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

Stem definitionDrug idCAS RN
tyrosine kinase inhibitors 785 302962-49-8

Description:

MoleculeDescription

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:

PropertyValueReference
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 ┬ÁM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability) 15 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H

Approvals:

DateAgencyCompanyOrphan
June 28, 2006 FDA BRISTOL MYERS SQUIBB

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients 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 termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients 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:

SourceCodeDescription
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)

DiseaseRelationSNOMED_IDDOID
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 levelDissociation constantType (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 strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
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:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Mast/stem cell growth factor receptor Kit Kinase INHIBITOR Kd 9.24 CHEMBL CHEMBL
Proto-oncogene tyrosine-protein kinase Src Kinase INHIBITOR Kd 9.68 CHEMBL CHEMBL
Tyrosine-protein kinase Fyn Kinase INHIBITOR Kd 9.10 CHEMBL CHEMBL
Tyrosine-protein kinase Yes Kinase INHIBITOR Kd 9.52 CHEMBL CHEMBL
Ephrin type-A receptor 2 Kinase INHIBITOR Kd 9.07 CHEMBL CHEMBL
Tyrosine-protein kinase Lck Kinase INHIBITOR Kd 9.70 CHEMBL CHEMBL
Platelet-derived growth factor receptor beta Kinase INHIBITOR Kd 9.20 CHEMBL CHEMBL
Tyrosine-protein kinase ABL1 Kinase INHIBITOR IC50 9.60 IUPHAR CHEMBL
Vascular endothelial growth factor receptor 1 Kinase Kd 5.30 CHEMBL
Serine/threonine-protein kinase mTOR Kinase IC50 4.46 CHEMBL
Vascular endothelial growth factor receptor 2 Kinase Kd 5.54 CHEMBL
Fibroblast growth factor receptor 3 Kinase Kd 5.41 CHEMBL
Serine/threonine-protein kinase 35 Kinase Kd 6.11 CHEMBL
Platelet-derived growth factor receptor alpha Kinase Kd 9.33 CHEMBL
Casein kinase I isoform epsilon Kinase Kd 5.82 CHEMBL
Receptor-interacting serine/threonine-protein kinase 2 Kinase Kd 7.51 CHEMBL
Myelin transcription factor 1 Unclassified IC50 7.20 CHEMBL
Ephrin type-B receptor 4 Kinase Kd 9.47 CHEMBL
Tyrosine-protein kinase JAK2 Kinase Kd 6 CHEMBL
Cyclin-G-associated kinase Kinase Kd 8.59 CHEMBL
Serine/threonine-protein kinase SBK1 Kinase Kd 5.92 CHEMBL
Aurora kinase A Kinase Kd 5.03 CHEMBL
MAP kinase p38 Kinase IC50 7 CHEMBL
Tyrosine-protein kinase SYK Kinase Kd 5.54 CHEMBL
Wee1-like protein kinase Kinase Kd 5.15 CHEMBL
RAF proto-oncogene serine/threonine-protein kinase Kinase Kd 6.24 CHEMBL
Tyrosine-protein kinase BTK Kinase Kd 8.85 CHEMBL
Mitogen-activated protein kinase kinase kinase 13 Kinase Kd 5.28 CHEMBL
Ephrin type-A receptor 1 Kinase Kd 8.39 CHEMBL
Mitogen-activated protein kinase kinase kinase kinase 1 Kinase Kd 6.01 CHEMBL
Serine/threonine-protein kinase Nek11 Kinase Kd 6.33 CHEMBL
Serine/threonine-protein kinase B-raf Kinase Kd 6.30 CHEMBL
Tyrosine-protein kinase Fgr Kinase INHIBITOR Kd 9.30 CHEMBL
Serine/threonine-protein kinase MRCK alpha Kinase Kd 5.70 CHEMBL
Mitogen-activated protein kinase kinase kinase 7 Kinase Kd 5.43 CHEMBL
Tyrosine-protein kinase FRK Kinase INHIBITOR Kd 9.51 CHEMBL
Ephrin type-A receptor 8 Kinase Kd 9.62 CHEMBL
Ephrin type-A receptor 3 Kinase Kd 10.03 CHEMBL
Serine/threonine-protein kinase 10 Kinase Kd 5.92 CHEMBL
Tyrosine-protein kinase JAK3 Kinase Kd 6.19 CHEMBL
Tyrosine-protein kinase CSK Kinase Kd 9 CHEMBL
Serine/threonine-protein kinase TNNI3K Kinase Kd 7.96 CHEMBL
Receptor tyrosine-protein kinase erbB-2 Kinase Kd 5.85 CHEMBL
Tyrosine-protein kinase HCK Kinase INHIBITOR Kd 9.46 CHEMBL
Fibroblast growth factor receptor 1 Kinase Kd 5.43 CHEMBL
Fibroblast growth factor receptor 2 Kinase Kd 5.85 CHEMBL
Chaperone activity of bc1 complex-like, mitochondrial Kinase Kd 6.72 CHEMBL
Serine/threonine-protein kinase 25 Kinase Kd 5.47 CHEMBL
Mitogen-activated protein kinase kinase kinase 4 Kinase Kd 6.51 CHEMBL
Mitogen-activated protein kinase kinase kinase kinase 5 Kinase Kd 7.35 CHEMBL
Misshapen-like kinase 1 Kinase Kd 6.37 CHEMBL
Serine/threonine-protein kinase 36 Kinase Kd 6.68 CHEMBL
Receptor tyrosine-protein kinase erbB-4 Kinase Kd 7.26 CHEMBL
Ephrin type-A receptor 6 Kinase Kd 5.68 CHEMBL
TRAF2 and NCK-interacting protein kinase Kinase Kd 5.70 CHEMBL
Membrane-associated tyrosine- and threonine-specific cdc2-inhibitory kinase Kinase Kd 6.89 CHEMBL
Aurora kinase B Kinase IC50 5.19 CHEMBL
STE20-like serine/threonine-protein kinase Kinase Kd 6.14 CHEMBL
Bone morphogenetic protein receptor type-1B Kinase Kd 7.28 CHEMBL
Non-receptor tyrosine-protein kinase TYK2 Kinase Kd 6.96 CHEMBL
Serine/threonine-protein kinase 4 Kinase Kd 5.42 CHEMBL
Protein-tyrosine kinase 6 Kinase Kd 8.11 CHEMBL
Serine/threonine-protein kinase TAO2 Kinase Kd 5.27 CHEMBL
Serine/threonine-protein kinase Nek2 Kinase Kd 5.19 CHEMBL
Tyrosine-protein kinase Lyn Kinase INHIBITOR Kd 9.24 CHEMBL
Cytoplasmic tyrosine-protein kinase BMX Kinase Kd 8.85 CHEMBL
Ephrin type-A receptor 5 Kinase Kd 9.62 CHEMBL
LIM domain kinase 1 Kinase Kd 6.24 CHEMBL
Ephrin type-A receptor 4 Kinase Kd 8.92 CHEMBL
Ephrin type-B receptor 1 Kinase Kd 9.35 CHEMBL
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform Kinase IC50 4.42 CHEMBL
Activated CDC42 kinase 1 Kinase Kd 8.25 CHEMBL
Mitogen-activated protein kinase kinase kinase kinase 3 Kinase Kd 6.19 CHEMBL
Dual specificity testis-specific protein kinase 1 Kinase Kd 7.48 CHEMBL
Activin receptor type-1 Kinase Kd 6.21 CHEMBL
Serine/threonine-protein kinase MRCK gamma Kinase Kd 5.92 CHEMBL
Serine/threonine-protein kinase MRCK beta Kinase Kd 5.68 CHEMBL
Mitogen-activated protein kinase kinase kinase 2 Kinase Kd 6.85 CHEMBL
Serine/threonine-protein kinase ULK3 Kinase Kd 5.34 CHEMBL
Abelson tyrosine-protein kinase 2 Kinase Kd 9.77 CHEMBL
Serine/threonine-protein kinase 26 Kinase Kd 5.72 CHEMBL
Activin receptor type-2B Kinase Kd 6.24 CHEMBL
Tyrosine-protein kinase Blk Kinase INHIBITOR Kd 9.68 CHEMBL
Receptor tyrosine-protein kinase erbB-3 Kinase Kd 7.74 CHEMBL
Ephrin type-B receptor 6 Kinase Kd 10.41 CHEMBL
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform Kinase IC50 4.52 CHEMBL
Serine/threonine-protein kinase SIK2 Kinase Kd 8.19 CHEMBL
Serine/threonine-protein kinase TAO3 Kinase Kd 5.64 CHEMBL
Tyrosine-protein kinase Srms Kinase INHIBITOR Kd 7.89 CHEMBL
Serine/threonine-protein kinase SIK3 Kinase Kd 7.55 CHEMBL
Dual specificity mitogen-activated protein kinase kinase; MEK1/2 Kinase IC50 5.77 CHEMBL
Wee1-like protein kinase 2 Kinase Kd 6.70 CHEMBL
Macrophage colony-stimulating factor 1 receptor Kinase Kd 9.24 CHEMBL
Discoidin domain-containing receptor 2 Kinase Kd 8.52 CHEMBL
Serine/threonine-protein kinase receptor R3 Kinase Kd 6.34 CHEMBL
Activin receptor type-1B Kinase Kd 6.48 CHEMBL
Bone morphogenetic protein receptor type-1A Kinase Kd 5.15 CHEMBL
TGF-beta receptor type-1 Kinase Kd 6.64 CHEMBL
TGF-beta receptor type-2 Kinase Kd 5.54 CHEMBL
Eukaryotic translation initiation factor 2-alpha kinase 4 Kinase Kd 5.80 CHEMBL
Proto-oncogene tyrosine-protein kinase receptor Ret Kinase Kd 6.41 CHEMBL
Myotonin-protein kinase Kinase Kd 5.89 CHEMBL
Epithelial discoidin domain-containing receptor 1 Kinase Kd 9.16 CHEMBL
Mitogen-activated protein kinase kinase kinase kinase 4 Kinase Kd 5.51 CHEMBL
Activin receptor type-2A Kinase Kd 6.68 CHEMBL
Myosin light chain kinase 2, skeletal/cardiac muscle Kinase Kd 5.46 CHEMBL
Mitogen-activated protein kinase kinase kinase 19 Kinase Kd 7.10 CHEMBL
Ephrin type-B receptor 2 Kinase Kd 9.41 CHEMBL
Mitogen-activated protein kinase 11 Kinase Kd 6.39 CHEMBL
Dual specificity mitogen-activated protein kinase kinase 2 Kinase Kd 5.85 CHEMBL
Tyrosine-protein kinase TXK Kinase Kd 8.68 CHEMBL
Serine/threonine-protein kinase VRK2 Kinase Kd 5.49 CHEMBL
LIM domain kinase 2 Kinase Kd 7.07 CHEMBL
Ephrin type-B receptor 3 Kinase Kd 8.16 CHEMBL
Tyrosine-protein kinase Tec Kinase Kd 7.89 CHEMBL
Mitogen-activated protein kinase kinase kinase 3 Kinase Kd 6.55 CHEMBL
Serine/threonine-protein kinase NLK Kinase Kd 6.59 CHEMBL
Mitogen-activated protein kinase kinase kinase kinase 2 Kinase Kd 5.89 CHEMBL
Serine/threonine-protein kinase SIK1 Kinase Kd 8.41 CHEMBL
Mitogen-activated protein kinase 14 Kinase Kd 7.57 CHEMBL
Bcr/Abl fusion protein Kinase IC50 9.10 CHEMBL
Breakpoint cluster region protein Kinase WOMBAT-PK
Dual specificity mitogen-activated protein kinase kinase 5 Kinase Kd 8.48 CHEMBL
Mitogen-activated protein kinase kinase kinase MLT Kinase Kd 7.35 CHEMBL
Dual specificity mitogen-activated protein kinase kinase 1 Kinase Kd 6 CHEMBL
Receptor-type tyrosine-protein kinase FLT3 Kinase Kd 5.49 CHEMBL
Epidermal growth factor receptor Kinase Kd 7.10 CHEMBL
Proto-oncogene tyrosine-protein kinase Src Kinase Kd 7.96 CHEMBL
Tyrosine-protein kinase Blk Kinase IC50 8.10 CHEMBL
Proto-oncogene tyrosine-protein kinase LCK Kinase Ki 10.19 CHEMBL
Calcium-dependent protein kinase 1 Kinase Kd 6.19 CHEMBL
Tubulin alpha-1A chain Structural Kd 7.26 CHEMBL

External reference:

IDSource
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:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
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