Dasatinib

ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS

Key facts

Dasatinib is an ofp drug catalogued in DrugCentral. It was first approved by the FDA in 2006. DrugCentral lists 145 molecular targets, including EPHB6, Lck and EPHA3. Recorded indications include Blastic phase chronic myeloid leukemia, Chronic Myelocytic Leukemia Accelerated Phase, Chronic phase chronic myeloid leukemia and Philadelphia Chromosome Positive Chronic Myelocytic Leukemia.

• Approval status: ofp (first approved 2006 by the FDA).
• Molecular targets: EPHB6, Lck, EPHA3 and ABL2 (145 listed in DrugCentral).
• Indications: Blastic phase chronic myeloid leukemia, Chronic Myelocytic Leukemia Accelerated Phase, Chronic phase chronic myeloid leukemia, Philadelphia Chromosome Positive Chronic Myelocytic Leukemia and Philadelphia chromosome-positive acute lymphoblastic leukemia.
• ATC code: L01EA02 (BCR-ABL tyrosine kinase inhibitors).
• Molecular formula: C22H26ClN7O2S; molecular weight 488.01 g/mol.

Indications & contraindications

Drug–disease relationships curated by DrugCentral (OMOP / SNOMED concepts).

Indications (5)

• Blastic phase chronic myeloid leukemia
• Chronic Myelocytic Leukemia Accelerated Phase
• Chronic phase chronic myeloid leukemia
• Philadelphia Chromosome Positive Chronic Myelocytic Leukemia
• Philadelphia chromosome-positive acute lymphoblastic leukemia

Contraindications (20)

• Acute hemorrhage
• Anemia
• Ascites
• Body fluid retention
• Breastfeeding (mother)
• Cerebral hemorrhage
• Chronic heart failure
• Congenital long QT syndrome
• Disease of liver
• Edema
• Gastrointestinal hemorrhage
• Left heart failure
• Myocardial infarction
• Neutropenic disorder
• Pericardial effusion
• Pleural Effusions
• Pregnancy, function
• Prolonged QT interval
• Thrombocytopenic disorder
• Torsades de pointes

Mechanism & targets

Molecular targets (145)

Target	Gene	Action	Activity
Ephrin type-B receptor 6	EPHB6	unknown	Kd 10.41
Proto-oncogene tyrosine-protein kinase LCK	Lck	unknown	Ki 10.19
Ephrin type-A receptor 3	EPHA3	unknown	Kd 10.03
Abelson tyrosine-protein kinase 2	ABL2	unknown	Kd 9.77
Tyrosine-protein kinase Lck	LCK	inhibitor	Kd 9.70
Tyrosine-protein kinase Blk	BLK	inhibitor	Kd 9.68
Proto-oncogene tyrosine-protein kinase Src	SRC	inhibitor	Kd 9.68
Ephrin type-A receptor 5	EPHA5	unknown	Kd 9.62
Ephrin type-A receptor 8	EPHA8	unknown	Kd 9.62
Tyrosine-protein kinase ABL1	ABL1	inhibitor	IC50 9.60
Tyrosine-protein kinase Yes	YES1	inhibitor	Kd 9.52
Tyrosine-protein kinase FRK	FRK	inhibitor	Kd 9.51
Ephrin type-B receptor 4	EPHB4	unknown	Kd 9.47
Tyrosine-protein kinase HCK	HCK	inhibitor	Kd 9.46
Ephrin type-B receptor 2	EPHB2	unknown	Kd 9.41
Ephrin type-B receptor 1	EPHB1	unknown	Kd 9.35
Platelet-derived growth factor receptor alpha	PDGFRA	unknown	Kd 9.33
Tyrosine-protein kinase Fgr	FGR	inhibitor	Kd 9.30
Tyrosine-protein kinase Lyn	LYN	inhibitor	Kd 9.24
Macrophage colony-stimulating factor 1 receptor	CSF1R	unknown	Kd 9.24

Regulatory approvals (2)

Date	Agency	Marketed as	Applicant	Orphan
2006-11-20	EMA	—	BRISTOL-MYERS SQUIBB PHARMA EEIG
2006-06-28	FDA	—	BRISTOL MYERS SQUIBB	Yes

ATC classification

ATC code	Therapeutic hierarchy
L01EA02	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS › ANTINEOPLASTIC AGENTS › PROTEIN KINASE INHIBITORS › BCR-ABL tyrosine kinase inhibitors

Pharmacogenomics

Drug-label and guideline annotations from PharmGKB and CPIC.

• EMA label: ABL1, BCR · Testing Required
• FDA label: ABL1, BCR · Testing Required
• HCSC label: ABL1, BCR · Testing Required
• PMDA label: ABL1, BCR · Testing Required

Reported adverse-event signals

Strongest FDA FAERS disproportionality signals (log-likelihood ratio). A signal is a statistical association in spontaneous reports, not proof that the drug causes the event.

MedDRA term	LLR
Pleural effusion	4890.3
Drug resistance	1015.5
Philadelphia chromosome positive	911.3
Adverse event	823.1
Hospitalisation	789.9
Cytogenetic analysis abnormal	679.1
Pulmonary oedema	669.1
Chylothorax	647.8
Acute lymphocytic leukaemia recurrent	600.8
Malignant neoplasm progression	562.9
Blast crisis in myelogenous leukaemia	492.4
Hepatotoxicity	479.5

Chemical structure

Full physicochemical, ADMET and 3D-structure analysis of Dasatinib is on its molecule page.

• Molecular formula: C₂₂H₂₆ClN₇O₂S
• Molecular weight: 488.01 g/mol
• CAS number: 302962-49-8
• InChIKey: ZBNZXTGUTAYRHI-UHFFFAOYSA-N
• PubChem CID: 3062316

CC1=NC(NC2=NC=C(S2)C(=O)NC2=C(C)C=CC=C2Cl)=CC(=N1)N1CCN(CCO)CC1

Frequently asked questions

Answers are generated from the structured data on this page, not written by hand.

What is Dasatinib used for?

DrugCentral lists the following indications for Dasatinib: Blastic phase chronic myeloid leukemia, Chronic Myelocytic Leukemia Accelerated Phase, Chronic phase chronic myeloid leukemia, Philadelphia Chromosome Positive Chronic Myelocytic Leukemia and Philadelphia chromosome-positive acute lymphoblastic leukemia.

How does Dasatinib work?

Its molecular targets in DrugCentral include EPHB6, Lck, EPHA3 and ABL2.

When was Dasatinib first approved?

Dasatinib was first approved by the FDA in 2006.

What is the chemical formula of Dasatinib?

Dasatinib has the molecular formula C22H26ClN7O2S and a molecular weight of 488.01 g/mol.

Sources

• DrugCentral drug card 785 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
• ChEMBL CHEMBL1421 — compound record and bioactivity
• PubChem CID 3062316 — chemical identifiers
• DrugBank DB01254 — drug record
• FDA UNII RBZ1571X5H — substance identity
• DailyMed: FDA labels for Dasatinib — current prescribing information (label search)
• UniProt O15197 (EPHB6) — target protein
• UniProt P29320 (EPHA3) — target protein
• UniProt P42684 (ABL2) — target protein
• UniProt P06239 (LCK) — target protein
• UniProt P51451 (BLK) — target protein
• UniProt P12931 (SRC) — target protein
• FDA Adverse Event Reporting System (openFDA FAERS) — adverse-event signals, as aggregated by DrugCentral
• PharmGKB / CPIC — pharmacogenomic label annotations

How this page is built: methodology · editorial policy & corrections.