands
- Rapid weight gain
- Dizziness, lightheadedness, or fainting
- Severe nausea, vomiting, or diarrhea
- Yellowing of skin or eyes (jaundice)
- Dark urine or pale stools
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, such as foods or drugs. Be sure to describe the symptoms you experienced.
Certain health conditions, including low levels of potassium or magnesium in your blood.
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 is crucial because many drugs can interact with this medication, such as those used to treat HIV, infections, or seizures.
* If you are breast-feeding. Please note that you should not breast-feed while taking this medication and for 2 weeks after your last dose.
This list is not exhaustive, and it is crucial to discuss all your medications and health conditions with your doctor and pharmacist to ensure safe use. Do not start, stop, or change the dose of any medication without consulting your doctor first. It is your responsibility to verify that it is safe to take this medication with all 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, such as foods or drugs. Be sure to describe the symptoms you experienced.
Certain health conditions, including low levels of potassium or magnesium in your blood.
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 is crucial because many drugs can interact with this medication, such as those used to treat HIV, infections, or seizures.
* If you are breast-feeding. Please note that you should not breast-feed while taking this medication and for 2 weeks after your last dose.
This list is not exhaustive, and it is crucial to discuss all your medications and health conditions with your doctor and pharmacist to ensure safe use. Do not start, stop, or change the dose of any medication without consulting your doctor first. It is your responsibility to verify that it is safe to take this medication with all 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 medication. 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 your doctor, as some formulations of this medication may contain lactose. Additionally, avoid consuming grapefruit and grapefruit juice while taking this medication.
Blood-Related Risks
This medication may suppress the bone marrow's ability to produce essential blood cells, potentially leading to 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 an increased risk of bleeding. To reduce this risk, exercise caution, avoid injuries, and use a soft toothbrush and an electric razor. In rare cases, bleeding complications can be life-threatening.
Respiratory Risks
There is a potential risk of developing a severe lung condition called pulmonary arterial hypertension, which may occur at any time during treatment, even after more than a year of taking this medication. Consult your doctor if you have any concerns.
Special Considerations
If you are 65 years or older, use this medication with caution, as you may be more susceptible to side effects.
This medication 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 with care. Pregnant individuals should not handle crushed or broken tablets, and if accidental contact occurs, the area should be washed immediately with soap and water.
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 medication and for 30 days after the last dose, unless otherwise advised 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 the last dose, unless otherwise advised by your doctor. If your partner becomes pregnant, inform the doctor immediately.
Pediatric Considerations
If you are administering this medication to a child, consult your doctor if the child's weight changes, as the dosage may need to be adjusted. This medication may affect growth in children and adolescents in some cases, and regular growth checks may be necessary. Discuss any concerns with your doctor.
It is crucial that you inform all your healthcare providers, including doctors, nurses, pharmacists, and dentists, that you are taking this medication. 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 your doctor, as some formulations of this medication may contain lactose. Additionally, avoid consuming grapefruit and grapefruit juice while taking this medication.
Blood-Related Risks
This medication may suppress the bone marrow's ability to produce essential blood cells, potentially leading to 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 an increased risk of bleeding. To reduce this risk, exercise caution, avoid injuries, and use a soft toothbrush and an electric razor. In rare cases, bleeding complications can be life-threatening.
Respiratory Risks
There is a potential risk of developing a severe lung condition called pulmonary arterial hypertension, which may occur at any time during treatment, even after more than a year of taking this medication. Consult your doctor if you have any concerns.
Special Considerations
If you are 65 years or older, use this medication with caution, as you may be more susceptible to side effects.
This medication 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 with care. Pregnant individuals should not handle crushed or broken tablets, and if accidental contact occurs, the area should be washed immediately with soap and water.
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 medication and for 30 days after the last dose, unless otherwise advised 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 the last dose, unless otherwise advised by your doctor. If your partner becomes pregnant, inform the doctor immediately.
Pediatric Considerations
If you are administering this medication to a child, consult your doctor if the child's weight changes, as the dosage may need to be adjusted. This medication may affect growth in children and adolescents in some cases, and regular growth checks may be necessary. Discuss any concerns with your doctor.
Overdose Information
Overdose Symptoms:
- Myelosuppression (low blood counts)
- Fluid retention (pleural effusion, pericardial effusion)
- Gastrointestinal disturbances
What to Do:
There is no specific antidote for dasatinib overdose. Management should consist of general supportive measures. Call 1-800-222-1222 (Poison Control Center) immediately or seek emergency medical attention.
Drug Interactions
Contraindicated Interactions
- Strong CYP3A4 inducers (e.g., rifampin, phenytoin, carbamazepine, phenobarbital, St. John's Wort) - may significantly decrease dasatinib exposure.
- Proton Pump Inhibitors (PPIs) (e.g., omeprazole, esomeprazole, lansoprazole, pantoprazole, rabeprazole) - significantly decrease dasatinib solubility and absorption.
Major Interactions
- Strong CYP3A4 inhibitors (e.g., ketoconazole, itraconazole, clarithromycin, ritonavir, atazanavir, indinavir, nefazodone, nelfinavir, saquinavir, telithromycin, voriconazole) - may significantly increase dasatinib exposure, requiring dose reduction.
- H2-receptor antagonists (e.g., famotidine, ranitidine, cimetidine) - may decrease dasatinib absorption; separate administration by at least 2 hours or avoid.
- Antacids (e.g., aluminum hydroxide/magnesium hydroxide) - may decrease dasatinib absorption; separate administration by at least 2 hours.
Moderate Interactions
- Moderate CYP3A4 inhibitors (e.g., erythromycin, diltiazem, verapamil, fluconazole, grapefruit juice) - may increase dasatinib exposure, monitor for toxicity.
- Moderate CYP3A4 inducers (e.g., efavirenz, bosentan, modafinil) - may decrease dasatinib exposure, monitor for reduced efficacy.
- QT-prolonging agents (e.g., antiarrhythmics, antipsychotics, macrolides, fluoroquinolones) - additive risk of QT prolongation.
Minor Interactions
- Not available
Monitoring
Baseline Monitoring
Complete Blood Count (CBC) with differential
Rationale: To establish baseline hematologic parameters and assess for pre-existing myelosuppression.
Timing: Prior to initiation of therapy.
Liver Function Tests (LFTs) (ALT, AST, bilirubin)
Rationale: To assess baseline hepatic function and identify pre-existing impairment.
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 levels, as imbalances can increase risk of QT prolongation.
Timing: Prior to initiation of therapy.
Electrocardiogram (ECG)
Rationale: To assess baseline QTc interval and identify pre-existing cardiac abnormalities.
Timing: Prior to initiation of therapy.
Pulmonary function assessment (e.g., chest X-ray, physical exam for signs of fluid retention)
Rationale: To assess for baseline pulmonary status and identify risk factors for fluid retention/PAH.
Timing: Prior to initiation of therapy.
Routine Monitoring
Complete Blood Count (CBC) with differential
Frequency: Every week for the first 2 months, then monthly or as clinically indicated.
Target: Maintain ANC > 1.0 x 10^9/L, Platelets > 50 x 10^9/L (dose adjustments for lower values).
Action Threshold: Grade 3/4 neutropenia or thrombocytopenia requires dose interruption or reduction.
Liver Function Tests (LFTs)
Frequency: Monthly or as clinically indicated.
Target: Within normal limits or baseline.
Action Threshold: Grade 3/4 elevations require dose interruption or reduction.
Electrolytes (Potassium, Magnesium)
Frequency: Periodically, especially if on concomitant medications or with risk factors for QT prolongation.
Target: Maintain within normal limits.
Action Threshold: Correct hypokalemia or hypomagnesemia prior to and during therapy.
Electrocardiogram (ECG)
Frequency: Periodically, especially if risk factors for QT prolongation are present or new cardiac symptoms develop.
Target: QTc < 500 ms.
Action Threshold: QTc > 500 ms requires dose interruption and re-evaluation.
Fluid status assessment (weight, edema, dyspnea)
Frequency: Regularly, at each visit.
Target: No significant fluid retention.
Action Threshold: Development of pleural effusion, pericardial effusion, or pulmonary edema requires intervention (diuretics, dose interruption/reduction, or discontinuation).
Pulmonary arterial hypertension (PAH) symptoms
Frequency: Monitor for new or worsening dyspnea, fatigue, peripheral edema.
Target: Not applicable.
Action Threshold: If PAH is suspected, perform diagnostic work-up including echocardiogram and right heart catheterization. Discontinue dasatinib if PAH is confirmed.
Symptom Monitoring
- Fever, chills, sore throat (signs of infection/myelosuppression)
- Unusual bleeding or bruising (thrombocytopenia)
- Fatigue, weakness, pallor (anemia)
- Shortness of breath, cough, chest pain, swelling in ankles/legs (fluid retention, pleural effusion, pulmonary edema, PAH)
- Dizziness, lightheadedness, fainting (QT prolongation)
- Nausea, vomiting, diarrhea, abdominal pain
- Rash, skin changes
- Muscle pain, cramps
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 and visceral abnormalities, based on animal data.
Third Trimester:
Potential for adverse developmental effects, including skeletal and visceral abnormalities, 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:
L5 (Contraindicated/Hazardous) - Potential for serious adverse effects in the infant due to the drug's mechanism of action and potential for systemic exposure.
Pediatric Use
Dasatinib is approved for pediatric patients 1 year of age and older with CML-CP and Ph+ ALL. Dosing is based on body surface area. 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. However, elderly patients may be more susceptible to certain adverse reactions, such as fluid retention. Dose adjustments are not routinely required based on age alone, but careful monitoring is warranted.
Clinical Information
Clinical Pearls
- Dasatinib is effective in patients resistant or intolerant to imatinib, including those with most BCR-ABL mutations, except T315I.
- Fluid retention, particularly pleural effusion, is a common and important side effect. Monitor for symptoms (dyspnea, cough, weight gain) and manage with diuretics, dose reduction, or interruption.
- Pulmonary arterial hypertension (PAH) is a rare but serious adverse event. Discontinue dasatinib if PAH is confirmed.
- Myelosuppression (neutropenia, thrombocytopenia, anemia) is dose-limiting. Regular CBC monitoring and dose adjustments are crucial.
- Dasatinib absorption is pH-dependent. Avoid concomitant use with PPIs, H2-receptor antagonists, and separate antacid administration.
- Patients should be advised to report any signs of bleeding, infection, or cardiac symptoms immediately.
- Adherence is critical for optimal outcomes in CML/ALL.
Alternative Therapies
- Imatinib (Gleevec)
- Nilotinib (Tasigna)
- Bosutinib (Bosulif)
- Ponatinib (Iclusig)
- Asciminib (Scemblix)
- Omacetaxine (Synribo - for CML with T315I mutation)
- Chemotherapy (for Ph+ ALL or advanced CML)
- Allogeneic hematopoietic stem cell transplantation
Cost & Coverage
Average Cost:
$15,000 - $20,000+ per 30 tablets (50mg or 100mg)
Insurance Coverage:
Specialty Tier (requires prior authorization, may have step therapy requirements)
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 discuss them with your doctor, nurse, pharmacist, or other healthcare provider. In the event of a suspected overdose, immediately call your local poison control center or seek emergency medical attention. When seeking help, be prepared to provide details about the medication taken, the amount, and the time it occurred.