Dasaren 140 mg (Tablet)

Indications

• Treatment of Philadelphia chromosome-positive chronic myeloid leukemia in chronic phase
• Treatment of Chronic, accelerated, or myeloid or lymphoid blast phase CML with resistance or intolerance to prior therapy including Imatinib
• Treatment of Philadelphia chromosome-positive acute lymphoblastic leukemia with resistance or intolerance to prior therapy
• Treatment of pediatric patients 1 year of age and older with Ph+ CML in chronic phase

Pharmacology

• Inhibition of BCR-ABL, SRC family, c-KIT, EPHA2, and PDGFRβ kinases
• Active against leukemic cell lines overexpressing BCR-ABL
• Active in variants of imatinib mesylate-sensitive and resistant disease
• Predicted to bind to multiple conformations of the ABL kinase
• Absorption between 0.5 to 6 hours following oral administration
• Apparent volume of distribution is 2505 (CV% 93%)
• Metabolized primarily by CYP3A4
• Elimination primarily via the feces

Dosage & Administration

• Recommended starting dosage for chronic phase CML in adults: 100 mg once daily
• Recommended starting dosage for accelerated phase CML, myeloid or lymphoid blast phase CML, or Ph+ ALL in adults: 140 mg once daily
• Recommended starting dosage for pediatric patients varies with body weight
• Tablets should not be crushed, cut, or chewed, they should be swallowed whole

Interaction

• Coadministration with strong CYP3A inhibitors can increase Dasaren concentrations
• Concomitant use of strong CYP3A4 inhibitors should be avoided
• Coadministration with strong CYP3A inducers may decrease Dasaren concentrations and reduce efficacy
• Coadministration with gastric acid reducing agents may decrease Dasaren concentrations

Contraindications

• Known hypersensitivity to Dasatinib or to any component of the formulation

Side Effects

• Myelosuppression
• Bleeding-related events
• Fluid retention
• Cardiovascular events
• Pulmonary arterial hypertension
• QT prolongation
• Severe dermatologic reactions
• Tumor lysis syndrome
• Effects on growth and development in pediatric patients

Pregnancy & Lactation

• Can cause fetal harm when administered to a pregnant woman
• Females of reproductive potential should use effective contraceptive methods during treatment and for 30 days after the final dose
• Breastfeeding is not recommended during treatment and for 2 weeks after the final dose

Precautions & Warnings

• Severe thrombocytopenia, neutropenia, and anemia
• Bleeding that can be serious and fatal
• Potential for fluid retention
• Risk of cardiac dysfunction
• Possible development of pulmonary arterial hypertension
• Risk of QT prolongation
• Potential for severe mucocutaneous dermatologic reactions
• Possibility of tumor lysis syndrome

Overdose Effects

• Severe myelosuppression and bleeding reported with 280 mg per day for 1 week

Therapeutic Class

• Targeted Cancer Therapy

Storage Conditions

• Store below 30°C in a dry place
• Protect from light
• Keep out of the reach of children

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