Dasatinib 50mg Tablets

Dasatinib is a small-molecule 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 active and inactive conformations of the BCR-ABL kinase, making it effective against imatinib-resistant CML and ALL, including those with BCR-ABL mutations (except T315I). By inhibiting these kinases, dasatinib blocks proliferation and induces apoptosis in leukemia cells.

Urgent Side Effects: Seek Medical Help Immediately

While rare, some people may experience severe and potentially life-threatening side effects when taking this medication. If you notice 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, 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, gum bleeding, abnormal vaginal bleeding, unexplained bruises or bruising that worsens, 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 headaches or dizziness, fainting, or changes in vision.
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 may 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 rapid 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, rapid 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 liver problems may be higher.

Common Side Effects

Most people experience no side effects or only mild side effects when taking this medication. 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
Arm or leg pain
* 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

If you have questions about side effects or want to report any side effects, contact your doctor or the FDA at 1-800-332-1088. You can also report side effects online at https://www.fda.gov/medwatch.

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 allergic reaction 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, or 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, particularly those used to treat HIV, infections, or seizures.

Additional Considerations:

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 vital to discuss all your medications and health conditions with your doctor and pharmacist to ensure safe use.
* Always check with your doctor before starting, stopping, or changing the dose of any medication to avoid potential interactions or complications.

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, as some formulations of this medication 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, 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 increased bleeding tendencies. 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 with 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 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 take precautions:

Pregnant individuals should not handle crushed or broken tablets. If accidental contact occurs, wash the affected area with soap and water immediately.
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 giving this medication to a child, consult with 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.

• Strong CYP3A4 inducers (e.g., rifampin, phenytoin, carbamazepine, phenobarbital, St. John's Wort) - concomitant use is contraindicated due to significant decrease in dasatinib plasma concentrations.
• Proton Pump Inhibitors (PPIs) (e.g., omeprazole, esomeprazole, lansoprazole, pantoprazole, rabeprazole) - concomitant use is contraindicated due to significant decrease in dasatinib absorption.

• Strong CYP3A4 inhibitors (e.g., ketoconazole, itraconazole, clarithromycin, telithromycin, ritonavir, atazanavir, indinavir, nelfinavir, saquinavir, voriconazole) - may significantly increase dasatinib concentrations; avoid concomitant use or reduce dasatinib dose.
• H2-receptor antagonists (e.g., famotidine, ranitidine, cimetidine) - avoid concomitant use; if necessary, administer dasatinib at least 2 hours before or 2 hours after H2RAs.
• Antacids (e.g., aluminum hydroxide/magnesium hydroxide) - avoid concomitant use; if necessary, administer dasatinib at least 2 hours before or 2 hours after antacids.
• QTc prolonging drugs (e.g., amiodarone, disopyramide, procainamide, quinidine, sotalol, chloroquine, haloperidol, methadone, moxifloxacin, ondansetron, pimozide, thioridazine) - increased risk of QTc prolongation; use with caution and monitor ECG.

• Moderate CYP3A4 inhibitors (e.g., erythromycin, diltiazem, verapamil, fluconazole, grapefruit juice) - may increase dasatinib concentrations; use with caution and consider dose reduction.
• Warfarin and other anticoagulants - increased risk of bleeding; monitor INR/PT closely.
• Drugs that inhibit P-glycoprotein (P-gp) - potential for increased dasatinib exposure.

• Not available

• Signs of infection (fever, chills, sore throat)
• Unusual bleeding or bruising (petechiae, epistaxis, melena)
• Fatigue, pallor (anemia)
• Shortness of breath, cough, chest pain, swelling in ankles/legs (fluid retention, pleural/pericardial effusion, pulmonary hypertension)
• Abdominal pain, nausea, vomiting, diarrhea
• Muscle pain, joint pain
• Skin rash
• Headache, dizziness
• Signs of cardiac dysfunction (palpitations, chest discomfort)

Dasatinib can cause fetal harm when administered to a pregnant woman. Based on animal studies and its mechanism of action, it is expected to cause serious adverse developmental effects. Avoid use during pregnancy. Women of reproductive potential should be advised to use effective contraception during treatment and for 30 days after the last dose. Males with female partners of reproductive potential should use effective contraception during treatment and for 90 days after the last dose.

It is not known whether dasatinib is excreted in human milk. Due to the potential for serious adverse reactions in breastfed infants, breastfeeding is not recommended during treatment with dasatinib and for 2 weeks after the last dose.

Dasatinib is approved for pediatric patients with Ph+ CML (chronic phase) and Ph+ ALL. Dosing is weight-based (mg/m²). Monitor growth and development closely. Pediatric patients may be at higher risk for certain adverse events like musculoskeletal pain and fluid retention.

Clinical studies did not include sufficient numbers of subjects aged 65 and over to determine whether they respond differently from younger subjects. However, elderly patients may be at increased risk for certain adverse events, particularly fluid retention (pleural effusion, pericardial effusion) and cardiac events. Use with caution and monitor closely.

• Dasatinib is a potent multi-targeted TKI effective in imatinib-resistant CML and ALL, including many BCR-ABL mutations.
• Strict adherence to dosing instructions regarding food and concomitant medications (especially acid-reducing agents and strong CYP3A4 inhibitors/inducers) is crucial for optimal absorption and efficacy.
• Fluid retention, particularly pleural effusion, is a common and important side effect. Patients should be educated on symptoms (shortness of breath, cough, swelling) and monitored regularly.
• Myelosuppression (neutropenia, thrombocytopenia, anemia) is dose-limiting and requires frequent CBC monitoring and potential dose adjustments.
• QTc prolongation can occur; baseline and periodic ECGs are recommended, especially in patients with cardiac risk factors or on concomitant QTc-prolonging drugs. Correct electrolyte abnormalities (K+, Mg++) promptly.
• Pulmonary arterial hypertension (PAH) is a rare but serious adverse event; patients presenting with new or worsening dyspnea should be evaluated for PAH.

• Other BCR-ABL Tyrosine Kinase Inhibitors for CML/Ph+ ALL: Imatinib (Gleevec), Nilotinib (Tasigna), Bosutinib (Bosulif), Ponatinib (Iclusig), Asciminib (Scemblix).
• Chemotherapy (for ALL, often in combination with TKIs)
• Allogeneic hematopoietic stem cell transplantation (HSCT)

If your symptoms or health issues persist or worsen, it's 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 be sure to check with your pharmacist for more information. If you have any questions or concerns about your 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 emergency medical attention. When seeking help, be prepared to provide details about the medication taken, the amount, and the time it happened.