dasatinib 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: 2.38 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: 2.38
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:

None

ADMET properties:

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

Approvals:

Date	Agency	Company	Orphan
June 28, 2006	FDA	BRISTOL MYERS SQUIBB

FDA Adverse Event Reporting System (Female)

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	1145.26	18.33	560	15476	82392	46587634
Prescribed underdose	312.39	18.33	127	15909	11926	46658100
Adverse event	310.36	18.33	175	15861	34009	46636017
Cytogenetic analysis abnormal	232.44	18.33	51	15985	525	46669501
Malignant neoplasm progression	212.71	18.33	177	15859	64749	46605277
Philadelphia chromosome positive	175.08	18.33	36	16000	263	46669763
Drug resistance	168.63	18.33	93	15943	17275	46652751
Exposure via body fluid	162.45	18.33	37	15999	457	46669569
Acute lymphocytic leukaemia recurrent	150.21	18.33	47	15989	2048	46667978
Hospitalisation	148.39	18.33	143	15893	63242	46606784
Pulmonary oedema	144.24	18.33	128	15908	50977	46619049
Rash	123.98	18.33	333	15703	356179	46313847
Pericardial effusion	121.56	18.33	87	15949	25456	46644570
Blast crisis in myelogenous leukaemia	114.39	18.33	28	16008	480	46669546
Chronic myeloid leukaemia	107.55	18.33	38	15998	2420	46667606
Chylothorax	103.17	18.33	23	16013	256	46669770
Fluid retention	98.92	18.33	104	15932	50942	46619084
Nausea	96.37	18.33	477	15559	686977	45983049
Diarrhoea	85.98	18.33	399	15637	559203	46110823
Headache	68.16	18.33	334	15702	478018	46192008
Fatigue	67.77	18.33	397	15639	608300	46061726
Bone pain	62.86	18.33	79	15957	46811	46623215
Death	62.57	18.33	254	15782	335294	46334732
Chronic myeloid leukaemia transformation	61.63	18.33	13	16023	109	46669917
Thrombocytopenia	56.10	18.33	130	15906	126451	46543575
Large granular lymphocytosis	51.76	18.33	12	16024	161	46669865
Blast cell crisis	51.23	18.33	10	16026	54	46669972
Acute lymphocytic leukaemia	51.20	18.33	23	16013	2750	46667276
Bone marrow transplant	47.89	18.33	15	16021	655	46669371
Alopecia	46.69	18.33	142	15894	162272	46507754
Therapeutic response delayed	46.50	18.33	14	16022	535	46669491
Enterocolitis haemorrhagic	46.03	18.33	18	16018	1522	46668504
Leukaemia recurrent	45.21	18.33	17	16019	1292	46668734
Pancytopenia	45.19	18.33	94	15942	84964	46585062
Fall	44.81	18.33	29	16007	329068	46340958
Chronic myeloid leukaemia recurrent	44.59	18.33	11	16025	195	46669831
Polymerase chain reaction positive	41.01	18.33	8	16028	43	46669983
Aspiration pleural cavity	40.96	18.33	14	16022	807	46669219
Product dose omission issue	39.11	18.33	137	15899	168383	46501643
Drug hypersensitivity	36.70	18.33	19	16017	243806	46426220
Lymphoid tissue hyperplasia	36.14	18.33	9	16027	166	46669860
Dyspnoea	35.71	18.33	300	15736	515248	46154778
Enterococcal bacteraemia	35.45	18.33	14	16022	1215	46668811
Pulmonary hypertension	35.11	18.33	52	15984	35941	46634085
Anaemia	35.09	18.33	177	15859	255602	46414424
Platelet count decreased	35.08	18.33	94	15942	99930	46570096
Nephrotic syndrome	33.61	18.33	21	16015	4900	46665126
Myalgia	32.01	18.33	104	15932	122984	46547042
Neutropenia	28.65	18.33	111	15925	143093	46526933
Systemic candida	27.55	18.33	15	16021	2712	46667314
Hepatitis chronic active	27.50	18.33	6	16030	60	46669966
Condition aggravated	26.58	18.33	27	16009	245025	46425001
Graft versus host disease	25.86	18.33	20	16016	6568	46663458
Pleurisy	25.02	18.33	21	16015	7741	46662285
Stem cell transplant	24.43	18.33	12	16024	1754	46668272
Acne	24.23	18.33	32	16004	19887	46650139
Hypotension	23.69	18.33	27	16009	232562	46437464
Normal newborn	23.08	18.33	18	16018	5983	46664043
Cytopenia	22.96	18.33	20	16016	7748	46662278
Gene mutation identification test positive	22.36	18.33	6	16030	150	46669876
Leukaemia	22.35	18.33	14	16022	3281	46666745
Chronic graft versus host disease	22.15	18.33	13	16023	2712	46667314
Infusion related reaction	22.14	18.33	4	16032	101204	46568822
Acute graft versus host disease	22.13	18.33	15	16021	4015	46666011
Demyelinating polyneuropathy	21.84	18.33	8	16028	565	46669461
Lymphocytosis	21.77	18.33	12	16024	2222	46667804
Cytomegalovirus colitis	21.67	18.33	11	16025	1724	46668302
Therapy cessation	21.14	18.33	35	16001	26594	46643432
Intentional product use issue	20.96	18.33	52	15984	52728	46617298
Pulmonary arterial hypertension	20.47	18.33	34	16002	25894	46644132
Gene mutation	20.07	18.33	9	16027	1071	46668955
Toxicity to various agents	20.06	18.33	26	16010	211740	46458286
Somnolence	19.66	18.33	15	16021	156506	46513520
Subdural haematoma	19.18	18.33	23	16013	12974	46657052
Full blood count decreased	18.72	18.33	30	16006	22181	46647845
Skin toxicity	18.65	18.33	13	16023	3641	46666385
White blood cell count decreased	18.50	18.33	82	15954	112149	46557877
Blast cell proliferation	18.39	18.33	3	16033	4	46670022

FDA Adverse Event Reporting System (Male)

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	1524.04	16.44	749	14929	73317	29863483
Adverse event	376.30	16.44	176	15502	15165	29921635
Drug resistance	319.68	16.44	172	15506	19961	29916839
Philadelphia chromosome positive	269.61	16.44	53	15625	178	29936622
Prescribed underdose	257.31	16.44	110	15568	7649	29929151
Malignant neoplasm progression	211.51	16.44	223	15455	72064	29864736
Hospitalisation	176.67	16.44	162	15516	44157	29892643
Chronic myeloid leukaemia	169.16	16.44	60	15618	2517	29934283
Blast crisis in myelogenous leukaemia	168.86	16.44	42	15636	492	29936308
Cytogenetic analysis abnormal	158.33	16.44	38	15640	379	29936421
Headache	119.02	16.44	281	15397	182025	29754775
Chylothorax	114.27	16.44	32	15646	608	29936192
Fluid retention	110.63	16.44	97	15581	24901	29911899
Drug intolerance	105.19	16.44	124	15554	45167	29891633
Pulmonary oedema	101.47	16.44	120	15558	43855	29892945
Pericardial effusion	95.46	16.44	83	15595	21061	29915739
Large granular lymphocytosis	91.85	16.44	20	15658	123	29936677
Gene mutation	89.40	16.44	28	15650	793	29936007
Fatigue	89.24	16.44	367	15311	320306	29616494
Rash	62.38	16.44	231	15447	191658	29745142
Acquired gene mutation	61.20	16.44	23	15655	1138	29935662
Diarrhoea	54.56	16.44	329	15349	333774	29603026
Acne	52.88	16.44	42	15636	9394	29927406
Pulmonary hypertension	52.45	16.44	57	15621	18979	29917821
Chronic myeloid leukaemia transformation	51.30	16.44	13	15665	165	29936635
Blast cell proliferation	49.90	16.44	8	15670	3	29936797
Loss of therapeutic response	47.77	16.44	11	15667	90	29936710
Death	47.42	16.44	334	15344	356949	29579851
Aspiration pleural cavity	46.08	16.44	17	15661	798	29936002
Acute lymphocytic leukaemia recurrent	42.85	16.44	23	15655	2644	29934156
Acute lymphocytic leukaemia	39.82	16.44	23	15655	3049	29933751
Bone marrow transplant	39.75	16.44	16	15662	952	29935848
Lymphoid tissue hyperplasia	39.38	16.44	9	15669	71	29936729
Bone pain	37.50	16.44	48	15630	18978	29917822
Hypotension	35.14	16.44	32	15646	200533	29736267
Toxicity to various agents	35.12	16.44	25	15653	177158	29759642
Intentional product use issue	33.84	16.44	65	15613	36375	29900425
Product dose omission issue	32.80	16.44	114	15564	91517	29845283
Therapy cessation	32.72	16.44	40	15638	15097	29921703
Gene mutation identification test positive	31.42	16.44	9	15669	186	29936614
Thrombocytopenia	30.39	16.44	147	15531	136897	29799903
Chronic myeloid leukaemia recurrent	29.91	16.44	8	15670	127	29936673
Natural killer cell count increased	29.84	16.44	5	15673	4	29936796
Therapy change	29.79	16.44	18	15660	2591	29934209
Pulmonary arterial hypertension	27.64	16.44	29	15649	9272	29927528
Neoplasm recurrence	26.95	16.44	15	15663	1852	29934948
Pleurisy	26.66	16.44	21	15657	4639	29932161
Leukaemia recurrent	26.60	16.44	14	15664	1547	29935253
Condition aggravated	26.59	16.44	20	15658	137846	29798954
Platelet count decreased	26.58	16.44	118	15560	106011	29830789
Chromosome analysis abnormal	26.12	16.44	7	15671	112	29936688
Anterior interosseous syndrome	25.86	16.44	5	15673	15	29936785
Clonal evolution	25.78	16.44	7	15671	118	29936682
Hyphaema	24.89	16.44	9	15669	399	29936401
Oedema	24.41	16.44	63	15615	42930	29893870
Drug clearance decreased	23.27	16.44	12	15666	1271	29935529
Blast cell crisis	23.26	16.44	6	15672	82	29936718
Hyperplasia	22.42	16.44	9	15669	532	29936268
Nausea	22.18	16.44	245	15433	296712	29640088
Bradycardia	21.73	16.44	4	15674	65522	29871278
Cytopenia	21.48	16.44	24	15654	8232	29928568
Gelatinous transformation of the bone marrow	20.94	16.44	4	15674	11	29936789
B-cell small lymphocytic lymphoma	20.10	16.44	6	15672	144	29936656
Fall	19.75	16.44	41	15637	181831	29754969
Rectosigmoid cancer	19.57	16.44	6	15672	158	29936642
Acute kidney injury	18.63	16.44	77	15601	273765	29663035
Allogenic bone marrow transplantation therapy	18.60	16.44	4	15674	23	29936777
Cardiac arrest	18.50	16.44	13	15665	92837	29843963
Hyperkalaemia	18.07	16.44	6	15672	66004	29870796
Overdose	17.89	16.44	11	15667	84326	29852474
Febrile neutropenia	17.86	16.44	106	15572	106587	29830213
Hyperchromic anaemia	17.80	16.44	4	15674	29	29936771
Pericarditis	17.41	16.44	22	15656	8584	29928216
Loss of consciousness	17.34	16.44	10	15668	79365	29857435
Pancytopenia	17.24	16.44	89	15589	84963	29851837
Peripheral arterial occlusive disease	16.96	16.44	17	15661	5151	29931649
Treatment failure	16.86	16.44	48	15630	34631	29902169
Central nervous system leukaemia	16.77	16.44	6	15672	258	29936542
Bone development abnormal	16.48	16.44	4	15674	42	29936758

Pharmacologic Action:

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

Drug Use (View source of the data)

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
Gastrointestinal hemorrhage	contraindication	74474003
Left heart failure	contraindication	85232009
Prolonged QT interval	contraindication	111975006
Disease of liver	contraindication	235856003	DOID:409
Edema	contraindication	267038008
Anemia	contraindication	271737000	DOID:2355
Cerebral hemorrhage	contraindication	274100004
Pregnancy, function	contraindication	289908002
Thrombocytopenic disorder	contraindication	302215000	DOID:1588
Neutropenic disorder	contraindication	303011007	DOID:1227
Pericardial effusion	contraindication	373945007	DOID:118
Ascites	contraindication	389026000
Breastfeeding (mother)	contraindication	413712001
Congenital long QT syndrome	contraindication	442917000
Pleural Effusions	contraindication

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)

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	May 9, 2021	PEDIATRIC EXCLUSIVITY
140MG	SPRYCEL	BRISTOL MYERS SQUIBB	N021986	Oct. 28, 2010	RX	TABLET	ORAL	May 9, 2021	PEDIATRIC EXCLUSIVITY
20MG	SPRYCEL	BRISTOL MYERS SQUIBB	N021986	June 28, 2006	RX	TABLET	ORAL	May 9, 2021	PEDIATRIC EXCLUSIVITY
50MG	SPRYCEL	BRISTOL MYERS SQUIBB	N021986	June 28, 2006	RX	TABLET	ORAL	May 9, 2021	PEDIATRIC EXCLUSIVITY
70MG	SPRYCEL	BRISTOL MYERS SQUIBB	N021986	June 28, 2006	RX	TABLET	ORAL	May 9, 2021	PEDIATRIC EXCLUSIVITY
80MG	SPRYCEL	BRISTOL MYERS SQUIBB	N021986	Oct. 28, 2010	RX	TABLET	ORAL	May 9, 2021	PEDIATRIC EXCLUSIVITY
100MG	SPRYCEL	BRISTOL MYERS SQUIBB	N021986	May 30, 2008	RX	TABLET	ORAL	Dec. 21, 2021	TREATMENT OF PEDIATRIC PATIENTS ONE YEAR OF AGE AND OLDER WITH NEWLY DIAGNOSED PHILADELPHIA CHROMOSOME-POSITIVE (PH+) ACUTE LYMPHOBLASTIC LEUKEMIA (ALL) IN COMBINULLTION WITH CHEMOTHERAPY
140MG	SPRYCEL	BRISTOL MYERS SQUIBB	N021986	Oct. 28, 2010	RX	TABLET	ORAL	Dec. 21, 2021	TREATMENT OF PEDIATRIC PATIENTS ONE YEAR OF AGE AND OLDER WITH NEWLY DIAGNOSED PHILADELPHIA CHROMOSOME-POSITIVE (PH+) ACUTE LYMPHOBLASTIC LEUKEMIA (ALL) IN COMBINULLTION WITH CHEMOTHERAPY
20MG	SPRYCEL	BRISTOL MYERS SQUIBB	N021986	June 28, 2006	RX	TABLET	ORAL	Dec. 21, 2021	TREATMENT OF PEDIATRIC PATIENTS ONE YEAR OF AGE AND OLDER WITH NEWLY DIAGNOSED PHILADELPHIA CHROMOSOME-POSITIVE (PH+) ACUTE LYMPHOBLASTIC LEUKEMIA (ALL) IN COMBINULLTION WITH CHEMOTHERAPY
50MG	SPRYCEL	BRISTOL MYERS SQUIBB	N021986	June 28, 2006	RX	TABLET	ORAL	Dec. 21, 2021	TREATMENT OF PEDIATRIC PATIENTS ONE YEAR OF AGE AND OLDER WITH NEWLY DIAGNOSED PHILADELPHIA CHROMOSOME-POSITIVE (PH+) ACUTE LYMPHOBLASTIC LEUKEMIA (ALL) IN COMBINULLTION WITH CHEMOTHERAPY
70MG	SPRYCEL	BRISTOL MYERS SQUIBB	N021986	June 28, 2006	RX	TABLET	ORAL	Dec. 21, 2021	TREATMENT OF PEDIATRIC PATIENTS ONE YEAR OF AGE AND OLDER WITH NEWLY DIAGNOSED PHILADELPHIA CHROMOSOME-POSITIVE (PH+) ACUTE LYMPHOBLASTIC LEUKEMIA (ALL) IN COMBINULLTION WITH CHEMOTHERAPY
80MG	SPRYCEL	BRISTOL MYERS SQUIBB	N021986	Oct. 28, 2010	RX	TABLET	ORAL	Dec. 21, 2021	TREATMENT OF PEDIATRIC PATIENTS ONE YEAR OF AGE AND OLDER WITH NEWLY DIAGNOSED PHILADELPHIA CHROMOSOME-POSITIVE (PH+) ACUTE LYMPHOBLASTIC LEUKEMIA (ALL) IN COMBINULLTION WITH CHEMOTHERAPY
100MG	SPRYCEL	BRISTOL MYERS SQUIBB	N021986	May 30, 2008	RX	TABLET	ORAL	June 21, 2022	PEDIATRIC EXCLUSIVITY
140MG	SPRYCEL	BRISTOL MYERS SQUIBB	N021986	Oct. 28, 2010	RX	TABLET	ORAL	June 21, 2022	PEDIATRIC EXCLUSIVITY
20MG	SPRYCEL	BRISTOL MYERS SQUIBB	N021986	June 28, 2006	RX	TABLET	ORAL	June 21, 2022	PEDIATRIC EXCLUSIVITY
50MG	SPRYCEL	BRISTOL MYERS SQUIBB	N021986	June 28, 2006	RX	TABLET	ORAL	June 21, 2022	PEDIATRIC EXCLUSIVITY
70MG	SPRYCEL	BRISTOL MYERS SQUIBB	N021986	June 28, 2006	RX	TABLET	ORAL	June 21, 2022	PEDIATRIC EXCLUSIVITY
80MG	SPRYCEL	BRISTOL MYERS SQUIBB	N021986	Oct. 28, 2010	RX	TABLET	ORAL	June 21, 2022	PEDIATRIC EXCLUSIVITY
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
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
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
50MG	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
70MG	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
80MG	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
100MG	SPRYCEL	BRISTOL MYERS SQUIBB	N021986	May 30, 2008	RX	TABLET	ORAL	May 9, 2025	PEDIATRIC EXCLUSIVITY
140MG	SPRYCEL	BRISTOL MYERS SQUIBB	N021986	Oct. 28, 2010	RX	TABLET	ORAL	May 9, 2025	PEDIATRIC EXCLUSIVITY
20MG	SPRYCEL	BRISTOL MYERS SQUIBB	N021986	June 28, 2006	RX	TABLET	ORAL	May 9, 2025	PEDIATRIC EXCLUSIVITY
50MG	SPRYCEL	BRISTOL MYERS SQUIBB	N021986	June 28, 2006	RX	TABLET	ORAL	May 9, 2025	PEDIATRIC EXCLUSIVITY
70MG	SPRYCEL	BRISTOL MYERS SQUIBB	N021986	June 28, 2006	RX	TABLET	ORAL	May 9, 2025	PEDIATRIC EXCLUSIVITY
80MG	SPRYCEL	BRISTOL MYERS SQUIBB	N021986	Oct. 28, 2010	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 COMBINULLTION WITH CHEMOTHERAPY
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 COMBINULLTION WITH CHEMOTHERAPY
20MG	SPRYCEL	BRISTOL MYERS SQUIBB	N021986	June 28, 2006	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 COMBINULLTION WITH CHEMOTHERAPY
50MG	SPRYCEL	BRISTOL MYERS SQUIBB	N021986	June 28, 2006	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 COMBINULLTION WITH CHEMOTHERAPY
70MG	SPRYCEL	BRISTOL MYERS SQUIBB	N021986	June 28, 2006	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 COMBINULLTION WITH CHEMOTHERAPY
80MG	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 COMBINULLTION 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	June 21, 2026	PEDIATRIC EXCLUSIVITY
20MG	SPRYCEL	BRISTOL MYERS SQUIBB	N021986	June 28, 2006	RX	TABLET	ORAL	June 21, 2026	PEDIATRIC EXCLUSIVITY
50MG	SPRYCEL	BRISTOL MYERS SQUIBB	N021986	June 28, 2006	RX	TABLET	ORAL	June 21, 2026	PEDIATRIC EXCLUSIVITY
70MG	SPRYCEL	BRISTOL MYERS SQUIBB	N021986	June 28, 2006	RX	TABLET	ORAL	June 21, 2026	PEDIATRIC EXCLUSIVITY
80MG	SPRYCEL	BRISTOL MYERS SQUIBB	N021986	Oct. 28, 2010	RX	TABLET	ORAL	June 21, 2026	PEDIATRIC EXCLUSIVITY

Bioactivity Summary:

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 Fyn	Kinase	P06241	FYN_HUMAN	INHIBITOR	Kd	9.10	CHEMBL	CHEMBL
Tyrosine-protein kinase Yes	Kinase	P07947	YES_HUMAN	INHIBITOR	Kd	9.52	CHEMBL	CHEMBL
Ephrin type-A receptor 2	Kinase	P29317	EPHA2_HUMAN	INHIBITOR	Kd	9.07	CHEMBL	CHEMBL
Tyrosine-protein kinase Lck	Kinase	P06239	LCK_HUMAN	INHIBITOR	Kd	9.70	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
Vascular endothelial growth factor receptor 1	Kinase	P17948	VGFR1_HUMAN		Kd	5.30	CHEMBL
Serine/threonine-protein kinase mTOR	Kinase	P42345	MTOR_HUMAN		IC50	4.46	CHEMBL
Vascular endothelial growth factor receptor 2	Kinase	P35968	VGFR2_HUMAN		Kd	5.54	CHEMBL
Fibroblast growth factor receptor 3	Kinase	P22607	FGFR3_HUMAN		Kd	5.41	CHEMBL
Serine/threonine-protein kinase 35	Kinase	Q8TDR2	STK35_HUMAN		Kd	6.11	CHEMBL
Platelet-derived growth factor receptor alpha	Kinase	P16234	PGFRA_HUMAN		Kd	9.33	CHEMBL
Casein kinase I isoform epsilon	Kinase	P49674	KC1E_HUMAN		Kd	5.82	CHEMBL
Receptor-interacting serine/threonine-protein kinase 2	Kinase	O43353	RIPK2_HUMAN		Kd	7.51	CHEMBL
Myelin transcription factor 1	Unclassified	Q01538	MYT1_HUMAN		IC50	7.20	CHEMBL
Ephrin type-B receptor 4	Kinase	P54760	EPHB4_HUMAN		Kd	9.47	CHEMBL
Tyrosine-protein kinase JAK2	Kinase	O60674	JAK2_HUMAN		Kd	6	CHEMBL
Cyclin-G-associated kinase	Kinase	O14976	GAK_HUMAN		Kd	8.59	CHEMBL
Serine/threonine-protein kinase SBK1	Kinase	Q52WX2	SBK1_HUMAN		Kd	5.92	CHEMBL
Aurora kinase A	Kinase	O14965	AURKA_HUMAN		Kd	5.03	CHEMBL
MAP kinase p38	Kinase	O15264 P53778 Q15759 Q16539	MK11_HUMAN MK12_HUMAN MK13_HUMAN MK14_HUMAN		IC50	7	CHEMBL
Tyrosine-protein kinase SYK	Kinase	P43405	KSYK_HUMAN		Kd	5.54	CHEMBL
Wee1-like protein kinase	Kinase	P30291	WEE1_HUMAN		Kd	5.15	CHEMBL
RAF proto-oncogene serine/threonine-protein kinase	Kinase	P04049	RAF1_HUMAN		Kd	6.24	CHEMBL
Tyrosine-protein kinase BTK	Kinase	Q06187	BTK_HUMAN		Kd	8.85	CHEMBL
Mitogen-activated protein kinase kinase kinase 13	Kinase	O43283	M3K13_HUMAN		Kd	5.28	CHEMBL
Ephrin type-A receptor 1	Kinase	P21709	EPHA1_HUMAN		Kd	8.39	CHEMBL
Mitogen-activated protein kinase kinase kinase kinase 1	Kinase	Q92918	M4K1_HUMAN		Kd	6.01	CHEMBL
Serine/threonine-protein kinase Nek11	Kinase	Q8NG66	NEK11_HUMAN		Kd	6.33	CHEMBL
Serine/threonine-protein kinase B-raf	Kinase	P15056	BRAF_HUMAN		Kd	6.30	CHEMBL
Tyrosine-protein kinase Fgr	Kinase	P09769	FGR_HUMAN	INHIBITOR	Kd	9.30	CHEMBL
Serine/threonine-protein kinase MRCK alpha	Kinase	Q5VT25	MRCKA_HUMAN		Kd	5.70	CHEMBL
Mitogen-activated protein kinase kinase kinase 7	Kinase	O43318	M3K7_HUMAN		Kd	5.43	CHEMBL
Tyrosine-protein kinase FRK	Kinase	P42685	FRK_HUMAN	INHIBITOR	Kd	9.51	CHEMBL
Ephrin type-A receptor 8	Kinase	P29322	EPHA8_HUMAN		Kd	9.62	CHEMBL
Ephrin type-A receptor 3	Kinase	P29320	EPHA3_HUMAN		Kd	10.03	CHEMBL
Serine/threonine-protein kinase 10	Kinase	O94804	STK10_HUMAN		Kd	5.92	CHEMBL
Tyrosine-protein kinase JAK3	Kinase	P52333	JAK3_HUMAN		Kd	6.19	CHEMBL
Tyrosine-protein kinase CSK	Kinase	P41240	CSK_HUMAN		Kd	9	CHEMBL
Serine/threonine-protein kinase TNNI3K	Kinase	Q59H18	TNI3K_HUMAN		Kd	7.96	CHEMBL
Receptor tyrosine-protein kinase erbB-2	Kinase	P04626	ERBB2_HUMAN		Kd	5.85	CHEMBL
Tyrosine-protein kinase HCK	Kinase	P08631	HCK_HUMAN	INHIBITOR	Kd	9.46	CHEMBL
Fibroblast growth factor receptor 1	Kinase	P11362	FGFR1_HUMAN		Kd	5.43	CHEMBL
Fibroblast growth factor receptor 2	Kinase	P21802	FGFR2_HUMAN		Kd	5.85	CHEMBL
Chaperone activity of bc1 complex-like, mitochondrial	Kinase	Q8NI60	COQ8A_HUMAN		Kd	6.72	CHEMBL
Serine/threonine-protein kinase 25	Kinase	O00506	STK25_HUMAN		Kd	5.47	CHEMBL
Mitogen-activated protein kinase kinase kinase 4	Kinase	Q9Y6R4	M3K4_HUMAN		Kd	6.51	CHEMBL
Mitogen-activated protein kinase kinase kinase kinase 5	Kinase	Q9Y4K4	M4K5_HUMAN		Kd	7.35	CHEMBL
Misshapen-like kinase 1	Kinase	Q8N4C8	MINK1_HUMAN		Kd	6.37	CHEMBL
Serine/threonine-protein kinase 36	Kinase	Q9NRP7	STK36_HUMAN		Kd	6.68	CHEMBL
Receptor tyrosine-protein kinase erbB-4	Kinase	Q15303	ERBB4_HUMAN		Kd	7.26	CHEMBL
Ephrin type-A receptor 6	Kinase	Q9UF33	EPHA6_HUMAN		Kd	5.68	CHEMBL
TRAF2 and NCK-interacting protein kinase	Kinase	Q9UKE5	TNIK_HUMAN		Kd	5.70	CHEMBL
Membrane-associated tyrosine- and threonine-specific cdc2-inhibitory kinase	Kinase	Q99640	PMYT1_HUMAN		Kd	6.89	CHEMBL
Aurora kinase B	Kinase	Q96GD4	AURKB_HUMAN		IC50	5.19	CHEMBL
STE20-like serine/threonine-protein kinase	Kinase	Q9H2G2	SLK_HUMAN		Kd	6.14	CHEMBL
Bone morphogenetic protein receptor type-1B	Kinase	O00238	BMR1B_HUMAN		Kd	7.28	CHEMBL
Non-receptor tyrosine-protein kinase TYK2	Kinase	P29597	TYK2_HUMAN		Kd	6.96	CHEMBL
Serine/threonine-protein kinase 4	Kinase	Q13043	STK4_HUMAN		Kd	5.42	CHEMBL
Protein-tyrosine kinase 6	Kinase	Q13882	PTK6_HUMAN		Kd	8.11	CHEMBL
Serine/threonine-protein kinase TAO2	Kinase	Q9UL54	TAOK2_HUMAN		Kd	5.27	CHEMBL
Serine/threonine-protein kinase Nek2	Kinase	P51955	NEK2_HUMAN		Kd	5.19	CHEMBL
Tyrosine-protein kinase Lyn	Kinase	P07948	LYN_HUMAN	INHIBITOR	Kd	9.24	CHEMBL
Cytoplasmic tyrosine-protein kinase BMX	Kinase	P51813	BMX_HUMAN		Kd	8.85	CHEMBL
Ephrin type-A receptor 5	Kinase	P54756	EPHA5_HUMAN		Kd	9.62	CHEMBL
LIM domain kinase 1	Kinase	P53667	LIMK1_HUMAN		Kd	6.24	CHEMBL
Ephrin type-A receptor 4	Kinase	P54764	EPHA4_HUMAN		Kd	8.92	CHEMBL
Ephrin type-B receptor 1	Kinase	P54762	EPHB1_HUMAN		Kd	9.35	CHEMBL
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform	Kinase	P42336	PK3CA_HUMAN		IC50	4.42	CHEMBL
Activated CDC42 kinase 1	Kinase	Q07912	ACK1_HUMAN		Kd	8.25	CHEMBL
Mitogen-activated protein kinase kinase kinase kinase 3	Kinase	Q8IVH8	M4K3_HUMAN		Kd	6.19	CHEMBL
Dual specificity testis-specific protein kinase 1	Kinase	Q15569	TESK1_HUMAN		Kd	7.48	CHEMBL
Activin receptor type-1	Kinase	Q04771	ACVR1_HUMAN		Kd	6.21	CHEMBL
Serine/threonine-protein kinase MRCK gamma	Kinase	Q6DT37	MRCKG_HUMAN		Kd	5.92	CHEMBL
Serine/threonine-protein kinase MRCK beta	Kinase	Q9Y5S2	MRCKB_HUMAN		Kd	5.68	CHEMBL
Mitogen-activated protein kinase kinase kinase 2	Kinase	Q9Y2U5	M3K2_HUMAN		Kd	6.85	CHEMBL
Serine/threonine-protein kinase ULK3	Kinase	Q6PHR2	ULK3_HUMAN		Kd	5.34	CHEMBL
Abelson tyrosine-protein kinase 2	Kinase	P42684	ABL2_HUMAN		Kd	9.77	CHEMBL
Serine/threonine-protein kinase 26	Kinase	Q9P289	STK26_HUMAN		Kd	5.72	CHEMBL
Activin receptor type-2B	Kinase	Q13705	AVR2B_HUMAN		Kd	6.24	CHEMBL
Tyrosine-protein kinase Blk	Kinase	P51451	BLK_HUMAN	INHIBITOR	Kd	9.68	CHEMBL
Receptor tyrosine-protein kinase erbB-3	Kinase	P21860	ERBB3_HUMAN		Kd	7.74	CHEMBL
Ephrin type-B receptor 6	Kinase	O15197	EPHB6_HUMAN		Kd	10.41	CHEMBL
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform	Kinase	O00329	PK3CD_HUMAN		IC50	4.52	CHEMBL
Serine/threonine-protein kinase SIK2	Kinase	Q9H0K1	SIK2_HUMAN		Kd	8.19	CHEMBL
Serine/threonine-protein kinase TAO3	Kinase	Q9H2K8	TAOK3_HUMAN		Kd	5.64	CHEMBL
Tyrosine-protein kinase Srms	Kinase	Q9H3Y6	SRMS_HUMAN	INHIBITOR	Kd	7.89	CHEMBL
Serine/threonine-protein kinase SIK3	Kinase	Q9Y2K2	SIK3_HUMAN		Kd	7.55	CHEMBL
Dual specificity mitogen-activated protein kinase kinase; MEK1/2	Kinase	P36507 Q02750	MP2K1_HUMAN MP2K2_HUMAN		IC50	5.77	CHEMBL
Wee1-like protein kinase 2	Kinase	P0C1S8	WEE2_HUMAN		Kd	6.70	CHEMBL
Macrophage colony-stimulating factor 1 receptor	Kinase	P07333	CSF1R_HUMAN		Kd	9.24	CHEMBL
Discoidin domain-containing receptor 2	Kinase	Q16832	DDR2_HUMAN		Kd	8.52	CHEMBL
Serine/threonine-protein kinase receptor R3	Kinase	P37023	ACVL1_HUMAN		Kd	6.34	CHEMBL
Activin receptor type-1B	Kinase	P36896	ACV1B_HUMAN		Kd	6.48	CHEMBL
Bone morphogenetic protein receptor type-1A	Kinase	P36894	BMR1A_HUMAN		Kd	5.15	CHEMBL
TGF-beta receptor type-1	Kinase	P36897	TGFR1_HUMAN		Kd	6.64	CHEMBL
TGF-beta receptor type-2	Kinase	P37173	TGFR2_HUMAN		Kd	5.54	CHEMBL
Eukaryotic translation initiation factor 2-alpha kinase 4	Kinase	Q9P2K8	E2AK4_HUMAN		Kd	5.80	CHEMBL
Proto-oncogene tyrosine-protein kinase receptor Ret	Kinase	P07949	RET_HUMAN		Kd	6.41	CHEMBL
Myotonin-protein kinase	Kinase	Q09013	DMPK_HUMAN		Kd	5.89	CHEMBL
Epithelial discoidin domain-containing receptor 1	Kinase	Q08345	DDR1_HUMAN		Kd	9.16	CHEMBL
Mitogen-activated protein kinase kinase kinase kinase 4	Kinase	O95819	M4K4_HUMAN		Kd	5.51	CHEMBL
Activin receptor type-2A	Kinase	P27037	AVR2A_HUMAN		Kd	6.68	CHEMBL
Myosin light chain kinase 2, skeletal/cardiac muscle	Kinase	Q9H1R3	MYLK2_HUMAN		Kd	5.46	CHEMBL
Mitogen-activated protein kinase kinase kinase 19	Kinase	Q56UN5	M3K19_HUMAN		Kd	7.10	CHEMBL
Ephrin type-B receptor 2	Kinase	P29323	EPHB2_HUMAN		Kd	9.41	CHEMBL
Mitogen-activated protein kinase 11	Kinase	Q15759	MK11_HUMAN		Kd	6.39	CHEMBL
Dual specificity mitogen-activated protein kinase kinase 2	Kinase	P36507	MP2K2_HUMAN		Kd	5.85	CHEMBL
Tyrosine-protein kinase TXK	Kinase	P42681	TXK_HUMAN		Kd	8.68	CHEMBL
Serine/threonine-protein kinase VRK2	Kinase	Q86Y07	VRK2_HUMAN		Kd	5.49	CHEMBL
LIM domain kinase 2	Kinase	P53671	LIMK2_HUMAN		Kd	7.07	CHEMBL
Ephrin type-B receptor 3	Kinase	P54753	EPHB3_HUMAN		Kd	8.16	CHEMBL
Tyrosine-protein kinase Tec	Kinase	P42680	TEC_HUMAN		Kd	7.89	CHEMBL
Mitogen-activated protein kinase kinase kinase 3	Kinase	Q99759	M3K3_HUMAN		Kd	6.55	CHEMBL
Serine/threonine-protein kinase NLK	Kinase	Q9UBE8	NLK_HUMAN		Kd	6.59	CHEMBL
Mitogen-activated protein kinase kinase kinase kinase 2	Kinase	Q12851	M4K2_HUMAN		Kd	5.89	CHEMBL
Serine/threonine-protein kinase SIK1	Kinase	P57059	SIK1_HUMAN		Kd	8.41	CHEMBL
Mitogen-activated protein kinase 14	Kinase	Q16539	MK14_HUMAN		Kd	7.57	CHEMBL
Bcr/Abl fusion protein	Kinase	P00519 P11274	ABL1_HUMAN BCR_HUMAN		IC50	9.10	CHEMBL
Breakpoint cluster region protein	Kinase	P11274	BCR_HUMAN				WOMBAT-PK
Dual specificity mitogen-activated protein kinase kinase 5	Kinase	Q13163	MP2K5_HUMAN		Kd	8.48	CHEMBL
Mitogen-activated protein kinase kinase kinase MLT	Kinase	Q9NYL2	MLTK_HUMAN		Kd	7.35	CHEMBL
Dual specificity mitogen-activated protein kinase kinase 1	Kinase	Q02750	MP2K1_HUMAN		Kd	6	CHEMBL
Receptor-type tyrosine-protein kinase FLT3	Kinase	P36888	FLT3_HUMAN		Kd	5.49	CHEMBL
Epidermal growth factor receptor	Kinase	P00533	EGFR_HUMAN		Kd	7.10	CHEMBL
Proto-oncogene tyrosine-protein kinase Src	Kinase		SRC_CHICK		Kd	7.96	CHEMBL
Tyrosine-protein kinase Blk	Kinase		BLK_MOUSE		IC50	8.10	CHEMBL
Proto-oncogene tyrosine-protein kinase LCK	Kinase		LCK_MOUSE		Ki	10.19	CHEMBL
Calcium-dependent protein kinase 1	Kinase		CDPK1_PLAF7		Kd	6.19	CHEMBL
Tubulin alpha-1A chain	Structural		TBA1A_RAT		Kd	7.26	CHEMBL

External reference:

ID	Source
4025488	VUID
N0000179780	NUI
D03658	KEGG_DRUG
863127-77-9	SECONDARY_CAS_RN
4025488	VANDF
C1328005	UMLSCUI
CHEBI:49375	CHEBI
1N1	PDB_CHEM_ID
CHEMBL1421	ChEMBL_ID
DB01254	DRUGBANK_ID
D000069439	MESH_DESCRIPTOR_UI
3062316	PUBCHEM_CID
5678	IUPHAR_LIGAND_ID
RBZ1571X5H	UNII
475342	RXNORM
21648	MMSL
83173	MMSL
d05831	MMSL
011616	NDDF
422756008	SNOMEDCT_US
423658008	SNOMEDCT_US

Pharmaceutical products:

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	0003-0527	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	0003-0852	TABLET	100 mg	ORAL	NDA	27 sections
SPRYCEL	HUMAN PRESCRIPTION DRUG LABEL	1	0003-0855	TABLET	80 mg	ORAL	NDA	27 sections
SPRYCEL	HUMAN PRESCRIPTION DRUG LABEL	1	0003-0857	TABLET	140 mg	ORAL	NDA	27 sections
SPRYCEL	HUMAN PRESCRIPTION DRUG LABEL	1	54868-5759	TABLET	70 mg	ORAL	NDA	28 sections