Dasatinib
SPRYCEL
What it isBCR-ABL and SRC family tyrosine kinase inhibitor; CML and Philadelphia-positive ALL.
Why this oneIt penetrates the CNS and overcomes most imatinib-resistant mutations.
What limits itPleural effusion in a substantial minority, and pulmonary hypertension. Acid suppression reduces absorption; myelosuppression.
FDA-approved for
- CML (2006)
FDA label
Read the full label on DailyMed ↗
| FDA dosing | Population | Start | Target | Max |
|---|---|---|---|---|
| Chronic phase CML | Adults | 100 mg QD | 100 mg QD | per dose escalation |
| Accelerated/myeloid or lymphoid blast phase CML, or Ph+ ALL | Adults | 140 mg QD | 140 mg QD | per dose escalation |
| Chronic phase CML or Ph+ ALL | Pediatric (>=10 kg) | Weight-based QD (10-<20 kg 40 mg; 20-<30 kg 60 mg; 30-<45 kg 70 mg; >=45 kg 100 mg) | per weight | per weight/escalation |
Renal Undefined
Hepatic Undefined
Instructions
- Take orally once daily, with or without a meal.
- Swallow whole; do not crush, cut, or chew.
- Recalculate pediatric dose every 3 months for weight changes.
- Avoid concomitant strong CYP3A4 inducers and St. John's wort.
- For Ph+ ALL peds: begin on/before day 15 of induction, continue 2 years.
Cautions
- Myelosuppression
- Bleeding-related events
- Fluid retention (incl. pleural/pericardial effusion)
- Cardiovascular toxicity
- Pulmonary arterial hypertension
- QT prolongation
- Severe dermatologic reactions
- Tumor lysis syndrome
- Effects on growth/development in pediatrics
- Hepatotoxicity
Adverse reactions
- Adults, single agent (≥15%): myelosuppression
- Fluid retention events
- Diarrhea
- Headache
- Skin rash
- Hemorrhage
- Dyspnea
- Fatigue
- Nausea
- Musculoskeletal pain
- Pediatric + chemotherapy (≥30%): mucositis, febrile neutropenia, pyrexia, diarrhea, nausea/vomiting, musculoskeletal/abdominal pain, cough, headache, rash, fatigue, constipation, arrhythmia, hypertension, edema, infections, hypotension, decreased appetite, hypersensitivity, dyspnea, epistaxis, peripheral neuropathy, altered consciousness
Pregnancy Can cause fetal harm (hydrops fetalis, fetal leukopenia/thrombocytopenia); animal embryofetal toxicity.
Lactation Undefined
NO BOXED WARNINGS
Principal riskPleural effusion; pulmonary hypertension
Cost, est. cash$5,000–$30,000+/month or cycle
Generic entry2016
Classes and tags
Clinical profile
Legacy pregnancy categoryD
Defining liabilityMyelosuppression and agent-specific hepatic, cardiac, pulmonary, neurologic or reproductive toxicity require oncology monitoring.
Mechanism of action: Dasatinib ballicule
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