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

Stem definitionDrug idCAS RN
proteasome inhibitors 391 179324-69-7

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • LDP-341
  • PS-341
  • bortezomib
  • velcade
  • radiciol
A pyrazine and boronic acid derivative that functions as a reversible PROTEASOME INHIBITOR. It is used as an ANTINEOPLASTIC AGENT in the treatment of MULTIPLE MYELOMA and MANTLE CELL LYMPHOMA.
  • Molecular weight: 384.24
  • Formula: C19H25BN4O4
  • CLOGP: 0.78
  • LIPINSKI: 0
  • HAC: 8
  • HDO: 4
  • TPSA: 124.44
  • ALOGS: -3.86
  • ROTB: 9

  • Status: ONP

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

Drug dosage:

None

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 1 Benet LZ, Broccatelli F, Oprea TI
S (Water solubility) 3.30 mg/mL Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 0.08 ┬ÁM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
Vd (Volume of distribution) 10 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 19 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.17 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 18 hours Lombardo F, Berellini G, Obach RS

Approvals:

DateAgencyCompanyOrphan
Nov. 14, 2019 EMA FRESENIUS KABI DEUTSCHLAND GMBH
Aug. 22, 2019 PMDA Janssen Pharmaceutical K.K.
May 13, 2003 FDA MILLENNIUM 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
Plasma cell myeloma 4287.96 13.56 1693 52651 42785 46588933
Neuropathy peripheral 1954.62 13.56 1250 53094 89643 46542075
Plasma cell myeloma recurrent 462.04 13.56 153 54191 2254 46629464
Thrombocytopenia 415.99 13.56 617 53727 125964 46505754
Platelet count decreased 367.14 13.56 514 53830 99510 46532208
Disease progression 317.01 13.56 457 53887 90843 46540875
Plasmacytoma 315.58 13.56 116 54228 2361 46629357
Rheumatoid arthritis 263.72 13.56 3 54341 240212 46391506
Diarrhoea 257.16 13.56 1305 53039 558297 46073421
Plasma cell leukaemia 205.84 13.56 70 54274 1123 46630595
Pneumonia 196.92 13.56 912 53432 375408 46256310
Constipation 190.98 13.56 538 53806 173559 46458159
Neutropenia 186.82 13.56 472 53872 142732 46488986
White blood cell count decreased 178.92 13.56 400 53944 111831 46519887
Drug hypersensitivity 154.64 13.56 46 54298 243779 46387939
Headache 145.13 13.56 208 54136 478144 46153574
Pancytopenia 142.10 13.56 309 54035 84749 46546969
Full blood count decreased 127.56 13.56 143 54201 22068 46609650
Tumour lysis syndrome 126.96 13.56 88 54256 7148 46624570
Polyneuropathy 123.60 13.56 105 54239 11539 46620179
Sepsis 120.41 13.56 390 53954 135624 46496094
Exposure during pregnancy 111.89 13.56 3 54341 108209 46523509
Unevaluable event 106.37 13.56 192 54152 45983 46585735
Laboratory test abnormal 106.17 13.56 132 54212 22715 46609003
Maternal exposure during pregnancy 105.44 13.56 3 54341 102546 46529172
Neutrophil count decreased 103.15 13.56 183 54161 43243 46588475
Arthralgia 102.26 13.56 167 54177 364436 46267282
Peripheral sensory neuropathy 101.31 13.56 74 54270 6529 46625189
Amyloidosis 98.58 13.56 40 54304 1071 46630647
Drug ineffective 96.77 13.56 434 53910 677404 45954314
Febrile neutropenia 96.37 13.56 285 54059 94342 46537376
Deep vein thrombosis 86.74 13.56 246 54098 79527 46552191
Dehydration 85.46 13.56 390 53954 159150 46472568
Drug interaction 83.94 13.56 68 54276 203026 46428692
Chalazion 82.63 13.56 25 54319 269 46631449
Anaemia 81.58 13.56 543 53801 255236 46376482
Orthostatic hypotension 80.44 13.56 120 54224 24538 46607180
Contraindicated product administered 76.55 13.56 4 54340 79943 46551775
Herpes zoster 76.43 13.56 212 54132 67660 46564058
Light chain analysis increased 76.16 13.56 33 54311 1045 46630673
Posterior reversible encephalopathy syndrome 76.06 13.56 91 54253 15050 46616668
Hordeolum 72.50 13.56 40 54304 2161 46629557
Overdose 70.74 13.56 16 54328 101963 46529755
Septic shock 70.36 13.56 186 54158 57707 46574011
Primary amyloidosis 69.59 13.56 15 54329 31 46631687
Pain 69.29 13.56 303 54041 476645 46155073
Protein total increased 62.66 13.56 38 54306 2455 46629263
Product use in unapproved indication 62.64 13.56 239 54105 90034 46541684
Monoclonal immunoglobulin present 59.75 13.56 25 54319 725 46630993
Injection site pain 58.05 13.56 26 54318 107126 46524592
Cardiac amyloidosis 57.91 13.56 22 54322 492 46631226
Hyperviscosity syndrome 56.35 13.56 17 54327 181 46631537
Renal failure 55.87 13.56 271 54073 113323 46518395
Stem cell transplant 55.18 13.56 31 54313 1735 46629983
Cytopenia 55.18 13.56 56 54288 7712 46624006
Condition aggravated 54.11 13.56 129 54215 244923 46386795
Pyrexia 53.26 13.56 630 53714 348172 46283546
Haematotoxicity 52.97 13.56 52 54292 6881 46624837
Autonomic neuropathy 50.88 13.56 22 54322 693 46631025
Myelodysplastic syndrome 50.58 13.56 76 54268 15635 46616083
Haemoglobin decreased 49.95 13.56 288 54056 128661 46503057
Musculoskeletal stiffness 49.69 13.56 26 54318 97967 46533751
Coombs indirect test positive 49.44 13.56 11 54333 28 46631690
Wrong technique in product usage process 48.33 13.56 4 54340 54418 46577300
Thrombosis 47.04 13.56 158 54186 55911 46575807
Pathological fracture 45.32 13.56 51 54293 7899 46623819
Therapy partial responder 45.19 13.56 40 54304 4642 46627076
Atrial fibrillation 44.54 13.56 238 54106 103352 46528366
Suicide attempt 43.89 13.56 6 54338 55030 46576688
Cytomegalovirus infection reactivation 43.73 13.56 25 54319 1447 46630271
Anxiety 43.22 13.56 92 54252 181865 46449853
Bone marrow failure 41.96 13.56 101 54243 29568 46602150
Therapeutic product effect decreased 41.75 13.56 22 54322 82579 46549139
Depression 41.24 13.56 85 54259 170019 46461699
Off label use 40.71 13.56 644 53700 379197 46252521
Hypercalcaemia 40.39 13.56 81 54263 20965 46610753
Mesenteric abscess 39.94 13.56 11 54333 82 46631636
Hypocalcaemia 39.85 13.56 93 54251 26692 46605026
Peripheral sensorimotor neuropathy 39.74 13.56 22 54322 1196 46630522
Migraine 39.50 13.56 16 54328 70010 46561708
Rash 39.16 13.56 607 53737 355905 46275813
Pneumonia fungal 39.08 13.56 35 54309 4125 46627593
Peripheral motor neuropathy 38.39 13.56 23 54321 1453 46630265
Endocarditis bacterial 38.10 13.56 17 54327 578 46631140
Ileus paralytic 37.92 13.56 35 54309 4288 46627430
Body dysmorphic disorder 37.53 13.56 12 54332 157 46631561
Blood pressure increased 37.31 13.56 56 54288 126610 46505108
Large intestinal ulcer perforation 37.24 13.56 10 54334 67 46631651
Abdominal discomfort 36.25 13.56 76 54268 151089 46480629
Malignant neoplasm progression 35.65 13.56 160 54184 64766 46566952
Electrolyte imbalance 35.11 13.56 68 54276 17158 46614560
Cytomegalovirus infection 35.02 13.56 70 54274 18074 46613644
Glossodynia 35.00 13.56 5 54339 44368 46587350
Nasal abscess 34.33 13.56 11 54333 145 46631573
Treatment failure 33.85 13.56 35 54309 93052 46538666
Ageusia 33.43 13.56 53 54291 11419 46620299
Crossmatch incompatible 33.42 13.56 8 54336 31 46631687
Plasmablastic lymphoma 32.92 13.56 12 54332 238 46631480
Adverse drug reaction 32.87 13.56 120 54224 44242 46587476
Hepatitis B reactivation 32.80 13.56 21 54323 1493 46630225
Mobility decreased 32.34 13.56 15 54329 60579 46571139
Gastrointestinal fungal infection 32.02 13.56 12 54332 258 46631460
Morganella infection 31.94 13.56 14 54330 456 46631262
Fibromyalgia 31.51 13.56 3 54341 36460 46595258
Fatigue 31.39 13.56 928 53416 607769 46023949
Swelling 31.21 13.56 61 54283 124450 46507268
Target skin lesion 31.09 13.56 9 54335 82 46631636
Alopecia 30.88 13.56 92 54252 162322 46469396
Inappropriate antidiuretic hormone secretion 30.39 13.56 57 54287 14045 46617673
Palpitations 30.15 13.56 40 54304 95219 46536499
Bone pain 29.95 13.56 121 54223 46769 46584949
Blood potassium decreased 29.94 13.56 105 54239 37958 46593760
Large intestine perforation 29.29 13.56 40 54304 7540 46624178
Blood stem cell harvest failure 29.12 13.56 8 54336 59 46631659
Inappropriate schedule of product administration 29.09 13.56 20 54324 64993 46566725
Taste disorder 28.98 13.56 35 54309 5843 46625875
Mantle cell lymphoma 28.87 13.56 14 54330 577 46631141
Therapy non-responder 28.56 13.56 109 54235 41043 46590675
Suicidal ideation 28.51 13.56 15 54329 56367 46575351
Oedema peripheral 28.16 13.56 297 54047 159409 46472309
Pleural effusion 28.11 13.56 179 54165 82773 46548945
Clostridium bacteraemia 27.98 13.56 10 54334 187 46631531
Colitis 27.64 13.56 101 54243 37246 46594472
Joint swelling 27.48 13.56 100 54244 165973 46465745
Adenoviral haemorrhagic cystitis 27.20 13.56 9 54335 132 46631586
Hypertension 27.03 13.56 127 54217 196229 46435489
Spinal cord compression 26.97 13.56 27 54317 3657 46628061
Sinus polyp 26.68 13.56 11 54333 307 46631411
Hypoaesthesia 26.35 13.56 232 54112 118637 46513081
Syncope 26.12 13.56 210 54134 104593 46527125
Product quality issue 25.93 13.56 5 54339 35643 46596075
Anaphylactic reaction 25.60 13.56 15 54329 53097 46578621
Acute lymphocytic leukaemia 25.40 13.56 23 54321 2750 46628968
Bone lesion 25.36 13.56 30 54314 4901 46626817
Malaise 25.29 13.56 255 54089 330977 46300741
Bronchiolitis 25.06 13.56 21 54323 2264 46629454
Osteolysis 24.58 13.56 22 54322 2590 46629128
Graft versus host disease 24.31 13.56 34 54310 6554 46625164
Stress 24.23 13.56 15 54329 51536 46580182
Osteoarthritis 24.08 13.56 22 54322 62003 46569715
Blood lactate dehydrogenase increased 24.01 13.56 65 54279 20435 46611283
Renal impairment 23.68 13.56 158 54186 74214 46557504
Joint ankylosis 23.53 13.56 12 54332 552 46631166
Hypokalaemia 23.38 13.56 179 54165 87845 46543873
Refractory cytopenia with multilineage dysplasia 23.20 13.56 8 54336 134 46631584
Arthritis 22.93 13.56 34 54310 77282 46554436
Pain in extremity 22.82 13.56 192 54152 258488 46373230
Salmonella sepsis 22.79 13.56 9 54335 224 46631494
Blood pressure fluctuation 22.73 13.56 4 54340 30444 46601274
Flushing 22.70 13.56 25 54319 64589 46567129
Nasal congestion 22.61 13.56 14 54330 48099 46583619
Intraductal proliferative breast lesion 22.56 13.56 21 54323 2601 46629117
Heart rate increased 22.07 13.56 33 54311 74758 46556960
Hypothyroidism 21.55 13.56 5 54339 31333 46600385
Joint stiffness 21.50 13.56 3 54341 27105 46604613
Injection site swelling 21.49 13.56 10 54334 40317 46591401
Hepatic enzyme increased 21.43 13.56 39 54305 81748 46549970
Peritonitis viral 21.42 13.56 6 54338 48 46631670
Discomfort 21.36 13.56 14 54330 46656 46585062
Neuralgia 21.35 13.56 64 54280 21319 46610399
Failure to thrive 21.11 13.56 32 54312 6632 46625086
5q minus syndrome 21.09 13.56 8 54336 178 46631540
Asthenia 20.78 13.56 491 53853 310584 46321134
Varicella zoster virus infection 20.61 13.56 19 54325 2324 46629394
Seasonal allergy 20.60 13.56 47 54297 13287 46618431
Enterococcal sepsis 20.51 13.56 15 54329 1325 46630393
Myalgia 20.43 13.56 74 54270 123014 46508704
Pulmonary arterial hypertension 20.26 13.56 3 54341 25925 46605793
Guillain-Barre syndrome 20.12 13.56 22 54322 3300 46628418
Arthropathy 19.94 13.56 43 54301 84657 46547061
Blood creatine phosphokinase increased 19.93 13.56 4 54340 27720 46603998
Osteonecrosis of jaw 19.80 13.56 86 54258 34316 46597402
Drug withdrawal syndrome 19.58 13.56 4 54340 27380 46604338
Hypoalbuminaemia 19.46 13.56 39 54305 10088 46621630
Somnolence 19.38 13.56 105 54239 156416 46475302
Pregnancy 19.33 13.56 4 54340 27133 46604585
VIth nerve paresis 18.73 13.56 6 54338 79 46631639
Multiple allergies 18.71 13.56 32 54312 7339 46624379
Serotonin syndrome 18.48 13.56 3 54341 24217 46607501
Plasma cells decreased 18.31 13.56 5 54339 36 46631682
Full blood count increased 18.24 13.56 12 54332 894 46630824
Gait disturbance 18.23 13.56 97 54247 145166 46486552
Cardiotoxicity 18.15 13.56 30 54314 6692 46625026
Hyperhidrosis 18.13 13.56 49 54295 89259 46542459
Chest discomfort 17.97 13.56 50 54294 90219 46541499
Incorrect dose administered 17.86 13.56 16 54328 45534 46586184
Injury 17.83 13.56 15 54329 44012 46587706
Fungal oesophagitis 17.83 13.56 10 54334 558 46631160
Mucosal erosion 17.76 13.56 14 54330 1384 46630334
Neurotoxicity 17.60 13.56 45 54299 13672 46618046
Acute myopia 17.54 13.56 6 54338 98 46631620
Meningitis cryptococcal 17.45 13.56 13 54331 1182 46630536
Hypophosphataemia 17.42 13.56 31 54313 7336 46624382
Rhabdomyolysis 17.32 13.56 14 54330 41895 46589823
Injection site bruising 17.26 13.56 10 54334 35626 46596092
Blood pressure systolic increased 17.20 13.56 6 54338 28781 46602937
Human chorionic gonadotropin increased 17.14 13.56 13 54331 1214 46630504
Loss of personal independence in daily activities 17.10 13.56 25 54319 57158 46574560
Human herpesvirus 8 infection 17.09 13.56 7 54337 192 46631526
Compression fracture 16.99 13.56 28 54316 6229 46625489
Chronic graft versus host disease in skin 16.98 13.56 10 54334 612 46631106
Aggression 16.95 13.56 3 54341 22741 46608977
Wound 16.83 13.56 15 54329 42787 46588931
Renal amyloidosis 16.80 13.56 6 54338 112 46631606
Myocardial infarction 16.60 13.56 58 54286 97470 46534248
Infection in an immunocompromised host 16.56 13.56 9 54335 472 46631246
Pneumonia pneumococcal 16.49 13.56 15 54329 1803 46629915
Acute myeloid leukaemia 16.49 13.56 48 54296 15730 46615988
Transplant 16.47 13.56 10 54334 647 46631071
Cough 16.43 13.56 180 54164 230069 46401649
Cardio-respiratory arrest 16.17 13.56 28 54316 59841 46571877
Hypoglossal nerve paresis 16.14 13.56 6 54338 126 46631592
Myeloma cast nephropathy 16.06 13.56 6 54338 128 46631590
Toxicity to various agents 15.92 13.56 340 54004 211426 46420292
Hypersensitivity 15.89 13.56 106 54238 150215 46481503
Therapeutic product effect incomplete 15.77 13.56 43 54301 78110 46553608
Pseudomyopia 15.67 13.56 5 54339 65 46631653
Hypotension 15.47 13.56 367 53977 232222 46399496
Disease recurrence 15.43 13.56 52 54292 18419 46613299
Clavicle fracture 15.36 13.56 18 54326 2911 46628807
Blood immunoglobulin A increased 15.35 13.56 8 54336 385 46631333
Crying 15.30 13.56 3 54341 21138 46610580
Hyperproteinaemia 15.20 13.56 5 54339 72 46631646
JC virus CSF test positive 15.13 13.56 4 54340 25 46631693
Coma 15.12 13.56 28 54316 58321 46573397
Dysarthria 14.91 13.56 13 54331 37485 46594233
Ileus 14.90 13.56 43 54301 14021 46617697
Injection site haemorrhage 14.86 13.56 3 54341 20706 46611012
Duodenal stenosis 14.82 13.56 9 54335 583 46631135
Sensory level abnormal 14.81 13.56 6 54338 160 46631558
Infection 14.80 13.56 228 54116 133364 46498354
Staphylococcal bacteraemia 14.76 13.56 23 54321 4881 46626837
Infection reactivation 14.70 13.56 10 54334 787 46630931
Cardiac failure congestive 14.49 13.56 167 54177 91583 46540135
Lactic acidosis 14.42 13.56 11 54333 33898 46597820
Sleep apnoea syndrome 14.38 13.56 4 54340 22197 46609521
Skin exfoliation 14.35 13.56 76 54268 32862 46598856
Toxic skin eruption 14.23 13.56 39 54305 12348 46619370
Cryptococcosis 14.10 13.56 10 54334 842 46630876
Atelectasis 14.06 13.56 51 54293 18739 46612979
Blepharitis 13.96 13.56 15 54329 2206 46629512
Mucosal inflammation 13.75 13.56 85 54259 38891 46592827
Bacteraemia 13.74 13.56 42 54302 14137 46617581
Blood immunoglobulin A decreased 13.72 13.56 7 54337 322 46631396
Underdose 13.69 13.56 3 54341 19555 46612163
Therapy cessation 13.59 13.56 7 54337 26622 46605096

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
Plasma cell myeloma 4440.62 12.27 2198 62092 51264 29836924
Neuropathy peripheral 2049.13 12.27 1475 62815 69000 29819188
Plasma cell myeloma recurrent 505.65 12.27 211 64079 3203 29884985
Thrombocytopenia 380.07 12.27 879 63411 136165 29752023
Platelet count decreased 361.72 12.27 740 63550 105389 29782799
Disease progression 314.47 12.27 592 63698 79282 29808906
Plasmacytoma 285.71 12.27 141 64149 3215 29884973
Pneumonia 238.89 12.27 1373 62917 332933 29555255
Polyneuropathy 234.39 12.27 198 64092 11625 29876563
Drug interaction 228.95 12.27 72 64218 199496 29688692
Unevaluable event 215.92 12.27 302 63988 31483 29856705
Completed suicide 198.10 12.27 3 64287 99489 29788699
Plasma cell leukaemia 181.41 12.27 70 64220 855 29887333
Drug abuse 161.18 12.27 3 64287 82069 29806119
Tumour lysis syndrome 157.51 12.27 165 64125 12720 29875468
Orthostatic hypotension 138.36 12.27 211 64079 23768 29864420
Herpes zoster 134.17 12.27 235 64055 29708 29858480
Amyloidosis 122.61 12.27 69 64221 2070 29886118
White blood cell count decreased 111.01 12.27 414 63876 83533 29804655
Peripheral sensory neuropathy 109.14 12.27 95 64195 5806 29882382
Overdose 104.76 12.27 26 64264 84311 29803877
Constipation 103.54 12.27 498 63792 112408 29775780
Headache 98.90 12.27 149 64141 182157 29706031
Autonomic neuropathy 96.04 12.27 44 64246 844 29887344
Diarrhoea 94.60 12.27 1113 63177 332990 29555198
Deep vein thrombosis 93.37 12.27 314 63976 60187 29828001
Light chain analysis increased 93.24 12.27 45 64245 975 29887213
Hypercalcaemia 89.71 12.27 122 64168 12373 29875815
Fatigue 79.80 12.27 1043 63247 319630 29568558
Rhabdomyolysis 78.17 12.27 20 64270 63560 29824628
Neutropenia 76.59 12.27 505 63785 128035 29760153
Ileus paralytic 73.83 12.27 75 64215 5573 29882615
Pancytopenia 73.51 12.27 369 63921 84683 29803505
Full blood count decreased 68.63 12.27 122 64168 15595 29872593
Product use issue 66.75 12.27 234 64056 45782 29842406
Psoriasis 66.32 12.27 7 64283 42499 29845689
Blood creatine phosphokinase increased 64.05 12.27 9 64281 43839 29844349
Product use in unapproved indication 63.86 12.27 320 63970 73373 29814815
Myelodysplastic syndrome 59.12 12.27 127 64163 18651 29869537
Osteonecrosis of jaw 58.71 12.27 126 64164 18492 29869696
Hypertension 57.58 12.27 108 64182 121246 29766942
Thrombosis 56.35 12.27 209 64081 42022 29846166
Depression 55.97 12.27 67 64223 90370 29797818
Spinal compression fracture 55.95 12.27 68 64222 6166 29882022
Cardiac amyloidosis 55.67 12.27 29 64261 743 29887445
Pyrexia 53.94 12.27 909 63381 293580 29594608
Adverse drug reaction 52.73 12.27 138 64152 23007 29865181
Atrial fibrillation 51.71 12.27 403 63887 107721 29780467
Seizure 49.06 12.27 85 64205 98390 29789798
Aggression 48.56 12.27 10 64280 36897 29851291
Arthralgia 48.25 12.27 141 64149 135650 29752538
Suicidal ideation 47.07 12.27 10 64280 36104 29852084
Neuralgia 45.38 12.27 81 64209 10385 29877803
Spinal cord compression 44.88 12.27 47 64243 3619 29884569
Anxiety 44.38 12.27 78 64212 89793 29798395
Chalazion 44.30 12.27 14 64276 89 29888099
Inappropriate schedule of product administration 44.24 12.27 15 64275 39713 29848475
Drug hypersensitivity 43.20 12.27 50 64240 68469 29819719
Stem cell transplant 42.86 12.27 36 64254 2095 29886093
Cytopenia 42.54 12.27 69 64221 8187 29880001
Hypoaesthesia 41.11 12.27 227 64063 54003 29834185
Therapy partial responder 41.10 12.27 45 64245 3646 29884542
Protein total increased 40.82 12.27 35 64255 2095 29886093
Laboratory test abnormal 40.76 12.27 105 64185 17337 29870851
Off label use 39.72 12.27 753 63537 248537 29639651
Infection 39.54 12.27 295 63995 77779 29810409
Rash 39.03 12.27 603 63687 191286 29696902
Compression fracture 38.03 12.27 39 64251 2930 29885258
Neutrophil count decreased 37.20 12.27 185 64105 42269 29845919
Abdominal pain 36.72 12.27 158 64132 135496 29752692
Condition aggravated 36.45 12.27 162 64128 137704 29750484
Wrong technique in product usage process 36.04 12.27 11 64279 31144 29857044
Hypoglycaemia 35.73 12.27 34 64256 50947 29837241
Blood pressure increased 34.98 12.27 63 64227 71865 29816323
Osteolysis 34.82 12.27 28 64262 1532 29886656
Myocardial infarction 34.81 12.27 145 64145 125480 29762708
Hallucination 34.05 12.27 33 64257 49026 29839162
Disseminated varicella zoster virus infection 34.04 12.27 23 64267 961 29887227
Paraesthesia 33.84 12.27 216 64074 54111 29834077
Pathological fracture 33.81 12.27 43 64247 4083 29884105
Septic shock 33.72 12.27 243 64047 63364 29824824
Monoclonal immunoglobulin present 33.28 12.27 22 64268 886 29887302
Adenocarcinoma of colon 33.00 12.27 38 64252 3254 29884934
Squamous cell carcinoma of skin 31.53 12.27 64 64226 9031 29879157
Oroantral fistula 31.47 12.27 14 64276 250 29887938
Plasma cell myeloma refractory 31.15 12.27 9 64281 40 29888148
Hyperkalaemia 31.05 12.27 59 64231 65951 29822237
Hyperviscosity syndrome 30.24 12.27 13 64277 213 29887975
Ageusia 29.86 12.27 62 64228 8891 29879297
Flushing 29.74 12.27 13 64277 29479 29858709
Rash pruritic 29.50 12.27 111 64179 22461 29865727
Meningitis pneumococcal 29.21 12.27 11 64279 125 29888063
Pulmonary embolism 28.80 12.27 275 64015 77860 29810328
Bradycardia 28.74 12.27 61 64229 65465 29822723
Bone pain 28.65 12.27 98 64192 18928 29869260
Agitation 28.47 12.27 45 64245 54028 29834160
Sepsis 28.19 12.27 456 63834 145939 29742249
Blood stem cell harvest failure 28.04 12.27 7 64283 15 29888173
Drug ineffective 27.95 12.27 539 63751 339848 29548340
Asthma 27.92 12.27 22 64268 36152 29852036
Diverticular perforation 27.45 12.27 34 64256 3143 29885045
Bone marrow failure 26.95 12.27 131 64159 29654 29858534
Dehydration 26.92 12.27 393 63897 123146 29765042
Intentional product misuse 26.87 12.27 21 64269 34646 29853542
Hiccups 26.53 12.27 61 64229 9373 29878815
Angioedema 26.43 12.27 21 64269 34363 29853825
Haematochezia 26.18 12.27 21 64269 34201 29853987
Ileus 25.99 12.27 83 64207 15472 29872716
Cytomegalovirus infection 25.80 12.27 110 64180 23564 29864624
Stress 25.57 12.27 6 64284 20229 29867959
Electrocardiogram QT prolonged 24.99 12.27 24 64266 35811 29852377
VIth nerve paralysis 24.95 12.27 17 64273 720 29887468
Brief psychotic disorder with marked stressors 24.94 12.27 10 64280 136 29888052
Somnolence 24.78 12.27 115 64175 96648 29791540
Cerebrovascular accident 24.60 12.27 94 64196 83383 29804805
Asthenia 24.26 12.27 634 63656 220656 29667532
Peripheral sensorimotor neuropathy 24.25 12.27 21 64269 1274 29886914
Primary amyloidosis 24.18 12.27 8 64282 60 29888128
Coronary artery disease 23.76 12.27 44 64246 49668 29838520
Drug-induced liver injury 23.74 12.27 8 64282 21266 29866922
Tooth deposit 23.46 12.27 9 64281 108 29888080
Haemoglobin decreased 23.31 12.27 359 63931 113739 29774449
Gastrointestinal amyloidosis 23.12 12.27 6 64284 16 29888172
H1N1 influenza 23.01 12.27 18 64272 946 29887242
Erythema 22.96 12.27 87 64203 77364 29810824
Guillain-Barre syndrome 22.88 12.27 40 64250 5043 29883145
Hyperhidrosis 22.84 12.27 71 64219 67019 29821169
Therapy non-responder 22.79 12.27 124 64166 29329 29858859
Osteonecrosis 22.47 12.27 81 64209 16054 29872134
Jaundice 22.37 12.27 22 64268 32464 29855724
Renal failure 22.36 12.27 395 63895 128571 29759617
Gastric ulcer 22.32 12.27 3 64287 15118 29873070
Rib fracture 22.29 12.27 69 64221 12651 29875537
Bone lesion 22.26 12.27 28 64262 2629 29885559
Acute myeloid leukaemia 22.26 12.27 87 64203 17919 29870269
Drug level increased 22.11 12.27 6 64284 18348 29869840
Contraindicated product administered 21.99 12.27 5 64285 17226 29870962
Malaise 21.86 12.27 241 64049 166721 29721467
Abnormal behaviour 21.86 12.27 14 64276 25609 29862579
Basal cell carcinoma 21.82 12.27 80 64210 15988 29872200
Emotional distress 21.30 12.27 4 64286 15761 29872427
Rectal adenocarcinoma 21.17 12.27 16 64274 799 29887389
Respirovirus test positive 21.10 12.27 7 64283 53 29888135
Colitis ulcerative 20.98 12.27 3 64287 14431 29873757
Bacteraemia 20.73 12.27 77 64213 15483 29872705
Bone disorder 20.54 12.27 45 64245 6696 29881492
Lactic acidosis 20.51 12.27 22 64268 31191 29856997
Neutropenic sepsis 20.09 12.27 62 64228 11347 29876841
Respiratory arrest 19.93 12.27 20 64270 29238 29858950
Bacterial infection 19.91 12.27 66 64224 12544 29875644
Metabolic acidosis 19.88 12.27 31 64259 37430 29850758
Mobility decreased 19.83 12.27 16 64274 25983 29862205
Peripheral motor neuropathy 19.83 12.27 21 64269 1638 29886550
Progressive multifocal leukoencephalopathy 19.77 12.27 53 64237 8960 29879228
Enterococcal infection 19.72 12.27 50 64240 8174 29880014
Myalgia 19.69 12.27 91 64199 76576 29811612
Anaphylactic reaction 19.21 12.27 19 64271 27963 29860225
Conjunctival irritation 19.13 12.27 8 64282 122 29888066
Metapneumovirus infection 19.05 12.27 13 64277 552 29887636
Blood calcium increased 18.98 12.27 28 64262 3059 29885129
Performance status decreased 18.94 12.27 32 64258 3925 29884263
Blood lactate dehydrogenase increased 18.91 12.27 91 64199 20510 29867678
Pallor 18.65 12.27 11 64279 21038 29867150
Blood immunoglobulin M increased 18.65 12.27 9 64281 195 29887993
Clostridium difficile colitis 18.55 12.27 65 64225 12703 29875485
Monoclonal gammopathy 18.55 12.27 10 64280 275 29887913
Accidental overdose 18.51 12.27 8 64282 18267 29869921
Dysarthria 18.41 12.27 23 64267 30467 29857721
Hordeolum 18.33 12.27 14 64276 710 29887478
Morganella infection 18.30 12.27 11 64279 374 29887814
Febrile neutropenia 18.21 12.27 326 63964 106367 29781821
Cystitis haemorrhagic 18.18 12.27 35 64255 4752 29883436
B precursor type acute leukaemia 18.10 12.27 7 64283 86 29888102
Incorrect dose administered 18.01 12.27 25 64265 31661 29856527
Parainfluenzae virus infection 17.91 12.27 22 64268 2016 29886172
Pleural effusion 17.88 12.27 240 64050 73826 29814362
Product quality issue 17.81 12.27 9 64281 18765 29869423
Hypersensitivity 17.81 12.27 58 64232 53970 29834218
Blood immunoglobulin A increased 17.80 12.27 10 64280 299 29887889
Genital erythema 17.68 12.27 8 64282 149 29888039
Acute lymphocytic leukaemia 17.66 12.27 27 64263 3045 29885143
Palmar-plantar erythrodysaesthesia syndrome 17.65 12.27 5 64285 14865 29873323
Infusion related reaction 17.62 12.27 148 64142 40416 29847772
Blood immunoglobulin G increased 17.50 12.27 15 64275 897 29887291
Dyskinesia 17.20 12.27 13 64277 21821 29866367
Adenovirus infection 17.19 12.27 32 64258 4236 29883952
Renal amyloidosis 16.89 12.27 6 64284 57 29888131
Full blood count increased 16.75 12.27 14 64276 809 29887379
Cardiac arrest 16.50 12.27 124 64166 92726 29795462
Acute febrile neutrophilic dermatosis 16.42 12.27 16 64274 1130 29887058
Autonomic nervous system imbalance 16.41 12.27 23 64267 2398 29885790
Hallucination, visual 16.41 12.27 7 64283 16106 29872082
Disturbance in attention 16.40 12.27 14 64276 22115 29866073
Pleuritic pain 16.38 12.27 26 64264 3029 29885159
Haematotoxicity 16.37 12.27 39 64251 6131 29882057
Hepatic cirrhosis 16.21 12.27 7 64283 15992 29872196
Malignant neoplasm progression 16.14 12.27 231 64059 72056 29816132
Blood triglycerides increased 16.12 12.27 5 64285 14012 29874176
Cardio-respiratory arrest 15.94 12.27 66 64224 57240 29830948
Cholestasis 15.94 12.27 18 64272 24932 29863256
Hyperlipidaemia 15.92 12.27 5 64285 13902 29874286
Gastrooesophageal reflux disease 15.90 12.27 28 64262 32227 29855961
Toxicity to various agents 15.88 12.27 495 63795 176688 29711500
Demyelinating polyneuropathy 15.85 12.27 16 64274 1180 29887008
Mantle cell lymphoma 15.80 12.27 18 64272 1523 29886665
Injury 15.80 12.27 14 64276 21717 29866471
Visceral leishmaniasis 15.75 12.27 11 64279 485 29887703
Nephrolithiasis 15.74 12.27 18 64272 24792 29863396
Hepatocellular injury 15.60 12.27 19 64271 25452 29862736
Refractory anaemia with an excess of blasts 15.50 12.27 10 64280 386 29887802
Laryngeal cancer metastatic 15.28 12.27 6 64284 77 29888111
Injection site pain 15.22 12.27 26 64264 30284 29857904
Pregnancy of partner 15.19 12.27 9 64281 298 29887890
Haemorrhagic fever 15.17 12.27 5 64285 37 29888151
Blood culture positive 15.17 12.27 33 64257 4886 29883302
Body height decreased 15.04 12.27 28 64262 3706 29884482
Spinal pain 14.98 12.27 31 64259 4433 29883755
Escherichia sepsis 14.92 12.27 29 64261 3965 29884223
Mantle cell lymphoma recurrent 14.90 12.27 10 64280 413 29887775
Anaemia 14.86 12.27 566 63724 207426 29680762
Depressed level of consciousness 14.81 12.27 38 64252 38184 29850004
Seasonal allergy 14.79 12.27 32 64258 4721 29883467
Refractory cytopenia with multilineage dysplasia 14.53 12.27 7 64283 151 29888037
Blastic plasmacytoid dendritic cell neoplasia 14.50 12.27 6 64284 89 29888099
Musculoskeletal stiffness 14.43 12.27 35 64255 35846 29852342
Sopor 14.41 12.27 3 64287 10988 29877200
Coma 14.34 12.27 42 64248 40407 29847781
Periodontitis 14.32 12.27 18 64272 1689 29886499
Tachycardia 14.31 12.27 96 64194 73643 29814545
Pneumocystis jirovecii infection 14.29 12.27 16 64274 1329 29886859
Cellulitis orbital 14.20 12.27 9 64281 337 29887851
Serratia sepsis 14.18 12.27 4 64286 16 29888172
Haematuria 14.18 12.27 49 64241 44785 29843403
Hypercapnic coma 14.08 12.27 7 64283 162 29888026
Oesophageal adenocarcinoma 13.88 12.27 13 64277 874 29887314
Type 2 diabetes mellitus 13.74 12.27 6 64284 13616 29874572
Ascites 13.70 12.27 36 64254 35885 29852303
Depressed mood 13.60 12.27 10 64280 17019 29871169
Plasmablastic lymphoma 13.58 12.27 8 64282 262 29887926
Hepatitis B reactivation 13.42 12.27 23 64267 2854 29885334
Respiratory depression 13.41 12.27 4 64286 11499 29876689
Hepatitis 13.35 12.27 17 64273 22339 29865849
Hyposmia 13.34 12.27 7 64283 182 29888006
Diabetic ketoacidosis 13.27 12.27 9 64281 15977 29872211
Secondary amyloidosis 13.19 12.27 5 64285 58 29888130
Glomerular filtration rate decreased 13.16 12.27 4 64286 11358 29876830
Product prescribing error 13.14 12.27 10 64280 16723 29871465
Blood pressure fluctuation 13.06 12.27 11 64279 17492 29870696
Atrial flutter 13.05 12.27 63 64227 14218 29873970
Pruritus 13.03 12.27 177 64113 118027 29770161
Acute myocardial infarction 12.91 12.27 64 64226 52875 29835313
Agranulocytosis 12.78 12.27 17 64273 21925 29866263
Melaena 12.76 12.27 32 64258 32405 29855783
Hypogammaglobulinaemia 12.66 12.27 32 64258 5220 29882968
Wheezing 12.58 12.27 30 64260 30908 29857280
Refractory cancer 12.56 12.27 6 64284 127 29888061
Blood glucose increased 12.49 12.27 79 64211 61451 29826737
Respiratory tract infection 12.48 12.27 66 64224 15440 29872748
Blepharitis 12.47 12.27 13 64277 996 29887192
Aphasia 12.44 12.27 14 64276 19425 29868763
Mesothelioma malignant 12.31 12.27 6 64284 133 29888055
Encephalitis viral 12.28 12.27 14 64276 1186 29887002

Pharmacologic Action:

SourceCodeDescription
ATC L01XG01 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
ANTINEOPLASTIC AGENTS
OTHER ANTINEOPLASTIC AGENTS
Proteasome inhibitors
FDA MoA N0000175075 Proteasome Inhibitors
FDA EPC N0000175604 Proteasome Inhibitor
MeSH PA D000970 Antineoplastic Agents
CHEBI has role CHEBI:35610 cytostatic
CHEBI has role CHEBI:35820 antiprotozoal agent
CHEBI has role CHEBI:37670 protease inhibitors
CHEBI has role CHEBI:52726 proteasome inhibitors

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Multiple myeloma indication 109989006 DOID:9538
Mantle cell lymphoma indication 443487006
Orthostatic hypotension contraindication 28651003
Dehydration contraindication 34095006
Low blood pressure contraindication 45007003
Chronic heart failure contraindication 48447003
Disorder of cardiovascular system contraindication 49601007 DOID:1287
Interstitial pneumonia contraindication 64667001
Adult respiratory distress syndrome contraindication 67782005 DOID:11394
Pulmonary hypertension contraindication 70995007 DOID:6432
Diabetes mellitus contraindication 73211009 DOID:9351
Intestinal obstruction contraindication 81060008 DOID:8437
Prolonged QT interval contraindication 111975006
Pneumonia contraindication 233604007 DOID:552
Disease of liver contraindication 235856003 DOID:409
Syncope contraindication 271594007
Pregnancy, function contraindication 289908002
Thrombocytopenic disorder contraindication 302215000 DOID:1588
Peripheral nerve disease contraindication 302226006
Neutropenic disorder contraindication 303011007 DOID:1227
Breastfeeding (mother) contraindication 413712001
Posterior reversible encephalopathy syndrome contraindication 450886002
Chemotherapy-Induced Hyperuricemia contraindication

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 9.39 acidic
pKa2 12.09 acidic
pKa3 13.65 acidic
pKa4 2.9 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
3.5MG/VIAL VELCADE TAKEDA PHARMS USA N021602 May 13, 2003 RX INJECTABLE INTRAVENOUS, SUBCUTANEOUS Oct. 8, 2021 TREATMENT OF PATIENTS WITH MANTLE CELL LYMPHOMA WHO HAVE NOT RECEIVED AT LEAST 1 PRIOR THERAPY
3.5MG/VIAL VELCADE TAKEDA PHARMS USA N021602 May 13, 2003 RX INJECTABLE INTRAVENOUS, SUBCUTANEOUS April 8, 2022 PEDIATRIC EXCLUSIVITY

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Proteasome subunit beta type-2 Enzyme INHIBITOR IC50 6.23 CHEMBL CHEMBL
Proteasome subunit beta type-1 Enzyme INHIBITOR IC50 7.28 CHEMBL CHEMBL
Proteasome subunit beta type-8 Enzyme INHIBITOR IC50 8.09 CHEMBL CHEMBL
Proteasome subunit beta type-5 Enzyme INHIBITOR Ki 9.26 CHEMBL CHEMBL
Proteasome subunit alpha type-1 Enzyme INHIBITOR Ki 9.21 WOMBAT-PK CHEMBL
Lysosomal protective protein Enzyme IC50 5.04 CHEMBL
Chymase Enzyme IC50 5.92 CHEMBL
Chymotrypsinogen B Enzyme Ki 6.49 CHEMBL
Nuclear factor NF-kappa-B complex Unclassified IC50 8.01 CHEMBL
Neutrophil elastase Enzyme Ki 5.64 CHEMBL
26S proteasome non-ATPase regulatory subunit 1 Cytosolic other Ki 7.74 WOMBAT-PK
Cytochrome P450 2C19 Enzyme Ki 4.74 WOMBAT-PK
PH and SEC7 domain-containing protein 1 Unclassified Ki 7.74 WOMBAT-PK
Prothrombin Enzyme Ki 4.89 CHEMBL
Cathepsin G Enzyme Ki 6.20 CHEMBL
Alpha-chymotrypsin Unclassified Ki 5.62 CHEMBL

External reference:

IDSource
69G8BD63PP UNII
4021393 VUID
N0000148811 NUI
D03150 KEGG_DRUG
4021393 VANDF
C1176309 UMLSCUI
CHEBI:52717 CHEBI
BO2 PDB_CHEM_ID
CHEMBL325041 ChEMBL_ID
DB00188 DRUGBANK_ID
D000069286 MESH_DESCRIPTOR_UI
8331 INN_ID
387447 PUBCHEM_CID
6391 IUPHAR_LIGAND_ID
356733 RXNORM
17263 MMSL
233935 MMSL
46756 MMSL
d04871 MMSL
009985 NDDF
398907002 SNOMEDCT_US
407097007 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Bortezomib HUMAN PRESCRIPTION DRUG LABEL 1 43598-865 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 3.50 mg INTRAVENOUS NDA 26 sections
VELCADE HUMAN PRESCRIPTION DRUG LABEL 1 63020-049 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 3.50 mg INTRAVENOUS NDA 32 sections
Bortezomib HUMAN PRESCRIPTION DRUG LABEL 1 63323-721 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 1 mg INTRAVENOUS NDA 28 sections