Dasatinib 140mg Tablets

Dasatinib is a small-molecule kinase inhibitor. It inhibits the BCR-ABL kinase, which is a key driver of chronic myeloid leukemia (CML) and Philadelphia chromosome-positive acute lymphoblastic leukemia (Ph+ ALL). It also inhibits other kinases, including SRC family kinases (SRC, LCK, YES, FYN), c-KIT, EPHA2, and PDGFRβ, which are implicated in various cancers.

Urgent Side Effects: Seek Medical Help Right Away

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 immediately:

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 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 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 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). Symptoms include chest pain, rapid 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.

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 if they bother you or persist:

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 medical guidance)

Reporting Side Effects

If you have questions about side effects or experience any unusual symptoms, contact 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
+ Ranitidine
Any other medications you are taking, including prescription and over-the-counter (OTC) drugs, natural products, and vitamins. This is crucial because many medications can interact with this drug, particularly those used to treat HIV, infections, or seizures.
* If you are breastfeeding. Please note that you should not breastfeed 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.

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 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. 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. 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 are pregnant or plan to become pregnant, use effective birth control while taking this drug 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 Patients

If you are administering 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, 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)
• Proton Pump Inhibitors (PPIs) (e.g., omeprazole, esomeprazole, lansoprazole)

• Strong CYP3A4 inhibitors (e.g., ketoconazole, itraconazole, clarithromycin, ritonavir, atazanavir, indinavir, nefazodone, nelfinavir, saquinavir, telithromycin, voriconazole) - require dose reduction or alternative.
• H2-receptor antagonists (e.g., famotidine, ranitidine) - avoid concurrent use.

• Moderate CYP3A4 inhibitors (e.g., erythromycin, diltiazem, verapamil, fluconazole) - monitor closely, consider dose adjustment.
• Antacids - separate administration by at least 2 hours.

• Grapefruit juice - avoid consumption.

• Signs of bleeding (e.g., bruising, petechiae, melena, hematuria)
• Signs of infection (e.g., fever, chills, sore throat)
• Symptoms of fluid retention (e.g., shortness of breath, cough, chest pain, swelling in ankles/legs, rapid weight gain)
• Symptoms of pulmonary arterial hypertension (PAH) (e.g., dyspnea, fatigue, chest pain, syncope)
• Symptoms of cardiac dysfunction (e.g., chest pain, palpitations, dizziness)
• Fatigue, weakness
• Rash, skin changes
• Gastrointestinal symptoms (e.g., nausea, vomiting, diarrhea, abdominal pain)
• Musculoskeletal pain

Dasatinib can cause fetal harm when administered to a pregnant woman. Based on animal studies and its mechanism of action, dasatinib is expected to cause serious birth defects. Advise pregnant women of the potential risk to the 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.

It is not known whether dasatinib is excreted in human milk. Due to 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 pediatric patients with Philadelphia chromosome-positive (Ph+) chronic myeloid leukemia (CML) in chronic phase and Ph+ acute lymphoblastic leukemia (ALL). Dosing is weight-based. Safety and efficacy in pediatric patients younger than 1 year of age have not been established. Pediatric patients may be at increased risk for musculoskeletal adverse reactions.

No specific dose adjustment is required based on age. However, elderly patients (≥65 years) may have an increased incidence of certain adverse reactions, particularly fluid retention (e.g., pleural effusion, peripheral edema) and cardiac events. Monitor closely for these adverse effects.

• Dasatinib is a potent multi-targeted TKI, effective in CML and Ph+ ALL, including some imatinib-resistant cases.
• A significant and common side effect is fluid retention, particularly pleural effusion, which can be severe and require dose modification or intervention. Monitor for dyspnea, cough, and weight gain.
• Pulmonary arterial hypertension (PAH) is a rare but serious and potentially irreversible adverse event. Patients should be evaluated for PAH if they develop new or worsening dyspnea.
• Myelosuppression (neutropenia, thrombocytopenia, anemia) is common and requires frequent monitoring and potential dose adjustments.
• Dasatinib absorption is pH-dependent; avoid concomitant use with PPIs and H2 blockers. Separate antacid administration by at least 2 hours.
• QT prolongation can occur; correct hypokalemia and hypomagnesemia prior to and during therapy. Use with caution in patients with pre-existing cardiac conditions or on other QT-prolonging drugs.
• Patients should be advised to swallow tablets whole and not to crush, cut, or chew them due to potential for skin exposure and altered absorption.

• Imatinib (Gleevec)
• Nilotinib (Tasigna)
• Bosutinib (Bosulif)
• Ponatinib (Iclusig)
• Omacetaxine (Synribo) - for CML resistant/intolerant to 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 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 emergency medical attention. When seeking help, be prepared to provide details about the medication taken, the amount, and the time it happened.