Home → Drug Library → Sprycel

Sprycel

dasatinib
BCR-ABL/SRC Kinase Inhibitor BMS FDA Approved 2006
Indications Dosing Forms Contraindications Warnings Adverse Reactions Pharmacology Clinical Studies Tumor Types
1. Indications and Usage

Newly diagnosed adults with Ph+ CML in chronic phase; Ph+ CML with resistance or intolerance to prior therapy including imatinib (chronic, accelerated, or myeloid/lymphoid blast phase); Ph+ ALL with resistance or intolerance to prior therapy; Pediatric patients with Ph+ CML in chronic phase.

2. Dosage and Administration

CML chronic phase: 100 mg orally once daily
CML accelerated/blast or Ph+ ALL: 140 mg orally once daily (may increase to 180 mg)
Pediatric: Tablets dosed by body weight; oral powder formulation available
Take with or without food. Do not crush or cut tablets.

3. Dosage Forms and Strengths

Tablets: 20 mg, 50 mg, 70 mg, 80 mg, 100 mg, 140 mg

4. Contraindications

None listed.

5. Warnings and Precautions
  • Myelosuppression: Grade 3-4 neutropenia (36%), thrombocytopenia (24%), anemia (13%). Monitor CBC every 2 weeks × 12 weeks, then monthly.
  • Pleural Effusion: In 28% of CML-CP patients (Grade 3-4 in 3%). Consider chest X-ray if respiratory symptoms develop.
  • Pulmonary Arterial Hypertension (PAH): May occur after initiation, including years after start. Evaluate if suspected; permanently D/C if confirmed.
  • Cardiac Dysfunction: CHF, QT prolongation, MI reported. Monitor ECGs and electrolytes.
  • Hemorrhage: Severe CNS and GI hemorrhage reported (4%). Fatal hemorrhage in 1%.
  • Fluid Retention: Edema (23%), pleural effusion (28%), pericardial effusion (4%), ascites (1%).
6. Adverse Reactions
Most Common Adverse Reactions

Fluid retention (35%), diarrhea (31%), headache (33%), pleural effusion (28%), musculoskeletal pain (22%), rash (21%), nausea (24%), fatigue (19%), dyspnea (17%), hemorrhage (15%), vomiting (12%)

Fluid retention
35%
Headache
33%
Diarrhea
31%
Pleural Effusion
28%
Nausea
24%
Musculoskeletal Pain
22%
Rash
21%
Fatigue
19%
Dyspnea
17%
Hemorrhage
15%

Consult the complete prescribing information for a comprehensive list of adverse reactions and their frequencies.

12. Clinical Pharmacology
Mechanism of Action

Dasatinib is a kinase inhibitor that inhibits BCR-ABL, SRC family kinases (SRC, LCK, YES, FYN), c-KIT, EPHA2, and PDGFRβ. It binds to multiple conformations of ABL kinase, including both active and inactive forms, making it effective against many imatinib-resistant BCR-ABL mutations (except T315I). Dasatinib achieves 325-fold greater potency against unmutated BCR-ABL compared to imatinib in vitro.

Pharmacokinetics

Tmax: 0.5-6 hours. Half-life: 3-5 hours. Protein binding: 96%. Metabolized primarily by CYP3A4. Excreted in feces (85%) and urine (4%). Steady-state by Day 7.

14. Clinical Studies

Clinical efficacy and safety data supporting the approval are available in the full prescribing information and from the clinical trials listed below.

Pivotal Clinical Trials
Additional Resources
📋 All Dasatinib Trials on ClinicalTrials.gov ↗ 📚 PubMed: Dasatinib Clinical Trials ↗
Approved Tumor Types
Chronic Myeloid Leukemia