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

Stem definitionDrug idCAS RN
tyrosine kinase inhibitors 4810 936563-96-1

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • imbruvica
  • PCI-32765
  • CRA-032765
  • PCI-32765-00
  • ibrutinib
Ibrutinib is a small-molecule inhibitor of BTK. Ibrutinib forms a covalent bond with a cysteine residue in the BTK active site, leading to inhibition of BTK enzymatic activity. BTK is a signaling molecule of the B-cell antigen receptor (BCR) and cytokine receptor pathways. BTK's role in signaling through the B-cell surface receptors results in activation of pathways necessary for B-cell trafficking, chemotaxis, and adhesion. Nonclinical studies show that ibrutinib inhibits malignant B-cell proliferation and survival in vivo as well as cell migration and substrate adhesion in vitro.
  • Molecular weight: 440.51
  • Formula: C25H24N6O2
  • CLOGP: 4.07
  • LIPINSKI: 0
  • HAC: 8
  • HDO: 1
  • TPSA: 99.16
  • ALOGS: -4.34
  • ROTB: 5

  • Status: OFP

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

Drug dosage:

None

ADMET properties:

PropertyValueReference
Vd (Volume of distribution) 9.75 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 16.40 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.03 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 5 hours Lombardo F, Berellini G, Obach RS

Approvals:

DateAgencyCompanyOrphan
Oct. 21, 2014 EMA
Nov. 13, 2013 FDA PHARMACYCLICS INC

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
Death 341.43 15.94 491 15499 335057 46335015
Atrial fibrillation 278.99 15.94 252 15738 103338 46566734
Incorrect dose administered 249.99 15.94 169 15821 45381 46624691
Chronic lymphocytic leukaemia 246.16 15.94 74 15916 2826 46667246
Contusion 177.02 15.94 182 15808 87305 46582767
Off label use 160.49 15.94 381 15609 379460 46290612
Petechiae 131.92 15.94 71 15919 12599 46657473
Mantle cell lymphoma 115.21 15.94 29 15961 562 46669510
White blood cell count increased 113.71 15.94 105 15885 44114 46625958
Disease progression 103.01 15.94 141 15849 91159 46578913
Lymphocytosis 92.02 15.94 33 15957 2201 46667871
Tumour lysis syndrome 90.91 15.94 46 15944 7190 46662882
Platelet count decreased 87.48 15.94 137 15853 99887 46570185
Drug ineffective 77.86 15.94 71 15919 677767 45992305
Lymphadenopathy 73.69 15.94 73 15917 33415 46636657
Pleural effusion 71.64 15.94 113 15877 82839 46587233
Drug hypersensitivity 70.74 15.94 3 15987 243822 46426250
Rheumatoid arthritis 69.54 15.94 3 15987 240212 46429860
Subdural haematoma 61.30 15.94 44 15946 12953 46657119
Epistaxis 60.28 15.94 91 15899 64214 46605858
Lymphocyte count increased 57.58 15.94 25 15965 2765 46667307
Progressive multifocal leukoencephalopathy 57.19 15.94 40 15950 11306 46658766
Haematoma 53.24 15.94 60 15930 31812 46638260
Onychoclasis 51.23 15.94 28 15962 5116 46664956
Thrombocytopenia 50.93 15.94 125 15865 126456 46543616
Haemorrhage intracranial 50.87 15.94 39 15951 12685 46657387
Product use in unapproved indication 50.83 15.94 102 15888 90171 46579901
Cerebral haemorrhage 48.39 15.94 54 15936 28317 46641755
Ecchymosis 48.04 15.94 35 15955 10541 46659531
Pneumonia 46.33 15.94 252 15738 376068 46294004
Autoimmune haemolytic anaemia 44.69 15.94 24 15966 4234 46665838
Capillary permeability increased 44.04 15.94 8 15982 27 46670045
Haemorrhage 43.59 15.94 72 15918 54797 46615275
Product use issue 42.97 15.94 98 15892 94546 46575526
Pericardial effusion 42.51 15.94 48 15942 25495 46644577
Increased tendency to bruise 39.99 15.94 30 15960 9444 46660628
Hospice care 39.82 15.94 24 15966 5271 46664801
Completed suicide 38.61 15.94 3 15987 145917 46524155
Haematotympanum 37.72 15.94 6 15984 6 46670066
Non-small cell lung cancer 36.63 15.94 19 15971 3125 46666947
Haemoglobin decreased 36.53 15.94 112 15878 128837 46541235
Aspergillus infection 36.38 15.94 25 15965 6865 46663207
Muscle spasms 35.88 15.94 108 15882 123005 46547067
Hospitalisation 34.92 15.94 71 15919 63314 46606758
Neutropenia 34.79 15.94 118 15872 143086 46526986
Hyperuricaemia 31.95 15.94 20 15970 4697 46665375
Blood blister 31.36 15.94 14 15976 1654 46668418
Condition aggravated 30.00 15.94 24 15966 245028 46425044
Toxicity to various agents 29.54 15.94 18 15972 211748 46458324
Cytopenia 29.28 15.94 23 15967 7745 46662327
Eye haemorrhage 29.03 15.94 22 15968 7030 46663042
Chronic lymphocytic leukaemia refractory 28.82 15.94 6 15984 47 46670025
Haematuria 28.02 15.94 40 15950 26818 46643254
Leukocytosis 27.64 15.94 37 15953 23361 46646711
Pain 27.19 15.94 79 15911 476869 46193203
Blood count abnormal 27.06 15.94 32 15958 17846 46652226
Sepsis 27.02 15.94 105 15885 135909 46534163
Splenomegaly 26.82 15.94 24 15966 9664 46660408
Neutrophil count decreased 26.76 15.94 51 15939 43375 46626697
Diarrhoea 26.00 15.94 299 15691 559303 46110769
Febrile neutropenia 24.77 15.94 80 15910 94547 46575525
Purpura 24.32 15.94 23 15967 9935 46660137
Urinary tract infection 24.03 15.94 143 15847 220123 46449949
Nonspecific reaction 23.93 15.94 12 15978 1838 46668234
Discouragement 23.50 15.94 5 15985 44 46670028
Meningitis cryptococcal 22.37 15.94 10 15980 1185 46668887
Ear haemorrhage 21.80 15.94 10 15980 1258 46668814
Bronchopulmonary aspergillosis 21.61 15.94 19 15971 7477 46662595
Nail disorder 20.75 15.94 19 15971 7877 46662195
Chronic lymphocytic leukaemia recurrent 20.73 15.94 6 15984 200 46669872
Overdose 20.24 15.94 5 15985 101974 46568098
Haemothorax 20.10 15.94 11 15979 2013 46668059
Infusion related reaction 20.01 15.94 5 15985 101203 46568869
Splenic haematoma 20.00 15.94 5 15985 94 46669978
Skin haemorrhage 19.15 15.94 16 15974 5875 46664197
Hypercalcaemia 18.59 15.94 29 15961 21017 46649055
Haemorrhagic diathesis 18.51 15.94 13 15977 3695 46666377
Leukostasis syndrome 17.68 15.94 4 15986 48 46670024
Psoriasis 17.36 15.94 3 15987 78601 46591471
Pyrexia 17.32 15.94 189 15801 348613 46321459
Arthropathy 17.10 15.94 4 15986 84696 46585376
Breast haematoma 16.96 15.94 5 15985 178 46669894
Campylobacter gastroenteritis 16.85 15.94 6 15984 392 46669680
Lichenification 16.83 15.94 6 15984 393 46669679
Therapeutic product effect decreased 16.48 15.94 4 15986 82597 46587475
Gingival bleeding 16.25 15.94 20 15970 11619 46658453
Pseudohyperkalaemia 16.12 15.94 3 15987 12 46670060
Hypogammaglobulinaemia 16.11 15.94 14 15976 5424 46664648
Septic shock 16.10 15.94 50 15940 57843 46612229

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
Atrial fibrillation 608.30 13.87 656 31061 107468 29813293
Chronic lymphocytic leukaemia 382.18 13.87 154 31563 4474 29916287
Incorrect dose administered 352.85 13.87 282 31435 31404 29889357
Death 332.05 13.87 975 30742 356308 29564453
Mantle cell lymphoma 272.67 13.87 90 31627 1451 29919310
Off label use 269.74 13.87 720 30997 248570 29672191
Disease progression 217.24 13.87 339 31378 79535 29841226
Contusion 205.93 13.87 207 31510 31073 29889688
Lymphocytosis 199.43 13.87 76 31641 1894 29918867
Lymphocyte count increased 190.75 13.87 79 31638 2463 29918298
Haemorrhage 172.82 13.87 228 31489 45851 29874910
Lymphadenopathy 138.27 13.87 149 31568 24227 29896534
White blood cell count increased 134.57 13.87 187 31530 39486 29881275
Toxicity to various agents 127.88 13.87 18 31699 177165 29743596
Subdural haematoma 121.95 13.87 124 31593 18848 29901913
Platelet count decreased 115.52 13.87 308 31409 105821 29814940
Pleural effusion 115.24 13.87 247 31470 73819 29846942
Product use issue 105.52 13.87 181 31536 45835 29874926
Tumour lysis syndrome 105.05 13.87 96 31621 12789 29907972
Bronchopulmonary aspergillosis 101.08 13.87 92 31625 12192 29908569
Petechiae 94.59 13.87 78 31639 9053 29911708
Cerebral aspergillosis 94.49 13.87 40 31677 1318 29919443
Pneumonia 94.30 13.87 640 31077 333666 29587095
Completed suicide 88.43 13.87 4 31713 99488 29821273
Increased tendency to bruise 80.21 13.87 49 31668 3532 29917229
Haematoma 79.82 13.87 112 31605 23841 29896920
Microsporidia infection 74.71 13.87 27 31690 577 29920184
Pericardial effusion 67.69 13.87 97 31620 21047 29899714
Basal cell carcinoma 67.21 13.87 84 31633 15984 29904777
Haemothorax 65.59 13.87 43 31674 3506 29917255
Hypogammaglobulinaemia 65.40 13.87 50 31667 5202 29915559
Mantle cell lymphoma recurrent 64.13 13.87 22 31695 401 29920360
Epistaxis 63.95 13.87 160 31557 52821 29867940
Scleroderma 60.20 13.87 29 31688 1298 29919463
Autoimmune haemolytic anaemia 58.06 13.87 42 31675 4017 29916744
Atrial flutter 57.10 13.87 73 31644 14208 29906553
Product use in unapproved indication 54.65 13.87 187 31530 73506 29847255
Overdose 53.31 13.87 12 31705 84325 29836436
Drug ineffective 53.22 13.87 184 31533 340203 29580558
Aspergillus infection 50.26 13.87 58 31659 10156 29910605
Haemoglobin decreased 49.98 13.87 246 31471 113852 29806909
Splenomegaly 49.38 13.87 66 31651 13414 29907347
Haematuria 48.54 13.87 130 31587 44704 29876057
Chronic lymphocytic leukaemia recurrent 48.33 13.87 18 31699 420 29920341
Cerebral haemorrhage 46.90 13.87 106 31611 32781 29887980
Mantle cell lymphoma refractory 44.29 13.87 12 31705 93 29920668
Post procedural haemorrhage 44.20 13.87 48 31669 7862 29912899
Plasma cell myeloma 42.06 13.87 4 31713 53458 29867303
Platelet count abnormal 39.80 13.87 27 31690 2330 29918431
Cardiac failure 39.50 13.87 184 31533 83234 29837527
Subdural haemorrhage 39.45 13.87 29 31688 2843 29917918
Ecchymosis 38.95 13.87 41 31676 6481 29914280
White blood cell count abnormal 38.89 13.87 28 31689 2658 29918103
Hospitalisation 37.81 13.87 118 31599 44201 29876560
Blood blister 37.60 13.87 22 31695 1465 29919296
Neutrophil count decreased 37.11 13.87 114 31603 42340 29878421
Blood immunoglobulin M increased 36.43 13.87 12 31705 192 29920569
Agitation 33.55 13.87 8 31709 54065 29866696
Vomiting 33.46 13.87 120 31597 219698 29701063
Skin haemorrhage 32.76 13.87 28 31689 3412 29917349
Condition aggravated 32.75 13.87 60 31657 137806 29782955
Surgery 32.65 13.87 50 31667 11501 29909260
Haemorrhage subcutaneous 31.66 13.87 23 31694 2214 29918547
Haemorrhagic diathesis 31.19 13.87 25 31692 2786 29917975
Nausea 30.00 13.87 188 31529 296769 29623992
Angina bullosa haemorrhagica 29.99 13.87 8 31709 58 29920703
Somnolence 29.94 13.87 35 31682 96728 29824033
Blood urine present 29.62 13.87 44 31673 9856 29910905
Ureteric compression 29.15 13.87 7 31710 31 29920730
Granuloma skin 28.97 13.87 11 31706 271 29920490
Metabolic acidosis 28.94 13.87 3 31714 37458 29883303
Pericarditis 28.30 13.87 40 31677 8566 29912195
Suicide attempt 28.20 13.87 3 31714 36694 29884067
COVID-19 28.17 13.87 60 31657 17818 29902943
Polymyositis 28.01 13.87 18 31699 1418 29919343
Blood pressure decreased 27.24 13.87 8 31709 47067 29873694
Hypoglycaemia 27.15 13.87 10 31707 50971 29869790
Stomatitis 27.08 13.87 94 31623 37185 29883576
Splenic rupture 26.90 13.87 18 31699 1518 29919243
Drug hypersensitivity 26.83 13.87 20 31697 68499 29852262
Haemorrhage intracranial 26.69 13.87 53 31664 14979 29905782
Hospice care 26.61 13.87 28 31689 4424 29916337
Chronic graft versus host disease 26.59 13.87 27 31690 4092 29916669
Lymphoma transformation 26.44 13.87 9 31708 160 29920601
Pericardial haemorrhage 26.27 13.87 23 31694 2895 29917866
Iodine uptake abnormal 25.80 13.87 5 31712 5 29920756
Hallucination 25.50 13.87 10 31707 49049 29871712
Anxiety 25.21 13.87 35 31682 89836 29830925
Depressed level of consciousness 25.04 13.87 5 31712 38217 29882544
Peripheral swelling 24.81 13.87 129 31588 60945 29859816
Ear haemorrhage 24.75 13.87 14 31703 874 29919887
Mass 24.69 13.87 34 31683 7106 29913655
Blood pressure increased 24.49 13.87 24 31693 71904 29848857
Squamous cell carcinoma 24.36 13.87 41 31676 10209 29910552
Brain abscess 23.87 13.87 21 31696 2660 29918101
Intentional product misuse 23.86 13.87 4 31713 34663 29886098
Haemolytic anaemia 23.74 13.87 40 31677 9970 29910791
Onychoclasis 23.35 13.87 17 31700 1642 29919119
Psoriasis 23.21 13.87 8 31709 42498 29878263
Immunodeficiency common variable 22.67 13.87 8 31709 159 29920602
Tremor 22.52 13.87 28 31689 75335 29845426
Splenic haemorrhage 22.46 13.87 10 31707 373 29920388
Neutropenia 22.34 13.87 221 31496 128319 29792442
Rhabdomyolysis 21.89 13.87 21 31696 63559 29857202
Eye operation 21.77 13.87 9 31708 279 29920482
Eye haemorrhage 21.60 13.87 23 31694 3684 29917077
Haemorrhagic disorder 21.45 13.87 11 31706 564 29920197
Gastric haemorrhage 21.35 13.87 37 31680 9430 29911331
Suicidal ideation 21.15 13.87 6 31711 36108 29884653
Prostatic operation 21.13 13.87 9 31708 301 29920460
Leukostasis syndrome 21.04 13.87 5 31712 21 29920740
Chronic lymphocytic leukaemia transformation 21.00 13.87 8 31709 199 29920562
Leukocytosis 20.93 13.87 60 31657 21442 29899319
Immunodeficiency 20.48 13.87 24 31693 4270 29916491
Pulmonary embolism 20.38 13.87 32 31685 78103 29842658
Lymphocyte count decreased 20.35 13.87 55 31662 19000 29901761
Loss of consciousness 20.24 13.87 33 31684 79342 29841419
Arrhythmia 20.19 13.87 79 31638 33090 29887671
Pulmonary mass 20.14 13.87 39 31678 10823 29909938
Cryptococcosis 19.94 13.87 16 31701 1786 29918975
International normalised ratio increased 19.92 13.87 13 31704 47726 29873035
Pseudomonas infection 19.88 13.87 38 31679 10444 29910317
Conjunctival haemorrhage 19.85 13.87 19 31698 2681 29918080
Muscle spasms 19.82 13.87 127 31590 64711 29856050
Renal impairment 19.65 13.87 37 31680 84147 29836614
Herpes zoster 19.61 13.87 73 31644 29870 29890891
Mucormycosis 19.60 13.87 26 31691 5242 29915519
Bladder operation 19.50 13.87 6 31711 76 29920685
Electrocardiogram QT prolonged 19.13 13.87 7 31710 35828 29884933
Skin cancer 19.13 13.87 32 31685 7929 29912832
Pneumonia cryptococcal 19.04 13.87 11 31706 715 29920046
Subarachnoid haemorrhage 18.94 13.87 36 31681 9850 29910911
Thrombocytopenia 18.89 13.87 225 31492 136819 29783942
Gamma-glutamyltransferase increased 18.89 13.87 4 31713 29346 29891415
Aggression 18.41 13.87 8 31709 36899 29883862
Blood count abnormal 18.23 13.87 39 31678 11613 29909148
Hypotension 18.19 13.87 131 31586 200434 29720327
Discouragement 17.56 13.87 3 31714 0 29920761
Lymph node haemorrhage 17.56 13.87 3 31714 0 29920761
Abnormal behaviour 17.54 13.87 3 31714 25620 29895141
Cerebral fungal infection 17.53 13.87 7 31710 198 29920563
Skin mass 17.51 13.87 20 31697 3462 29917299
Pyoderma gangrenosum 17.47 13.87 12 31705 1057 29919704
Cardiac tamponade 17.40 13.87 23 31694 4621 29916140
Meningitis enteroviral 16.98 13.87 5 31712 54 29920707
Blood urea increased 16.97 13.87 6 31711 31375 29889386
Acute kidney injury 16.95 13.87 197 31520 273645 29647116
Diffuse large B-cell lymphoma 16.85 13.87 30 31687 7811 29912950
Therapeutic product effect decreased 16.71 13.87 5 31712 29071 29891690
Confusional state 16.50 13.87 80 31637 134754 29786007
Pyrexia 16.49 13.87 418 31299 294071 29626690
Cardiomyopathy 16.46 13.87 44 31673 15099 29905662
Hypercalcaemia 16.40 13.87 39 31678 12456 29908305
Thyroxine increased 16.28 13.87 5 31712 63 29920698
Tachyarrhythmia 16.10 13.87 18 31699 3043 29917718
Anaphylactic reaction 15.74 13.87 5 31712 27977 29892784
Urticaria 15.57 13.87 21 31696 54585 29866176
Skin lesion 15.54 13.87 49 31668 18445 29902316
Scrotal haematocoele 15.51 13.87 4 31713 25 29920736
Mastoid effusion 15.48 13.87 3 31714 3 29920758
C-reactive protein increased 15.39 13.87 14 31703 43459 29877302
Flushing 15.34 13.87 6 31711 29486 29891275
Hypersensitivity 15.19 13.87 21 31696 54007 29866754
Prostatectomy 15.15 13.87 6 31711 166 29920595
Human rhinovirus test positive 15.08 13.87 6 31711 168 29920593
Marginal zone lymphoma 15.00 13.87 4 31713 29 29920732
Hyperphosphataemia 14.93 13.87 15 31702 2244 29918517
Aspartate aminotransferase increased 14.69 13.87 28 31689 63394 29857367
Malaise 14.67 13.87 110 31607 166852 29753909
Deep vein thrombosis 14.64 13.87 26 31691 60475 29860286
Peptic ulcer haemorrhage 14.64 13.87 8 31709 467 29920294
Procedural haemorrhage 14.50 13.87 15 31702 2323 29918438
Product use complaint 14.41 13.87 11 31706 1141 29919620
Blood glucose increased 14.39 13.87 27 31690 61503 29859258
Myositis 14.29 13.87 33 31684 10344 29910417
Febrile neutropenia 14.18 13.87 174 31543 106519 29814242
Lymphoedema 14.16 13.87 18 31699 3481 29917280
Infective exacerbation of chronic obstructive airways disease 14.15 13.87 12 31705 1446 29919315
Seizure 14.13 13.87 55 31662 98420 29822341
Pruritus 13.96 13.87 71 31646 118133 29802628
Vitreous haemorrhage 13.93 13.87 14 31703 2096 29918665

Pharmacologic Action:

SourceCodeDescription
ATC L01EL01 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
ANTINEOPLASTIC AGENTS
PROTEIN KINASE INHIBITORS
Bruton's tyrosine kinase (BTK) inhibitors
FDA MoA N0000175076 Protein Kinase Inhibitors
FDA EPC N0000175605 Kinase Inhibitor
CHEBI has role CHEBI:35610 cytostatic
CHEBI has role CHEBI:76617 abl inhibitors

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Chronic lymphoid leukemia, disease indication 92814006
Waldenström macroglobulinemia indication 190818004 DOID:0050747
Chronic graft-versus-host disease indication 402356004
Mantle cell lymphoma indication 443487006
Pregnancy, function contraindication 289908002

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 4.7 Basic
pKa2 0.18 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
140MG IMBRUVICA PHARMACYCLICS INC N205552 Nov. 13, 2013 RX CAPSULE ORAL Feb. 12, 2021 TREATMENT OF PATIENTS WITH CHRONIC LYMPHOCYTIC LEUKEMIA (CLL) WHO HAVE RECEIVED AT LEAST ONE PRIOR THERAPY
140MG IMBRUVICA PHARMACYCLICS INC N205552 Nov. 13, 2013 RX CAPSULE ORAL July 28, 2021 TREATMENT OF PATIENTS WITH CHRONIC LYMPHOCYTIC LEUKEMIA WITH 17P DELETION WHO HAVE NOT RECEIVED AT LEAST ONE PRIOR THERAPY
140MG IMBRUVICA PHARMACYCLICS INC N205552 Nov. 13, 2013 RX CAPSULE ORAL Aug. 24, 2021 IBRUTINIB IN COMBINULLTION WITH RITUXIMAB
70MG IMBRUVICA PHARMACYCLICS INC N205552 Dec. 20, 2017 RX CAPSULE ORAL Aug. 24, 2021 IBRUTINIB IN COMBINULLTION WITH RITUXIMAB
140MG IMBRUVICA PHARMACYCLICS INC N210563 Feb. 16, 2018 RX TABLET ORAL Aug. 24, 2021 IBRUTINIB IN COMBINULLTION WITH RITUXIMAB
280MG IMBRUVICA PHARMACYCLICS INC N210563 Feb. 16, 2018 RX TABLET ORAL Aug. 24, 2021 IBRUTINIB IN COMBINULLTION WITH RITUXIMAB
420MG IMBRUVICA PHARMACYCLICS INC N210563 Feb. 16, 2018 RX TABLET ORAL Aug. 24, 2021 IBRUTINIB IN COMBINULLTION WITH RITUXIMAB
560MG IMBRUVICA PHARMACYCLICS INC N210563 Feb. 16, 2018 RX TABLET ORAL Aug. 24, 2021 IBRUTINIB IN COMBINULLTION WITH RITUXIMAB
140MG IMBRUVICA PHARMACYCLICS INC N205552 Nov. 13, 2013 RX CAPSULE ORAL Jan. 25, 2022 INFORMATION ADDED TO THE PRESCRIBING INFORMATION TO INCLUDE EFFICACY AND SAFETY DATA FROM A STUDY IN PATIENTS WITH TREATMENT NULLIVE CLL/SLL TREATED WITH IBRUTINIB IN COMBINULLTION WITH OBINUTUZUMAB OR CHLORAMBUCIL IN COMBINULLTION WITH OBINUTUZUMAB
70MG IMBRUVICA PHARMACYCLICS INC N205552 Dec. 20, 2017 RX CAPSULE ORAL Jan. 25, 2022 INFORMATION ADDED TO THE PRESCRIBING INFORMATION TO INCLUDE EFFICACY AND SAFETY DATA FROM A STUDY IN PATIENTS WITH TREATMENT NULLIVE CLL/SLL TREATED WITH IBRUTINIB IN COMBINULLTION WITH OBINUTUZUMAB OR CHLORAMBUCIL IN COMBINULLTION WITH OBINUTUZUMAB
140MG IMBRUVICA PHARMACYCLICS INC N210563 Feb. 16, 2018 RX TABLET ORAL Jan. 25, 2022 INFORMATION ADDED TO THE PRESCRIBING INFORMATION TO INCLUDE EFFICACY AND SAFETY DATA FROM A STUDY IN PATIENTS WITH TREATMENT NULLIVE CLL/SLL TREATED WITH IBRUTINIB IN COMBINULLTION WITH OBINUTUZUMAB OR CHLORAMBUCIL IN COMBINULLTION WITH OBINUTUZUMAB
280MG IMBRUVICA PHARMACYCLICS INC N210563 Feb. 16, 2018 RX TABLET ORAL Jan. 25, 2022 INFORMATION ADDED TO THE PRESCRIBING INFORMATION TO INCLUDE EFFICACY AND SAFETY DATA FROM A STUDY IN PATIENTS WITH TREATMENT NULLIVE CLL/SLL TREATED WITH IBRUTINIB IN COMBINULLTION WITH OBINUTUZUMAB OR CHLORAMBUCIL IN COMBINULLTION WITH OBINUTUZUMAB
420MG IMBRUVICA PHARMACYCLICS INC N210563 Feb. 16, 2018 RX TABLET ORAL Jan. 25, 2022 INFORMATION ADDED TO THE PRESCRIBING INFORMATION TO INCLUDE EFFICACY AND SAFETY DATA FROM A STUDY IN PATIENTS WITH TREATMENT NULLIVE CLL/SLL TREATED WITH IBRUTINIB IN COMBINULLTION WITH OBINUTUZUMAB OR CHLORAMBUCIL IN COMBINULLTION WITH OBINUTUZUMAB
560MG IMBRUVICA PHARMACYCLICS INC N210563 Feb. 16, 2018 RX TABLET ORAL Jan. 25, 2022 INFORMATION ADDED TO THE PRESCRIBING INFORMATION TO INCLUDE EFFICACY AND SAFETY DATA FROM A STUDY IN PATIENTS WITH TREATMENT NULLIVE CLL/SLL TREATED WITH IBRUTINIB IN COMBINULLTION WITH OBINUTUZUMAB OR CHLORAMBUCIL IN COMBINULLTION WITH OBINUTUZUMAB
140MG IMBRUVICA PHARMACYCLICS INC N205552 Nov. 13, 2013 RX CAPSULE ORAL Jan. 29, 2022 TREATMENT OF PATIENTS WITH WALDENSTROMS MACROGLOBULINEMIA
140MG IMBRUVICA PHARMACYCLICS INC N205552 Nov. 13, 2013 RX CAPSULE ORAL March 4, 2023 INDICATED FOR THE TREATMENT OF PATIENTS WITH CHRONIC LYMPHOCYTIC LEUKEMIA WITHOUT 17P DELETION WHO HAVE NOT RECEIVED AT LEAST ONE PRIOR THERAPY (FIRST LINE THERAPY)
140MG IMBRUVICA PHARMACYCLICS INC N205552 Nov. 13, 2013 RX CAPSULE ORAL May 6, 2023 FOR TREATMENT OF PATIENTS WITH SMALL LYMPHOCYTIC LYMPHOMA (SLL)
140MG IMBRUVICA PHARMACYCLICS INC N205552 Nov. 13, 2013 RX CAPSULE ORAL Jan. 18, 2024 TREATMENT OF PATIENTS WITH MARGINULLL ZONE LYMPHOMA (MZL) WHO REQUIRE SYSTEMIC THERAPY AND HAVE RECEIVED AT LEAST ONE PRIOR ANTI-CD20-BASED THERAPY
140MG IMBRUVICA PHARMACYCLICS INC N205552 Nov. 13, 2013 RX CAPSULE ORAL Aug. 2, 2024 TREATMENT OF ADULT PATIENTS WITH CHRONIC GRAFT VERSUS HOST DISEASE (CGVHD)

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Tyrosine-protein kinase BTK Kinase INHIBITOR Ki 9.14 SCIENTIFIC LITERATURE SCIENTIFIC LITERATURE
Tyrosine-protein kinase Lyn Kinase Ki 7.85 SCIENTIFIC LITERATURE
Epidermal growth factor receptor Kinase IC50 8.25 CHEMBL
Cytoplasmic tyrosine-protein kinase BMX Kinase IC50 9.10 CHEMBL
Proto-oncogene tyrosine-protein kinase receptor Ret Kinase IC50 7.43 CHEMBL
Fibroblast growth factor receptor 2 Kinase IC50 6.55 CHEMBL
Tyrosine-protein kinase Blk Kinase INHIBITOR IC50 10 SCIENTIFIC LITERATURE
Tyrosine-protein kinase Fgr Kinase INHIBITOR IC50 8.48 SCIENTIFIC LITERATURE
Tyrosine-protein kinase Fyn Kinase INHIBITOR IC50 7.54 SCIENTIFIC LITERATURE
Tyrosine-protein kinase HCK Kinase INHIBITOR IC50 7.54 SCIENTIFIC LITERATURE
Tyrosine-protein kinase Lck Kinase INHIBITOR IC50 8.20 SCIENTIFIC LITERATURE
Proto-oncogene tyrosine-protein kinase Src Kinase INHIBITOR IC50 7.72 SCIENTIFIC LITERATURE
Tyrosine-protein kinase Yes Kinase INHIBITOR IC50 8.39 SCIENTIFIC LITERATURE
Tyrosine-protein kinase ITK/TSK Kinase INHIBITOR IC50 8.31 SCIENTIFIC LITERATURE
Tyrosine-protein kinase Tec Kinase INHIBITOR IC50 8.15 SCIENTIFIC LITERATURE
Tyrosine-protein kinase TXK Kinase INHIBITOR IC50 8.70 SCIENTIFIC LITERATURE
Receptor tyrosine-protein kinase erbB-2 Kinase INHIBITOR IC50 8.19 SCIENTIFIC LITERATURE
Receptor tyrosine-protein kinase erbB-4 Kinase INHIBITOR IC50 8.47 SCIENTIFIC LITERATURE
Tyrosine-protein kinase JAK3 Kinase INHIBITOR IC50 7.49 SCIENTIFIC LITERATURE

External reference:

IDSource
D10223 KEGG_DRUG
4032872 VANDF
C2830052 UMLSCUI
CHEBI:76612 CHEBI
1E8 PDB_CHEM_ID
CHEMBL1873475 ChEMBL_ID
DB09053 DRUGBANK_ID
C551803 MESH_SUPPLEMENTAL_RECORD_UI
24821094 PUBCHEM_CID
6912 IUPHAR_LIGAND_ID
9566 INN_ID
1X70OSD4VX UNII
1442981 RXNORM
207254 MMSL
29840 MMSL
d08170 MMSL
015287 NDDF
710228002 SNOMEDCT_US
715598009 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Imbruvica HUMAN PRESCRIPTION DRUG LABEL 1 57962-014 TABLET, FILM COATED 140 mg ORAL NDA 30 sections
Imbruvica HUMAN PRESCRIPTION DRUG LABEL 1 57962-070 CAPSULE 70 mg ORAL NDA 30 sections
Imbruvica HUMAN PRESCRIPTION DRUG LABEL 1 57962-140 CAPSULE 140 mg ORAL NDA 30 sections
Imbruvica HUMAN PRESCRIPTION DRUG LABEL 1 57962-280 TABLET, FILM COATED 280 mg ORAL NDA 30 sections
Imbruvica HUMAN PRESCRIPTION DRUG LABEL 1 57962-420 TABLET, FILM COATED 420 mg ORAL NDA 30 sections
Imbruvica HUMAN PRESCRIPTION DRUG LABEL 1 57962-560 TABLET, FILM COATED 560 mg ORAL NDA 30 sections