About
Dasatinib is a potent, orally available tyrosine kinase inhibitor (TKI) that targets multiple kinases, including BCR-ABL, SRC family kinases, c-KIT, EPHA2, and PDGFRβ. It is primarily used in the treatment of Philadelphia chromosome-positive (Ph+) chronic myeloid leukemia (CML) and Ph+ acute lymphoblastic leukemia (ALL) that are resistant or intolerant to prior therapy, including imatinib. By inhibiting these key kinases, dasatinib blocks the signaling pathways that drive the proliferation and survival of cancer cells.
Dasatinib is rapidly absorbed after oral administration and undergoes extensive metabolism, primarily by CYP3A4. Its broad spectrum of kinase inhibition contributes to its efficacy in patients who have developed resistance to other TKIs, often due to mutations in the BCR-ABL kinase domain. Regular monitoring of blood counts and fluid retention is essential during treatment.
Uses
- Treatment of chronic myeloid leukemia (CML).
- Management of Philadelphia chromosome-positive ALL.
- Used in CML patients resistant to imatinib.
- Therapy for CML patients intolerant to imatinib.
Directions For Use
Take orally once daily, with or without food, as directed by your physician. Do not crush, cut, or chew the tablets.
Benefits
- Effective in imatinib-resistant CML.
- Targets multiple oncogenic kinases.
- Achieves high rates of hematologic and cytogenetic response.
- Improves progression-free and overall survival in CML.
- Available as an oral tablet for convenient administration.
- Offers a crucial treatment option for advanced CML.
Side Effects
- Myelosuppression (thrombocytopenia, neutropenia, anemia)
- Fluid retention (pleural effusion, peripheral edema)
- Diarrhea
- Nausea
- Fatigue
- Headache
- Rash
- Dyspnea (shortness of breath)
- Musculoskeletal pain
- Hemorrhage
- QT prolongation
- Hypertension
Safety Measures
- Alcohol - Limit or avoid alcohol consumption as it may exacerbate gastrointestinal side effects and potentially interact with the drug's metabolism.
- Pregnancy - Dasatinib can cause fetal harm. It is contraindicated in pregnancy. Women of childbearing potential must use highly effective contraception during treatment and for a period after.
- Breastfeeding - Breastfeeding is not recommended during dasatinib treatment and for at least 2 weeks after the last dose, due to potential excretion in breast milk and harm to the infant.
- Liver - Use with caution in patients with hepatic impairment; dose adjustments may be necessary due to its metabolism primarily by CYP3A4.
- Kidney - Use with caution in patients with severe renal impairment; close monitoring for adverse effects is advised, though renal excretion is not a major elimination pathway.
- Lung - Monitor closely for pulmonary adverse events, especially pleural effusion, pulmonary hypertension, and interstitial lung disease, which are known side effects.
Disclaimer
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