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dasatinib 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
tyrosine kinase inhibitors	785	302962-49-8

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: dasatinib sprycel spyrcel BMS-354825 dasatinib hydrate	A pyrimidine and thiazole derived ANTINEOPLASTIC AGENT and PROTEIN KINASE INHIBITOR of BCR-ABL KINASE. It is used in the treatment of patients with CHRONIC MYELOID LEUKEMIA who are resistant or intolerant to IMATINIB. Molecular weight: 488.01 Formula: C22H26ClN7O2S CLOGP: 2.71 LIPINSKI: 0 HAC: 9 HDO: 3 TPSA: 106.51 ALOGS: -4.58 ROTB: 7 Status: ONP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

dasatinib
sprycel
spyrcel
BMS-354825
dasatinib hydrate

A pyrimidine and thiazole derived ANTINEOPLASTIC AGENT and PROTEIN KINASE INHIBITOR of BCR-ABL KINASE. It is used in the treatment of patients with CHRONIC MYELOID LEUKEMIA who are resistant or intolerant to IMATINIB.

Molecular weight: 488.01
Formula: C22H26ClN7O2S
CLOGP: 2.71
LIPINSKI: 0
HAC: 9
HDO: 3
TPSA: 106.51
ALOGS: -4.58
ROTB: 7

Status: ONP

Legend:
OFP - off patent
OFM - off market
ONP - on patent

Drug dosage:

Dose	Unit	Route
0.10	g	O

ADMET properties:

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Property	Value	Reference
MRTD (Maximum Recommended Therapeutic Daily Dose)	5.85 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BDDCS (Biopharmaceutical Drug Disposition Classification System)	2	Benet LZ, Broccatelli F, Oprea TI
BA (Bioavailability)	15 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
EoM (Fraction excreted unchanged in urine)	0.10 %	Benet LZ, Broccatelli F, Oprea TI

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Approvals:

Date	Agency	Company	Orphan
June 28, 2006	FDA	BRISTOL MYERS SQUIBB
Nov. 20, 2006	EMA	BRISTOL-MYERS SQUIBB PHARMA EEIG

FDA Adverse Event Reporting System (Female)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Pleural effusion	1431.28	18.52	667	20102	92543	63375710
Cytogenetic analysis abnormal	339.31	18.52	75	20694	845	63467408
Adverse event	322.54	18.52	226	20543	67333	63400920
Drug resistance	316.35	18.52	153	20616	22780	63445473
Hospitalisation	257.35	18.52	217	20552	84864	63383389
Philadelphia chromosome positive	252.68	18.52	51	20718	355	63467898
Pulmonary oedema	246.63	18.52	177	20592	54696	63413557
Prescribed underdose	243.68	18.52	140	20629	29549	63438704
Malignant neoplasm progression	215.11	18.52	193	20576	81928	63386325
Acute lymphocytic leukaemia recurrent	213.20	18.52	62	20707	2207	63466046

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FDA Adverse Event Reporting System (Male)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Pleural effusion	1811.75	15.62	897	19289	80649	34856096
Adverse event	471.22	15.62	226	19960	18651	34918094
Drug resistance	442.11	15.62	240	19946	25687	34911058
Philadelphia chromosome positive	346.23	15.62	72	20114	304	34936441
Prescribed underdose	272.61	15.62	123	20063	8810	34927935
Hospitalisation	259.24	15.62	234	19952	56668	34880077
Malignant neoplasm progression	248.13	15.62	279	19907	87767	34848978
Cytogenetic analysis abnormal	247.20	15.62	62	20124	677	34936068
Chylothorax	229.09	15.62	59	20127	722	34936023
Drug intolerance	208.72	15.62	212	19974	59358	34877387

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FDA Adverse Event Reporting System (Geriatric)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Pleural effusion	2698.34	15.38	1250	29825	144012	79569301
Drug resistance	531.23	15.38	280	30795	41933	79671380
Philadelphia chromosome positive	462.81	15.38	95	30980	595	79712718
Chylothorax	411.80	15.38	88	30987	687	79712626
Malignant neoplasm progression	357.57	15.38	346	30729	135644	79577669
Cytogenetic analysis abnormal	322.32	15.38	78	30997	1112	79712201
Pulmonary oedema	289.05	15.38	254	30821	88000	79625313
Pericardial effusion	283.18	15.38	193	30882	46044	79667269
Hospitalisation	272.77	15.38	253	30822	93983	79619330
Prescribed underdose	262.59	15.38	156	30919	29358	79683955

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	L01EA02	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS ANTINEOPLASTIC AGENTS PROTEIN KINASE INHIBITORS BCR-ABL tyrosine kinase inhibitors
CHEBI has role	CHEBI:35610	antineoplastic agents
CHEBI has role	CHEBI:38637	tyrosine kinase inhibitors
CHEBI has role	CHEBI:149553	anticoronaviral drug
MeSH PA	D000970	Antineoplastic Agents
MeSH PA	D004791	Enzyme Inhibitors
MeSH PA	D047428	Protein Kinase Inhibitors

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Drug Use | Suggest Off label Use Form| |View source of the data|

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Disease	Relation	SNOMED_ID	DOID
Blastic phase chronic myeloid leukemia	indication	413656006
Chronic phase chronic myeloid leukemia	indication	413847001
Philadelphia chromosome-positive acute lymphoblastic leukemia	indication	425688002
Philadelphia Chromosome Positive Chronic Myelocytic Leukemia	indication
Chronic Myelocytic Leukemia Accelerated Phase	indication
Acute hemorrhage	contraindication	8573003
Myocardial infarction	contraindication	22298006	DOID:5844
Torsades de pointes	contraindication	31722008
Body fluid retention	contraindication	43498006
Chronic heart failure	contraindication	48447003

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🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	8.56	acidic
pKa2	7.72	Basic
pKa3	4.89	Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

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Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Exclusivity date	Description
100MG	SPRYCEL	BRISTOL MYERS SQUIBB	N021986	May 30, 2008	RX	TABLET	ORAL	Nov. 9, 2024	TREATMENT OF PEDIATRIC PATIENTS WITH PHILADELPHIA CHROMOSOME-POSITIVE (PH+) CHRONIC MYELOID LEUKEMIA (CML) IN CHRONIC PHASE
100MG	SPRYCEL	BRISTOL MYERS SQUIBB	N021986	May 30, 2008	RX	TABLET	ORAL	May 9, 2025	PEDIATRIC EXCLUSIVITY
100MG	SPRYCEL	BRISTOL MYERS SQUIBB	N021986	May 30, 2008	RX	TABLET	ORAL	Dec. 21, 2025	INDICATED FOR THE TREATMENT OF PEDIATRIC PATIENTS 1 YEAR OF AGE AND OLDER WITH NEWLY DIAGNOSED PHILADELPHIA CHROMOSOME-POSITIVE ACUTE LYMPHOBLASTIC LEUKEMIA (ALL) IN COMBINATION WITH CHEMOTHERAPY
100MG	SPRYCEL	BRISTOL MYERS SQUIBB	N021986	May 30, 2008	RX	TABLET	ORAL	June 21, 2026	PEDIATRIC EXCLUSIVITY
140MG	SPRYCEL	BRISTOL MYERS SQUIBB	N021986	Oct. 28, 2010	RX	TABLET	ORAL	Nov. 9, 2024	TREATMENT OF PEDIATRIC PATIENTS WITH PHILADELPHIA CHROMOSOME-POSITIVE (PH+) CHRONIC MYELOID LEUKEMIA (CML) IN CHRONIC PHASE
140MG	SPRYCEL	BRISTOL MYERS SQUIBB	N021986	Oct. 28, 2010	RX	TABLET	ORAL	May 9, 2025	PEDIATRIC EXCLUSIVITY
140MG	SPRYCEL	BRISTOL MYERS SQUIBB	N021986	Oct. 28, 2010	RX	TABLET	ORAL	Dec. 21, 2025	INDICATED FOR THE TREATMENT OF PEDIATRIC PATIENTS 1 YEAR OF AGE AND OLDER WITH NEWLY DIAGNOSED PHILADELPHIA CHROMOSOME-POSITIVE ACUTE LYMPHOBLASTIC LEUKEMIA (ALL) IN COMBINATION WITH CHEMOTHERAPY
140MG	SPRYCEL	BRISTOL MYERS SQUIBB	N021986	Oct. 28, 2010	RX	TABLET	ORAL	June 21, 2026	PEDIATRIC EXCLUSIVITY
20MG	SPRYCEL	BRISTOL MYERS SQUIBB	N021986	June 28, 2006	RX	TABLET	ORAL	Nov. 9, 2024	TREATMENT OF PEDIATRIC PATIENTS WITH PHILADELPHIA CHROMOSOME-POSITIVE (PH+) CHRONIC MYELOID LEUKEMIA (CML) IN CHRONIC PHASE
20MG	SPRYCEL	BRISTOL MYERS SQUIBB	N021986	June 28, 2006	RX	TABLET	ORAL	May 9, 2025	PEDIATRIC EXCLUSIVITY

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Bioactivity Summary:

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Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Mast/stem cell growth factor receptor Kit	Kinase	P10721	KIT_HUMAN	INHIBITOR	Kd	9.24	CHEMBL	CHEMBL
Proto-oncogene tyrosine-protein kinase Src	Kinase	P12931	SRC_HUMAN	INHIBITOR	Kd	9.68	CHEMBL	CHEMBL
Tyrosine-protein kinase Lck	Kinase	P06239	LCK_HUMAN	INHIBITOR	Kd	9.70	CHEMBL	CHEMBL
Tyrosine-protein kinase Yes	Kinase	P07947	YES_HUMAN	INHIBITOR	Kd	9.52	CHEMBL	CHEMBL
Tyrosine-protein kinase Fyn	Kinase	P06241	FYN_HUMAN	INHIBITOR	Kd	9.10	CHEMBL	CHEMBL
Ephrin type-A receptor 2	Kinase	P29317	EPHA2_HUMAN	INHIBITOR	Kd	9.07	CHEMBL	CHEMBL
Platelet-derived growth factor receptor beta	Kinase	P09619	PGFRB_HUMAN	INHIBITOR	Kd	9.20	CHEMBL	CHEMBL
Tyrosine-protein kinase ABL1	Kinase	P00519	ABL1_HUMAN	INHIBITOR	IC50	9.60	IUPHAR	CHEMBL
Serine/threonine-protein kinase B-raf	Kinase	P15056	BRAF_HUMAN		Kd	6.30	CHEMBL
Receptor-type tyrosine-protein kinase FLT3	Kinase	P36888	FLT3_HUMAN		Kd	5.49	CHEMBL

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External reference:

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ID	Source
1N1	PDB_CHEM_ID
011616	NDDF
21648	MMSL
3062316	PUBCHEM_CID
4025488	VUID
4025488	VANDF
422756008	SNOMEDCT_US
423658008	SNOMEDCT_US
475342	RXNORM
5678	IUPHAR_LIGAND_ID

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
SPRYCEL	HUMAN PRESCRIPTION DRUG LABEL	1	0003-0524	TABLET	70 mg	ORAL	NDA	27 sections
SPRYCEL	HUMAN PRESCRIPTION DRUG LABEL	1	0003-0524	TABLET	70 mg	ORAL	NDA	27 sections
SPRYCEL	HUMAN PRESCRIPTION DRUG LABEL	1	0003-0524	TABLET	70 mg	ORAL	NDA	27 sections
SPRYCEL	HUMAN PRESCRIPTION DRUG LABEL	1	0003-0527	TABLET	20 mg	ORAL	NDA	27 sections
SPRYCEL	HUMAN PRESCRIPTION DRUG LABEL	1	0003-0527	TABLET	20 mg	ORAL	NDA	27 sections
SPRYCEL	HUMAN PRESCRIPTION DRUG LABEL	1	0003-0527	TABLET	20 mg	ORAL	NDA	27 sections
SPRYCEL	HUMAN PRESCRIPTION DRUG LABEL	1	0003-0528	TABLET	50 mg	ORAL	NDA	27 sections
SPRYCEL	HUMAN PRESCRIPTION DRUG LABEL	1	0003-0528	TABLET	50 mg	ORAL	NDA	27 sections
SPRYCEL	HUMAN PRESCRIPTION DRUG LABEL	1	0003-0528	TABLET	50 mg	ORAL	NDA	27 sections
SPRYCEL	HUMAN PRESCRIPTION DRUG LABEL	1	0003-0852	TABLET	100 mg	ORAL	NDA	27 sections

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