Dasatinib

Dasatinib, at nanomolar concentrations, inhibits the following kinases: BCR-ABL, SRC family (SRC, LCK, YES, FYN), c-KIT, EPHA2, and PDGFRβ. Based on modeling studies, dasatinib is predicted to bind to multiple conformations of the ABL kinase.

• Dasatinib tablets are indicated for the treatment of adult patients with newly diagnosed Philadelphia chromosome-positive (Ph+) chronic myeloid leukemia (CML) in chronic phase. chronic, accelerated, or myeloid or lymphoid blast phase Ph+ CML with resistance or intolerance to prior therapy including imatinib.ICD-10: C95.90

• None. None.contraindicated

Chronic phase CML in adults: 100 mg once daily. ( 2 ) Accelerated phase CML, myeloid or lymphoid blast phase CML, or Ph+ ALL in adults: 140 mg once daily. ( 2 ) Chronic phase CML and ALL in pediatrics: starting dose based on body weight. ( 2 ) Administer orally, with or without a meal. Do not crush, cut, or chew tablets. ( 2 ) 2.1 Dosage of Dasatinib Tablets in Adult Patients The recommended starting dosage of dasatinib tablets for chronic phase CML in adults is 100 mg administered orally once daily. The recommended starting dosage of dasatinib tablets for accelerated phase CML, myeloid or lymphoid blast phase CML, or Ph+ ALL in adults is 140 mg administered orally once daily. Tablets should not be crushed, cut, or chewed; they should be swallowed whole. Dasatinib tablets can be taken with or without a meal, either in the morning or in the evening. 2.2 Dosage of Dasatinib Tablets in Pediatric Patients with CML or Ph+ ALL The recommended starting dosage for pediatrics is based on body weight as shown in Table 1. The recommended dose should be administered orally once daily with or without food. Recalculate the dose every 3 months based on changes in body weight, or more often if necessary. Do not crush, cut or chew tablets. Swallow tablets whole. There are additional administration considerations for pediatric patients who have difficulty swallowing tablets whole [see Use in Specific Populations (8.4) and Clinical Pharmacology (12.3)].

Myelosuppression and Bleeding Events: Severe thrombocytopenia, neutropenia, and anemia may occur. Use caution if used concomitantly with medications that inhibit platelet function or anticoagulants. Monitor complete blood counts regularly. Transfuse and interrupt dasatinib tablets when indicated. ( 2.5 , 5.1 , 5.2 ) Fluid Retention: Fluid retention, sometimes severe, including pleural effusions. Manage with supportive care measures and/or dose modification. ( 2.5 , 5.3 ) Cardiovascular Toxicity: Monitor patients for signs or symptoms and treat appropriately. ( 5.4 ) Pulmonary Arterial Hypertension (PAH): Dasatinib tablets may increase the risk of developing PAH which may be reversible on discontinuation. Consider baseline risk and evaluate patients for signs and symptoms of PAH during treatment. Stop dasatinib tablets if PAH is confirmed. ( 5.5 ) QT Prolongation: Use dasatinib tablets with caution in patients who have or may develop prolongation of the QT interval. ( 5.6 ) Severe Dermatologic Reactions: Individual cases of severe mucocutaneous dermatologic reactions have been reported. ( 5.7 ) Tumor Lysis Syndrome: Tumor lysis syndrome has been reported. Maintain adequate hydration and correct uric acid levels prior to initiating therapy with dasatinib tablets. ( 5.8 ) Embryo-Fetal Toxicity: Can cause fetal harm. Advise patients of reproductive potential of potential risk to fetus and to use effective contraception.

The following clinically significant adverse reactions are discussed in greater detail in other sections of the labeling: • Myelosuppression [see Dosage and Administration (2.5) and Warnings and Precautions (5.1) ] . • Bleeding-related events [see Warnings and Precautions (5.2) ] . • Fluid retention [see Warnings and Precautions (5.3) ] . • Cardiovascular toxicity [see Warnings and Precautions (5.4) ] . • Pulmonary arterial hypertension [see Warnings and Precautions (5.5) ] . • QT prolongation [see Warnings and Precautions (5.6) ] . • Severe dermatologic reactions [see Warnings and Precautions (5.7) ] . • Tumor lysis syndrome [see Warnings and Precautions (5.8) ] . • Effects on growth and development in pediatric patients [see Warnings and Precautions (5.10) ] . • Hepatotoxicity [see Warnings and Precautions (5.11) ] . Most common adverse reactions (≥15%) in patients receiving dasatinib tablets as single-agent therapy included myelosuppression, fluid retention events, diarrhea, headache, skin rash, hemorrhage, dyspnea, fatigue, nausea, and musculoskeletal pain. ( 6 ) Most common adverse reactions (≥30%) in pediatric patients receiving dasatinib tablets in combination with chemotherapy included mucositis, febrile neutropenia, pyrexia, diarrhea, nausea, vomiting, musculoskeletal pain, abdominal pain, cough, headache, rash, fatigue, constipation, arrhythmia, hypertension, edema, infections (bacterial, viral and fungal), hypotension, decreased appetite, hypersensitivity, dyspnea, epistaxis, peripheral neuropathy, and altered state of consciousness.

Lactation: Advise women not to breastfeed. ( 8.2 ) 8.1 Pregnancy Risk Summary Based on limited human data, dasatinib can cause fetal harm when administered to a pregnant woman. Adverse pharmacologic effects including hydrops fetalis, fetal leukopenia, and fetal thrombocytopenia have been reported with maternal exposure to dasatinib. Animal reproduction studies in rats have demonstrated extensive mortality during organogenesis, the fetal period, and in neonates. Skeletal malformations were observed in a limited number of surviving rat and rabbit conceptuses. These findings occurred at dasatinib plasma concentrations below those in humans receiving therapeutic doses of dasatinib [see Data] . Advise a pregnant woman of the potential risk to a fetus. The estimated background risk in the U.S. general population of major birth defects is 2% to 4% and of miscarriage is 15% to 20% of clinically recognized pregnancies. Clinical Considerations Fetal/Neonatal Adverse Reactions Transplacental transfer of dasatinib has been reported. Dasatinib has been measured in fetal plasma and amniotic fluid at concentrations comparable to those in maternal plasma. Hydrops fetalis, fetal leukopenia, and fetal thrombocytopenia have been reported with maternal exposure to dasatinib.

Metabolism

The pharmacokinetics of dasatinib exhibits dose proportional increases in AUC and linear elimination characteristics over the dose range of 15 mg/day (0.15 times the lowest approved recommended dose) to 240 mg/day (1.7 times the highest approved recommended dose). At 100 mg QD, the maximum concentration at steady state (C max ) is 82.2 ng/mL (CV% 69%), area under the plasma drug concentration time curve (AUC) is 397 ng/mL*hr (CV% 55%).

Experience with overdose of dasatinib in clinical studies is limited to isolated cases. The highest overdosage of 280 mg per day for 1 week was reported in two patients and both developed severe myelosuppression and bleeding. Since dasatinib is associated with severe myelosuppression [see Warnings and Precautions (5.1) and Adverse Reactions (6.1) ] , monitor patients who ingest more than the recommended dosage closely for myelosuppression and give appropriate supportive treatment. Acute overdose in animals was associated with cardiotoxicity. Evidence of cardiotoxicity included ventricular necrosis and valvular/ventricular/atrial hemorrhage at single doses ≥100 mg/kg (600 mg/m 2 ) in rodents. There was a tendency for increased systolic and diastolic blood pressure in monkeys at single doses ≥10 mg/kg (120 mg/m 2 ).

• Jun 28, 2006NDANDA021986Bristol Myers Squibb
• Jun 10, 2016ANDAANDA202103Apotex
• Nov 23, 2021ANDAANDA203180Apotex
• Dec 5, 2023NDANDA216099Handa Therap
• Mar 3, 2025ANDAANDA217217Biocon Pharma
• Mar 3, 2025ANDAANDA218719Zydus Pharms
• Mar 3, 2025ANDAANDA213383Dr Reddys
• Apr 22, 2025ANDAANDA216547Eugia Pharma

1. 1Pleural Effusion3,2168.8%
2. 2Fatigue2,5296.9%
3. 3Diarrhoea2,1605.9%
4. 4Nausea2,1315.8%
5. 5Death2,0885.7%
6. 6Headache1,9955.5%
7. 7Rash1,5914.3%
8. 8Drug Ineffective1,5094.1%
9. 9Dyspnoea1,4934.1%
10. 10Adverse Event1,4694.0%
11. 11Off Label Use1,2383.4%
12. 12Hospitalisation1,2043.3%
13. 13Pulmonary Oedema1,0052.7%
14. 14Vomiting9492.6%
15. 15Pyrexia8842.4%

Recent PubMed references pinned to Dasatinib as a MeSH major topic. Citations link to pubmed.ncbi.nlm.nih.gov.

• A Comprehensive Echocardiographic Assessment of Patients With Chronic Myeloid Leukemia on Dasatinib.
  Echocardiography (Mount Kisco, N.Y.) · 2026 · Chen C, Appadurai V, Hernandez MP, et al.
  PMID 42206579DOI 10.1111/echo.70517
• [Safety of blinatumomab combined with dasatinib in the treatment of pediatric Philadelphia chromosome-positive acute lymphoblastic leukemia].
  Zhongguo dang dai er ke za zhi = Chinese journal of contemporary pediatrics · 2026 · Zheng FY, Ding MM, Lu AD, et al.
  PMID 42015695DOI 10.7499/j.issn.1008-8830.2508146
• Senolytics alleviate cyclophosphamide-induced premature ovarian insufficiency by eliminating senescent cells.
  European journal of histochemistry : EJH · 2026 · Su H, Ma R, Su D, et al.
  PMID 42011821DOI 10.4081/ejh.2026.4537
• Dasatinib and quercetin senolytic treatment delays early onset intervertebral disc degeneration in SM/J mice.
  Bone research · 2026 · Novais EJ, Ottone OK, Jagannath S, et al.
  PMID 41974671DOI 10.1038/s41413-026-00526-4
• Response-adapted dasatinib de-escalation strategy compared to upfront Low-dose dasatinib: A prospective cohort study.
  Leukemia research · 2026 · Halder R, Singh R, Rainchwar S, et al.
  PMID 41932299DOI 10.1016/j.leukres.2026.108218
• Outcomes of Patients Treated With Dasatinib 50 mg/d: A Pooled Analysis.
  Clinical lymphoma, myeloma & leukemia · 2026 · Haddad FG, Jabbour E, Sasaki K, et al.
  PMID 41876352DOI 10.1016/j.clml.2026.02.013
• Dasatinib boosts γδ T cell expansion and memory phenotypes with enhanced antitumor immunity.
  Cancer immunology, immunotherapy : CII · 2026 · Lin JR, Song YC, Chou YL, et al.
  PMID 41770421DOI 10.1007/s00262-026-04335-w
• Nitrogen blowing DµSPE of sunitinib, imatinib, and dasatinib using LDH/MIL-101(Cr)-NO(2) composite prior to HPLC-PDA.
  Bioanalysis · 2026 · Mottagi Khosrowshahi H, Abolhasani J, Afshar Mogaddam MR, et al.
  PMID 41755504DOI 10.1080/17576180.2026.2631964

The 10 most recently updated of 409 ClinicalTrials.gov registrations naming Dasatinib as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

• A Study on the Tolerability, Safety and Effectiveness of Asciminib in Patients With Philadelphia Chromosome-positive Chronic Myeloid Leukemia in the Chronic Phase in Germany
  Recruiting · Observational · 380 enrolled · Novartis Pharmaceuticals
  NCT07549516updated 2026-06-12
• Phase II Study Assessing the Safety and Efficacy of Dasatinib in Combination With Ropeginterferon in Patients With Newly Diagnosed Chronic Myeloid Leukemia in Chronic Phase
  Not yet recruiting · Phase 2 · Interventional · 40 enrolled · M.D. Anderson Cancer Center
  NCT07269470updated 2026-06-11
• Dasatinib in Combination With Bevacizumab to Treat Advanced Solid Tumors
  Completed · Phase 1 · Interventional · 50 enrolled · National Cancer Institute (NCI)
  NCT01445509updated 2026-06-11
• Asciminib Roll-over Study
  Recruiting · Phase 4 · Interventional · 347 enrolled · Novartis Pharmaceuticals
  NCT04877522updated 2026-06-10
• A Study of Oral Asciminib Versus Other TKIs in Adult Patients With Newly Diagnosed Ph+ CML-CP
  Active not recruiting · Phase 3 · Interventional · 405 enrolled · Novartis Pharmaceuticals
  NCT04971226updated 2026-06-08
• Study of Chemotherapy-Free Induction Regimen for Ph+ Acute Lymphoblastic Leukemia With Inotuzumab Ozogamicin (InO)
  Recruiting · Phase 2 · Interventional · 25 enrolled · University of Chicago
  NCT04747912updated 2026-06-05
• Dasatinib for HIV-1 Reservoir Reduction
  Recruiting · Phase 1 · Interventional · 14 enrolled · National Institute of Allergy and Infectious Diseases (NIAID)
  NCT07342491updated 2026-06-04
• Targeted Therapy Directed by Genetic Testing in Treating Patients With Advanced Refractory Solid Tumors, Lymphomas, or Multiple Myeloma (The MATCH Screening Trial)
  Active not recruiting · Phase 2 · Interventional · 6,452 enrolled · National Cancer Institute (NCI)
  NCT02465060updated 2026-06-03
• A Study Testing the Combination of Dasatinib or Imatinib to Chemotherapy Treatment With Blinatumomab for Children, Adolescents, and Young Adults With Philadelphia Chromosome Positive (Ph+) or ABL-Class Philadelphia Chromosome-Like (Ph-Like) B-cell Acute Lymphoblastic Leukemia (B-ALL)
  Recruiting · Phase 2 · Interventional · 222 enrolled · National Cancer Institute (NCI)
  NCT06124157updated 2026-06-03
• Asciminib as Initial Therapy for Patients With Chronic Myeloid Leukemia in Chronic Phase
  Recruiting · Phase 2 · Interventional · 100 enrolled · University of Alabama at Birmingham
  NCT05143840updated 2026-06-02

Frequently asked questions

How does Dasatinib work?

Dasatinib, at nanomolar concentrations, inhibits the following kinases: BCR-ABL, SRC family (SRC, LCK, YES, FYN), c-KIT, EPHA2, and PDGFRβ. Based on modeling studies, dasatinib is predicted to bind to multiple conformations of the ABL kinase.

What is Dasatinib used for?

According to FDA labeling, Dasatinib carries indications including: Dasatinib tablets are indicated for the treatment of adult patients with newly diagnosed Philadelphia chromosome-positive (Ph+) chronic myeloid leukemia (CML) in chronic phase. chronic, accelerated, or myeloid or lymphoid blast phase Ph+ CML with resistance or intolerance to prior therapy including imatinib.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.

What class of drug is Dasatinib?

Dasatinib is classified as BCR-ABL tyrosine kinase inhibitors, Protein Kinase Inhibitors, Cellular Proliferation Alteration.

What are the brand names for Dasatinib?

Dasatinib is marketed under brand names including Phyrago, Sprycel.

What are the contraindications for Dasatinib?

Dasatinib labeling lists contraindications including: None. None.. Always consult the full prescribing information and a clinician.