carfilzomib 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |

Stem definitionDrug idCAS RN
proteasome inhibitors 4483 868540-17-4

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • carfilzomib
  • kyprolis
  • PR-171
  • PR 171
epoxomicin derivative proteasome inhibitor with antiproliferative and proapoptotic effects on primary human acute myeloid leukaemia cells
  • Molecular weight: 719.92
  • Formula: C40H57N5O7
  • CLOGP: 4.21
  • LIPINSKI: 3
  • HAC: 12
  • HDO: 4
  • TPSA: 158.47
  • ALOGS: -5.17
  • ROTB: 20
  • Status: OFP
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

None

ADMET properties:

PropertyValueReference
Vd (Volume of distribution) 0.13 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 39.50 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.02 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 1.10 hours Lombardo F, Berellini G, Obach RS
BA (Bioavailability) 0 %

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
kinase-safety-class ACVR2B,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK5,CDK9,EIF2AK3,EPHB4,ERBB2,GRK2,ITK,MAPK7,MET,NTRK2,PDK1,PDK2,PDK4,PIK3CB,PRKDC,TEK 22
kinase-selectivity-class GRK2,PDK4 2
pfas-class PFAS structural alert (1 = True, 0 = False) 0

Approvals:

DateAgencyCompanyOrphan
July 4, 2016 PMDA Ono Pharmaceutical
July 20, 2012 FDA ONYX PHARMS

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
Thrombocytopenia 571.97 18.33 454 22882 208271 90396840
Plasma cell myeloma 457.44 18.33 219 23117 40609 90564502
Intercepted product preparation error 429.42 18.33 93 23243 1227 90603884
Thrombotic microangiopathy 421.65 18.33 157 23179 15586 90589525
Plasma cell myeloma refractory 330.07 18.33 72 23264 984 90604127
Cytopenia 298.87 18.33 126 23210 17323 90587788
Plasma cell myeloma recurrent 282.29 18.33 84 23252 4144 90600967
Neutropenia 281.26 18.33 317 23019 224587 90380524
Off label use 226.93 18.33 708 22628 1101544 89503567
Death 207.86 18.33 399 22937 456152 90148959
Tumour lysis syndrome 202.59 18.33 84 23252 11068 90594043
Anaemia 200.92 18.33 340 22996 352462 90252649
Therapy partial responder 187.04 18.33 98 23238 21945 90583166
Platelet count decreased 186.41 18.33 202 23134 136767 90468344
Neuropathy peripheral 184.66 18.33 201 23135 136769 90468342
Disease progression 175.81 18.33 209 23127 156406 90448705
Cardiac failure 158.68 18.33 167 23169 109329 90495782
Cytokine release syndrome 157.41 18.33 95 23241 27878 90577233
Pancytopenia 147.47 18.33 168 23168 120095 90485016
Myelosuppression 147.12 18.33 117 23219 53474 90551637
Acute kidney injury 144.28 18.33 279 23057 320108 90285003
Light chain analysis increased 130.74 18.33 37 23299 1525 90603586
Pyrexia 130.21 18.33 419 22917 660066 89945045
Unevaluable event 123.99 18.33 107 23229 54741 90550370
Hypogammaglobulinaemia 118.64 18.33 57 23279 10617 90594494
Plasmacytoma 117.49 18.33 39 23297 2754 90602357
Renal failure 115.42 18.33 155 23181 130852 90474259
Pneumonia 115.18 18.33 393 22943 637666 89967445
Sepsis 107.02 18.33 177 23159 179637 90425474
Osteolysis 100.87 18.33 37 23299 3513 90601598
COVID-19 94.87 18.33 162 23174 168681 90436430
Atypical haemolytic uraemic syndrome 94.49 18.33 26 23310 965 90604146
COVID-19 pneumonia 82.80 18.33 54 23282 18123 90586988
Drug hypersensitivity 82.40 18.33 11 23325 463598 90141513
Febrile infection 79.54 18.33 27 23309 2042 90603069
Pulmonary embolism 78.10 18.33 129 23207 130691 90474420
Haemolytic uraemic syndrome 75.09 18.33 28 23308 2783 90602328
Arthropathy 74.79 18.33 5 23331 366237 90238874
Joint swelling 74.38 18.33 19 23317 503281 90101830
Bone marrow disorder 73.03 18.33 28 23308 3004 90602107
Glossodynia 70.04 18.33 3 23333 321776 90283335
Arthralgia 66.12 18.33 62 23274 778460 89826651
Leukopenia 65.12 18.33 103 23233 100607 90504504
Musculoskeletal stiffness 63.76 18.33 3 23333 296529 90308582
Neutrophil count decreased 63.50 18.33 85 23251 71447 90533664
Wound 62.25 18.33 4 23332 302976 90302135
Posterior reversible encephalopathy syndrome 61.76 18.33 49 23287 22290 90582821
Swelling 61.55 18.33 16 23320 419042 90186069
Alopecia 60.36 18.33 26 23310 495045 90110066
Body dysmorphic disorder 59.42 18.33 15 23321 396 90604715
White blood cell count decreased 59.16 18.33 132 23204 166977 90438134
Pulmonary oedema 58.55 18.33 76 23260 62004 90543107
Acute pulmonary oedema 57.69 18.33 34 23302 9546 90595565
Abdominal discomfort 56.72 18.33 26 23310 477302 90127809
Lymphopenia 56.53 18.33 47 23289 22834 90582277
Haemolytic anaemia 56.35 18.33 36 23300 11661 90593450
Plasma cell leukaemia 56.11 18.33 18 23318 1140 90603971
Product use issue 53.68 18.33 10 23326 329909 90275202
Pericarditis 51.49 18.33 5 23331 270146 90334965
Pneumonitis 51.21 18.33 60 23276 44110 90561001
Plasma cells increased 48.79 18.33 10 23326 99 90605012
Laboratory test abnormal 48.76 18.33 57 23279 41797 90563314
Respiratory failure 48.18 18.33 99 23237 118319 90486792
Full blood count decreased 47.87 18.33 48 23288 29641 90575470
Condition aggravated 47.54 18.33 50 23286 595495 90009616
Blister 45.38 18.33 6 23330 254992 90350119
Bone pain 45.13 18.33 67 23269 61916 90543195
Microangiopathic haemolytic anaemia 44.95 18.33 14 23322 805 90604306
Cardiac failure congestive 44.33 18.33 86 23250 98608 90506503
Pain 44.26 18.33 122 23214 996219 89608892
Cerebellar haemangioma 44.01 18.33 9 23327 88 90605023
Pulmonary hypertension 43.16 18.33 54 23282 42469 90562642
Hypertensive crisis 42.83 18.33 36 23300 17748 90587363
Joint ankylosis 42.34 18.33 15 23321 1288 90603823
Blood cholesterol increased 41.97 18.33 3 23333 208009 90397102
Protein total increased 39.78 18.33 19 23317 3490 90601621
Pneumococcal sepsis 39.33 18.33 13 23323 905 90604206
Blood calcium increased 38.92 18.33 29 23307 12029 90593082
Acute respiratory failure 38.08 18.33 51 23285 42867 90562244
Haemolysis 38.06 18.33 25 23311 8485 90596626
Migraine 37.69 18.33 3 23333 190389 90414722
Natural killer cell count decreased 36.96 18.33 8 23328 105 90605006
Polyneuropathy 36.31 18.33 34 23302 19307 90585804
Respiratory tract infection 36.23 18.33 59 23277 59019 90546092
Cardiotoxicity 35.88 18.33 27 23309 11362 90593749
Pathological fracture 35.19 18.33 25 23311 9635 90595476
Stem cell transplant 35.02 18.33 15 23321 2139 90602972
Injury 34.27 18.33 5 23331 197344 90407767
Type 2 diabetes mellitus 33.38 18.33 6 23330 203238 90401873
Liver injury 32.90 18.33 3 23333 170564 90434547
Blood disorder 32.70 18.33 22 23314 7768 90597343
Abdominal pain upper 32.50 18.33 23 23313 332651 90272460
Deep vein thrombosis 31.98 18.33 72 23264 91548 90513563
Influenza 31.56 18.33 93 23243 139171 90465940
Weight increased 31.22 18.33 37 23299 417890 90187221
Thrombotic thrombocytopenic purpura 31.16 18.33 17 23319 4121 90600990
Cardiac disorder 31.15 18.33 54 23282 56818 90548293
Discomfort 30.94 18.33 16 23320 274319 90330792
Cerebral toxoplasmosis 30.38 18.33 12 23324 1393 90603718
Progressive multifocal leukoencephalopathy 30.31 18.33 28 23308 15627 90589484
B-cell aplasia 29.98 18.33 8 23328 264 90604847
Dyspnoea 29.85 18.33 352 22984 880603 89724508
Wheezing 29.78 18.33 12 23324 238068 90367043
Occupational exposure to product 29.60 18.33 14 23322 2517 90602594
Jugular vein occlusion 28.95 18.33 6 23330 63 90605048
Pneumonia pneumococcal 28.73 18.33 14 23322 2688 90602423
Immunoglobulins decreased 28.69 18.33 12 23324 1614 90603497
Cardiac failure acute 28.42 18.33 24 23312 11905 90593206
Light chain analysis abnormal 27.87 18.33 7 23329 181 90604930
Inflammation 27.80 18.33 6 23330 178586 90426525
Pulmonary arterial hypertension 27.77 18.33 34 23302 26153 90578958
Pulmonary alveolar haemorrhage 27.75 18.33 18 23318 5980 90599131
Lower respiratory tract infection 27.71 18.33 15 23321 250644 90354467
Urticaria 27.54 18.33 24 23312 312710 90292401
Psoriasis 27.45 18.33 3 23333 147751 90457360
Post procedural diarrhoea 27.39 18.33 8 23328 369 90604742
Hypersensitivity 27.29 18.33 47 23289 454630 90150481
Atrial fibrillation 27.25 18.33 86 23250 133525 90471586
Hepatitis E 26.90 18.33 12 23324 1887 90603224
Candida pneumonia 26.87 18.33 7 23329 210 90604901
Fatigue 26.82 18.33 431 22905 1153592 89451519
Completed suicide 26.81 18.33 3 23333 145055 90460056
Hepatitis B reactivation 26.30 18.33 15 23321 3959 90601152
Febrile neutropenia 26.19 18.33 95 23241 158254 90446857
Osteoarthritis 25.93 18.33 9 23327 195721 90409390
Central nervous system vasculitis 25.85 18.33 10 23326 1099 90604012
Diarrhoea 25.77 18.33 361 22975 938829 89666282
Secondary immunodeficiency 25.60 18.33 12 23324 2114 90602997
Fibrosis 25.44 18.33 17 23319 5935 90599176
Bronchopulmonary aspergillosis 25.26 18.33 22 23314 11376 90593735
Acute lymphocytic leukaemia 25.11 18.33 13 23323 2835 90602276
Injection site pain 24.77 18.33 7 23329 173692 90431419
Drug interaction 24.60 18.33 21 23315 276432 90328679
Alveolar proteinosis 24.41 18.33 9 23327 867 90604244
Bone lesion 24.24 18.33 17 23319 6420 90598691
Pruritus 24.19 18.33 66 23270 541459 90063652
Myeloma cast nephropathy 23.82 18.33 6 23330 157 90604954
Immune effector cell-associated neurotoxicity syndrome 23.52 18.33 16 23320 5752 90599359
Escherichia sepsis 23.40 18.33 16 23320 5800 90599311
Overdose 23.16 18.33 6 23330 157703 90447408
Pneumonia bacterial 23.08 18.33 22 23314 12768 90592343
Rhinovirus infection 23.04 18.33 16 23320 5947 90599164
Infusion site extravasation 23.02 18.33 20 23316 10308 90594803
Sleep disorder due to general medical condition, insomnia type 22.95 18.33 3 23333 128691 90476420
Pneumonia parainfluenzae viral 22.92 18.33 7 23329 377 90604734
Sinusitis 22.91 18.33 33 23303 343055 90262056
Treatment failure 22.58 18.33 27 23309 303901 90301210
Contusion 22.45 18.33 19 23317 251197 90353914
Meningitis listeria 22.45 18.33 8 23328 699 90604412
Listeria sepsis 22.13 18.33 8 23328 728 90604383
Ill-defined disorder 22.03 18.33 10 23326 184881 90420230
Depression 22.02 18.33 27 23309 300574 90304537
Intervertebral discitis 21.99 18.33 14 23322 4506 90600605
Multiple organ dysfunction syndrome 21.97 18.33 52 23284 68284 90536827
Syncope 21.44 18.33 79 23257 132584 90472527
Therapeutic product effect decreased 21.33 18.33 24 23312 277547 90327564
Pneumonia cytomegaloviral 21.29 18.33 12 23324 3099 90602012
Klebsiella sepsis 21.28 18.33 10 23326 1771 90603340
Paraproteinaemia 21.11 18.33 6 23330 251 90604860
Anxiety disorder 20.90 18.33 14 23322 4908 90600203
Anxiety 20.48 18.33 30 23306 309742 90295369
Aspergilloma 20.41 18.33 6 23330 283 90604828
Acute cardiac event 20.39 18.33 4 23332 31 90605080
Clostridial sepsis 20.17 18.33 7 23329 566 90604545
Conjunctivitis viral 20.04 18.33 6 23330 302 90604809
Hypergammaglobulinaemia benign monoclonal 20.02 18.33 8 23328 958 90604153
Ejection fraction decreased 20.00 18.33 29 23307 26224 90578887
Sepsis syndrome 19.96 18.33 8 23328 965 90604146
Protein total abnormal 19.72 18.33 7 23329 605 90604506
Hypertension 19.71 18.33 192 23144 457340 90147771
B-cell type acute leukaemia 19.64 18.33 7 23329 612 90604499
Acute respiratory distress syndrome 19.44 18.33 30 23306 28656 90576455
Abdominal pain 19.38 18.33 46 23290 395675 90209436
Asthenia 19.23 18.33 216 23120 533535 90071576
Pulmonary sepsis 19.15 18.33 10 23326 2221 90602890
Stomatitis 18.75 18.33 26 23310 274672 90330439
Thrombosis 18.61 18.33 51 23285 73200 90531911
Leukaemic infiltration extramedullary 18.59 18.33 5 23331 170 90604941
Venoocclusive liver disease 18.42 18.33 14 23322 5979 90599132
Corneal leukoma 18.38 18.33 4 23332 54 90605057
Infusion site pain 18.35 18.33 24 23312 19714 90585397

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
Thrombocytopenia 446.82 17.21 574 26390 189705 42404666
Plasma cell myeloma 355.73 17.21 271 26693 47307 42547064
Plasma cell myeloma recurrent 342.27 17.21 131 26833 5626 42588745
Thrombotic microangiopathy 335.78 17.21 171 26793 14611 42579760
Plasma cell myeloma refractory 271.74 17.21 78 26886 1332 42593039
Intercepted product preparation error 258.22 17.21 115 26849 7274 42587097
Plasmacytoma 219.53 17.21 88 26876 4276 42590095
Therapy partial responder 219.03 17.21 144 26820 19877 42574494
Off label use 185.65 17.21 844 26120 637491 41956880
Pneumonia 181.97 17.21 632 26332 421517 42172854
Neutropenia 168.57 17.21 382 26582 199049 42395322
Neuropathy peripheral 145.92 17.21 244 26720 101609 42492762
Cytopenia 142.46 17.21 105 26859 17392 42576979
Plasma cell leukaemia 142.11 17.21 46 26918 1194 42593177
Unevaluable event 130.11 17.21 133 26831 34155 42560216
Drug interaction 128.33 17.21 11 26953 266988 42327383
Haemolytic uraemic syndrome 104.31 17.21 44 26920 2435 42591936
Platelet count decreased 103.31 17.21 253 26711 138328 42456043
Tumour lysis syndrome 98.75 17.21 94 26870 22137 42572234
Deep vein thrombosis 96.60 17.21 174 26790 76783 42517588
Myelosuppression 94.28 17.21 122 26842 40339 42554032
Death 89.94 17.21 556 26408 470629 42123742
Cardiac failure 87.06 17.21 202 26762 106654 42487717
Pyrexia 78.89 17.21 471 26493 393571 42200800
Disease progression 75.74 17.21 231 26733 143425 42450946
Condition aggravated 72.96 17.21 37 26927 260717 42333654
Fatigue 63.27 17.21 481 26483 435160 42159211
Pancytopenia 62.65 17.21 190 26774 117553 42476818
Infection 62.61 17.21 184 26780 111884 42482487
Anaemia 61.14 17.21 343 26621 279935 42314436
Atypical haemolytic uraemic syndrome 61.07 17.21 20 26944 539 42593832
Polyneuropathy 57.74 17.21 65 26899 18596 42575775
Influenza 56.70 17.21 123 26841 62052 42532319
Light chain analysis increased 56.29 17.21 26 26938 1788 42592583
COVID-19 56.05 17.21 181 26783 115767 42478604
Sepsis 54.57 17.21 260 26704 199074 42395297
Thrombotic thrombocytopenic purpura 50.65 17.21 31 26933 3773 42590598
Hypogammaglobulinaemia 48.51 17.21 48 26916 11843 42582528
COVID-19 pneumonia 48.50 17.21 64 26900 21549 42572822
Myelodysplastic syndrome 47.45 17.21 65 26899 22680 42571691
Acute kidney injury 47.42 17.21 395 26569 366942 42227429
Microangiopathic haemolytic anaemia 47.06 17.21 20 26944 1127 42593244
Ejection fraction decreased 45.90 17.21 63 26901 22024 42572347
Osteolysis 44.69 17.21 28 26936 3552 42590819
Leukopenia 42.94 17.21 124 26840 74622 42519749
Device related sepsis 42.58 17.21 28 26936 3859 42590512
Cardiac disorder 41.44 17.21 94 26870 48838 42545533
Hypertension 41.38 17.21 212 26752 166992 42427379
Hypercalcaemia 41.33 17.21 54 26910 18004 42576367
Bronchopneumopathy 40.56 17.21 15 26949 584 42593787
Respiratory tract infection 40.22 17.21 65 26899 26257 42568114
SARS-CoV-2 sepsis 39.88 17.21 12 26952 243 42594128
Renal failure 39.66 17.21 188 26776 143538 42450833
Myeloma cast nephropathy 39.39 17.21 10 26954 104 42594267
Pruritus 39.20 17.21 37 26927 188734 42405637
Laboratory test abnormal 38.22 17.21 59 26905 22919 42571452
Product use in unapproved indication 37.31 17.21 37 26927 184419 42409952
Pulmonary hypertension 37.10 17.21 59 26905 23510 42570861
White blood cell count decreased 36.17 17.21 152 26812 110244 42484127
Atrial fibrillation 35.93 17.21 179 26785 139414 42454957
Progressive multifocal leukoencephalopathy 35.37 17.21 40 26924 11496 42582875
Rhabdomyolysis 35.35 17.21 4 26960 78015 42516356
Arthralgia 35.21 17.21 47 26917 205191 42389180
Cardiac dysfunction 33.67 17.21 23 26941 3376 42590995
Bone lesion 33.26 17.21 23 26941 3443 42590928
Lymphodepletion 32.04 17.21 7 26957 35 42594336
Infusion site extravasation 31.89 17.21 27 26937 5454 42588917
Abdominal pain 30.31 17.21 46 26918 190425 42403946
Infusion site erythema 30.06 17.21 22 26942 3600 42590771
B-cell type acute leukaemia 29.58 17.21 13 26951 795 42593576
Escherichia bacteraemia 29.21 17.21 25 26939 5124 42589247
JC virus infection 28.98 17.21 20 26944 2984 42591387
Pathological fracture 28.62 17.21 25 26939 5268 42589103
Infusion site pain 28.20 17.21 25 26939 5370 42589001
Cerebral toxoplasmosis 27.68 17.21 17 26947 2081 42592290
Cardiac failure acute 26.99 17.21 38 26926 13595 42580776
Haematotoxicity 26.94 17.21 34 26930 10951 42583420
Blood immunoglobulin M increased 26.59 17.21 9 26955 269 42594102
Drug hypersensitivity 26.42 17.21 15 26949 99374 42494997
Pneumonia influenzal 26.40 17.21 16 26948 1913 42592458
Dizziness 26.34 17.21 76 26888 249178 42345193
Infection susceptibility increased 26.24 17.21 13 26951 1045 42593326
Dyspnoea 25.90 17.21 408 26556 442213 42152158
Haemolytic anaemia 25.81 17.21 35 26929 12092 42582279
Product dose omission issue 25.80 17.21 36 26928 154329 42440042
Seizure 25.75 17.21 23 26941 120538 42473833
Atrial flutter 25.53 17.21 42 26922 17209 42577162
Hepatitis B reactivation 25.51 17.21 22 26942 4556 42589815
H1N1 influenza 25.06 17.21 13 26951 1151 42593220
Monoclonal immunoglobulin present 24.73 17.21 13 26951 1183 42593188
Protein total increased 24.48 17.21 17 26947 2561 42591810
Bile acid malabsorption 24.24 17.21 7 26957 122 42594249
Hypertensive crisis 24.10 17.21 31 26933 10175 42584196
Overdose 23.81 17.21 19 26945 105245 42489126
Salmonellosis 23.73 17.21 13 26951 1285 42593086
Coma 23.63 17.21 3 26961 53551 42540820
Parainfluenzae virus infection 23.39 17.21 19 26945 3624 42590747
Spinal pain 23.36 17.21 25 26939 6757 42587614
Hyponatraemia 23.34 17.21 18 26946 101444 42492927
Acute pulmonary oedema 23.19 17.21 28 26936 8623 42585748
Headache 23.15 17.21 76 26888 239293 42355078
Pulmonary embolism 23.13 17.21 142 26822 119470 42474901
Paraproteinaemia 22.99 17.21 9 26955 410 42593961
Erythema 22.94 17.21 21 26943 108772 42485599
Morganella infection 22.79 17.21 10 26954 609 42593762
Bone pain 22.74 17.21 48 26916 23744 42570627
Anxiety 22.59 17.21 25 26939 118535 42475836
Pneumonia respiratory syncytial viral 22.52 17.21 13 26951 1421 42592950
Monoclonal immunoglobulin increased 22.41 17.21 9 26955 439 42593932
Rhinovirus infection 22.31 17.21 24 26940 6524 42587847
Pulmonary oedema 22.04 17.21 79 26885 53193 42541178
Injection site pain 21.64 17.21 5 26959 57793 42536578
Renal disorder 21.62 17.21 53 26911 28927 42565444
Bronchial haemorrhage 21.56 17.21 10 26954 694 42593677
Factor VII deficiency 21.46 17.21 5 26959 35 42594336
Periodontal inflammation 21.08 17.21 4 26960 8 42594363
Sodium retention 20.92 17.21 6 26958 102 42594269
Phlebitis 20.82 17.21 19 26945 4239 42590132
Stress echocardiogram abnormal 20.76 17.21 4 26960 9 42594362
Suicidal ideation 20.53 17.21 3 26961 48158 42546213
Infusion site thrombosis 20.35 17.21 6 26958 113 42594258
Infusion related reaction 20.11 17.21 84 26880 60722 42533649
Lymphopenia 20.03 17.21 43 26921 21520 42572851
Hepatitis viral 20.01 17.21 10 26954 819 42593552
Brain natriuretic peptide increased 19.95 17.21 23 26941 6747 42587624
Cardiotoxicity 19.80 17.21 24 26940 7421 42586950
Influenza A virus test positive 19.67 17.21 8 26956 403 42593968
Myocardial necrosis marker increased 19.27 17.21 13 26951 1869 42592502
Incorrect dose administered 19.02 17.21 5 26959 52969 42541402
Avian influenza 18.84 17.21 4 26960 17 42594354
Vomiting 18.81 17.21 107 26857 289616 42304755
Posterior reversible encephalopathy syndrome 18.68 17.21 31 26933 12790 42581581
Therapy non-responder 18.66 17.21 75 26889 53284 42541087
Left ventricular failure 18.64 17.21 21 26943 6010 42588361
Febrile convulsion 18.44 17.21 9 26955 700 42593671
Neutrophil count decreased 18.23 17.21 84 26880 63331 42531040
Respirovirus test positive 18.21 17.21 5 26959 72 42594299
Weight decreased 18.10 17.21 69 26895 207879 42386492
Somnolence 18.02 17.21 39 26925 141066 42453305
Pneumonia mycoplasmal 17.63 17.21 9 26955 771 42593600

FDA Adverse Event Reporting System (Geriatric)

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
Thrombocytopenia 883.73 17.53 882 43726 348003 110196688
Plasma cell myeloma 724.34 17.53 398 44210 62538 110482153
Thrombotic microangiopathy 684.47 17.53 300 44308 28849 110515842
Plasma cell myeloma recurrent 590.84 17.53 185 44423 6857 110537834
Intercepted product preparation error 571.50 17.53 179 44429 6641 110538050
Plasma cell myeloma refractory 496.23 17.53 123 44485 1878 110542813
Cytopenia 426.96 17.53 219 44389 29897 110514794
Neutropenia 411.70 17.53 622 43986 373998 110170693
Therapy partial responder 365.60 17.53 212 44396 36849 110507842
Off label use 329.31 17.53 1331 43277 1498854 109045837
Plasmacytoma 326.52 17.53 110 44498 5152 110539539
Pneumonia 315.92 17.53 919 43689 875795 109668896
Platelet count decreased 295.54 17.53 412 44196 230031 110314660
Death 291.38 17.53 773 43835 698096 109846595
Disease progression 274.50 17.53 410 44198 243624 110301067
Tumour lysis syndrome 271.84 17.53 164 44444 30637 110514054
Unevaluable event 266.40 17.53 208 44400 59019 110485672
Anaemia 258.77 17.53 635 43973 546451 109998240
Myelosuppression 233.16 17.53 236 44372 94104 110450587
Neuropathy peripheral 228.94 17.53 320 44288 178957 110365734
Pyrexia 202.17 17.53 805 43803 897460 109647231
Cardiac failure 202.00 17.53 309 44299 187317 110357374
Sepsis 197.81 17.53 419 44189 326927 110217764
Pancytopenia 187.09 17.53 317 44291 209296 110335395
Acute kidney injury 181.03 17.53 615 43993 634815 109909876
Hypogammaglobulinaemia 172.25 17.53 105 44503 19971 110524720
Light chain analysis increased 169.21 17.53 55 44553 2300 110542391
Plasma cell leukaemia 163.27 17.53 52 44556 2036 110542655
Renal failure 150.86 17.53 302 44306 226272 110318419
COVID-19 149.45 17.53 315 44293 244745 110299946
Haemolytic uraemic syndrome 145.80 17.53 60 44548 4925 110539766
Deep vein thrombosis 142.96 17.53 225 44383 139662 110405029
COVID-19 pneumonia 138.57 17.53 117 44491 37026 110507665
Osteolysis 136.58 17.53 59 44549 5464 110539227
Cytokine release syndrome 133.41 17.53 153 44455 70153 110474538
Atypical haemolytic uraemic syndrome 131.42 17.53 41 44567 1499 110543192
Drug interaction 118.80 17.53 28 44580 500155 110044536
Drug hypersensitivity 110.67 17.53 24 44584 454066 110090625
Condition aggravated 109.56 17.53 82 44526 734754 109809937
Arthralgia 101.58 17.53 99 44509 779533 109765158
Pulmonary embolism 94.75 17.53 243 44365 214231 110330460
Microangiopathic haemolytic anaemia 91.22 17.53 33 44575 1910 110542781
Pulmonary oedema 90.72 17.53 153 44455 100506 110444185
Joint swelling 90.14 17.53 33 44575 442812 110101879
Respiratory tract infection 87.10 17.53 125 44483 71492 110473199
Alopecia 85.43 17.53 21 44587 364732 110179959
Polyneuropathy 84.40 17.53 83 44525 31929 110512762
Atrial fibrillation 83.28 17.53 242 44366 229400 110315291
White blood cell count decreased 82.48 17.53 241 44367 229149 110315542
Thrombotic thrombocytopenic purpura 81.77 17.53 45 44563 7066 110537625
Completed suicide 81.08 17.53 4 44604 242377 110302314
Myelodysplastic syndrome 80.42 17.53 87 44521 37397 110507294
Lymphopenia 77.17 17.53 88 44520 40082 110504609
Arthropathy 76.88 17.53 12 44596 287510 110257181
Glossodynia 76.44 17.53 3 44605 222001 110322690
Musculoskeletal stiffness 76.38 17.53 11 44597 279811 110264880
Abdominal discomfort 75.78 17.53 32 44576 393826 110150865
Pruritus 69.87 17.53 79 44529 581481 109963210
Wound 69.43 17.53 7 44601 234430 110310261
Swelling 68.36 17.53 28 44580 351013 110193678
Posterior reversible encephalopathy syndrome 68.15 17.53 76 44532 33785 110510906
Haemolytic anaemia 68.13 17.53 61 44547 20859 110523832
Impaired healing 66.59 17.53 3 44605 196714 110347977
Ejection fraction decreased 66.07 17.53 82 44526 40798 110503893
Respiratory failure 65.10 17.53 213 44395 215119 110329572
Febrile infection 64.90 17.53 33 44575 4415 110540276
Acute pulmonary oedema 64.33 17.53 54 44554 16942 110527749
Myeloma cast nephropathy 63.77 17.53 16 44592 257 110544434
Pulmonary hypertension 63.68 17.53 94 44514 55126 110489565
Protein total increased 63.02 17.53 33 44575 4691 110540000
Influenza 63.02 17.53 180 44428 168921 110375770
Fatigue 62.37 17.53 756 43852 1215202 109329489
Blister 61.90 17.53 9 44599 227367 110317324
Weight increased 60.94 17.53 48 44560 419596 110125095
Neutrophil count decreased 60.75 17.53 144 44464 120797 110423894
Pathological fracture 57.87 17.53 44 44564 11988 110532703
Pain 57.18 17.53 196 44412 954759 109589932
Cardiac failure acute 55.39 17.53 58 44550 24020 110520671
Infection 55.16 17.53 290 44318 361910 110182781
Bone marrow disorder 54.92 17.53 29 44579 4194 110540497
Immunoglobulins decreased 54.04 17.53 24 44584 2375 110542316
Hepatitis B reactivation 53.80 17.53 35 44573 7449 110537242
Blood cholesterol increased 53.47 17.53 6 44602 184779 110359912
Febrile neutropenia 53.40 17.53 261 44347 316506 110228185
Acute respiratory failure 53.25 17.53 103 44505 75157 110469534
Leukopenia 52.18 17.53 155 44453 148636 110396055
Cardiac failure congestive 50.79 17.53 155 44453 150845 110393846
Haematotoxicity 50.68 17.53 52 44556 21030 110523661
Injury 50.68 17.53 6 44602 177259 110367432
Headache 50.20 17.53 185 44423 882192 109662499
Bone pain 49.62 17.53 92 44516 65041 110479650
SARS-CoV-2 sepsis 49.52 17.53 13 44595 252 110544439
Irritable bowel syndrome 48.36 17.53 5 44603 164210 110380481
Abdominal pain 48.27 17.53 83 44525 512906 110031785
Hypertension 47.98 17.53 361 44247 509723 110034968
Product use issue 47.36 17.53 34 44574 311661 110233030
Urticaria 46.87 17.53 36 44572 318821 110225870
Progressive multifocal leukoencephalopathy 46.80 17.53 54 44554 24902 110519789
Full blood count decreased 46.52 17.53 61 44547 32038 110512653
Infusion site extravasation 46.19 17.53 38 44570 11596 110533095
Type 2 diabetes mellitus 46.01 17.53 8 44600 177224 110367467
Device related sepsis 45.95 17.53 32 44576 7615 110537076
Septic shock 45.08 17.53 153 44455 157375 110387316
Atrial flutter 44.66 17.53 52 44556 24210 110520481
Bronchopneumopathy 44.38 17.53 16 44592 917 110543774
B-cell type acute leukaemia 44.10 17.53 18 44590 1446 110543245
Laboratory test abnormal 43.74 17.53 70 44538 44009 110500682
Rhinovirus infection 43.68 17.53 37 44571 11752 110532939
Abdominal pain upper 43.45 17.53 46 44562 349065 110195626
Plasma cells increased 42.56 17.53 10 44598 120 110544571
Injection site pain 42.10 17.53 10 44598 177912 110366779
Pericarditis 41.80 17.53 18 44590 219096 110325595
Wheezing 41.24 17.53 26 44582 255204 110289487
Brain natriuretic peptide increased 41.16 17.53 35 44573 11174 110533517
Bone lesion 41.06 17.53 29 44579 7058 110537633
Paraproteinaemia 40.35 17.53 13 44595 528 110544163
Cerebellar haemangioma 39.98 17.53 9 44599 88 110544603
Dizziness 39.92 17.53 146 44462 698047 109846644
Cardiac dysfunction 39.66 17.53 27 44581 6196 110538495
Hypertensive crisis 39.56 17.53 49 44559 24323 110520368
Anxiety 39.13 17.53 49 44559 345029 110199662
Body dysmorphic disorder 38.88 17.53 12 44596 423 110544268
Dry mouth 38.82 17.53 16 44592 199932 110344759
Osteoarthritis 38.16 17.53 13 44595 182610 110362081
Pneumonia influenzal 38.12 17.53 22 44586 3783 110540908
Migraine 38.04 17.53 11 44597 171641 110373050
Overdose 37.52 17.53 24 44584 233770 110310921
Dyspnoea 37.35 17.53 640 43968 1106232 109438459
Hypercalcaemia 36.92 17.53 67 44541 46590 110498101
Contusion 36.04 17.53 25 44583 233336 110311355
Cardiotoxicity 35.89 17.53 39 44569 16842 110527849
Hypersensitivity 35.63 17.53 68 44540 403930 110140761
Inflammation 35.10 17.53 17 44591 193221 110351470
Hepatic enzyme increased 34.90 17.53 47 44561 320845 110223846
Parainfluenzae virus infection 34.64 17.53 26 44582 6948 110537743
Discomfort 34.51 17.53 22 44586 214685 110330006
Pneumonia bacterial 33.64 17.53 47 44561 26214 110518477
Lymphodepletion 33.18 17.53 7 44601 49 110544642
Pneumonitis 33.02 17.53 86 44522 76445 110468246
Intentional product misuse 32.38 17.53 7 44601 132897 110411794
Light chain analysis abnormal 32.04 17.53 9 44599 227 110544464
Hyperviscosity syndrome 31.87 17.53 11 44597 554 110544137
Sleep disorder due to general medical condition, insomnia type 31.67 17.53 3 44605 105640 110439051
Left ventricular dysfunction 31.52 17.53 43 44565 23450 110521241
Natural killer cell count decreased 31.52 17.53 8 44600 135 110544556
Pulmonary sepsis 31.51 17.53 22 44586 5256 110539435
C-reactive protein increased 31.51 17.53 25 44583 217894 110326797
Cerebral toxoplasmosis 31.03 17.53 18 44590 3124 110541567
Bone marrow infiltration 30.76 17.53 12 44596 856 110543835
Renal disorder 30.56 17.53 64 44544 49415 110495276
Depression 30.14 17.53 51 44557 317284 110227407
Rhabdomyolysis 30.04 17.53 6 44602 120395 110424296
Infusion site pain 29.86 17.53 36 44572 17383 110527308
Ill-defined disorder 29.73 17.53 13 44595 156840 110387851
Escherichia sepsis 29.65 17.53 28 44580 10244 110534447
Liver injury 29.25 17.53 12 44596 150401 110394290
Stomatitis 28.96 17.53 40 44568 270202 110274489
Blood calcium increased 28.84 17.53 36 44572 18004 110526687
Blood disorder 28.81 17.53 27 44581 9783 110534908
Pulmonary arterial hypertension 28.66 17.53 49 44559 32519 110512172
Respiratory distress 28.29 17.53 76 44532 68798 110475893
Wound infection 28.24 17.53 3 44605 96462 110448229
Febrile bone marrow aplasia 28.16 17.53 35 44573 17430 110527261
Salmonellosis 28.11 17.53 15 44593 2216 110542475
Drug intolerance 28.10 17.53 78 44530 406434 110138257
Cardiomyopathy 27.62 17.53 49 44559 33476 110511215
Paraesthesia 27.61 17.53 43 44565 276478 110268213
Myocardial necrosis marker increased 27.53 17.53 18 44590 3862 110540829
Cardiac disorder 27.24 17.53 80 44528 76200 110468491
Coma 27.15 17.53 7 44601 117862 110426829
Medication error 26.82 17.53 5 44603 105361 110439330
Sepsis syndrome 26.72 17.53 13 44595 1583 110543108
Weight decreased 26.63 17.53 98 44510 467959 110076732
Monoclonal immunoglobulin present 26.28 17.53 15 44593 2525 110542166
Thrombophlebitis 26.22 17.53 23 44585 7656 110537035
Meningitis listeria 26.12 17.53 12 44596 1285 110543406
Infusion site erythema 26.07 17.53 28 44580 11931 110532760
Intervertebral discitis 26.02 17.53 22 44586 6968 110537723
Infection susceptibility increased 25.49 17.53 18 44590 4380 110540311
Acute lymphocytic leukaemia 25.37 17.53 20 44588 5745 110538946
Protein total abnormal 25.31 17.53 10 44598 738 110543953
Sinusitis 25.23 17.53 51 44557 296637 110248054
Pneumonia respiratory syncytial viral 25.18 17.53 15 44593 2734 110541957
Respiratory syncytial virus infection 24.93 17.53 30 44578 14454 110530237
Suicidal ideation 24.91 17.53 4 44604 93933 110450758
Lactic acidosis 24.50 17.53 4 44604 92807 110451884
Jugular vein occlusion 24.49 17.53 6 44602 87 110544604
Product dose omission issue 24.34 17.53 59 44549 321723 110222968
Escherichia bacteraemia 24.30 17.53 25 44583 10139 110534552
Product use in unapproved indication 23.95 17.53 96 44512 447281 110097410
Platelet count abnormal 23.86 17.53 20 44588 6262 110538429
Hypercholesterolaemia 23.79 17.53 4 44604 90833 110453858
Bacterial sepsis 23.77 17.53 25 44583 10401 110534290
B-cell aplasia 23.51 17.53 8 44600 386 110544305
Multiple organ dysfunction syndrome 23.41 17.53 122 44486 151588 110393103
Asthma 23.05 17.53 41 44567 250250 110294441
Hypervolaemia 22.80 17.53 57 44551 49403 110495288
Stress echocardiogram abnormal 22.55 17.53 4 44604 9 110544682
Treatment failure 22.44 17.53 49 44559 277185 110267506
Spinal compression fracture 22.20 17.53 32 44576 18360 110526331
Acute respiratory distress syndrome 22.15 17.53 59 44549 53139 110491552
Post procedural diarrhoea 21.80 17.53 8 44600 482 110544209
Musculoskeletal pain 21.78 17.53 25 44583 182998 110361693
Dysphagia 21.73 17.53 18 44590 153582 110391109
Vomiting 21.68 17.53 249 44359 910426 109634265
Infectious pleural effusion 21.59 17.53 17 44591 4874 110539817
Asthenia 21.59 17.53 394 44214 688605 109856086
Haemolysis 21.55 17.53 29 44579 15610 110529081
Hypoaesthesia 21.19 17.53 61 44547 314162 110230529
Arthritis 20.93 17.53 22 44586 167564 110377127
Injection site erythema 20.93 17.53 6 44602 94170 110450521
Stem cell transplant 20.87 17.53 16 44592 4411 110540280
Intercepted product administration error 20.53 17.53 9 44599 863 110543828
Osteoporosis 20.41 17.53 5 44603 87147 110457544
Left ventricular failure 20.28 17.53 24 44584 11365 110533326
Dry skin 20.27 17.53 9 44599 107644 110437047
Acute myocardial infarction 20.23 17.53 77 44531 83700 110460991
Road traffic accident 20.19 17.53 9 44599 107389 110437302
Inappropriate schedule of product administration 20.00 17.53 32 44576 203605 110341086
Therapeutic product effect decreased 19.92 17.53 43 44565 244273 110300418
Bacteraemia 19.70 17.53 49 44559 42341 110502350
Seizure 19.68 17.53 37 44571 221148 110323543
Klebsiella bacteraemia 19.53 17.53 16 44592 4853 110539838
Morganella infection 19.45 17.53 10 44598 1369 110543322
Bronchial haemorrhage 19.39 17.53 10 44598 1377 110543314
Neck pain 19.26 17.53 13 44595 123117 110421574
Pneumonia parainfluenzae viral 19.25 17.53 8 44600 673 110544018
Psoriasis 19.08 17.53 17 44591 139976 110404715
H1N1 influenza 19.01 17.53 13 44595 3005 110541686
Candida pneumonia 18.99 17.53 9 44599 1034 110543657
Haemoglobin decreased 18.99 17.53 168 44440 248559 110296132
Hepatitis viral 18.81 17.53 10 44598 1465 110543226
Klebsiella infection 18.79 17.53 31 44577 19978 110524713
Factor VII deficiency 18.76 17.53 5 44603 103 110544588
Joint ankylosis 18.74 17.53 12 44596 2485 110542206
Sodium retention 18.71 17.53 6 44602 240 110544451
Erythema 18.62 17.53 58 44550 291389 110253302
Hepatitis E 18.62 17.53 15 44593 4444 110540247
Sciatica 18.58 17.53 7 44601 92392 110452299
Refusal of treatment by patient 18.57 17.53 21 44587 9473 110535218
Influenza A virus test positive 18.53 17.53 9 44599 1091 110543600
Tricuspid valve incompetence 18.53 17.53 34 44574 23839 110520852
Hypoglycaemia 18.51 17.53 12 44596 116092 110428599
Pulmonary fibrosis 18.49 17.53 9 44599 102033 110442658
Febrile convulsion 18.46 17.53 9 44599 1101 110543590
Bile acid malabsorption 18.39 17.53 7 44601 467 110544224
Panel-reactive antibody increased 18.37 17.53 3 44605 3 110544688
Lower limb fracture 18.29 17.53 4 44604 75344 110469347
Feeling abnormal 18.14 17.53 130 44478 180581 110364110
B precursor type acute leukaemia 18.02 17.53 7 44601 494 110544197
Squamous cell carcinoma of skin 18.01 17.53 28 44580 17175 110527516
Secondary immunodeficiency 17.99 17.53 15 44593 4661 110540030
Vascular pain 17.98 17.53 9 44599 1164 110543527
Phlebitis 17.96 17.53 21 44587 9820 110534871
Granulocyte count decreased 17.95 17.53 14 44594 3960 110540731
Gastrooesophageal reflux disease 17.94 17.53 28 44580 179948 110364743
Listeria sepsis 17.76 17.53 8 44600 818 110543873
Central nervous system vasculitis 17.74 17.53 10 44598 1644 110543047
Bronchopulmonary aspergillosis 17.71 17.53 38 44570 29825 110514866
Respirovirus test positive 17.69 17.53 5 44603 129 110544562
Clostridium difficile colitis 17.67 17.53 48 44560 43730 110500961
Conjunctivitis viral 17.60 17.53 6 44602 291 110544400

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC L01XG02 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
ANTINEOPLASTIC AGENTS
OTHER ANTINEOPLASTIC AGENTS
Proteasome inhibitors
FDA MoA N0000175075 Proteasome Inhibitors
FDA EPC N0000175604 Proteasome Inhibitor
CHEBI has role CHEBI:35610 antineoplastic agent
CHEBI has role CHEBI:52726 proteasome inhibitor

Related Drugs by ATC class:

L01XG Proteasome inhibitors 2 drugs
bortezomibixazomib

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

DiseaseRelationSNOMED_IDDOID
Multiple myeloma indication 109989006 DOID:9538
Relapse multiple myeloma indication




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 13.37 acidic
pKa2 5.23 Basic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
10MG/VIAL KYPROLIS ONYX PHARMS AMGEN N202714 June 7, 2018 RX POWDER INTRAVENOUS RE47954 Oct. 21, 2029 USE IN COMBINATION WITH LENALIDOMIDE PLUS DEXAMETHASONE FOR THE TREATMENT OF PATIENTS WITH RELAPSED OR REFRACTORY MULTIPLE MYELOMA WHO HAVE RECEIVED ONE TO THREE LINES OF THERAPY
30MG/VIAL KYPROLIS ONYX PHARMS AMGEN N202714 June 3, 2016 RX POWDER INTRAVENOUS RE47954 Oct. 21, 2029 USE IN COMBINATION WITH LENALIDOMIDE PLUS DEXAMETHASONE FOR THE TREATMENT OF PATIENTS WITH RELAPSED OR REFRACTORY MULTIPLE MYELOMA WHO HAVE RECEIVED ONE TO THREE LINES OF THERAPY
60MG/VIAL KYPROLIS ONYX PHARMS AMGEN N202714 July 20, 2012 RX POWDER INTRAVENOUS RE47954 Oct. 21, 2029 USE IN COMBINATION WITH LENALIDOMIDE PLUS DEXAMETHASONE FOR THE TREATMENT OF PATIENTS WITH RELAPSED OR REFRACTORY MULTIPLE MYELOMA WHO HAVE RECEIVED ONE TO THREE LINES OF THERAPY
10MG/VIAL KYPROLIS ONYX PHARMS AMGEN N202714 June 7, 2018 RX POWDER INTRAVENOUS 12636340 April 29, 2041 TREATMENT OF PATIENTS WITH RELAPSED OR REFRACTORY MULTIPLE MYELOMA WHO HAVE RECEIVED ONE TO THREE LINES OF THERAPY IN COMBINATION WITH DARATUMUMAB AND DEXAMETHASONE
30MG/VIAL KYPROLIS ONYX PHARMS AMGEN N202714 June 3, 2016 RX POWDER INTRAVENOUS 12636340 April 29, 2041 TREATMENT OF PATIENTS WITH RELAPSED OR REFRACTORY MULTIPLE MYELOMA WHO HAVE RECEIVED ONE TO THREE LINES OF THERAPY IN COMBINATION WITH DARATUMUMAB AND DEXAMETHASONE
60MG/VIAL KYPROLIS ONYX PHARMS AMGEN N202714 July 20, 2012 RX POWDER INTRAVENOUS 12636340 April 29, 2041 TREATMENT OF PATIENTS WITH RELAPSED OR REFRACTORY MULTIPLE MYELOMA WHO HAVE RECEIVED ONE TO THREE LINES OF THERAPY IN COMBINATION WITH DARATUMUMAB AND DEXAMETHASONE

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
10MG/VIAL KYPROLIS ONYX PHARMS AMGEN N202714 June 7, 2018 RX POWDER INTRAVENOUS May 22, 2028 ADDITIONAL CLINICAL TRIAL INFORMATION ADDED TO PEDIATRIC USE SUBSECTION
30MG/VIAL KYPROLIS ONYX PHARMS AMGEN N202714 June 3, 2016 RX POWDER INTRAVENOUS May 22, 2028 ADDITIONAL CLINICAL TRIAL INFORMATION ADDED TO PEDIATRIC USE SUBSECTION
60MG/VIAL KYPROLIS ONYX PHARMS AMGEN N202714 July 20, 2012 RX POWDER INTRAVENOUS May 22, 2028 ADDITIONAL CLINICAL TRIAL INFORMATION ADDED TO PEDIATRIC USE SUBSECTION
10MG/VIAL KYPROLIS ONYX PHARMS AMGEN N202714 June 7, 2018 RX POWDER INTRAVENOUS Nov. 22, 2028 PEDIATRIC EXCLUSIVITY
30MG/VIAL KYPROLIS ONYX PHARMS AMGEN N202714 June 3, 2016 RX POWDER INTRAVENOUS Nov. 22, 2028 PEDIATRIC EXCLUSIVITY
60MG/VIAL KYPROLIS ONYX PHARMS AMGEN N202714 July 20, 2012 RX POWDER INTRAVENOUS Nov. 22, 2028 PEDIATRIC EXCLUSIVITY

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
Proteasome subunit beta type-5 Enzyme INHIBITOR IC50 8.22 SCIENTIFIC LITERATURE SCIENTIFIC LITERATURE
Cathepsin B Enzyme IC50 4.96 CHEMBL
Proteasome subunit beta type-8 Enzyme IC50 7.85 CHEMBL
Proteasome subunit beta type-1 Enzyme IC50 5.84 CHEMBL
Proteasome subunit beta type-2 Enzyme IC50 6.69 CHEMBL
Potassium voltage-gated channel subfamily H member 2 Ion channel IC50 4.04 CHEMBL
Proteasome subunit beta type-9 Enzyme IC50 5.62 CHEMBL
Proteasome subunit beta type-10 Enzyme IC50 6.21 CHEMBL
Proteasome subunit beta type-6 Enzyme IC50 6.05 CHEMBL
Proteasome subunit beta type-7 Enzyme IC50 7.37 CHEMBL
Glutathione S-transferase omega-1 Enzyme IC50 6.82 CHEMBL

External reference:

IDSource
72X6E3J5AR UNII
D08880 KEGG_DRUG
4031662 VUID
N0000185509 NUI
4031662 VANDF
C2001856 UMLSCUI
CHEBI:65347 CHEBI
CHEMBL451887 ChEMBL_ID
11556711 PUBCHEM_CID
DB08889 DRUGBANK_ID
8859 INN_ID
C524865 MESH_SUPPLEMENTAL_RECORD_UI
7420 IUPHAR_LIGAND_ID
1302966 RXNORM
192152 MMSL
28679 MMSL
d07882 MMSL
014536 NDDF
713463006 SNOMEDCT_US
714783001 SNOMEDCT_US
3BV PDB_CHEM_ID

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
KYPROLIS HUMAN PRESCRIPTION DRUG LABEL 1 76075-101 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 60 mg INTRAVENOUS NDA 30 sections
KYPROLIS HUMAN PRESCRIPTION DRUG LABEL 1 76075-102 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 30 mg INTRAVENOUS NDA 30 sections
KYPROLIS HUMAN PRESCRIPTION DRUG LABEL 1 76075-103 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 10 mg INTRAVENOUS NDA 30 sections