Dasanix 50 mg (Tablet)

Indications

• Treatment of adult patients with Philadelphia chromosome-positive (Ph+) chronic myeloid leukemia (CML)
• Treatment of pediatric patients 1 year of age and older with Ph+ CML in chronic phase
• Treatment of newly diagnosed Ph+ acute lymphoblastic leukemia (ALL)
• Treatment of newly diagnosed Ph+ ALL in combination with chemotherapy

Pharmacology

• Inhibition of BCR-ABL, SRC family, c-KIT, EPHA2, and PDGFRβ kinases
• Modeling studies predicting binding to multiple conformations of the ABL kinase
• Activity in leukemic cell lines representing variants of imatinib mesylate-sensitive and resistant disease
• Inhibition of CML and ALL cell lines overexpressing BCR-ABL
• Prediction of overcoming imatinib resistance and multi-drug resistance gene overexpression

Absorption

Cmax observed between 0.5 to 6 hours, increased AUC with high-fat meal

Distribution

• Apparent volume of distribution: 2505 (CV% 93%)
• Binding of Dasatinib to human plasma proteins: approximately 96%
• P-gp substrate in vitro

Elimination

• Mean terminal half-life: 3 to 5 hours
• Apparent oral clearance: 363.8 l/hr (CV% 81.3%)
• Primary metabolism by CYP3A4
• Excretion primarily via feces

Dosage & Administration

• Recommended starting dosage: 100 mg once daily for chronic phase CML in adults, 140 mg once daily for accelerated phase CML or Ph+ ALL in adults
• Recommended starting dosages for pediatric patients based on body weight
• Tablets should not be crushed, cut, or chewed, and can be taken with or without a meal

Interaction

• Strong CYP3A4 inhibitors may increase Dasanix concentrations
• Strong CYP3A4 inducers may decrease Dasanix concentrations
• Coadministration with gastric acid reducing agents may decrease Dasanix concentrations

Contraindications

Known hypersensitivity to Dasatinib or 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

Potential fetal harm, effective contraceptive methods advised for females of reproductive potential, breastfeeding not recommended

Precautions & Warnings

• Severe (NCT CTCAE Grade 3 or 4) thrombocytopenia, neutropenia, and anemia
• Bleeding-related events
• Fluid retention
• Cardiovascular events
• Pulmonary arterial hypertension
• QT prolongation
• Severe dermatologic reactions
• Tumor lysis syndrome

Overdose Effects

Experience limited to isolated cases, severe myelosuppression and bleeding reported

Therapeutic Class

Targeted Cancer Therapy

Storage Conditions

Store below 30°C in a dry place, protect from light, keep out of reach of children

Related Brands

• Dasanix 20 mg (Tablet) - beacon-pharmaceuticals-plc
• Dasanix 100 mg (Tablet) - beacon-pharmaceuticals-plc