Dasatinib 70mg 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 the active and inactive conformations of the ABL kinase domain, making it effective against imatinib-resistant BCR-ABL mutations (except T315I). By inhibiting these kinases, dasatinib prevents the proliferation and survival of leukemia cells.

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 bruising that worsens, or uncontrollable bleeding.
Electrolyte imbalances: 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.
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): a potentially life-threatening condition that can occur in cancer patients. Call your doctor right away 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: which can be more likely if you already have liver disease. Call your doctor right away if you experience dark urine, fatigue, decreased appetite, nausea, stomach pain, light-colored stools, vomiting, or yellow skin and eyes.

Other Possible Side Effects

While many people may not experience side effects or may only have mild side effects, it's essential to discuss any concerns with your doctor. Common side effects include:

Constipation
Stomach pain
Headache
Fatigue or weakness
Muscle or joint pain
Pain in the arms or legs
* Diarrhea, vomiting, nausea, and decreased appetite (which can be managed with your doctor's guidance)

If any of these side effects bother you, don't improve, or are severe, call your doctor for advice.

Reporting Side Effects

If you have questions or concerns about side effects, call your doctor. You can also report side effects to the FDA at 1-800-332-1088 or 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.

Additionally, 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.

To ensure your safety, it is crucial to provide your doctor and pharmacist with a comprehensive list of all your medications (prescription and OTC), natural products, vitamins, and health problems. This will help determine whether it is safe for you to take this medication with your other medications and health conditions. Never start, stop, or change the dose of any medication without first consulting your doctor.

Important Information for Patients Taking This Medication

It is essential to 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 crucial, 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 necessary 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 crucial 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 medication 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 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 directed by your doctor. If you become pregnant, notify your doctor immediately.

If your partner may become pregnant, use birth control while taking this medication and for 30 days after the last dose, unless otherwise directed by your doctor. If your partner becomes pregnant, inform the doctor right away.

Pediatric Considerations

If your child is taking this medication and experiences weight changes, consult your doctor, as the dosage may need to be adjusted. This medication may affect growth in children and teenagers, and regular growth checks may be necessary. Discuss this with your doctor.

• Strong CYP3A4 inducers (e.g., rifampin, phenytoin, carbamazepine, phenobarbital, St. John's Wort) - significantly decrease dasatinib exposure.
• Proton Pump Inhibitors (PPIs) (e.g., omeprazole, esomeprazole, lansoprazole) - significantly decrease dasatinib absorption due to pH dependency.

• Strong CYP3A4 inhibitors (e.g., ketoconazole, itraconazole, clarithromycin, ritonavir, atazanavir, nefazodone) - significantly increase dasatinib exposure, requiring dose reduction.
• H2-receptor antagonists (e.g., famotidine, ranitidine) - decrease dasatinib absorption, separate administration by at least 2 hours or avoid if possible.
• Antacids (e.g., aluminum hydroxide/magnesium hydroxide) - decrease dasatinib absorption, separate administration by at least 2 hours.

• Moderate CYP3A4 inhibitors (e.g., erythromycin, diltiazem, verapamil, fluconazole) - may increase dasatinib exposure, monitor for toxicity.
• Moderate CYP3A4 inducers (e.g., efavirenz, modafinil) - may decrease dasatinib exposure, monitor for efficacy.

• Not specifically listed, but general caution with drugs affecting gastric pH or CYP3A4.

• Fever
• Unusual bleeding or bruising
• Fatigue, pallor (anemia)
• Shortness of breath, cough, chest pain (pleural/pericardial effusion, pulmonary hypertension)
• Swelling in ankles, feet, hands (edema)
• Dizziness, lightheadedness, syncope (QT prolongation)
• Yellowing of skin or eyes, dark urine, severe nausea/vomiting (hepatotoxicity)
• Severe headache, vision changes (CNS events, though rare)

Dasatinib is classified as Pregnancy Category D. It can cause fetal harm when administered to a pregnant woman based on animal studies. Avoid use during pregnancy. If a woman becomes pregnant while taking dasatinib, she should be apprised of the potential hazard to the fetus.

It is not known whether dasatinib is excreted in human milk. However, 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.

Dasatinib is approved for the treatment of pediatric patients with chronic phase CML and Ph+ ALL. Dosing is weight-based. Safety and efficacy in pediatric patients younger than 1 year of age have not been established.

No specific dose adjustment is required for elderly patients. However, elderly patients may be more susceptible to certain adverse reactions, such as fluid retention and myelosuppression. Monitor closely for adverse effects.

• Dasatinib is effective against most imatinib-resistant BCR-ABL mutations, except T315I.
• A common and important side effect is fluid retention, particularly pleural effusion. Monitor for symptoms like shortness of breath and weight gain. Diuretics may be used, and dose reduction or interruption may be necessary.
• Myelosuppression (neutropenia, thrombocytopenia, anemia) is common and often requires dose interruption or reduction.
• Dasatinib absorption is pH-dependent; avoid concomitant use with PPIs, H2-blockers, and antacids (separate antacid administration by at least 2 hours).
• Monitor ECG for QT prolongation, especially in patients with pre-existing cardiac conditions or those on other QT-prolonging medications. Correct hypokalemia and hypomagnesemia prior to and during therapy.
• Patients should be advised to avoid grapefruit products due to potential for increased dasatinib exposure.
• Pulmonary arterial hypertension (PAH) is a rare but serious adverse event that can occur with dasatinib, sometimes after prolonged use. Patients should be evaluated for PAH if they develop new or worsening dyspnea.

• Imatinib (Gleevec)
• Nilotinib (Tasigna)
• Bosutinib (Bosulif)
• Ponatinib (Iclusig) - for T315I mutation or refractory disease
• Asciminib (Scemblix) - for T315I mutation or refractory disease
• Chemotherapy (for Ph+ 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 medical attention. When seeking help, be prepared to provide details about the medication taken, the amount, and the time it happened.